Nathanael Gray - Publications

Affiliations: 
Harvard University, Cambridge, MA, United States 
Area:
Cell Biology, Organic Chemistry, Biochemistry

467 high-probability publications. We are testing a new system for linking publications to authors. You can help! If you notice any inaccuracies, please sign in and mark papers as correct or incorrect matches. If you identify any major omissions or other inaccuracies in the publication list, please let us know.

Year Citation  Score
2022 Morita K, He S, Nowak RP, Wang J, Zimmerman MW, Fu C, Durbin AD, Martel MW, Prutsch N, Gray NS, Fischer ES, Look AT. Retraction Notice to: Allosteric Activators of Protein Phosphatase 2A Display Broad Antitumor Activity Mediated by Dephosphorylation of MYBL2. Cell. 185: 3058. PMID 35931023 DOI: 10.1016/j.cell.2022.07.008  0.371
2022 Teng M, Luskin MR, Cowan-Jacob SW, Ding Q, Fabbro D, Gray NS. The Dawn of Allosteric BCR-ABL1 Drugs: From a Phenotypic Screening Hit to an Approved Drug. Journal of Medicinal Chemistry. PMID 35609336 DOI: 10.1021/acs.jmedchem.2c00373  0.825
2022 Li Z, Ishida R, Liu Y, Wang J, Li Y, Gao Y, Jiang J, Che J, Sheltzer JM, Robers MB, Zhang T, Westover KD, Nabet B, Gray NS. Synthesis and Structure-Activity relationships of cyclin-dependent kinase 11 inhibitors based on a diaminothiazole scaffold. European Journal of Medicinal Chemistry. 238: 114433. PMID 35597007 DOI: 10.1016/j.ejmech.2022.114433  0.854
2022 Beyett TS, To C, Heppner DE, Rana JK, Schmoker AM, Jang J, De Clercq DJH, Gomez G, Scott DA, Gray NS, Jänne PA, Eck MJ. Molecular basis for cooperative binding and synergy of ATP-site and allosteric EGFR inhibitors. Nature Communications. 13: 2530. PMID 35534503 DOI: 10.1038/s41467-022-30258-y  0.732
2022 Powell CE, Hatcher JM, Jiang J, Vatsan PS, Che J, Gray NS. Selective Macrocyclic Inhibitors of DYRK1A/B. Acs Medicinal Chemistry Letters. 13: 577-585. PMID 35450378 DOI: 10.1021/acsmedchemlett.1c00630  0.854
2022 Li X, Huang CH, Sánchez-Rivera FJ, Kennedy MC, Tschaharganeh DF, Morris JP, Montinaro A, O'Rourke KP, Banito A, Wilkinson JE, Chen CC, Ho YJ, Dow LE, Tian S, Luan W, ... ... Gray NS, et al. A preclinical platform for assessing antitumor effects and systemic toxicities of cancer drug targets. Proceedings of the National Academy of Sciences of the United States of America. 119: e2110557119. PMID 35442775 DOI: 10.1073/pnas.2110557119  0.308
2022 To C, Beyett TS, Jang J, Feng WW, Bahcall M, Haikala HM, Shin BH, Heppner DE, Rana JK, Leeper BA, Soroko KM, Poitras MJ, Gokhale PC, Kobayashi Y, Wahid K, ... ... Gray NS, et al. An allosteric inhibitor against the therapy-resistant mutant forms of EGFR in non-small cell lung cancer. Nature Cancer. PMID 35422503 DOI: 10.1038/s43018-022-00351-8  0.818
2022 Gero TW, Heppner DE, Beyett TS, To C, Azevedo SC, Jang J, Bunnell T, Feru F, Li Z, Hee Shin B, Soroko KM, Gokhale PC, Gray NS, Jänne PA, Eck MJ, et al. Quinazolinones as allosteric fourth-generation EGFR inhibitors for the treatment of NSCLC. Bioorganic & Medicinal Chemistry Letters. 128718. PMID 35378251 DOI: 10.1016/j.bmcl.2022.128718  0.814
2022 Silva MC, Nandi G, Donovan KA, Cai Q, Berry BC, Nowak RP, Fischer ES, Gray NS, Ferguson FM, Haggarty SJ. Discovery and Optimization of Tau Targeted Protein Degraders Enabled by Patient Induced Pluripotent Stem Cells-Derived Neuronal Models of Tauopathy. Frontiers in Cellular Neuroscience. 16: 801179. PMID 35317195 DOI: 10.3389/fncel.2022.801179  0.791
2022 Munshi M, Liu X, Kofides A, Tsakmaklis N, Guerrera ML, Hunter ZR, Palomba ML, Argyropoulos KV, Patterson CJ, Canning AG, Meid KE, Gustine J, Branagan AR, Flynn C, Sarosiek S, ... ... Gray NS, et al. A new role for the SRC family kinase HCK as a driver of SYK activation in MYD88 mutated lymphomas. Blood Advances. PMID 35255496 DOI: 10.1182/bloodadvances.2021006147  0.716
2022 Gao Y, Volegova M, Nasholm N, Das S, Kwiatkowski N, Abraham BJ, Zhang T, Gray NS, Gustafson C, Krajewska M, George RE. Synergistic Anti-Tumor Effect of Combining Selective CDK7 and BRD4 Inhibition in Neuroblastoma. Frontiers in Oncology. 11: 773186. PMID 35198433 DOI: 10.3389/fonc.2021.773186  0.409
2022 Son J, Jang J, Beyett TS, Eum Y, Haikala HM, Verano A, Lin M, Hatcher JM, Kwiatkowski NP, Eser PÖ, Poitras MJ, Wang S, Xu M, Gokhale PC, Cameron MD, ... ... Gray NS, et al. A novel HER2-selective kinase inhibitor is effective in HER2 mutant and amplified non-small cell lung cancer. Cancer Research. PMID 35149586 DOI: 10.1158/0008-5472.CAN-21-2693  0.839
2022 Ryu S, Park JE, Ham YJ, Lim DC, Kwiatkowski NP, Kim DH, Bhunia D, Kim ND, Yaffe MB, Son W, Kim N, Choi TI, Swain P, Kim CH, Lee JY, ... Gray NS, et al. Novel Macrocyclic Peptidomimetics Targeting the Polo-Box Domain of Polo-Like Kinase 1. Journal of Medicinal Chemistry. PMID 35029981 DOI: 10.1021/acs.jmedchem.1c01359  0.413
2021 Teng M, Lu W, Donovan KA, Sun J, Krupnick NM, Nowak RP, Li YD, Sperling AS, Zhang T, Ebert BL, Fischer ES, Gray NS. Development of PDE6D and CK1α Degraders through Chemical Derivatization of FPFT-2216. Journal of Medicinal Chemistry. PMID 34965125 DOI: 10.1021/acs.jmedchem.1c01832  0.813
2021 Privalsky TM, Soohoo AM, Wang J, Walsh CT, Wright GD, Gordon EM, Gray NS, Khosla C. Prospects for Antibacterial Discovery and Development. Journal of the American Chemical Society. 143: 21127-21142. PMID 34860516 DOI: 10.1021/jacs.1c10200  0.546
2021 Hatcher JM, Vatsan PS, Wang E, Jiang J, Gray NS. Development of Highly Potent and Selective Pyrazolopyridine Inhibitor of CDK8/19. Acs Medicinal Chemistry Letters. 12: 1689-1693. PMID 34795857 DOI: 10.1021/acsmedchemlett.1c00300  0.853
2021 Kaltheuner IH, Anand K, Moecking J, Düster R, Wang J, Gray NS, Geyer M. Abemaciclib is a potent inhibitor of DYRK1A and HIP kinases involved in transcriptional regulation. Nature Communications. 12: 6607. PMID 34785661 DOI: 10.1038/s41467-021-26935-z  0.566
2021 Vervoort SJ, Devlin JR, Kwiatkowski N, Teng M, Gray NS, Johnstone RW. Targeting transcription cycles in cancer. Nature Reviews. Cancer. 22: 5-24. PMID 34675395 DOI: 10.1038/s41568-021-00411-8  0.797
2021 Zhu H, Ficarro SB, Alexander WM, Fleming LE, Adelmant G, Zhang T, Willetts M, Decker J, Brehmer S, Krause M, East MP, Gray NS, Johnson GL, Kruppa G, Marto JA. PRM-LIVE with Trapped Ion Mobility Spectrometry and Its Application in Selectivity Profiling of Kinase Inhibitors. Analytical Chemistry. PMID 34606255 DOI: 10.1021/acs.analchem.1c02349  0.582
2021 Li Q, Jiang B, Guo J, Shao H, Del Priore IS, Chang Q, Kudo R, Li Z, Razavi P, Liu B, Boghossian AS, Rees MG, Ronan MM, Roth JA, Donovan KA, ... ... Gray NS, et al. INK4 tumor suppressor proteins mediate resistance to CDK4/6 kinase inhibitors. Cancer Discovery. PMID 34544752 DOI: 10.1158/2159-8290.CD-20-1726  0.796
2021 Powell CE, Du G, Bushman JW, He Z, Zhang T, Fischer ES, Gray NS. Selective degradation-inducing probes for studying cereblon (CRBN) biology. Rsc Medicinal Chemistry. 12: 1381-1390. PMID 34458741 DOI: 10.1039/d0md00382d  0.824
2021 Teng M, Jiang J, Ficarro SB, Seo HS, Bae JH, Donovan KA, Fischer ES, Zhang T, Dhe-Paganon S, Marto JA, Gray NS. Exploring Ligand-Directed -Acyl--alkylsulfonamide-Based Acylation Chemistry for Potential Targeted Degrader Development. Acs Medicinal Chemistry Letters. 12: 1302-1307. PMID 34413960 DOI: 10.1021/acsmedchemlett.1c00285  0.816
2021 Koikawa K, Kibe S, Suizu F, Sekino N, Kim N, Manz TD, Pinch BJ, Akshinthala D, Verma A, Gaglia G, Nezu Y, Ke S, Qiu C, Ohuchida K, Oda Y, ... ... Gray NS, et al. Targeting Pin1 renders pancreatic cancer eradicable by synergizing with immunochemotherapy. Cell. PMID 34388391 DOI: 10.1016/j.cell.2021.07.020  0.796
2021 Seong BKA, Dharia NV, Lin S, Donovan KA, Chong S, Robichaud A, Conway A, Hamze A, Ross L, Alexe G, Adane B, Nabet B, Ferguson FM, Stolte B, Wang EJ, ... ... Gray NS, et al. TRIM8 modulates the EWS/FLI oncoprotein to promote survival in Ewing sarcoma. Cancer Cell. PMID 34329586 DOI: 10.1016/j.ccell.2021.07.003  0.746
2021 Tang CC, Castro Andrade CD, O'Meara MJ, Yoon SH, Sato T, Brooks DJ, Bouxsein ML, Martins JDS, Wang J, Gray NS, Misof B, Roschger P, Boulin S, Klaushofer K, Velduis-Vlug A, et al. Dual targeting of salt inducible kinases and CSF1R uncouples bone formation and bone resorption. Elife. 10. PMID 34160349 DOI: 10.7554/eLife.67772  0.363
2021 Deng J, Thennavan A, Dolgalev I, Chen T, Li J, Marzio A, Poirier JT, Peng D, Bulatovic M, Mukhopadhyay S, Silver H, Papadopoulos E, Pyon V, Thakurdin C, Han H, ... ... Gray NS, et al. ULK1 inhibition overcomes compromised antigen presentation and restores antitumor immunity in LKB1 mutant lung cancer. Nature Cancer. 2: 503-514. PMID 34142094 DOI: 10.1038/s43018-021-00208-6  0.71
2021 Yang G, Wang J, Tan L, Munshi M, Liu X, Kofides A, Chen JG, Tsakmaklis N, Demos M, Guerrera ML, Xu L, Hunter ZR, Che J, Patterson CJ, Meid KE, ... ... Gray NSS, et al. The HCK/BTK inhibitor KIN-8194 is active in MYD88 driven lymphomas and overcomes mutated BTKCys481 ibrutinib resistance. Blood. PMID 34132782 DOI: 10.1182/blood.2021011405  0.702
2021 Arnett A, Moo KG, Flynn KJ, Sundberg TB, Johannessen L, Shamji AF, Gray NS, Decker T, Zheng Y, Gersuk VH, Rahman ZS, Levy DE, Marié IJ, Linsley PS, Xavier RJ, et al. The CDK8 inhibitor DCA promotes a tolerogenic chemical immunophenotype in CD4 T cells via a novel CDK8-GATA3-FOXP3 pathway. Molecular and Cellular Biology. MCB0008521. PMID 34124936 DOI: 10.1128/MCB.00085-21  0.793
2021 Vervoort SJ, Welsh SA, Devlin JR, Barbieri E, Knight DA, Offley S, Bjelosevic S, Costacurta M, Todorovski I, Kearney CJ, Sandow JJ, Fan Z, Blyth B, McLeod V, Vissers JHA, ... ... Gray N, et al. The PP2A-Integrator-CDK9 axis fine-tunes transcription and can be targeted therapeutically in cancer. Cell. PMID 34004147 DOI: 10.1016/j.cell.2021.04.022  0.33
2021 Carli ALE, Afshar-Sterle S, Rai A, Fang H, O'Keefe R, Tse J, Ferguson FM, Gray NS, Ernst M, Greening DW, Buchert M. Cancer stem cell marker DCLK1 reprograms small extracellular vesicles toward migratory phenotype in gastric cancer cells. Proteomics. e2000098. PMID 33991177 DOI: 10.1002/pmic.202000098  0.752
2021 Remenyi J, Naik RJ, Wang J, Razsolkov M, Verano A, Cai Q, Tan L, Toth R, Raggett S, Baillie C, Traynor R, Hastie CJ, Gray NS, Arthur JSC. Generation of a chemical genetic model for JAK3. Scientific Reports. 11: 10093. PMID 33980892 DOI: 10.1038/s41598-021-89356-4  0.745
2021 Dubiella C, Pinch BJ, Koikawa K, Zaidman D, Poon E, Manz TD, Nabet B, He S, Resnick E, Rogel A, Langer EM, Daniel CJ, Seo HS, Chen Y, Adelmant G, ... ... Gray NS, et al. Sulfopin is a covalent inhibitor of Pin1 that blocks Myc-driven tumors in vivo. Nature Chemical Biology. PMID 33972797 DOI: 10.1038/s41589-021-00786-7  0.836
2021 Jiang B, Jiang J, Kaltheuner IH, Iniguez AB, Anand K, Ferguson FM, Ficarro SB, Seong BKA, Greifenberg AK, Dust S, Kwiatkowski NP, Marto JA, Stegmaier K, Zhang T, Geyer M, ... Gray NS, et al. Structure-activity relationship study of THZ531 derivatives enables the discovery of BSJ-01-175 as a dual CDK12/13 covalent inhibitor with efficacy in Ewing sarcoma. European Journal of Medicinal Chemistry. 221: 113481. PMID 33945934 DOI: 10.1016/j.ejmech.2021.113481  0.86
2021 Du G, Jiang J, Wu Q, Henning NJ, Donovan KA, Yue H, Che J, Lu W, Fischer ES, Bardeesy N, Zhang T, Gray NS. Discovery of a Potent Degrader for Fibroblast Growth Factor Receptor 1/2. Angewandte Chemie (International Ed. in English). PMID 33915015 DOI: 10.1002/anie.202101328  0.792
2021 Jiang B, Gao Y, Che J, Lu W, Kaltheuner IH, Dries R, Kalocsay M, Berberich MJ, Jiang J, You I, Kwiatkowski N, Riching KM, Daniels DL, Sorger PK, Geyer M, ... ... Gray NS, et al. Discovery and resistance mechanism of a selective CDK12 degrader. Nature Chemical Biology. PMID 33753926 DOI: 10.1038/s41589-021-00765-y  0.827
2021 Koduri V, Duplaquet L, Lampson BL, Wang AC, Sabet AH, Ishoey M, Paulk J, Teng M, Harris IS, Endress JE, Liu X, Dasilva E, Paulo JA, Briggs KJ, Doench JG, ... ... Gray NS, et al. Targeting oncoproteins with a positive selection assay for protein degraders. Science Advances. 7. PMID 33547076 DOI: 10.1126/sciadv.abd6263  0.813
2021 Groendyke BJ, Nabet B, Mohardt ML, Zhang H, Peng K, Koide E, Coffey CR, Che J, Scott DA, Bass AJ, Gray NS. Discovery of a Pyrimidothiazolodiazepinone as a Potent and Selective Focal Adhesion Kinase (FAK) Inhibitor. Acs Medicinal Chemistry Letters. 12: 30-38. PMID 33488961 DOI: 10.1021/acsmedchemlett.0c00338  0.481
2021 Wells CI, Al-Ali H, Andrews DM, Asquith CRM, Axtman AD, Dikic I, Ebner D, Ettmayer P, Fischer C, Frederiksen M, Futrell RE, Gray NS, Hatch SB, Knapp S, Lücking U, et al. The Kinase Chemogenomic Set (KCGS): An Open Science Resource for Kinase Vulnerability Identification. International Journal of Molecular Sciences. 22. PMID 33429995 DOI: 10.3390/ijms22020566  0.552
2020 Donovan KA, Ferguson FM, Bushman JW, Eleuteri NA, Bhunia D, Ryu S, Tan L, Shi K, Yue H, Liu X, Dobrovolsky D, Jiang B, Wang J, Hao M, You I, ... ... Gray NS, et al. Mapping the Degradable Kinome Provides a Resource for Expedited Degrader Development. Cell. PMID 33275901 DOI: 10.1016/j.cell.2020.10.038  0.829
2020 Hatcher JM, Yang G, Wang L, Ficarro SB, Buhrlage S, Wu H, Marto JA, Treon SP, Gray NS. Discovery of a Selective, Covalent IRAK1 Inhibitor with Antiproliferative Activity in MYD88 Mutated B-Cell Lymphoma. Acs Medicinal Chemistry Letters. 11: 2238-2243. PMID 33214835 DOI: 10.1021/acsmedchemlett.0c00378  0.832
2020 Poon E, Liang T, Jamin Y, Walz S, Kwok C, Hakkert A, Barker K, Urban Z, Thway K, Zeid R, Hallsworth A, Box G, Ebus ME, Licciardello MP, Sbirkov Y, ... ... Gray NS, et al. Orally bioavailable CDK9/2 inhibitor shows mechanism-based therapeutic potential in MYCN-driven neuroblastoma. The Journal of Clinical Investigation. PMID 33016930 DOI: 10.1172/JCI134132  0.368
2020 Nabet B, Ferguson FM, Seong BKA, Kuljanin M, Leggett AL, Mohardt ML, Robichaud A, Conway AS, Buckley DL, Mancias JD, Bradner JE, Stegmaier K, Gray NS. Rapid and direct control of target protein levels with VHL-recruiting dTAG molecules. Nature Communications. 11: 4687. PMID 32948771 DOI: 10.1038/S41467-020-18377-W  0.739
2020 Fan Z, Devlin JR, Hogg SJ, Doyle MA, Harrison PF, Todorovski I, Cluse LA, Knight DA, Sandow JJ, Gregory G, Fox A, Beilharz TH, Kwiatkowski N, Scott NE, Vidakovic AT, ... ... Gray NS, et al. CDK13 cooperates with CDK12 to control global RNA polymerase II processivity. Science Advances. 6. PMID 32917631 DOI: 10.1126/Sciadv.Aaz5041  0.344
2020 Jiang J, Jiang B, He Z, Ficarro SB, Che J, Marto JA, Gao Y, Zhang T, Gray NS. Discovery of Covalent MKK4/7 Dual Inhibitor. Cell Chemical Biology. PMID 32916088 DOI: 10.1016/J.Chembiol.2020.08.014  0.865
2020 Powell CE, Du G, Che J, He Z, Donovan KA, Yue H, Wang ES, Nowak RP, Zhang T, Fischer ES, Gray NS. Selective Degradation of GSPT1 by Cereblon Modulators Identified via a Focused Combinatorial Library. Acs Chemical Biology. PMID 32865967 DOI: 10.1021/Acschembio.0C00520  0.824
2020 Ferguson FM, Liu Y, Harshbarger W, Huang L, Wang J, Deng X, Capuzzi SJ, Muratov EN, Tropsha A, Muthuswamy S, Westover KD, Gray NS. Correction to "Synthesis and Structure-Activity Relationships of DCLK1 Kinase Inhibitors Based on a 5,11-Dihydro-6-benzo[]pyrimido[5,4-][1,4]diazepin-6-one Scaffold". Journal of Medicinal Chemistry. PMID 32790356 DOI: 10.1021/acs.jmedchem.0c01338  0.838
2020 Schröder M, Tan L, Wang J, Liang Y, Gray NS, Knapp S, Chaikuad A. Catalytic Domain Plasticity of MKK7 Reveals Structural Mechanisms of Allosteric Activation and Diverse Targeting Opportunities. Cell Chemical Biology. PMID 32783966 DOI: 10.1016/J.Chembiol.2020.07.014  0.523
2020 Weisberg E, Parent A, Yang PL, Sattler M, Liu Q, Liu Q, Wang J, Meng C, Buhrlage SJ, Gray N, Griffin JD. Repurposing of Kinase Inhibitors for Treatment of COVID-19. Pharmaceutical Research. 37: 167. PMID 32778962 DOI: 10.1007/S11095-020-02851-7  0.838
2020 Liu Y, Ferguson FM, Li L, Kuljanin M, Mills CE, Subramanian K, Harshbarger W, Gondi S, Wang J, Sorger PK, Mancias JD, Gray NS, Westover KD. Chemical Biology Toolkit for DCLK1 Reveals Connection to RNA Processing. Cell Chemical Biology. PMID 32755567 DOI: 10.1016/J.Chembiol.2020.07.011  0.836
2020 Li Z, Powell CE, Groendyke BJ, Gero TW, Feru F, Feutrill J, Chen B, Li B, Szabo H, Gray NS, Scott DA. Discovery of a Series of Benzopyrimidodiazepinone TNK2 Inhibitors via Scaffold Morphing. Bioorganic & Medicinal Chemistry Letters. 127456. PMID 32739400 DOI: 10.1016/J.Bmcl.2020.127456  0.853
2020 Fassl A, Brain C, Abu-Remaileh M, Stukan I, Butter D, Stepien P, Feit AS, Bergholz J, Michowski W, Otto T, Sheng Q, Loo A, Michael W, Tiedt R, DeAngelis C, ... ... Gray N, et al. Increased lysosomal biomass is responsible for the resistance of triple-negative breast cancers to CDK4/6 inhibition. Science Advances. 6: eabb2210. PMID 32704543 DOI: 10.1126/Sciadv.Abb2210  0.83
2020 Weisberg E, Sattler M, Yang PL, Parent A, Gray N, Griffin JD. Current Therapies Under Investigation for COVID-19. Canadian Journal of Physiology and Pharmacology. PMID 32640179 DOI: 10.1139/Cjpp-2020-0286  0.53
2020 Giurisato E, Lonardi S, Telfer B, Lussoso S, Risa-Ebrí B, Zhang J, Russo I, Wang J, Santucci A, Finegan KG, Gray NS, Vermi W, Tournier C. Extracellular-regulated protein kinase 5-mediated control of p21 expression promotes macrophage proliferation associated with tumor growth and metastasis. Cancer Research. PMID 32561530 DOI: 10.1158/0008-5472.Can-19-2416  0.414
2020 Klein IA, Boija A, Afeyan LK, Hawken SW, Fan M, Dall'Agnese A, Oksuz O, Henninger JE, Shrinivas K, Sabari BR, Sagi I, Clark VE, Platt JM, Kar M, McCall PM, ... ... Gray NS, et al. Partitioning of cancer therapeutics in nuclear condensates. Science (New York, N.Y.). 368: 1386-1392. PMID 32554597 DOI: 10.1126/Science.Aaz4427  0.461
2020 Teng M, Ficarro SB, Yoon H, Che J, Zhou J, Fischer ES, Marto JA, Zhang T, Gray NS. Rationally Designed Covalent BCL6 Inhibitor That Targets a Tyrosine Residue in the Homodimer Interface. Acs Medicinal Chemistry Letters. 11: 1269-1273. PMID 32551010 DOI: 10.1021/Acsmedchemlett.0C00111  0.853
2020 Ferguson FM, Liu Y, Harshbarger W, Huang L, Wang J, Deng X, Capuzzi SJ, Muratov EN, Tropsha A, Muthuswamy S, Westover KD, Gray NS. Synthesis and structure activity relationships of DCLK1 kinase inhibitors based on a 5,11-dihydro-6H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6-one scaffold. Journal of Medicinal Chemistry. PMID 32530623 DOI: 10.1021/Acs.Jmedchem.0C00596  0.845
2020 Jang J, To C, De Clercq DJH, Park E, Ponthier CM, Shin BH, Mushajiang M, Nowak RP, Fischer ES, Eck MJ, Jänne PA, Gray NS. Mutant-Selective Allosteric EGFR Degraders are Effective Against a Broad Range of Drug-Resistant Mutations. Angewandte Chemie (International Ed. in English). PMID 32510788 DOI: 10.1002/Anie.202003500  0.721
2020 Gurbani D, Du G, Henning NJ, Rao S, Bera AK, Zhang T, Gray NS, Westover KD. Structure and Characterization of a Covalent Inhibitor of Src Kinase. Frontiers in Molecular Biosciences. 7: 81. PMID 32509799 DOI: 10.3389/Fmolb.2020.00081  0.858
2020 Liu Y, Hao M, Leggett A, Gao Y, Ficarro SB, Che J, He Z, Olson C, Marto JA, Kwiatkowski N, Zhang T, Gray NS. Discovery of MFH290: A Potent and Highly Selective Covalent Inhibitor for Cyclin-Dependent Kinase 12/13. Journal of Medicinal Chemistry. PMID 32502343 DOI: 10.1021/Acs.Jmedchem.9B01929  0.828
2020 Fan Z, Devlin JR, Hogg SJ, Doyle MA, Harrison PF, Todorovski I, Cluse LA, Knight DA, Sandow JJ, Gregory G, Fox A, Beilharz TH, Kwiatkowski N, Scott NE, Vidakovic AT, ... ... Gray NS, et al. CDK13 cooperates with CDK12 to control global RNA polymerase II processivity. Science Advances. 6: eaaz5041. PMID 32494677 DOI: 10.1126/sciadv.aaz5041  0.344
2020 Pinch BJ, Doctor ZM, Nabet B, Browne CM, Seo HS, Mohardt ML, Kozono S, Lian X, Manz TD, Chun Y, Kibe S, Zaidman D, Daitchman D, Yeoh ZC, Vangos NE, ... ... Gray NS, et al. Identification of a potent and selective covalent Pin1 inhibitor. Nature Chemical Biology. PMID 32483379 DOI: 10.1038/S41589-020-0550-9  0.834
2020 Jaeger MG, Schwalb B, Mackowiak SD, Velychko T, Hanzl A, Imrichova H, Brand M, Agerer B, Chorn S, Nabet B, Ferguson FM, Müller AC, Bergthaler A, Gray NS, Bradner JE, et al. Selective Mediator dependence of cell-type-specifying transcription. Nature Genetics. PMID 32483291 DOI: 10.1038/S41588-020-0635-0  0.699
2020 Gray NS, Teng M, Jiang J, He Z, Kwiatkowski NP, Donovan KA, Mills CE, Victor C, Hatcher JM, Fischer ES, Sorger PK, Zhang T. Development of CDK2 and CDK5 Dual Degrader TMX-2172. Angewandte Chemie (International Ed. in English). PMID 32415712 DOI: 10.1002/Anie.202004087  0.847
2020 Morita K, He S, Nowak RP, Wang J, Zimmerman MW, Fu C, Durbin AD, Martel MW, Prutsch N, Gray NS, Fischer ES, Look AT. Allosteric Activators of Protein Phosphatase 2A Display Broad Antitumor Activity Mediated by Dephosphorylation of MYBL2. Cell. PMID 32315619 DOI: 10.1016/J.Cell.2020.03.051  0.475
2020 Manz TD, Sivakumaren SC, Ferguson FM, Zhang T, Yasgar A, Seo HS, Ficarro SB, Card JD, Shim H, Miduturu CV, Simeonov A, Shen M, Marto JA, Dhe-Paganon S, Hall MD, ... ... Gray NS, et al. Discovery and Structure-Activity Relationship Study of (Z)-5-Methylenethiazolidin-4-one Derivatives as Potent and Selective Pan-phosphatidylinositol 5-Phosphate 4-Kinase Inhibitors. Journal of Medicinal Chemistry. PMID 32298120 DOI: 10.1021/Acs.Jmedchem.0C00227  0.867
2020 Ferguson FM, Nabet B, Raghavan S, Liu Y, Leggett AL, Kuljanin M, Kalekar RL, Yang A, He S, Wang J, Ng RWS, Sulahian R, Li L, Poulin EJ, Huang L, ... ... Gray NS, et al. Discovery of a selective inhibitor of doublecortin like kinase 1. Nature Chemical Biology. PMID 32251410 DOI: 10.1038/S41589-020-0506-0  0.863
2020 Santana-Codina N, Chandhoke AS, Yu Q, Małachowska B, Kuljanin M, Gikandi A, Stańczak M, Gableske S, Jedrychowski MP, Scott DA, Aguirre AJ, Fendler W, Gray NS, Mancias JD. Defining and Targeting Adaptations to Oncogenic KRAS Inhibition Using Quantitative Temporal Proteomics. Cell Reports. 30: 4584-4599.e4. PMID 32234489 DOI: 10.1016/j.celrep.2020.03.021  0.339
2020 Manz TD, Sivakumaren SC, Yasgar A, Hall MD, Davis MI, Seo HS, Card JD, Ficarro SB, Shim H, Marto JA, Dhe-Paganon S, Sasaki AT, Boxer MB, Simeonov A, Cantley LC, ... ... Gray NS, et al. Structure-Activity Relationship Study of Covalent Pan-phosphatidylinositol 5-Phosphate 4-Kinase Inhibitors. Acs Medicinal Chemistry Letters. 11: 346-352. PMID 32184968 DOI: 10.1021/Acsmedchemlett.9B00402  0.862
2020 Lochhead PA, Tucker JA, Tatum NJ, Wang J, Oxley D, Kidger AM, Johnson VP, Cassidy MA, Gray NS, Noble MEM, Cook SJ. Paradoxical activation of the protein kinase-transcription factor ERK5 by ERK5 kinase inhibitors. Nature Communications. 11: 1383. PMID 32170057 DOI: 10.1038/S41467-020-15031-3  0.583
2020 Weisberg E, Meng C, Case A, Sattler M, Tiv HL, Gokhale PC, Buhrlage S, Wang J, Gray N, Stone R, Liu S, Bhagwat SV, Tiu RV, Adamia S, Griffin JD. Correction: Evaluation of ERK as a therapeutic target in acute myelogenous leukemia. Leukemia. PMID 32144400 DOI: 10.1038/S41375-020-0782-4  0.664
2020 Sivakumaren SC, Shim H, Zhang T, Ferguson FM, Lundquist MR, Browne CM, Seo HS, Paddock MN, Manz TD, Jiang B, Hao MF, Krishnan P, Wang DG, Yang TJ, Kwiatkowski NP, ... ... Gray NS, et al. Targeting the PI5P4K Lipid Kinase Family in Cancer Using Covalent Inhibitors. Cell Chemical Biology. PMID 32130941 DOI: 10.1016/J.Chembiol.2020.02.003  0.837
2020 Liu J, Chen H, Ma L, He Z, Wang D, Liu Y, Lin Q, Zhang T, Gray N, Kaniskan HÜ, Jin J, Wei W. Light-induced control of protein destruction by opto-PROTAC. Science Advances. 6: eaay5154. PMID 32128407 DOI: 10.1126/Sciadv.Aay5154  0.732
2020 Thoreen CC, Kang SA, Chang JW, Liu Q, Zhang J, Gao Y, Reichling LJ, Sim T, Sabatini DM, Gray NS. Correction: An ATP-competitive mammalian target of rapamycin inhibitor reveals rapamycin-resistant functions of mTORC1. The Journal of Biological Chemistry. 295: 2886. PMID 32111721 DOI: 10.1074/Jbc.Aac120.012837  0.816
2020 Xiao H, Jedrychowski MP, Schweppe DK, Huttlin EL, Yu Q, Heppner DE, Li J, Long J, Mills EL, Szpyt J, He Z, Du G, Garrity R, Reddy A, Vaites LP, ... ... Gray NS, et al. A Quantitative Tissue-Specific Landscape of Protein Redox Regulation during Aging. Cell. PMID 32109415 DOI: 10.1016/J.Cell.2020.02.012  0.779
2020 Yang J, Meng C, Weisberg E, Case A, Lamberto I, Magin RS, Adamia S, Wang J, Gray N, Liu S, Stone R, Sattler M, Buhrlage S, Griffin JD. Inhibition of the deubiquitinase USP10 induces degradation of SYK. British Journal of Cancer. PMID 32015510 DOI: 10.1038/S41416-020-0731-Z  0.763
2020 Munshi M, Liu X, Chen JG, Xu L, Tsakmaklis N, Demos MG, Kofides A, Guerrera ML, Jimenez C, Chan GG, Hunter ZR, Palomba ML, Argyropoulos KV, Meid K, Keezer A, ... ... Gray NS, et al. SYK is activated by mutated MYD88 and drives pro-survival signaling in MYD88 driven B-cell lymphomas. Blood Cancer Journal. 10: 12. PMID 32005797 DOI: 10.1038/S41408-020-0277-6  0.695
2020 Weisberg E, Meng C, Case AE, Tiv HL, Gokhale PC, Buhrlage SJ, Yang J, Liu X, Wang J, Gray N, Adamia S, Sattler M, Stone R, Griffin JD. Effects of the multi-kinase inhibitor midostaurin in combination with chemotherapy in models of acute myeloid leukaemia. Journal of Cellular and Molecular Medicine. PMID 31967735 DOI: 10.1111/Jcmm.14927  0.768
2020 Weisberg E, Meng C, Case AE, Tiv HL, Gokhale PC, Toure AA, Buhrlage S, Liu X, Wang J, Gray N, Stone R, Adamia S, Winer E, Sattler M, Griffin JD. The combination of FLT3 and SYK kinase inhibitors is toxic to leukaemia cells with CBL mutations. Journal of Cellular and Molecular Medicine. PMID 31943762 DOI: 10.1111/Jcmm.14820  0.792
2020 Kurppa KJ, Liu Y, To C, Zhang T, Fan M, Vajdi A, Knelson EH, Xie Y, Lim K, Cejas P, Portell A, Lizotte PH, Ficarro SB, Li S, Chen T, ... ... Gray NS, et al. Treatment-Induced Tumor Dormancy through YAP-Mediated Transcriptional Reprogramming of the Apoptotic Pathway. Cancer Cell. 37: 104-122.e12. PMID 31935369 DOI: 10.1016/J.Ccell.2019.12.006  0.674
2020 Du G, Rao S, Gurbani D, Henning NJ, Jiang J, Che J, Yang A, Ficarro SB, Marto JA, Aguirre AJ, Sorger PK, Westover KD, Zhang T, Gray NS. Structure-based design of a potent and selective covalent inhibitor for SRC kinase that targets a p-Loop cysteine. Journal of Medicinal Chemistry. PMID 31935084 DOI: 10.1021/Acs.Jmedchem.9B01502  0.868
2020 Groendyke BJ, Powell CE, Feru F, Gero TW, Li Z, Szabo H, Pang K, Feutrill J, Chen B, Li B, Gray NS, Scott DA. Benzopyrimidodiazepinone inhibitors of TNK2. Bioorganic & Medicinal Chemistry Letters. 126948. PMID 31928839 DOI: 10.1016/J.Bmcl.2020.126948  0.83
2020 Kim JW, Berrios C, Kim M, Schade AE, Adelmant G, Yeerna H, Damato E, Iniguez AB, Florens L, Washburn MP, Stegmaier K, Gray NS, Tamayo P, Gjoerup O, Marto JA, et al. STRIPAK directs PP2A activity toward MAP4K4 to promote oncogenic transformation of human cells. Elife. 9. PMID 31913126 DOI: 10.7554/Elife.53003  0.542
2020 Seong BKA, Lin S, Donovan K, Robichaud A, Stolte B, Wang E, Dharia N, Nabet B, Piccioni F, Gray N, Fischer E, Stegmaier K. Abstract B50: Targeting EWS/FLI fusion oncoprotein stability/degradation in Ewing sarcoma Cancer Research. 80. DOI: 10.1158/1538-7445.Pedca19-B50  0.431
2020 Guhan SM, Shaughnessy M, Rajadurai A, Kumar R, Ji Z, Gray N, Tsao H. 104 The molecular context of vulnerability for CDK9 suppression in melanoma Journal of Investigative Dermatology. 140. DOI: 10.1016/J.Jid.2020.03.107  0.305
2019 de Wispelaere M, Carocci M, Burri DJ, Neidermyer WJ, Olson CM, Roggenbach I, Liang Y, Wang J, Whelan SPJ, Gray NS, Yang PL. A broad-spectrum antiviral molecule, QL47, selectively inhibits eukaryotic translation. The Journal of Biological Chemistry. PMID 31914414 DOI: 10.1074/Jbc.Ra119.011132  0.829
2019 Zhang H, Christensen CL, Dries R, Oser MG, Deng J, Diskin B, Li F, Pan Y, Zhang X, Yin Y, Papadopoulos E, Pyon V, Thakurdin C, Kwiatkowski N, Jani K, ... ... Gray NS, et al. CDK7 Inhibition Potentiates Genome Instability Triggering Anti-tumor Immunity in Small Cell Lung Cancer. Cancer Cell. PMID 31883968 DOI: 10.1016/J.Ccell.2019.11.003  0.736
2019 Zeng M, Xiong Y, Safaee N, Nowak RP, Donovan KA, Yuan CJ, Nabet B, Gero TW, Feru F, Li L, Gondi S, Ombelets LJ, Quan C, Jänne PA, Kostic M, ... ... Gray NS, et al. Exploring Targeted Degradation Strategy for Oncogenic KRAS. Cell Chemical Biology. PMID 31883964 DOI: 10.1016/J.Chembiol.2019.12.006  0.826
2019 You I, Erickson EC, Donovan KA, Eleuteri NA, Fischer ES, Gray NS, Toker A. Discovery of an AKT Degrader with Prolonged Inhibition of Downstream Signaling. Cell Chemical Biology. PMID 31859249 DOI: 10.1016/J.Chembiol.2019.11.014  0.422
2019 Chopra SS, Jenney A, Palmer A, Niepel M, Chung M, Mills C, Sivakumaren SC, Liu Q, Chen JY, Yapp C, Asara JM, Gray NS, Sorger PK. Torin2 Exploits Replication and Checkpoint Vulnerabilities to Cause Death of PI3K-Activated Triple-Negative Breast Cancer Cells. Cell Systems. PMID 31812693 DOI: 10.1016/J.Cels.2019.11.001  0.853
2019 De Clercq DJH, Heppner DE, To C, Jang J, Park E, Yun CH, Mushajiang M, Shin BH, Gero TW, Scott DA, Jänne PA, Eck MJ, Gray NS. Discovery and Optimization of Dibenzodiazepinones as Allosteric Mutant-Selective EGFR Inhibitors. Acs Medicinal Chemistry Letters. 10: 1549-1553. PMID 31749909 DOI: 10.1021/Acsmedchemlett.9B00381  0.85
2019 Li Z, Pinch BJ, Olson CM, Donovan KA, Nowak RP, Mills CE, Scott DA, Doctor ZM, Eleuteri NA, Chung M, Sorger PK, Fischer ES, Gray NS. Development and Characterization of a Wee1 Kinase Degrader. Cell Chemical Biology. PMID 31735695 DOI: 10.1016/J.Chembiol.2019.10.013  0.825
2019 Tarumoto Y, Lin S, Wang J, Milazzo JP, Xu Y, Lu B, Yang Z, Wei Y, Polyanskaya S, Wunderlich M, Gray NS, Stegmaier K, Vakoc CR. Salt-Inducible Kinase inhibition suppresses acute myeloid leukemia progression in vivo. Blood. PMID 31697837 DOI: 10.1182/Blood.2019001576  0.584
2019 Faust TB, Yoon H, Nowak RP, Donovan KA, Li Z, Cai Q, Eleuteri NA, Zhang T, Gray NS, Fischer ES. Structural complementarity facilitates E7820-mediated degradation of RBM39 by DCAF15. Nature Chemical Biology. PMID 31686031 DOI: 10.1038/s41589-019-0378-3  0.607
2019 Lian W, Jang J, Potisopon S, Li PC, Rahmeh A, Wang J, Kwiatkowski NP, Gray NS, Yang PL. Correction to Discovery of Immunologically Inspired Small Molecules That Target the Viral Envelope Protein. Acs Infectious Diseases. PMID 31675213 DOI: 10.1021/Acsinfecdis.9B00401  0.773
2019 Zhang T, Hatcher JM, Teng M, Gray NS, Kostic M. Recent Advances in Selective and Irreversible Covalent Ligand Development and Validation. Cell Chemical Biology. PMID 31631011 DOI: 10.1016/J.Chembiol.2019.09.012  0.815
2019 Menzl I, Zhang T, Berger-Becvar A, Grausenburger R, Heller G, Prchal-Murphy M, Edlinger L, Knab VM, Uras IZ, Grundschober E, Bauer K, Roth M, Skucha A, Liu Y, Hatcher JM, ... ... Gray NS, et al. A kinase-independent role for CDK8 in BCR-ABL1 leukemia. Nature Communications. 10: 4741. PMID 31628323 DOI: 10.1038/S41467-019-12656-X  0.86
2019 Remillard D, Buckley DL, Seo HS, Ferguson FM, Dhe-Paganon S, Bradner JE, Gray NS. Dual Inhibition of TAF1 and BET Bromodomains from the BI-2536 Kinase Inhibitor Scaffold. Acs Medicinal Chemistry Letters. 10: 1443-1449. PMID 31620231 DOI: 10.1021/Acsmedchemlett.9B00243  0.797
2019 Sulahian R, Kwon JJ, Walsh KH, Pailler E, Bosse TL, Thaker M, Almanza D, Dempster JM, Pan J, Piccioni F, Dumont N, Gonzalez A, Rennhack J, Nabet B, Bachman JA, ... ... Gray NS, et al. Synthetic Lethal Interaction of SHOC2 Depletion with MEK Inhibition in RAS-Driven Cancers. Cell Reports. 29: 118-134.e8. PMID 31577942 DOI: 10.1016/J.Celrep.2019.08.090  0.351
2019 Weisberg E, Meng C, Case A, Sattler M, Tiv HL, Gokhale PC, Buhrlage S, Wang J, Gray N, Stone R, Liu S, Bhagwat SV, Tiu RV, Adamia S, Griffin JD. Evaluation of ERK as a therapeutic target in acute myelogenous leukemia. Leukemia. PMID 31455850 DOI: 10.1038/S41375-019-0552-3  0.7
2019 de Wispelaere M, Du G, Donovan KA, Zhang T, Eleuteri NA, Yuan JC, Kalabathula J, Nowak RP, Fischer ES, Gray NS, Yang PL. Small molecule degraders of the hepatitis C virus protease reduce susceptibility to resistance mutations. Nature Communications. 10: 3468. PMID 31371704 DOI: 10.1038/S41467-019-11429-W  0.784
2019 Tang X, Drotar J, Li K, Clairmont CD, Brumm AS, Sullins AJ, Wu H, Liu XS, Wang J, Gray NS, Sur M, Jaenisch R. Pharmacological enhancement of gene expression exerts therapeutic effects on human Rett syndrome neurons and mutant mice. Science Translational Medicine. 11. PMID 31366578 DOI: 10.1126/Scitranslmed.Aau0164  0.446
2019 Weisberg E, Meng C, Case AE, Sattler M, Tiv HL, Gokhale PC, Buhrlage SJ, Liu X, Yang J, Wang J, Gray N, Stone RM, Adamia S, Dubreuil P, Letard S, et al. Comparison of effects of midostaurin, crenolanib, quizartinib, gilteritinib, sorafenib and BLU-285 on oncogenic mutants of KIT, CBL and FLT3 in haematological malignancies. British Journal of Haematology. PMID 31309543 DOI: 10.1111/Bjh.16092  0.762
2019 Ferguson FM, Doctor ZM, Ficarro SB, Marto JA, Kim ND, Sim T, Gray NS. Synthesis and structure activity relationships of a series of 4-amino-1H-pyrazoles as covalent inhibitors of CDK14. Bioorganic & Medicinal Chemistry Letters. PMID 31175010 DOI: 10.1016/J.Bmcl.2019.05.024  0.849
2019 Scott DA, Hatcher JM, Liu H, Fu M, Du G, Fontán L, Us I, Casalena G, Qiao Q, Wu H, Melnick A, Gray NS. Quinoline and thiazolopyridine allosteric inhibitors of MALT1. Bioorganic & Medicinal Chemistry Letters. PMID 31129051 DOI: 10.1016/J.Bmcl.2019.05.040  0.813
2019 Rodon Ahnert J, Gray N, Mok T, Gainor J. What It Takes to Improve a First-Generation Inhibitor to a Second- or Third-Generation Small Molecule. American Society of Clinical Oncology Educational Book. American Society of Clinical Oncology. Annual Meeting. 196-205. PMID 31099659 DOI: 10.1200/EDBK_242209  0.313
2019 To C, Jang J, Chen T, Park E, Mushajiang M, De Clercq DJH, Xu M, Wang S, Cameron MD, Heppner DE, Shin BH, Gero TW, Yang A, Dahlberg SE, Wong KK, ... ... Gray NS, et al. Single and dual targeting of mutant EGFR with an allosteric inhibitor. Cancer Discovery. PMID 31092401 DOI: 10.1158/2159-8290.Cd-18-0903  0.853
2019 Du L, Anderson A, Nguyen K, Ojeda SS, Ortiz-Rivera I, Nguyen TN, Zhang T, Kaoud TS, Gray NS, Dalby KN, Tsai KY. JNK2 is required for tumorigenic properties of melanoma cells. Acs Chemical Biology. PMID 31063355 DOI: 10.1021/acschembio.9b00083  0.368
2019 Rao S, Gurbani D, Du G, Everley RA, Browne CM, Chaikuad A, Li T, Schröder M, Gondi S, Ficarro SB, Sim T, Kim ND, Berberich MJ, Knapp S, Marto JA, ... ... Gray NS, et al. Leveraging Compound Promiscuity to Identify Targetable Cysteines within the Kinome. Cell Chemical Biology. PMID 30982749 DOI: 10.1016/J.Chembiol.2019.02.021  0.86
2019 Moret N, Clark NA, Hafner M, Wang Y, Lounkine E, Medvedovic M, Wang J, Gray N, Jenkins J, Sorger PK. Cheminformatics Tools for Analyzing and Designing Optimized Small-Molecule Collections and Libraries. Cell Chemical Biology. PMID 30956147 DOI: 10.1016/J.Chembiol.2019.02.018  0.555
2019 Hatcher JM, Du G, Fontán L, Us I, Qiao Q, Chennamadhavuni S, Shao J, Wu H, Melnick A, Gray NS, Scott DA. Peptide-based covalent inhibitors of MALT1 paracaspase. Bioorganic & Medicinal Chemistry Letters. PMID 30954428 DOI: 10.1016/J.Bmcl.2019.03.046  0.826
2019 Ferguson FM, Doctor ZM, Ficarro SB, Browne CM, Marto JA, Johnson JL, Yaron TM, Cantley LC, Kim ND, Sim T, Berberich MJ, Kalocsay M, Sorger PK, Gray NS. Discovery of Covalent CDK14 Inhibitors with Pan-TAIRE Family Specificity. Cell Chemical Biology. PMID 30930164 DOI: 10.1016/J.Chembiol.2019.02.015  0.863
2019 Silva MC, Ferguson FM, Cai Q, Donovan KA, Nandi G, Patnaik D, Zhang T, Huang HT, Lucente DE, Dickerson BC, Mitchison TJ, Fischer ES, Gray NS, Haggarty SJ. Targeted degradation of aberrant tau in frontotemporal dementia patient-derived neuronal cell models. Elife. 8. PMID 30907729 DOI: 10.7554/Elife.45457  0.775
2019 Olson CM, Liang Y, Leggett A, Park WD, Li L, Mills CE, Elsarrag SZ, Ficarro SB, Zhang T, Düster R, Geyer M, Sim T, Marto JA, Sorger PK, Westover KD, ... ... Gray NS, et al. Development of a Selective CDK7 Covalent Inhibitor Reveals Predominant Cell-Cycle Phenotype. Cell Chemical Biology. PMID 30905681 DOI: 10.1016/J.Chembiol.2019.02.012  0.859
2019 Rao S, Du G, Hafner M, Subramanian K, Sorger PK, Gray NS. A multi-targeted probe-based strategy to identify signaling vulnerabilities in cancers. The Journal of Biological Chemistry. PMID 30858179 DOI: 10.1074/Jbc.Ra118.006805  0.845
2019 Jiang B, Wang ES, Donovan KA, Liang Y, Fischer ES, Zhang T, Gray NS. Development of dual and selective degraders of cyclin-dependent kinases 4 and 6. Angewandte Chemie (International Ed. in English). PMID 30802347 DOI: 10.1002/Anie.201901336  0.817
2019 Sung Hsieh HH, Agarwal S, Cholok DJ, Loder SJ, Kaneko K, Huber A, Chung MT, Ranganathan K, Habbouche J, Li J, Butts J, Reimer J, Kaura A, Drake J, Breuler C, ... ... Gray N, et al. Coordinating Tissue Regeneration through TGF-β Activated Kinase 1 (TAK1) In-activation and Re-activation. Stem Cells (Dayton, Ohio). PMID 30786091 DOI: 10.1002/Stem.2991  0.634
2019 Pitts J, Hsia CY, Lian W, Wang J, Pfeil MP, Kwiatkowski N, Li Z, Jang J, Gray NS, Yang PL. Identification of small molecule inhibitors targeting the Zika virus envelope protein. Antiviral Research. PMID 30771406 DOI: 10.1016/J.Antiviral.2019.02.008  0.784
2019 Wang L, Ferrao R, Li Q, Hatcher JM, Choi HG, Buhrlage SJ, Gray NS, Wu H. Conformational flexibility and inhibitor binding to unphosphorylated interleukin-1 receptor-associated kinase 4 (IRAK4). The Journal of Biological Chemistry. PMID 30679311 DOI: 10.1074/Jbc.Ra118.005428  0.828
2019 Sharifnia T, Wawer MJ, Chen T, Huang QY, Weir BA, Sizemore A, Lawlor MA, Goodale A, Cowley GS, Vazquez F, Ott CJ, Francis JM, Sassi S, Cogswell P, Sheppard HE, ... ... Gray NS, et al. Small-molecule targeting of brachyury transcription factor addiction in chordoma. Nature Medicine. PMID 30664779 DOI: 10.1038/S41591-018-0312-3  0.36
2019 Li PC, Jang J, Hsia CY, Groomes P, Lian W, de Wispelaere M, Pitts JD, Wang J, Kwaitkowski N, Gray NS, Yang PL. Small molecules targeting the flavivirus E protein with broad-spectrum activity and antiviral efficacy in vivo. Acs Infectious Diseases. PMID 30608640 DOI: 10.1021/Acsinfecdis.8B00322  0.778
2019 De Matos Simoes R, Shirasaki R, Downey-Kopyscinski SL, Matthews G, Yiguo H, Sheffer M, Dhimolea E, Dashevsky O, Gandolfi S, Dempster J, Meyers RM, Bryan J, McFarland JM, Brueggenthies J, Tang H, ... ... Gray N, et al. Systematic Characterization of Genes Representing Preferential Molecular Vulnerabilities for Myeloma Cells Compared to Other Neoplasias - Implications for the Biology and Therapeutic Targeting of Myeloma Blood. 134: 4407-4407. DOI: 10.1182/Blood-2019-130901  0.383
2019 Fontan L, Hatcher J, Scott D, Qiao Q, Us I, Du G, Durant M, Wilson J, Wu H, Gray N, Melnick A. Chemically Induced Degradation of MALT1 to Treat B-Cell Lymphomas Blood. 134: 2073-2073. DOI: 10.1182/Blood-2019-130666  0.843
2019 Yang G, Wang J, Liu X, Munshi M, Chen JG, Kofides A, Xu L, Tsakmaklis N, Demos M, Guerrera ML, Chan GG, Jimenez C, Hunter ZR, Patterson C, Castillo JJ, ... ... Gray N, et al. A Novel HCK and BTK Dual Inhibitor Kin-8194 Shows Superior Activity over Ibrutinib and Overcomes BTKC481S Mediated Ibrutinib Resistance in Vitro and In Vivo in MYD88 Mutated B-Cell Lymphomas Blood. 134: 394-394. DOI: 10.1182/Blood-2019-130636  0.738
2019 Shirasaki R, Gandolfi S, De Matos Simoes R, Matthews GM, Buckley D, Raja J, Sievers QL, Dashevsky O, Poarch H, Tang H, Bariteau M, Sheffer M, Downey-Kopyscinski SL, Hengeveld P, Glassner B, ... ... Gray N, et al. Functional Characterization of E3 Ligases and Their Regulators: Therapeutic Implications for Development of New Proteolysis-Targeting Chimeric Degraders of Oncoproteins Blood. 134: 318-318. DOI: 10.1182/Blood-2019-130549  0.341
2019 Lin S, Tarumoto Y, Wang J, Milazzo J, Xu Y, Gray N, Vakoc C, Stegmaier K. Targeting Salt-Inducible Kinase 3 As a Therapeutic Approach for Acute Myeloid Leukemia Blood. 134: 3941-3941. DOI: 10.1182/Blood-2019-125278  0.606
2019 Morita K, He S, Nowak RP, Wang J, Gray N, Fischer ES, Look AT. Targeting T-ALL Cells with Potent Activators of the PP2A Protein Phosphatase Tumor Suppressor Blood. 134: 406-406. DOI: 10.1182/Blood-2019-123573  0.499
2019 Shaughnessy M, La Muraglia G, Rajadurai A, Kumar R, Olson C, Jiang B, Gray N, Tsao H. 705 Cyclin-dependent kinase 9 (CDK9) as a therapeutic target in uveal and triple-wild type melanoma Journal of Investigative Dermatology. 139: S121. DOI: 10.1016/J.Jid.2019.03.781  0.797
2019 Shirasaki R, de Matos Simoes R, Downey-Kopyscinski S, Matthews G, Hu Y, Sheffer M, Dhimolea E, Dashevsky O, Gandolfi S, Hengeveld P, Dempster J, Meyers R, Bryan J, Dharia N, McFarland J, ... ... Gray N, et al. CRISPR studies identify genes preferentially essential for myeloma cells vs. other neoplasias: implications for future therapies selective against MM Clinical Lymphoma Myeloma and Leukemia. 19: e48-e49. DOI: 10.1016/J.Clml.2019.09.073  0.304
2019 Szalat R, Lawlor M, Fulciniti M, Epstein CB, Xu Y, Samur A, Lin C, Rao P, farrell N, Wu S, Schwartz L, Wen K, Tai Y, Wang J, Gray N, et al. Genome wide chromatin accessibility profiling identifies chromatin signatures and novel transcription factor dependencies in multiple myeloma Clinical Lymphoma Myeloma and Leukemia. 19: e8-e9. DOI: 10.1016/J.Clml.2019.09.011  0.416
2018 Brand M, Jiang B, Bauer S, Donovan KA, Liang Y, Wang ES, Nowak RP, Yuan JC, Zhang T, Kwiatkowski N, Müller AC, Fischer ES, Gray NS, Winter GE. Homolog-Selective Degradation as a Strategy to Probe the Function of CDK6 in AML. Cell Chemical Biology. PMID 30595531 DOI: 10.1016/J.Chembiol.2018.11.006  0.782
2018 Dobrovolsky D, Wang ES, Morrow S, Leahy C, Faust T, Nowak RP, Donovan KA, Yang G, Li Z, Fischer ES, Treon SP, Weinstock DM, Gray NS. Bruton's Tyrosine Kinase degradation as a therapeutic strategy for cancer. Blood. PMID 30545835 DOI: 10.1182/Blood-2018-07-862953  0.852
2018 Browne CM, Jiang B, Ficarro SB, Doctor ZM, Johnson JL, Card JD, Sivakumaren SC, Alexander WM, Yaron T, Murphy CJ, Kwiatkowski NP, Zhang T, Cantley LC, Gray NS, Marto JA. A Chemoproteomic Strategy for Direct and Proteome-wide Covalent Inhibitor Target-site Identification. Journal of the American Chemical Society. PMID 30518210 DOI: 10.1021/Jacs.8B07911  0.848
2018 Brien GL, Remillard D, Shi J, Hemming ML, Chabon J, Wynne K, Dillon ET, Cagney G, Van Mierlo G, Baltissen MP, Vermeulen M, Qi J, Fröhling S, Gray NS, Bradner JE, et al. Targeted degradation of BRD9 reverses oncogenic gene expression in synovial sarcoma. Elife. 7. PMID 30431433 DOI: 10.7554/Elife.41305  0.307
2018 Zeng M, Kwiatkowski NP, Zhang T, Nabet B, Xu M, Liang Y, Quan C, Wang J, Hao M, Palakurthi S, Zhou S, Zeng Q, Kirschmeier PT, Meghani K, Leggett AL, ... ... Gray NS, et al. Targeting MYC dependency in ovarian cancer through inhibition of CDK7 and CDK12/13. Elife. 7. PMID 30422115 DOI: 10.7554/Elife.39030  0.691
2018 Tusa I, Cheloni G, Poteti M, Gozzini A, DeSouza NH, Shan Y, Deng X, Gray NS, Li S, Rovida E, Dello Sbarba P. Targeting the Extracellular Signal-Regulated Kinase 5 Pathway to Suppress Human Chronic Myeloid Leukemia Stem Cells. Stem Cell Reports. PMID 30245209 DOI: 10.1016/J.Stemcr.2018.08.016  0.594
2018 Lizotte PH, Hong RL, Luster TA, Cavanaugh ME, Taus LJ, Wang S, Dhaneshwar A, Mayman N, Yang A, Kulkarni M, Badalucco L, Fitzpatrick E, Kao HF, Kuraguchi M, Bittinger MA, ... ... Gray NS, et al. A high-throughput immune-oncology screen identifies EGFR inhibitors as potent enhancers of antigen-specific cytotoxic T-lymphocyte tumor cell killing. Cancer Immunology Research. PMID 30242021 DOI: 10.1158/2326-6066.Cir-18-0193  0.336
2018 Cho H, Shin I, Joo E, Choi S, Hur W, Kim H, Hong E, Kim ND, Choi HG, Gray NS, Sim T. First SAR study for overriding NRAS mutant driven acute myeloid leukemia. Journal of Medicinal Chemistry. PMID 30153003 DOI: 10.1021/acs.jmedchem.8b00882  0.655
2018 Wang J, Erazo T, Ferguson FM, Buckley DL, Gomez N, Muñoz-Guardiola P, Diéguez-Martínez N, Deng X, Hao M, Massefski W, Fedorov O, Offei-Addo NK, Park PM, Dai L, DiBona A, ... ... Gray NS, et al. Structural and atropisomeric factors governing the selectivity of pyrimido-benzodiazipinones as inhibitors of kinases and bromodomains. Acs Chemical Biology. PMID 30102854 DOI: 10.2210/Pdb6Cd5/Pdb  0.867
2018 Czarna A, Wang J, Zelencova D, Liu Y, Deng X, Choi HG, Zhang T, Zhou W, Chang JW, Kildalsen H, Seternes OM, Gray NS, Engh RA, Rothweiler U. Novel scaffolds for Dual specificity tyrosine-phosphorylation-regulated kinase (DYRK1A) inhibitors. Journal of Medicinal Chemistry. PMID 30095246 DOI: 10.1021/acs.jmedchem.7b01847  0.723
2018 Lian W, Jang J, Potisopon S, Li PC, Rahmeh A, Wang J, Kwiatkowski NP, Gray NS, Yang PL. Discovery of Immunologically Inspired Small Molecules that Target the Viral Envelope Protein. Acs Infectious Diseases. PMID 30027735 DOI: 10.1021/Acsinfecdis.8B00127  0.787
2018 Fontán L, Qiao Q, Hatcher JM, Casalena G, Us I, Teater M, Durant M, Du G, Xia M, Bilchuk N, Chennamadhavuni S, Palladino G, Inghirami G, Philippar U, Wu H, ... ... Gray NS, et al. Specific covalent inhibition of MALT1 paracaspase suppresses B cell lymphoma growth. The Journal of Clinical Investigation. PMID 30024860 DOI: 10.1172/Jci99436  0.83
2018 Chen S, Cai C, Sowalsky AG, Ye H, Ma F, Yuan X, Simon NI, Gray NS, Balk SP. BMX-mediated regulation of multiple tyrosine kinases contributes to castration resistance in prostate cancer. Cancer Research. PMID 30012673 DOI: 10.1158/0008-5472.Can-17-3615  0.374
2018 Chao LH, Jang J, Johnson A, Nguyen A, Gray N, Yang PL, Harrison SC. How small-molecule inhibitors of dengue-virus infection interfere with viral membrane fusion. Elife. 7. PMID 29999491 DOI: 10.7554/Elife.36461  0.719
2018 Jang J, Son J, Park E, Kosaka T, Saxon JA, De Clercq D, Choi HG, Tanizaki J, Eck MJ, Jänne PA, Gray NS. Discovery of a Highly Potent and Broadly Effective EGFR and HER2 Exon 20 Insertion Mutant Inhibitor. Angewandte Chemie (International Ed. in English). PMID 29978938 DOI: 10.1002/Anie.201805187  0.823
2018 Hatcher JM, Wang ES, Johannessen L, Kwiatkowski N, Sim T, Gray NS. Development of Highly Potent and Selective Steroidal Inhibitors and Degraders of CDK8. Acs Medicinal Chemistry Letters. 9: 540-545. PMID 29937979 DOI: 10.1021/Acsmedchemlett.8B00011  0.823
2018 de Wispelaere M, Lian W, Potisopon S, Li PC, Jang J, Ficarro SB, Clark MJ, Zhu X, Kaplan JB, Pitts JD, Wales TE, Wang J, Engen JR, Marto JA, Gray NS, et al. Inhibition of Flaviviruses by Targeting a Conserved Pocket on the Viral Envelope Protein. Cell Chemical Biology. PMID 29937406 DOI: 10.1016/J.Chembiol.2018.05.011  0.814
2018 Nowak RP, DeAngelo SL, Buckley D, He Z, Donovan KA, An J, Safaee N, Jedrychowski MP, Ponthier CM, Ishoey M, Zhang T, Mancias JD, Gray NS, Bradner JE, Fischer ES. Plasticity in binding confers selectivity in ligand-induced protein degradation. Nature Chemical Biology. PMID 29892083 DOI: 10.1038/S41589-018-0055-Y  0.705
2018 Weir MC, Shu ST, Patel RK, Hellwig S, Chen L, Tan L, Gray NS, Smithgall TE. Selective inhibition of the myeloid Src-family kinase Fgr potently suppresses AML cell growth in vitro and in vivo. Acs Chemical Biology. PMID 29763550 DOI: 10.1021/Acschembio.8B00154  0.437
2018 Powell CE, Gao Y, Tan L, Donovan KA, Nowak RP, Loehr A, Bahcall M, Fischer ES, Janne PA, George RE, Gray NS. Chemically Induced Degradation of Anaplastic Lymphoma Kinase (ALK). Journal of Medicinal Chemistry. PMID 29660984 DOI: 10.1021/Acs.Jmedchem.7B01655  0.764
2018 Bockorny B, Rusan M, Chen W, Liao RG, Li Y, Piccioni F, Wang J, Tan L, Thorner AR, Li T, Zhang Y, Miao CH, Ovesen T, Shapiro GI, Kwiatkowski DJ, ... Gray NS, et al. RAS-MAPK reactivation facilitates acquired resistance in FGFR1-amplified lung cancer and underlies a rationale for upfront FGFR-MEK blockade. Molecular Cancer Therapeutics. PMID 29654068 DOI: 10.1158/1535-7163.Mct-17-0464  0.366
2018 Ferguson FM, Gray NS. Kinase inhibitors: the road ahead. Nature Reviews. Drug Discovery. PMID 29545548 DOI: 10.1038/Nrd.2018.21  0.803
2018 Giurisato E, Xu Q, Lonardi S, Telfer B, Russo I, Pearson A, Finegan KG, Wang W, Wang J, Gray NS, Vermi W, Xia Z, Tournier C. Myeloid ERK5 deficiency suppresses tumor growth by blocking protumor macrophage polarization via STAT3 inhibition. Proceedings of the National Academy of Sciences of the United States of America. PMID 29507229 DOI: 10.1073/Pnas.1707929115  0.475
2018 Chen JG, Liu X, Munshi M, Xu L, Tsakmaklis N, Demos MG, Kofides A, Guerrera ML, Chan GG, Patterson CJ, Meid KE, Gustine J, Dubeau T, Severns P, Castillo JJ, ... ... Gray NS, et al. BTKdrives ibrutinib resistance via ERK1/2, and protects BTKMYD88 mutated cells by a paracrine mechanism. Blood. PMID 29496671 DOI: 10.1182/Blood-2017-10-811752  0.68
2018 Tusa I, Gagliardi S, Tubita A, Pandolfi S, Urso C, Borgognoni L, Wang J, Deng X, Gray NS, Stecca B, Rovida E. ERK5 is activated by oncogenic BRAF and promotes melanoma growth. Oncogene. PMID 29483645 DOI: 10.1038/S41388-018-0164-9  0.702
2018 Hatcher JM, Wu G, Zeng C, Zhu J, Meng F, Patel S, Wang W, Ficarro SB, Leggett AL, Powell CE, Marto JA, Zhang K, Ki Ngo JC, Fu XD, Zhang T, ... Gray NS, et al. SRPKIN-1: A Covalent SRPK1/2 Inhibitor that Potently Converts VEGF from Pro-angiogenic to Anti-angiogenic Isoform. Cell Chemical Biology. PMID 29478907 DOI: 10.1016/J.Chembiol.2018.01.013  0.841
2018 Jeselsohn R, Bergholz JS, Pun M, Cornwell M, Liu W, Nardone A, Xiao T, Li W, Qiu X, Buchwalter G, Feiglin A, Abell-Hart K, Fei T, Rao P, Long H, ... ... Gray N, et al. Allele-Specific Chromatin Recruitment and Therapeutic Vulnerabilities of ESR1 Activating Mutations. Cancer Cell. 33: 173-186.e5. PMID 29438694 DOI: 10.1016/J.Ccell.2018.01.004  0.307
2018 Eliades P, Abraham BJ, Ji Z, Miller DM, Christensen CL, Kwiatkowski N, Kumar R, Njauw CN, Taylor M, Miao B, Zhang T, Wong KK, Gray NS, Young RA, Tsao H. High MITF Expression is Associated with Super-enhancers and Suppressed by CDK7 Inhibition in Melanoma. The Journal of Investigative Dermatology. PMID 29408204 DOI: 10.1016/J.Jid.2017.09.056  0.305
2018 Zheng Y, Sethi R, Mangala LS, Taylor C, Goldsmith J, Wang M, Masuda K, Karaminejadranjbar M, Mannion D, Miranda F, Herrero-Gonzalez S, Hellner K, Chen F, Alsaadi A, Albukhari A, ... ... Gray NS, et al. Tuning microtubule dynamics to enhance cancer therapy by modulating FER-mediated CRMP2 phosphorylation. Nature Communications. 9: 476. PMID 29396402 DOI: 10.1038/S41467-017-02811-7  0.329
2018 Iniguez AB, Stolte B, Wang EJ, Conway AS, Alexe G, Dharia NV, Kwiatkowski N, Zhang T, Abraham BJ, Mora J, Kalev P, Leggett A, Chowdhury D, Benes CH, Young RA, ... Gray NS, et al. EWS/FLI Confers Tumor Cell Synthetic Lethality to CDK12 Inhibition in Ewing Sarcoma. Cancer Cell. PMID 29358035 DOI: 10.1016/J.Ccell.2017.12.009  0.389
2018 Ott CJ, Szalat R, Lawlor M, Samur MK, Xu Y, Epstein CB, Lin CY, Prabhala R, Farrell N, Walter LD, Schwartz L, Wen K, Tai Y, Fulciniti M, Wang J, ... Gray N, et al. Chromatin Accessibility Profiling Reveals Cis-Regulatory Heterogeneity and Novel Transcription Factor Dependencies in Multiple Myeloma Blood. 132: 1313-1313. DOI: 10.1182/Blood-2018-99-119941  0.52
2018 Morrow S, Dobrovolsky D, Wang E, Nowak RP, Donovan K, Faust T, Yang G, Li Z, Fischer E, Treon SP, Weinstock DM, Gray NS. Triple Degradation of BTK, IKZF1 and IKZF3 in B-Cell Malignancies Blood. 132: 263-263. DOI: 10.1182/Blood-2018-99-116895  0.859
2018 Shirasaki R, Gandolfi S, Simoes RDM, Matthews G, Downey S, Dashevsky O, Huihui T, Sheffer M, Dhimolea E, Bariteau M, Sorrel J, Kwiatkowski N, Zhang T, Gray N, Mitsiades C. Abstract 2834: Genomewide CRISPR studies of sequential treatment with CRBN-based degronimids: Insights into the molecular evolution of treatment resistance in myeloma and beyond Cancer Research. 78: 2834-2834. DOI: 10.1158/1538-7445.Am2018-2834  0.41
2018 Tan L, Gray NS. When Kinases Meet PROTACs Chinese Journal of Chemistry. 36: 971-977. DOI: 10.1002/Cjoc.201800293  0.328
2017 Gao Y, Zhang T, Terai H, Ficarro SB, Kwiatkowski N, Hao MF, Sharma B, Christensen CL, Chipumuro E, Wong KK, Marto JA, Hammerman PS, Gray NS, George RE. Overcoming Resistance to the THZ Series of Covalent Transcriptional CDK Inhibitors. Cell Chemical Biology. PMID 29276047 DOI: 10.1016/J.Chembiol.2017.11.007  0.606
2017 Terai H, Kitajima S, Potter DS, Matsui Y, Gutierrez Quiceno L, Chen T, Kim TJ, Rusan M, Thai TC, Piccioni F, Donovan KA, Kwiatkowski N, Hinohara K, Wei G, Gray NS, et al. ER stress signaling promotes the survival of cancer 'persister cells' tolerant to EGFR tyrosine kinase inhibitors. Cancer Research. PMID 29259014 DOI: 10.1158/0008-5472.Can-17-1904  0.371
2017 Olson CM, Jiang B, Erb MA, Liang Y, Doctor ZM, Zhang Z, Zhang T, Kwiatkowski N, Boukhali M, Green JL, Haas W, Nomanbhoy T, Fischer ES, Young RA, Bradner JE, ... ... Gray NS, et al. Pharmacological perturbation of CDK9 using selective CDK9 inhibition or degradation. Nature Chemical Biology. PMID 29251720 DOI: 10.1038/Nchembio.2538  0.854
2017 Wang L, Qiao Q, Ferrao R, Shen C, Hatcher JM, Buhrlage SJ, Gray NS, Wu H. Crystal structure of human IRAK1. Proceedings of the National Academy of Sciences of the United States of America. PMID 29208712 DOI: 10.1073/Pnas.1714386114  0.828
2017 Huang HT, Dobrovolsky D, Paulk J, Yang G, Weisberg EL, Doctor ZM, Buckley DL, Cho JH, Ko E, Jang J, Shi K, Choi HG, Griffin JD, Li Y, Treon SP, ... ... Gray NS, et al. A Chemoproteomic Approach to Query the Degradable Kinome Using a Multi-kinase Degrader. Cell Chemical Biology. PMID 29129717 DOI: 10.1016/J.Chembiol.2017.10.005  0.845
2017 Deng J, Wang ES, Jenkins RW, Li S, Dries R, Yates K, Chhabra S, Huang W, Liu H, Aref AR, Ivanova E, Paweletz CP, Bowden M, Zhou CW, Herter-Sprie GS, ... ... Gray NS, et al. CDK4/6 Inhibition Augments Anti-Tumor Immunity by Enhancing T Cell Activation. Cancer Discovery. PMID 29101163 DOI: 10.1158/2159-8290.Cd-17-0915  0.363
2017 Rusan M, Li K, Li Y, Christensen CL, Abraham BJ, Kwiatkowski N, Buczkowski KA, Bockorny B, Chen T, Li S, Rhee K, Zhang H, Chen W, Terai H, Tavares T, ... ... Gray NS, et al. Suppression of adaptive responses to targeted cancer therapy by transcriptional repression. Cancer Discovery. PMID 29054992 DOI: 10.1158/2159-8290.Cd-17-0461  0.318
2017 Kalan S, Amat R, Schachter MM, Kwiatkowski N, Abraham BJ, Liang Y, Zhang T, Olson CM, Larochelle S, Young RA, Gray NS, Fisher RP. Activation of the p53 Transcriptional Program Sensitizes Cancer Cells to Cdk7 Inhibitors. Cell Reports. 21: 467-481. PMID 29020632 DOI: 10.1016/J.Celrep.2017.09.056  0.832
2017 Weisberg EL, Schauer NJ, Yang J, Lamberto I, Doherty L, Bhatt S, Nonami A, Meng C, Letai A, Wright R, Tiv H, Gokhale PC, Ritorto MS, De Cesare V, Trost M, ... ... Gray NS, et al. Inhibition of USP10 induces degradation of oncogenic FLT3. Nature Chemical Biology. PMID 28967922 DOI: 10.1038/Nchembio.2486  0.748
2017 Huang HT, Seo HS, Zhang T, Wang Y, Jiang B, Li Q, Buckley DL, Nabet B, Roberts JM, Paulk J, Dastjerdi S, Winter GE, McLauchlan H, Moran J, Bradner JE, ... ... Gray NS, et al. MELK is not necessary for the proliferation of basal-like breast cancer cells. Elife. 6. PMID 28926338 DOI: 10.7554/Elife.26693  0.789
2017 Gilbert AS, Seoane PI, Sephton-Clark P, Bojarczuk A, Hotham R, Giurisato E, Sarhan AR, Hillen A, Velde GV, Gray NS, Alessi DR, Cunningham DL, Tournier C, Johnston SA, May RC. Vomocytosis of live pathogens from macrophages is regulated by the atypical MAP kinase ERK5. Science Advances. 3: e1700898. PMID 28835924 DOI: 10.1126/Sciadv.1700898  0.595
2017 Ferguson FM, Doctor ZM, Chaikuad A, Sim T, Kim ND, Knapp S, Gray NS. Characterization of a highly selective inhibitor of the Aurora kinases. Bioorganic & Medicinal Chemistry Letters. PMID 28818446 DOI: 10.1016/J.Bmcl.2017.08.016  0.867
2017 Johannessen L, Sundberg TB, O'Connell DJ, Kolde R, Berstler J, Billings KJ, Khor B, Seashore-Ludlow B, Fassl A, Russell CN, Latorre IJ, Jiang B, Graham DB, Perez JR, Sicinski P, ... ... Gray NS, et al. Small-molecule studies identify CDK8 as a regulator of IL-10 in myeloid cells. Nature Chemical Biology. PMID 28805801 DOI: 10.1038/Nchembio.2458  0.811
2017 Zeng M, Lu J, Li L, Feru F, Quan C, Gero TW, Ficarro SB, Xiong Y, Ambrogio C, Paranal RM, Catalano M, Shao J, Wong KK, Marto JA, Fischer ES, ... ... Gray NS, et al. Potent and Selective Covalent Quinazoline Inhibitors of KRAS G12C. Cell Chemical Biology. PMID 28781124 DOI: 10.1016/J.Chembiol.2017.06.017  0.833
2017 Lu J, Harrison RA, Li L, Zeng M, Gondi S, Scott D, Gray NS, Engen JR, Westover KD. KRAS G12C Drug Development: Discrimination between Switch II Pocket Configurations Using Hydrogen/Deuterium-Exchange Mass Spectrometry. Structure (London, England : 1993). PMID 28781083 DOI: 10.1016/J.Str.2017.07.003  0.692
2017 Drewry DH, Wells CI, Andrews DM, Angell R, Al-Ali H, Axtman AD, Capuzzi SJ, Elkins JM, Ettmayer P, Frederiksen M, Gileadi O, Gray N, Hooper A, Knapp S, Laufer S, et al. Progress towards a public chemogenomic set for protein kinases and a call for contributions. Plos One. 12: e0181585. PMID 28767711 DOI: 10.1371/Journal.Pone.0181585  0.493
2017 Wong KK, Liu Y, Li Y, Wang X, Liu F, Gao P, Quinn MM, Li F, Merlino AA, Benes CH, Liu Q, Gray NS. Gemcitabine and Chk1 inhibitor AZD7762 synergistically suppress the growth of Lkb1-deficient lung adenocarcinoma. Cancer Research. PMID 28754670 DOI: 10.1158/0008-5472.Can-17-0567  0.571
2017 Weir MC, Hellwig S, Tan L, Liu Y, Gray NS, Smithgall TE. Dual inhibition of Fes and Flt3 tyrosine kinases potently inhibits Flt3-ITD+ AML cell growth. Plos One. 12: e0181178. PMID 28727840 DOI: 10.1371/Journal.Pone.0181178  0.492
2017 Winter GE, Mayer A, Buckley DL, Erb MA, Roderick JE, Vittori S, Reyes JM, di Iulio J, Souza A, Ott CJ, Roberts JM, Zeid R, Scott TG, Paulk J, Lachance K, ... ... Gray NS, et al. BET Bromodomain Proteins Function as Master Transcription Elongation Factors Independent of CDK9 Recruitment. Molecular Cell. PMID 28673542 DOI: 10.1016/J.Molcel.2017.06.004  0.798
2017 Wang B, Deng Y, Chen Y, Yu K, Wang A, Liang Q, Wang W, Chen C, Wu H, Hu C, Miao W, Hur W, Wang W, Hu Z, Weisberg EL, ... ... Gray NS, et al. Structure-activity relationship investigation for benzonaphthyridinone derivatives as novel potent Bruton's tyrosine kinase (BTK) irreversible inhibitors. European Journal of Medicinal Chemistry. 137: 545-557. PMID 28628824 DOI: 10.1016/J.Ejmech.2017.06.016  0.707
2017 Mujahid N, Liang Y, Murakami R, Choi HG, Dobry AS, Wang J, Suita Y, Weng QY, Allouche J, Kemeny LV, Hermann AL, Roider EM, Gray NS, Fisher DE. A UV-Independent Topical Small-Molecule Approach for Melanin Production in Human Skin. Cell Reports. 19: 2177-2184. PMID 28614705 DOI: 10.1016/J.Celrep.2017.05.042  0.376
2017 Williams CAC, Gray NS, Findlay GM. A Simple Method to Identify Kinases That Regulate Embryonic Stem Cell Pluripotency by High-throughput Inhibitor Screening. Journal of Visualized Experiments : Jove. PMID 28570543 DOI: 10.3791/55515  0.395
2017 Zwang Y, Jonas O, Chen C, Rinne ML, Doench JG, Piccioni F, Tan L, Huang HT, Wang J, Ham YJ, O'Connell J, Bhola P, Doshi M, Whitman M, Cima M, ... ... Gray NS, et al. Synergistic interactions with PI3K inhibition that induce apoptosis. Elife. 6. PMID 28561737 DOI: 10.7554/Elife.24523  0.564
2017 Jang J, Son JB, To C, Bahcall M, Kim SY, Kang SY, Mushajiang M, Lee Y, Jänne PA, Choi HG, Gray NS. Discovery of a potent dual ALK and EGFR T790M inhibitor. European Journal of Medicinal Chemistry. 136: 497-510. PMID 28528303 DOI: 10.1016/J.Ejmech.2017.04.079  0.755
2017 Vollmer S, Strickson S, Zhang T, Gray N, Lee K, Rao V, Cohen P. The mechanism of activation of IRAK1 and IRAK4 by interleukin-1 and Toll-Like receptor agonists. The Biochemical Journal. PMID 28512203 DOI: 10.1042/Bcj20170097  0.363
2017 Manier S, Huynh D, Shen YJ, Zhou J, Yusufzai T, Salem KZ, Ebright RY, Shi J, Park J, Glavey SV, Devine WG, Liu CJ, Leleu X, Quesnel B, Roche-Lestienne C, ... ... Gray N, et al. Inhibiting the oncogenic translation program is an effective therapeutic strategy in multiple myeloma. Science Translational Medicine. 9. PMID 28490664 DOI: 10.1126/Scitranslmed.Aal2668  0.618
2017 Hatcher JM, Choi HG, Alessi DR, Gray NS. Small-Molecule Inhibitors of LRRK2. Advances in Neurobiology. 14: 241-264. PMID 28353288 DOI: 10.1007/978-3-319-49969-7_13  0.844
2017 Wu H, Huang Q, Qi Z, Chen Y, Wang A, Chen C, Liang Q, Wang J, Chen W, Dong J, Yu K, Hu C, Wang W, Liu X, Deng Y, ... ... Gray NS, et al. Irreversible inhibition of BTK kinase by a novel highly selective inhibitor CHMFL-BTK-11 suppresses inflammatory response in rheumatoid arthritis model. Scientific Reports. 7: 466. PMID 28352114 DOI: 10.1038/S41598-017-00482-4  0.626
2017 Liang Y, de Wispelaere M, Carocci M, Liu Q, Wang J, Yang PL, Gray NS. Structure-Activity Relationship Study of QL47: A Broad-Spectrum Antiviral Agent. Acs Medicinal Chemistry Letters. 8: 344-349. PMID 28337328 DOI: 10.1021/Acsmedchemlett.7B00008  0.758
2017 Cayrol F, Praditsuktavorn P, Fernando TM, Kwiatkowski N, Marullo R, Calvo-Vidal MN, Phillip J, Pera B, Yang SN, Takpradit K, Roman L, Gaudiano M, Crescenzo R, Ruan J, Inghirami G, ... ... Gray NS, et al. THZ1 targeting CDK7 suppresses STAT transcriptional activity and sensitizes T-cell lymphomas to BCL2 inhibitors. Nature Communications. 8: 14290. PMID 28134252 DOI: 10.1038/Ncomms14290  0.38
2017 Xiong Y, Lu J, Hunter J, Li L, Scott D, Choi HG, Lim SM, Manandhar A, Gondi S, Sim T, Westover KD, Gray NS. Covalent Guanosine Mimetic Inhibitors of G12C KRAS. Acs Medicinal Chemistry Letters. 8: 61-66. PMID 28105276 DOI: 10.1021/Acsmedchemlett.6B00373  0.744
2017 Sun Y, Alberta JA, Pilarz C, Calligaris D, Chadwick EJ, Ramkissoon SH, Ramkissoon LA, Garcia VM, Mazzola E, Goumnerova L, Kane M, Yao Z, Kieran MW, Ligon KL, Hahn WC, ... ... Gray NS, et al. A brain-penetrant RAF dimer antagonist for the noncanonical BRAF oncoprotein of pediatric low-grade astrocytomas. Neuro-Oncology. PMID 28082416 DOI: 10.1093/Neuonc/Now261  0.662
2017 Zwang Y, Jonas O, Chen C, Rinne ML, Doench JG, Piccioni F, Tan L, Huang H, Wang J, Ham YJ, O'Connell J, Bhola P, Doshi M, Whitman M, Cima M, ... ... Gray N, et al. Author response: Synergistic interactions with PI3K inhibition that induce apoptosis Elife. DOI: 10.7554/Elife.24523.023  0.456
2017 Yang G, Hatcher J, Wang J, Liu X, Munshi M, Chen J, Xu L, Tsakmaklis N, Demos M, Kofides A, Chan G, Hunter Z, Patterson C, Gustine J, Castillo JJ, ... Gray N, et al. A Novel, Highly Selective IRAK1 Inhibitor Jh-X-119-01 Shows Synergistic Tumor Cell Killing with Ibrutinib in MYD88 Mutated B-Cell Lymphoma Cells Blood. 130: 719-719. DOI: 10.1182/Blood.V130.Suppl_1.719.719  0.809
2017 Weir MC, Shu S, Hellwig S, Patel R, Chen L, Tan L, Gray N, Smithgall T. A Unique N-Phenylbenzamide Inhibitor Targeting Non-Receptor Tyrosine Kinases Potently Suppresses AML Cell Growth In Vitro and In Vivo Blood. 130: 3813-3813. DOI: 10.1182/Blood.V130.Suppl_1.3813.3813  0.503
2017 Tusa I, Cheloni G, Gray N, Gozzini A, Sbarba PD, Rovida E. Abstract 3904: Inhibition of the ERK5 pathway as a novel approach to target human chronic myeloid leukemia stem cells Cancer Research. 77: 3904-3904. DOI: 10.1158/1538-7445.Am2017-3904  0.454
2017 Rao S, Li T, Everley R, Du G, Sorger P, Gray N. Abstract 1222: Developing kinase inhibitors with polypharmacological profiles for the treatment of resistant cancers Cancer Research. 77: 1222-1222. DOI: 10.1158/1538-7445.Am2017-1222  0.869
2016 Ficarro SB, Browne CM, Card JD, Alexander WM, Zhang T, Park E, McNally R, Dhe-Paganon S, Seo HS, Lamberto I, Eck MJ, Buhrlage SJ, Gray NS, Marto JA. Leveraging Gas-Phase Fragmentation Pathways for Improved Identification and Selective Detection of Targets Modified by Covalent Probes. Analytical Chemistry. 88: 12248-12254. PMID 28193034 DOI: 10.1021/Acs.Analchem.6B03394  0.804
2016 Tan L, Gurbani D, Weisberg EL, Jones DS, Rao S, Singer WD, Bernard FM, Mowafy S, Jenney A, Du G, Nonami A, Griffin JD, Lauffenburger DA, Westover KD, Sorger PK, ... Gray NS, et al. Studies of TAK1-centered polypharmacology with novel covalent TAK1 inhibitors. Bioorganic & Medicinal Chemistry. PMID 28038940 DOI: 10.1016/J.Bmc.2016.11.034  0.864
2016 de Wispelaere M, Carocci M, Liang Y, Liu Q, Sun E, Vetter ML, Wang J, Gray NS, Yang PL. Discovery of host-targeted covalent inhibitors of dengue virus. Antiviral Research. PMID 28034743 DOI: 10.1016/J.Antiviral.2016.12.017  0.734
2016 Tan L, Gurbani D, Weisberg EL, Hunter JC, Li L, Jones DS, Ficarro SB, Mowafy S, Tam CP, Rao S, Du G, Griffin JD, Sorger PK, Marto JA, Westover KD, ... Gray NS, et al. Structure-guided development of covalent TAK1 inhibitors. Bioorganic & Medicinal Chemistry. PMID 28011204 DOI: 10.1016/J.Bmc.2016.11.035  0.856
2016 Beelontally R, Wilkie GS, Lau B, Goodmaker CJ, Ho CM, Swanson CM, Deng X, Wang J, Gray NS, Davison AJ, Strang BL. Identification of compounds with anti-human cytomegalovirus activity that inhibit production of IE2 proteins. Antiviral Research. PMID 27956134 DOI: 10.1016/J.Antiviral.2016.12.006  0.672
2016 Ferguson FM, Ni J, Zhang T, Tesar B, Sim T, Kim ND, Deng X, Brown JR, Zhao JJ, Gray NS. Discovery of a Series of 5,11-Dihydro-6H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6-ones as Selective PI3K-δ/γ Inhibitors. Acs Medicinal Chemistry Letters. 7: 908-912. PMID 27774127 DOI: 10.1021/Acsmedchemlett.6B00209  0.804
2016 Wein MN, Liang Y, Goransson O, Sundberg TB, Wang J, Williams EA, O'Meara MJ, Govea N, Beqo B, Nishimori S, Nagano K, Brooks DJ, Martins JS, Corbin B, Anselmo A, ... ... Gray NS, et al. SIKs control osteocyte responses to parathyroid hormone. Nature Communications. 7: 13176. PMID 27759007 DOI: 10.1038/Ncomms13176  0.463
2016 Wang A, Yan XE, Wu H, Wang W, Hu C, Chen C, Zhao Z, Zhao P, Li X, Wang L, Wang B, Ye Z, Wang J, Wang C, Zhang W, ... Gray NS, et al. Ibrutinib targets mutant-EGFR kinase with a distinct binding conformation. Oncotarget. PMID 27626175 DOI: 10.18632/Oncotarget.11951  0.68
2016 Zhang T, Kwiatkowski N, Olson CM, Dixon-Clarke SE, Abraham BJ, Greifenberg AK, Ficarro SB, Elkins JM, Liang Y, Hannett NM, Manz T, Hao M, Bartkowiak B, Greenleaf AL, Marto JA, ... ... Gray NS, et al. Covalent targeting of remote cysteine residues to develop CDK12 and CDK13 inhibitors. Nature Chemical Biology. PMID 27571479 DOI: 10.1038/Nchembio.2166  0.851
2016 Fan F, He Z, Kong LL, Chen Q, Yuan Q, Zhang S, Ye J, Liu H, Sun X, Geng J, Yuan L, Hong L, Xiao C, Zhang W, Sun X, ... ... Gray NS, et al. Pharmacological targeting of kinases MST1 and MST2 augments tissue repair and regeneration. Science Translational Medicine. 8: 352ra108. PMID 27535619 DOI: 10.1126/Scitranslmed.Aaf2304  0.798
2016 Williams CA, Fernandez-Alonso R, Wang J, Toth R, Gray NS, Findlay GM. Erk5 Is a Key Regulator of Naive-Primed Transition and Embryonic Stem Cell Identity. Cell Reports. PMID 27498864 DOI: 10.1016/J.Celrep.2016.07.033  0.498
2016 Pacold ME, Brimacombe KR, Chan SH, Rohde JM, Lewis CA, Swier LJ, Possemato R, Chen WW, Sullivan LB, Fiske BP, Cho S, Freinkman E, Birsoy K, Abu MR, Shaul YD, ... ... Gray NS, et al. Corrigendum: A PHGDH inhibitor reveals coordination of serine synthesis and one-carbon unit fate. Nature Chemical Biology. 12: 656. PMID 27434767 DOI: 10.1038/Nchembio0816-656  0.759
2016 Iorio F, Knijnenburg TA, Vis DJ, Bignell GR, Menden MP, Schubert M, Aben N, Gonçalves E, Barthorpe S, Lightfoot H, Cokelaer T, Greninger P, van Dyk E, Chang H, de Silva H, ... ... Gray NS, et al. A Landscape of Pharmacogenomic Interactions in Cancer. Cell. PMID 27397505 DOI: 10.1016/J.Cell.2016.06.017  0.692
2016 Lee S, Shang Y, Redmond SA, Urisman A, Tang AA, Li KH, Burlingame AL, Pak RA, Jovičić A, Gitler AD, Wang J, Gray NS, Seeley WW, Siddique T, Bigio EH, et al. Activation of HIPK2 Promotes ER Stress-Mediated Neurodegeneration in Amyotrophic Lateral Sclerosis. Neuron. PMID 27321923 DOI: 10.1016/J.Neuron.2016.05.021  0.415
2016 Sundberg TB, Liang Y, Wu H, Choi HG, Kim ND, Sim T, Johannessen L, Petrone A, Khor B, Graham DB, Latorre IJ, Phillips AJ, Schreiber SL, Perez J, Shamji AF, ... Gray NS, et al. Development of Chemical Probes for Investigation of Salt-Inducible Kinase Function In Vivo. Acs Chemical Biology. PMID 27224444 DOI: 10.1021/Acschembio.6B00217  0.827
2016 Hatcher JM, Weisberg E, Sim T, Stone RM, Liu S, Griffin JD, Gray NS. Discovery of a Highly Potent and Selective Indenoindolone Type 1 Pan-FLT3 Inhibitor. Acs Medicinal Chemistry Letters. 7: 476-81. PMID 27190596 DOI: 10.1021/Acsmedchemlett.5B00498  0.864
2016 Matthews JM, Bhatt S, Patricelli MP, Nomanbhoy TK, Jiang X, Natkunam Y, Gentles AJ, Martinez E, Zhu D, Chapman JR, Cortizas E, Shyam R, Chinichian S, Advani R, Tan L, ... ... Gray NS, et al. Pathophysiological significance and therapeutic targeting of germinal center kinase in diffuse large B-cell lymphoma. Blood. PMID 27151888 DOI: 10.1182/Blood-2016-02-696856  0.697
2016 Yang G, Buhrlage S, Tan L, Liu X, Chen J, Xu L, Tsakmaklis N, Chen JG, Patterson CJ, Brown JR, Castillo JJ, Zhang W, Zhang X, Liu S, Cohen P, ... ... Gray N, et al. HCK is a survival determinant transactivated by mutated MYD88, and a direct target of ibrutinib. Blood. PMID 27143257 DOI: 10.1182/Blood-2016-01-695098  0.679
2016 Udayakumar D, Pandita RK, Horikoshi N, Liu Y, Liu Q, Wong KK, Hunt CR, Gray NS, Minna JD, Pandita TK, Westover KD. Torin2 Suppresses Ionizing Radiation-Induced DNA Damage Repair. Radiation Research. PMID 27135971 DOI: 10.1667/Rr14373.1  0.728
2016 Pacold ME, Brimacombe KR, Chan SH, Rohde JM, Lewis CA, Swier LJ, Possemato R, Chen WW, Sullivan LB, Fiske BP, Cho S, Freinkman E, Birsoy K, Abu-Remaileh M, Shaul YD, ... ... Gray NS, et al. A PHGDH inhibitor reveals coordination of serine synthesis and one-carbon unit fate. Nature Chemical Biology. PMID 27110680 DOI: 10.1038/Nchembio.2070  0.811
2016 Clark MJ, Miduturu C, Schmidt AG, Zhu X, Pitts JD, Wang J, Potisopon S, Zhang J, Wojciechowski A, Hann Chu JJ, Gray NS, Yang PL. GNF-2 Inhibits Dengue Virus by Targeting Abl Kinases and the Viral E Protein. Cell Chemical Biology. 23: 443-452. PMID 27105280 DOI: 10.1016/J.Chembiol.2016.03.010  0.662
2016 Liu F, Wang J, Yang X, Li B, Wu H, Qi S, Chen C, Liu X, Yu K, Wang W, Zhao Z, Wang A, Chen YF, Wang L, Gray NS, et al. Discovery of a Highly Selective STK16 Kinase Inhibitor. Acs Chemical Biology. PMID 27082499 DOI: 10.1021/Acschembio.6B00250  0.73
2016 Liu X, Hunter ZR, Xu L, Chen J, Chen JG, Tsakmaklis N, Patterson CJ, Castillo JJ, Buhrlage S, Gray N, Treon SP, Yang G. Targeting Myddosome Assembly in Waldenstrom Macroglobulinaemia. British Journal of Haematology. PMID 27073043 DOI: 10.1111/Bjh.14103  0.64
2016 Westover KD, Jänne PA, Gray NS. Progress on Covalent Inhibition of KRASG12C. Cancer Discovery. 6: 233-4. PMID 26951837 DOI: 10.1158/2159-8290.Cd-16-0092  0.622
2016 Ho CM, Donovan-Banfield IZ, Tan L, Zhang T, Gray NS, Strang BL. Inhibition of IKKα by BAY61-3606 Reveals IKKα-Dependent Histone H3 Phosphorylation in Human Cytomegalovirus Infected Cells. Plos One. 11: e0150339. PMID 26930276 DOI: 10.1371/Journal.Pone.0150339  0.335
2016 Nishikawa JL, Boeszoermenyi A, Vale-Silva LA, Torelli R, Posteraro B, Sohn YJ, Ji F, Gelev V, Sanglard D, Sanguinetti M, Sadreyev RI, Mukherjee G, Bhyravabhotla J, Buhrlage SJ, Gray NS, et al. Inhibiting fungal multidrug resistance by disrupting an activator-Mediator interaction. Nature. PMID 26886795 DOI: 10.1038/Nature16963  0.657
2016 Amato KR, Wang S, Tan L, Hastings AK, Song W, Lovly CM, Meador CB, Ye F, Lu P, Balko JM, Colvin DC, Cates JM, Pao W, Gray NS, Chen J. EPHA2 Blockade Overcomes Acquired Resistance to EGFR Kinase Inhibitors in Lung Cancer. Cancer Research. PMID 26744526 DOI: 10.1158/0008-5472.Can-15-0717  0.315
2016 Bernstein BE, Gray N, Boyd MR, Corcoran RB, Stone RM, Armand P, Sykes DB, Gopal R, Gala MK, Liu D, Tothova Z, Nodelman O, Maus MV, Wu CJ. Chabner Colloquium: Answering the Big Questions in Cancer Research & 2016 STO Annual Meeting Oncologist. 21. DOI: 10.1634/Theoncologist.2016-Ma-1  0.419
2016 Buhrlage S, Weisberg E, Schauer N, Yang J, Lamberto I, Doherty L, Nonami A, Christie AL, Weinstock DM, Stone RM, Gray N, Griffin JD. Inhibition of USP10 Induces Degradation of Oncogenic FLT3: A Novel Approach to Therapy of Leukemia Blood. 128: 524-524. DOI: 10.1182/Blood.V128.22.524.524  0.668
2016 Brown FC, Still E, Cifani P, Reed C, Ficarro S, He J, Koche R, Bhola P, Romanienko P, Mark W, Krivtsov AV, Letai A, Gray N, Marto J, Armstrong SA, et al. Aberrant Phosphorylation of MEF2C Is Dispensable for Hematopoiesis, and Induces Chemotherapy Resistance and Susceptibility to MARK Kinase Inhibition Therapy in Acute Myeloid Leukemia Blood. 128: 436-436. DOI: 10.1182/Blood.V128.22.436.436  0.665
2016 Kieran MW, Sun Y, Pilarz C, Calligaris D, Chadwick EJ, Alberta JA, Ramkissoon SH, Ramkissoon LA, Garcia VM, Wilkinson K, Kane M, Goumnerova L, Chi SN, Manley P, Wright KD, ... ... Gray NS, et al. LG-47TYPE II RAF INHIBITORS INHIBIT BRAF MUTATIONS AND TRUNCATED FUSIONS IN PEDIATRIC LOW-GRADE GLIOMAS Neuro-Oncology. 18: iii89.2-iii89. DOI: 10.1093/Neuonc/Now075.47  0.701
2015 Neel VA, Todorova K, Wang J, Kwon E, Kang M, Liu Q, Gray N, Lee SW, Mandinova A. Sustained Akt activity is required to maintain cell viability in seborrheic keratosis, a benign epithelial tumor. The Journal of Investigative Dermatology. PMID 26739095 DOI: 10.1016/J.Jid.2015.12.023  0.72
2015 Maxson JE, Abel ML, Wang J, Deng X, Reckel S, Luty SB, Sun H, Gorenstein J, Hughes SB, Bottomly D, Wilmot B, McWeeney SK, Radich J, Hantschel O, Middleton RE, ... Gray NS, et al. Identification and Characterization of Tyrosine Kinase Nonreceptor 2 Mutations in Leukemia through Integration of Kinase Inhibitor Screening and Genomic Analysis. Cancer Research. PMID 26677978 DOI: 10.1158/0008-5472.Can-15-0817  0.669
2015 Debruyne DN, Bhatnagar N, Sharma B, Luther W, Moore NF, Cheung NK, Gray NS, George RE. ALK inhibitor resistance in ALK(F1174L)-driven neuroblastoma is associated with AXL activation and induction of EMT. Oncogene. PMID 26616860 DOI: 10.1038/onc.2015.434  0.343
2015 Ye S, Zhang J, Shen J, Gao Y, Li Y, Choy E, Cote G, Harmon D, Mankin H, Gray NS, Hornicek FJ, Duan Z. NVP-TAE684 reverses multidrug resistance (MDR) in human osteosarcoma by inhibiting P-glycoprotein (Pgp) function. British Journal of Pharmacology. PMID 26603906 DOI: 10.1111/Bph.13395  0.598
2015 Hatcher JM, Bahcall M, Choi HG, Gao Y, Sim T, George R, Janne PA, Gray NS. Discovery of inhibitors that overcome the G1202R ALK resistance mutation. Journal of Medicinal Chemistry. PMID 26568289 DOI: 10.1021/Acs.Jmedchem.5B01136  0.835
2015 Müller S, Chaikuad A, Gray NS, Knapp S. The ins and outs of selective kinase inhibitor development. Nature Chemical Biology. 11: 818-21. PMID 26485069 DOI: 10.1038/nchembio.1938  0.416
2015 Terai H, Tan L, Beauchamp EM, Hatcher JM, Liu Q, Meyerson M, Gray NS, Hammerman PS. Characterization of DDR2 Inhibitors for the Treatment of DDR2 Mutated Nonsmall Cell Lung Cancer. Acs Chemical Biology. PMID 26390252 DOI: 10.1021/Acschembio.5B00655  0.854
2015 Wu H, Wang A, Zhang W, Wang B, Chen C, Wang W, Hu C, Ye Z, Zhao Z, Wang L, Li X, Yu K, Liu J, Wu J, Yan XE, ... ... Gray NS, et al. Ibrutinib selectively and irreversibly targets EGFR (L858R, Del19) mutant but is moderately resistant to EGFR (T790M) mutant NSCLC Cells. Oncotarget. PMID 26375053 DOI: 10.18632/Oncotarget.5182  0.669
2015 Wilhelmsen K, Xu F, Farrar K, Tran A, Khakpour S, Sundar S, Prakash A, Wang J, Gray NS, Hellman J. Extracellular signal-regulated kinase 5 promotes acute cellular and systemic inflammation. Science Signaling. 8: ra86. PMID 26307013 DOI: 10.1126/Scisignal.Aaa3206  0.471
2015 Tan L, Akahane K, McNally R, Reyskens KM, Ficarro SB, Liu S, Herter-Sprie GS, Koyama S, Pattison MJ, Labella KM, Johannessen L, Akbay EA, Wong KK, Frank DA, Marto JA, ... ... Gray NS, et al. Development of Selective Covalent JAK3 Inhibitors. Journal of Medicinal Chemistry. PMID 26258521 DOI: 10.1021/Acs.Jmedchem.5B00710  0.854
2015 Wu H, Hu C, Wang A, Weisberg EL, Chen Y, Yun CH, Wang W, Liu Y, Liu X, Tian B, Wang J, Zhao Z, Liang Y, Li B, Wang L, ... ... Gray NS, et al. Discovery of a BTK/MNK dual inhibitor for lymphoma and leukemia. Leukemia. PMID 26165234 DOI: 10.1038/Leu.2015.180  0.854
2015 Lim SM, Xie T, Westover KD, Ficarro SB, Tae HS, Gurbani D, Sim T, Marto JA, Jänne PA, Crews CM, Gray NS. Development of small molecules targeting the pseudokinase Her3. Bioorganic & Medicinal Chemistry Letters. 25: 3382-9. PMID 26094118 DOI: 10.1016/J.Bmcl.2015.04.103  0.771
2015 Moccia M, Liu Q, Guida T, Federico G, Brescia A, Zhao Z, Choi HG, Deng X, Tan L, Wang J, Billaud M, Gray NS, Carlomagno F, Santoro M. Identification of Novel Small Molecule Inhibitors of Oncogenic RET Kinase. Plos One. 10: e0128364. PMID 26046350 DOI: 10.1371/Journal.Pone.0128364  0.775
2015 Tricker EM, Xu C, Uddin S, Capelletti M, Ercan D, Ogino A, Pratilas CA, Rosen N, Gray NS, Wong KK, Janne PA. Combined EGFR/MEK Inhibition Prevents the Emergence of Resistance in EGFR mutant Lung Cancer. Cancer Discovery. PMID 26036643 DOI: 10.1158/2159-8290.Cd-15-0063  0.324
2015 Hatcher JM, Zhang J, Choi HG, Ito G, Alessi DR, Gray NS. Discovery of a Pyrrolopyrimidine (JH-II-127), a Highly Potent, Selective, and Brain Penetrant LRRK2 Inhibitor. Acs Medicinal Chemistry Letters. 6: 584-9. PMID 26005538 DOI: 10.1021/Acsmedchemlett.5B00064  0.837
2015 Wang J, Gray NS. SnapShot: Kinase Inhibitors II. Molecular Cell. 58: 710.e1. PMID 26000855 DOI: 10.1016/j.molcel.2015.05.002  0.586
2015 Wang J, Gray NS. SnapShot: Kinase Inhibitors I. Molecular Cell. 58: 708.e1. PMID 26000854 DOI: 10.1016/J.Molcel.2015.05.001  0.587
2015 Malik N, Vollmer S, Nanda SK, Lopez-Pelaez M, Prescott A, Gray N, Cohen P. Suppression of Interferon β gene transcription by inhibitors of Bromodomain and Extra-Terminal (BET) family members. The Biochemical Journal. PMID 25891802 DOI: 10.1042/Bj20141523  0.387
2015 Nonami A, Sattler M, Weisberg E, Liu Q, Zhang J, Patricelli MP, Christie AL, Saur AM, Kohl NE, Kung AL, Yoon H, Sim T, Gray NS, Griffin JD. Identification of novel therapeutic targets in acute leukemias with NRAS mutations using a pharmacologic approach. Blood. 125: 3133-43. PMID 25833960 DOI: 10.1182/Blood-2014-12-615906  0.68
2015 Fallahi-Sichani M, Moerke NJ, Niepel M, Zhang T, Gray NS, Sorger PK. Systematic analysis of BRAF(V600E) melanomas reveals a role for JNK/c-Jun pathway in adaptive resistance to drug-induced apoptosis. Molecular Systems Biology. 11: 797. PMID 25814555 DOI: 10.15252/Msb.20145877  0.319
2015 Miao B, Ji Z, Tan L, Taylor M, Zhang J, Choi HG, Frederick DT, Kumar R, Wargo JA, Flaherty KT, Gray NS, Tsao H. EPHA2 is a mediator of vemurafenib resistance and a novel therapeutic target in melanoma. Cancer Discovery. 5: 274-87. PMID 25542448 DOI: 10.1158/2159-8290.Cd-14-0295  0.333
2015 Moroco JA, Baumgartner MP, Rust HL, Choi HG, Hur W, Gray NS, Camacho CJ, Smithgall TE. A Discovery Strategy for Selective Inhibitors of c-Src in Complex with the Focal Adhesion Kinase SH3/SH2-binding Region. Chemical Biology & Drug Design. 86: 144-55. PMID 25376742 DOI: 10.1111/Cbdd.12473  0.399
2015 Huang Z, Tan L, Wang H, Liu Y, Blais S, Deng J, Neubert TA, Gray NS, Li X, Mohammadi M. DFG-out mode of inhibition by an irreversible type-1 inhibitor capable of overcoming gate-keeper mutations in FGF receptors. Acs Chemical Biology. 10: 299-309. PMID 25317566 DOI: 10.1021/Cb500674S  0.507
2015 Calles A, Kwiatkowski N, Cammarata BK, Ercan D, Gray NS, Jänne PA. Tivantinib (ARQ 197) efficacy is independent of MET inhibition in non-small-cell lung cancer cell lines. Molecular Oncology. 9: 260-9. PMID 25226813 DOI: 10.1016/J.Molonc.2014.08.011  0.366
2015 Rovida E, Di Maira G, Tusa I, Cannito S, Paternostro C, Navari N, Vivoli E, Deng X, Gray NS, Esparís-Ogando A, David E, Pandiella A, Dello Sbarba P, Parola M, Marra F. The mitogen-activated protein kinase ERK5 regulates the development and growth of hepatocellular carcinoma. Gut. 64: 1454-65. PMID 25183205 DOI: 10.1136/Gutjnl-2014-306761  0.516
2015 Tan L, Nomanbhoy T, Gurbani D, Patricelli M, Hunter J, Geng J, Herhaus L, Zhang J, Pauls E, Ham Y, Choi HG, Xie T, Deng X, Buhrlage SJ, Sim T, ... ... Gray NS, et al. Discovery of type II inhibitors of TGFβ-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2). Journal of Medicinal Chemistry. 58: 183-96. PMID 25075558 DOI: 10.1021/Jm500480K  0.826
2015 Wang J, Mikse O, Liao RG, Li Y, Tan L, Janne PA, Gray NS, Wong KK, Hammerman PS. Ligand-associated ERBB2/3 activation confers acquired resistance to FGFR inhibition in FGFR3-dependent cancer cells. Oncogene. 34: 2167-77. PMID 24909170 DOI: 10.1038/Onc.2014.161  0.711
2015 Weisberg E, Nonami A, Chen Z, Liu F, Zhang J, Sattler M, Nelson E, Cowens K, Christie AL, Mitsiades C, Wong KK, Liu Q, Gray N, Griffin JD. Identification of Wee1 as a novel therapeutic target for mutant RAS-driven acute leukemia and other malignancies. Leukemia. 29: 27-37. PMID 24791855 DOI: 10.1038/Leu.2014.149  0.62
2015 Brown F, Still E, Cifani P, Ficarro S, Pouliot G, Drill E, Gonen M, He J, Balasubramanian S, Zhong S, Pavlick D, Yilmazel B, Krivtsov AV, Alonzo TA, Meshinchi S, ... ... Gray N, et al. Genomic and Proteomic Analysis of Primary Chemoresistance and Induction Failure in Acute Myeloid Leukemia Blood. 126: 88-88. DOI: 10.1182/Blood.V126.23.88.88  0.642
2015 Yang G, Buhrlage S, Tan L, Liu X, Chen J, Hunter Z, Xu L, Tsakmaklis N, Chen J, Patterson CJ, Castillo JJ, Zhang W, Gray N, Treon SP. HCK Is a Highly Relevant Target of Ibrutinib in MYD88 Mutated Waldenstrom's Macroglobulinemia and Diffuse Large B-Cell Lymphoma Blood. 126: 705-705. DOI: 10.1182/Blood.V126.23.705.705  0.697
2015 Yang G, Liu X, Chen J, Xu L, Tsakmaklis N, Chen J, Patterson CJ, Castillo JJ, Cohen P, Tan L, Buhrlage S, Gray N, Treon SP. Targeting IRAK1/IRAK4 Signaling in Waldenstrom's Macroglobulinemia Blood. 126: 4004-4004. DOI: 10.1182/Blood.V126.23.4004.4004  0.684
2015 Liu X, Hunter Z, Xu L, Chen J, Chen J, Tsakmaklis N, Patterson CJ, Castillo JJ, Buhrlage S, Gray N, Treon SP, Yang G. Targeting Myddosome Self-Assembly in Waldenstrom's Macroglobulinemia Blood. 126: 1563-1563. DOI: 10.1182/Blood.V126.23.1563.1563  0.66
2015 Amato K, Wang S, Hastings A, Youngblood V, Santapuram P, Chen H, Cates J, Colvin D, Ye F, Brantley-Sieders D, Cook R, Tan L, Gray N, Chen J. Abstract A12: Genetic and pharmacologic inhibition of EPHA2 promotes apoptosis in NSCLC Molecular Cancer Therapeutics. 14. DOI: 10.1158/1538-8514.Pi3K14-A12  0.459
2015 Chong C, Ercan D, Bahcall M, Capelletti M, Gray N, Janne P. Abstract 3644: Identification of existing targeted agents that inhibit NTRK and ROS1 in lung cancer Cancer Research. 75: 3644-3644. DOI: 10.1158/1538-7445.Am2015-3644  0.418
2015 Du L, Zhang T, Kaoud T, Gray N, Dalby K, Tsai KY. Abstract 1941: Distinct roles of c-Jun N-terminal kinase (JNK) isoforms in skin cancer Cancer Research. 75: 1941-1941. DOI: 10.1158/1538-7445.Am2015-1941  0.447
2015 Debruyne D, Sharma B, Gray N, George R. Abstract LB-C24: Resistance to ALK inhibition is associated with enhanced BRD4 dependence in ALK-mutated MYCN-amplified neuroblastoma Molecular Cancer Therapeutics. 14. DOI: 10.1158/1535-7163.Targ-15-Lb-C24  0.463
2014 Christensen CL, Kwiatkowski N, Abraham BJ, Carretero J, Al-Shahrour F, Zhang T, Chipumuro E, Herter-Sprie GS, Akbay EA, Altabef A, Zhang J, Shimamura T, Capelletti M, Reibel JB, Cavanaugh JD, ... ... Gray NS, et al. Targeting transcriptional addictions in small cell lung cancer with a covalent CDK7 inhibitor. Cancer Cell. 26: 909-22. PMID 25490451 DOI: 10.1016/J.Ccell.2014.10.019  0.539
2014 Chipumuro E, Marco E, Christensen CL, Kwiatkowski N, Zhang T, Hatheway CM, Abraham BJ, Sharma B, Yeung C, Altabef A, Perez-Atayde A, Wong KK, Yuan GC, Gray NS, Young RA, et al. CDK7 inhibition suppresses super-enhancer-linked oncogenic transcription in MYCN-driven cancer. Cell. 159: 1126-39. PMID 25416950 DOI: 10.1016/J.Cell.2014.10.024  0.323
2014 Gray NS, Fabbro D. Discovery of allosteric BCR-ABL inhibitors from phenotypic screen to clinical candidate. Methods in Enzymology. 548: 173-88. PMID 25399646 DOI: 10.1016/B978-0-12-397918-6.00007-0  0.38
2014 Umapathy G, El Wakil A, Witek B, Chesler L, Danielson L, Deng X, Gray NS, Johansson M, Kvarnbrink S, Ruuth K, Schönherr C, Palmer RH, Hallberg B. The kinase ALK stimulates the kinase ERK5 to promote the expression of the oncogene MYCN in neuroblastoma. Science Signaling. 7: ra102. PMID 25351247 DOI: 10.1126/Scisignal.2005470  0.648
2014 Tan L, Wang J, Tanizaki J, Huang Z, Aref AR, Rusan M, Zhu SJ, Zhang Y, Ercan D, Liao RG, Capelletti M, Zhou W, Hur W, Kim N, Sim T, ... ... Gray NS, et al. Development of covalent inhibitors that can overcome resistance to first-generation FGFR kinase inhibitors. Proceedings of the National Academy of Sciences of the United States of America. 111: E4869-77. PMID 25349422 DOI: 10.1073/Pnas.1403438111  0.585
2014 Xie T, Lim SM, Westover KD, Dodge ME, Ercan D, Ficarro SB, Udayakumar D, Gurbani D, Tae HS, Riddle SM, Sim T, Marto JA, Jänne PA, Crews CM, Gray NS. Pharmacological targeting of the pseudokinase Her3. Nature Chemical Biology. 10: 1006-12. PMID 25326665 DOI: 10.1038/Nchembio.1658  0.761
2014 Lopez-Pelaez M, Lamont DJ, Peggie M, Shpiro N, Gray NS, Cohen P. Protein kinase IKKβ-catalyzed phosphorylation of IRF5 at Ser462 induces its dimerization and nuclear translocation in myeloid cells. Proceedings of the National Academy of Sciences of the United States of America. 111: 17432-7. PMID 25326418 DOI: 10.1073/Pnas.1418399111  0.302
2014 Wagle N, Grabiner BC, Van Allen EM, Amin-Mansour A, Taylor-Weiner A, Rosenberg M, Gray N, Barletta JA, Guo Y, Swanson SJ, Ruan DT, Hanna GJ, Haddad RI, Getz G, Kwiatkowski DJ, et al. Response and acquired resistance to everolimus in anaplastic thyroid cancer. The New England Journal of Medicine. 371: 1426-33. PMID 25295501 DOI: 10.1056/Nejmoa1403352  0.588
2014 Duan Z, Zhang J, Ye S, Shen J, Choy E, Cote G, Harmon D, Mankin H, Hua Y, Zhang Y, Gray NS, Hornicek FJ. A-770041 reverses paclitaxel and doxorubicin resistance in osteosarcoma cells. Bmc Cancer. 14: 681. PMID 25236161 DOI: 10.1186/1471-2407-14-681  0.355
2014 Moore NF, Azarova AM, Bhatnagar N, Ross KN, Drake LE, Frumm S, Liu QS, Christie AL, Sanda T, Chesler L, Kung AL, Gray NS, Stegmaier K, George RE. Molecular rationale for the use of PI3K/AKT/mTOR pathway inhibitors in combination with crizotinib in ALK-mutated neuroblastoma. Oncotarget. 5: 8737-49. PMID 25228590 DOI: 10.18632/Oncotarget.2372  0.625
2014 Chaikuad A, Tacconi EM, Zimmer J, Liang Y, Gray NS, Tarsounas M, Knapp S. A unique inhibitor binding site in ERK1/2 is associated with slow binding kinetics. Nature Chemical Biology. 10: 853-60. PMID 25195011 DOI: 10.1038/Nchembio.1629  0.321
2014 Weisberg E, Nonami A, Chen Z, Nelson E, Chen Y, Liu F, Cho H, Zhang J, Sattler M, Mitsiades C, Wong KK, Liu Q, Gray NS, Griffin JD. Upregulation of IGF1R by mutant RAS in leukemia and potentiation of RAS signaling inhibitors by small-molecule inhibition of IGF1R. Clinical Cancer Research : An Official Journal of the American Association For Cancer Research. 20: 5483-95. PMID 25186968 DOI: 10.1158/1078-0432.Ccr-14-0902  0.48
2014 Ritorto MS, Ewan R, Perez-Oliva AB, Knebel A, Buhrlage SJ, Wightman M, Kelly SM, Wood NT, Virdee S, Gray NS, Morrice NA, Alessi DR, Trost M. Screening of DUB activity and specificity by MALDI-TOF mass spectrometry. Nature Communications. 5: 4763. PMID 25159004 DOI: 10.1038/Ncomms5763  0.739
2014 Derbyshire ER, Zuzarte-Luís V, Magalhães AD, Kato N, Sanschagrin PC, Wang J, Zhou W, Miduturu CV, Mazitschek R, Sliz P, Mota MM, Gray NS, Clardy J. Chemical interrogation of the malaria kinome. Chembiochem : a European Journal of Chemical Biology. 15: 1920-30. PMID 25111632 DOI: 10.1002/Cbic.201400025  0.536
2014 Kwiatkowski N, Zhang T, Rahl PB, Abraham BJ, Reddy J, Ficarro SB, Dastur A, Amzallag A, Ramaswamy S, Tesar B, Jenkins CE, Hannett NM, McMillin D, Sanda T, Sim T, ... ... Gray NS, et al. Targeting transcription regulation in cancer with a covalent CDK7 inhibitor. Nature. 511: 616-20. PMID 25043025 DOI: 10.1038/Nature13393  0.634
2014 Hunter JC, Gurbani D, Ficarro SB, Carrasco MA, Lim SM, Choi HG, Xie T, Marto JA, Chen Z, Gray NS, Westover KD. In situ selectivity profiling and crystal structure of SML-8-73-1, an active site inhibitor of oncogenic K-Ras G12C. Proceedings of the National Academy of Sciences of the United States of America. 111: 8895-900. PMID 24889603 DOI: 10.1073/Pnas.1404639111  0.678
2014 Vetter ML, Zhang Z, Liu S, Wang J, Cho H, Zhang J, Zhang W, Gray NS, Yang PL. Fluorescent visualization of Src by using dasatinib-BODIPY. Chembiochem : a European Journal of Chemical Biology. 15: 1317-24. PMID 24828915 DOI: 10.1002/Cbic.201402010  0.666
2014 Canning P, Tan L, Chu K, Lee SW, Gray NS, Bullock AN. Structural mechanisms determining inhibition of the collagen receptor DDR1 by selective and multi-targeted type II kinase inhibitors. Journal of Molecular Biology. 426: 2457-70. PMID 24768818 DOI: 10.1016/J.Jmb.2014.04.014  0.431
2014 Zhao Z, Wu H, Wang L, Liu Y, Knapp S, Liu Q, Gray NS. Exploration of type II binding mode: A privileged approach for kinase inhibitor focused drug discovery? Acs Chemical Biology. 9: 1230-41. PMID 24730530 DOI: 10.1021/Cb500129T  0.655
2014 Amato KR, Wang S, Hastings AK, Youngblood VM, Santapuram PR, Chen H, Cates JM, Colvin DC, Ye F, Brantley-Sieders DM, Cook RS, Tan L, Gray NS, Chen J. Genetic and pharmacologic inhibition of EPHA2 promotes apoptosis in NSCLC. The Journal of Clinical Investigation. 124: 2037-49. PMID 24713656 DOI: 10.1172/Jci72522  0.312
2014 Codeluppi S, Fernandez-Zafra T, Sandor K, Kjell J, Liu Q, Abrams M, Olson L, Gray NS, Svensson CI, Uhlén P. Interleukin-6 secretion by astrocytes is dynamically regulated by PI3K-mTOR-calcium signaling. Plos One. 9: e92649. PMID 24667246 DOI: 10.1371/Journal.Pone.0092649  0.446
2014 Decker S, Finter J, Forde AJ, Kissel S, Schwaller J, Mack TS, Kuhn A, Gray N, Follo M, Jumaa H, Burger M, Zirlik K, Pfeifer D, Miduturu CV, Eibel H, et al. PIM kinases are essential for chronic lymphocytic leukemia cell survival (PIM2/3) and CXCR4-mediated microenvironmental interactions (PIM1). Molecular Cancer Therapeutics. 13: 1231-45. PMID 24659821 DOI: 10.1158/1535-7163.Mct-13-0575-T  0.478
2014 Wu H, Wang W, Liu F, Weisberg EL, Tian B, Chen Y, Li B, Wang A, Wang B, Zhao Z, McMillin DW, Hu C, Li H, Wang J, Liang Y, ... ... Gray NS, et al. Discovery of a potent, covalent BTK inhibitor for B-cell lymphoma. Acs Chemical Biology. 9: 1086-91. PMID 24556163 DOI: 10.1021/Cb4008524  0.811
2014 Ficarro SB, Biagi JM, Wang J, Scotcher J, Koleva RI, Card JD, Adelmant G, He H, Askenazi M, Marshall AG, Young NL, Gray NS, Marto JA. Protected amine labels: a versatile molecular scaffold for multiplexed nominal mass and sub-Da isotopologue quantitative proteomic reagents. Journal of the American Society For Mass Spectrometry. 25: 636-50. PMID 24496597 DOI: 10.1007/S13361-013-0811-X  0.54
2014 Lim SM, Westover KD, Ficarro SB, Harrison RA, Choi HG, Pacold ME, Carrasco M, Hunter J, Kim ND, Xie T, Sim T, Jänne PA, Meyerson M, Marto JA, Engen JR, ... Gray NS, et al. Therapeutic targeting of oncogenic K-Ras by a covalent catalytic site inhibitor. Angewandte Chemie (International Ed. in English). 53: 199-204. PMID 24259466 DOI: 10.1002/Anie.201307387  0.787
2014 Banerjee S, Buhrlage SJ, Huang HT, Deng X, Zhou W, Wang J, Traynor R, Prescott AR, Alessi DR, Gray NS. Characterization of WZ4003 and HTH-01-015 as selective inhibitors of the LKB1-tumour-suppressor-activated NUAK kinases. The Biochemical Journal. 457: 215-25. PMID 24171924 DOI: 10.1042/Bj20131152  0.859
2014 Praditsuktavorn P, Pera B, Kwiatkowski N, Yang S, Zhang T, Gray N, Cerchietti L. Transcription Regulation Targeting in Peripheral T Cell Lymphomas Induces Apoptosis and Sensitization to BCL2 Inhibitors Blood. 124: 810-810. DOI: 10.1182/Blood.V124.21.810.810  0.516
2014 Maxson JE, Melissa AL, Wang J, Deng X, Luty SB, Sun H, Gorenstein J, Middleton R, Gray NS, Druker BJ, Tyner JW. Development and Repurposing of Small-Molecule Kinase Inhibitors to Target Novel Leukemogenic TNK2 Mutations Blood. 124: 435-435. DOI: 10.1182/Blood.V124.21.435.435  0.67
2014 Kawano Y, Sahin I, Moschetta M, Wang J, Manier S, Glavey S, Mishima Y, Kokubun K, Tsukamoto S, Sacco A, Anderson KC, Roccaro AM, Gray NS, Ghobrial IM. Citron Rho-Interacting Serine/Threonine kinase (CIT) Is a Novel Therapeutic Target in Multiple Myeloma Cells Blood. 124: 3430-3430. DOI: 10.1182/Blood.V124.21.3430.3430  0.445
2014 Moore N, Pukma S, Gray N, George R. Abstract 790: A high-throughput chemical screen identifies synergistic activity between neurotransmitter receptor inhibitors and crizotinib in ALK-mutated neuroblastoma Cancer Research. 74: 790-790. DOI: 10.1158/1538-7445.Am2014-790  0.462
2014 Wagle N, Grabiner BC, Allen EMV, Amin-Mansour A, Carter SC, Gray N, Barletta JA, Swanson SJ, Ruan D, Kwiatkowski DJ, Hanna GJ, Haddad RI, Sabatini D, Janne PA, Garraway LA, et al. Abstract 1724: Genomic mechanisms of exquisite sensitivity and acquired resistance to everolimus in a patient with anaplastic thyroid carcinoma Cancer Research. 74: 1724-1724. DOI: 10.1158/1538-7445.Am2014-1724  0.612
2014 Kim H, Tan L, Weisberg EL, Liu F, Canning P, Choi H, Ezell S, Zhao Z, Wu H, Wang J, Mandinova A, Bullock AN, Liu Q, Lee SW, Gray NS. Correction to Discovery of a Potent and Selective DDR1 Receptor Tyrosine Kinase Inhibitor Acs Chemical Biology. 9: 840-840. DOI: 10.1021/Cb5000949  0.633
2014 Chen J, Amato K, Wang S, Youngblood V, Brantley-Sieders D, Cook R, Tan L, Gray N. 297 Genetic and pharmacologic inhibition of EPHA2 promotes apoptosis in NSCLC European Journal of Cancer. 50: 98. DOI: 10.1016/S0959-8049(14)70423-X  0.319
2013 Deng X, Elkins JM, Zhang J, Yang Q, Erazo T, Gomez N, Choi HG, Wang J, Dzamko N, Lee JD, Sim T, Kim N, Alessi DR, Lizcano JM, Knapp S, ... Gray NS, et al. Structural determinants for ERK5 (MAPK7) and leucine rich repeat kinase 2 activities of benzo[e]pyrimido-[5,4-b]diazepine-6(11H)-ones. European Journal of Medicinal Chemistry. 70: 758-67. PMID 24239623 DOI: 10.1016/J.Ejmech.2013.10.052  0.849
2013 Mistry H, Hsieh G, Buhrlage SJ, Huang M, Park E, Cuny GD, Galinsky I, Stone RM, Gray NS, D'Andrea AD, Parmar K. Small-molecule inhibitors of USP1 target ID1 degradation in leukemic cells. Molecular Cancer Therapeutics. 12: 2651-62. PMID 24130053 DOI: 10.1158/1535-7163.Mct-13-0103-T  0.742
2013 Tannous BA, Kerami M, Van der Stoop PM, Kwiatkowski N, Wang J, Zhou W, Kessler AF, Lewandrowski G, Hiddingh L, Sol N, Lagerweij T, Wedekind L, Niers JM, Barazas M, Nilsson RJ, ... ... Gray NS, et al. Effects of the selective MPS1 inhibitor MPS1-IN-3 on glioblastoma sensitivity to antimitotic drugs. Journal of the National Cancer Institute. 105: 1322-31. PMID 23940287 DOI: 10.1093/Jnci/Djt168  0.491
2013 Kim HG, Tan L, Weisberg EL, Liu F, Canning P, Choi HG, Ezell SA, Wu H, Zhao Z, Wang J, Mandinova A, Griffin JD, Bullock AN, Liu Q, Lee SW, ... Gray NS, et al. Discovery of a potent and selective DDR1 receptor tyrosine kinase inhibitor. Acs Chemical Biology. 8: 2145-50. PMID 23899692 DOI: 10.1021/Cb400430T  0.731
2013 Kang SA, Pacold ME, Cervantes CL, Lim D, Lou HJ, Ottina K, Gray NS, Turk BE, Yaffe MB, Sabatini DM. mTORC1 phosphorylation sites encode their sensitivity to starvation and rapamycin. Science (New York, N.Y.). 341: 1236566. PMID 23888043 DOI: 10.1126/Science.1236566  0.785
2013 Yang G, Zhou Y, Liu X, Xu L, Cao Y, Manning RJ, Patterson CJ, Buhrlage SJ, Gray N, Tai YT, Anderson KC, Hunter ZR, Treon SP. A mutation in MYD88 (L265P) supports the survival of lymphoplasmacytic cells by activation of Bruton tyrosine kinase in Waldenström macroglobulinemia. Blood. 122: 1222-32. PMID 23836557 DOI: 10.1182/Blood-2012-12-475111  0.698
2013 Taipale M, Krykbaeva I, Whitesell L, Santagata S, Zhang J, Liu Q, Gray NS, Lindquist S. Chaperones as thermodynamic sensors of drug-target interactions reveal kinase inhibitor specificities in living cells. Nature Biotechnology. 31: 630-7. PMID 23811600 DOI: 10.1038/Nbt.2620  0.649
2013 Liao RG, Jung J, Tchaicha J, Wilkerson MD, Sivachenko A, Beauchamp EM, Liu Q, Pugh TJ, Pedamallu CS, Hayes DN, Gray NS, Getz G, Wong KK, Haddad RI, Meyerson M, et al. Inhibitor-sensitive FGFR2 and FGFR3 mutations in lung squamous cell carcinoma. Cancer Research. 73: 5195-205. PMID 23786770 DOI: 10.1158/0008-5472.Can-12-3950  0.543
2013 Marsilje TH, Pei W, Chen B, Lu W, Uno T, Jin Y, Jiang T, Kim S, Li N, Warmuth M, Sarkisova Y, Sun F, Steffy A, Pferdekamper AC, Li AG, ... ... Gray NS, et al. Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase 2 clinical trials. Journal of Medicinal Chemistry. 56: 5675-90. PMID 23742252 DOI: 10.1021/Jm400402Q  0.797
2013 Liu Y, Marks K, Cowley GS, Carretero J, Liu Q, Nieland TJ, Xu C, Cohoon TJ, Gao P, Zhang Y, Chen Z, Altabef AB, Tchaicha JH, Wang X, Choe S, ... ... Gray NS, et al. Metabolic and functional genomic studies identify deoxythymidylate kinase as a target in LKB1-mutant lung cancer. Cancer Discovery. 3: 870-9. PMID 23715154 DOI: 10.1158/2159-8290.Cd-13-0015  0.821
2013 Elkins JM, Wang J, Deng X, Pattison MJ, Arthur JS, Erazo T, Gomez N, Lizcano JM, Gray NS, Knapp S. X-ray crystal structure of ERK5 (MAPK7) in complex with a specific inhibitor. Journal of Medicinal Chemistry. 56: 4413-21. PMID 23656407 DOI: 10.1021/Jm4000837  0.705
2013 Liu F, Zhang X, Weisberg E, Chen S, Hur W, Wu H, Zhao Z, Wang W, Mao M, Cai C, Simon NI, Sanda T, Wang J, Look AT, Griffin JD, ... ... Gray NS, et al. Discovery of a selective irreversible BMX inhibitor for prostate cancer. Acs Chemical Biology. 8: 1423-8. PMID 23594111 DOI: 10.1021/Cb4000629  0.694
2013 Jain R, Jain D, Liu Q, Bartosinska B, Wang J, Schumann D, Kauschke SG, Eickelmann P, Piemonti L, Gray NS, Lammert E. Pharmacological inhibition of Eph receptors enhances glucose-stimulated insulin secretion from mouse and human pancreatic islets. Diabetologia. 56: 1350-5. PMID 23475368 DOI: 10.1007/S00125-013-2877-1  0.566
2013 Sanda T, Tyner JW, Gutierrez A, Ngo VN, Glover J, Chang BH, Yost A, Ma W, Fleischman AG, Zhou W, Yang Y, Kleppe M, Ahn Y, Tatarek J, Kelliher MA, ... ... Gray NS, et al. TYK2-STAT1-BCL2 pathway dependence in T-cell acute lymphoblastic leukemia. Cancer Discovery. 3: 564-77. PMID 23471820 DOI: 10.1158/2159-8290.Cd-12-0504  0.345
2013 Liu Q, Sabnis Y, Zhao Z, Zhang T, Buhrlage SJ, Jones LH, Gray NS. Developing irreversible inhibitors of the protein kinase cysteinome. Chemistry & Biology. 20: 146-59. PMID 23438744 DOI: 10.1016/J.Chembiol.2012.12.006  0.802
2013 Weisberg E, Liu Q, Zhang X, Nelson E, Sattler M, Liu F, Nicolais M, Zhang J, Mitsiades C, Smith RW, Stone R, Galinsky I, Nonami A, Griffin JD, Gray N. Selective Akt inhibitors synergize with tyrosine kinase inhibitors and effectively override stroma-associated cytoprotection of mutant FLT3-positive AML cells. Plos One. 8: e56473. PMID 23437141 DOI: 10.1371/Journal.Pone.0056473  0.705
2013 Liu Q, Xu C, Kirubakaran S, Zhang X, Hur W, Liu Y, Kwiatkowski NP, Wang J, Westover KD, Gao P, Ercan D, Niepel M, Thoreen CC, Kang SA, Patricelli MP, ... ... Gray NS, et al. Characterization of Torin2, an ATP-competitive inhibitor of mTOR, ATM, and ATR. Cancer Research. 73: 2574-86. PMID 23436801 DOI: 10.1158/0008-5472.Can-12-1702  0.861
2013 Guo Y, Chekaluk Y, Zhang J, Du J, Gray NS, Wu CL, Kwiatkowski DJ. TSC1 involvement in bladder cancer: diverse effects and therapeutic implications. The Journal of Pathology. 230: 17-27. PMID 23401075 DOI: 10.1002/Path.4176  0.349
2013 Cortot AB, Repellin CE, Shimamura T, Capelletti M, Zejnullahu K, Ercan D, Christensen JG, Wong KK, Gray NS, Jänne PA. Resistance to irreversible EGF receptor tyrosine kinase inhibitors through a multistep mechanism involving the IGF1R pathway. Cancer Research. 73: 834-43. PMID 23172312 DOI: 10.1158/0008-5472.Can-12-2066  0.318
2013 Yang Q, Liao L, Deng X, Chen R, Gray NS, Yates JR, Lee JD. BMK1 is involved in the regulation of p53 through disrupting the PML-MDM2 interaction. Oncogene. 32: 3156-64. PMID 22869143 DOI: 10.1038/Onc.2012.332  0.518
2013 Matthews JM, Tan L, Bhatt S, Patricelli M, Nomanbhoy T, Zhang J, Jiang X, Natkunam Y, Choi HG, Gentles AJ, Martinez E, Zhu D, Chapman JR, Shyam RM, Chinichian S, ... ... Gray NS, et al. Germinal Center Kinase Regulates The Proliferation and Survival Of Diffuse Large B-Cell Lymphoma Blood. 122: 643-643. DOI: 10.1182/Blood.V122.21.643.643  0.706
2013 Yang G, Liu X, Zhou Y, Xu L, Cao Y, Manning R, Patterson C, Tripsas CK, Hunter Z, Buhrlage S, Gray NS, Treon SP. PI3K/AKT Pathway Is Activated By MYD88 L265P and Use Of PI3K-Delta Inhibitors Induces Robust Tumor Cell Killing In Waldenstrom’s Macroglobulinemia Blood. 122: 4255-4255. DOI: 10.1182/Blood.V122.21.4255.4255  0.674
2013 Mistry H, Hsieh G, Buhrlage S, Huang M, Park E, Cuny G, Galinsky I, Stone RM, Gray NS, Parmar K, D'Andrea AD. Small Molecule Inhibitors of USP1 Target ID1 Degradation in Leukemic Cells and Cause Cytotoxicity Blood. 122: 2906-2906. DOI: 10.1182/Blood.V122.21.2906.2906  0.744
2013 Nonami A, Sattler M, Weisberg EL, Zhang J, Liu Q, Patricell M, Yoon H, Christie AL, Sauer AM, Kohl N, Kung AL, Sim T, Gray NS, Griffin JD. Using Small Molecules To Identify Critical Signaling Pathways Of Mutant N-RAS In Acute Leukemia Cells Blood. 122: 169-169. DOI: 10.1182/Blood.V122.21.169.169  0.642
2013 Miao B, Zhang J, Ji Z, Njauw CN, Taylor M, Kumar R, Gray N, Tsao H. Abstract 5605: Pharmacologic inhibition of EphA2 in NRAS and BRAF mutant melanomas. Cancer Research. 73: 5605-5605. DOI: 10.1158/1538-7445.Am2013-5605  0.48
2013 Bhatnagar N, Luther W, Sharma B, Liu Q, Gray N, George RE. Abstract 4454: The AXL tyrosine kinase receptor contributes to ALK-inhibitor resistance in neuroblastoma. Cancer Research. 73: 4454-4454. DOI: 10.1158/1538-7445.Am2013-4454  0.645
2012 Koliwad SK, Gray NE, Wang JC. Angiopoietin-like 4 (Angptl4): A glucocorticoid-dependent gatekeeper of fatty acid flux during fasting. Adipocyte. 1: 182-187. PMID 23700531 DOI: 10.4161/adip.20787  0.367
2012 Deng X, Choi HG, Buhrlage SJ, Gray NS. Leucine-rich repeat kinase 2 inhibitors: a patent review (2006 - 2011). Expert Opinion On Therapeutic Patents. 22: 1415-26. PMID 23126385 DOI: 10.1517/13543776.2012.729041  0.742
2012 Choi HG, Zhang J, Deng X, Hatcher JM, Patricelli MP, Zhao Z, Alessi DR, Gray NS. Brain Penetrant LRRK2 Inhibitor. Acs Medicinal Chemistry Letters. 3: 658-662. PMID 23066449 DOI: 10.1021/Ml300123A  0.837
2012 Ercan D, Xu C, Yanagita M, Monast CS, Pratilas CA, Montero J, Butaney M, Shimamura T, Sholl L, Ivanova EV, Tadi M, Rogers A, Repellin C, Capelletti M, Maertens O, ... ... Gray NS, et al. Reactivation of ERK signaling causes resistance to EGFR kinase inhibitors. Cancer Discovery. 2: 934-47. PMID 22961667 DOI: 10.1158/2159-8290.Cd-12-0103  0.379
2012 Reith AD, Bamborough P, Jandu K, Andreotti D, Mensah L, Dossang P, Choi HG, Deng X, Zhang J, Alessi DR, Gray NS. GSK2578215A; a potent and highly selective 2-arylmethyloxy-5-substitutent-N-arylbenzamide LRRK2 kinase inhibitor. Bioorganic & Medicinal Chemistry Letters. 22: 5625-9. PMID 22863203 DOI: 10.1016/J.Bmcl.2012.06.104  0.821
2012 Choi HG, Zhang J, Weisberg E, Griffin JD, Sim T, Gray NS. Development of 'DFG-out' inhibitors of gatekeeper mutant kinases. Bioorganic & Medicinal Chemistry Letters. 22: 5297-302. PMID 22819762 DOI: 10.1016/J.Bmcl.2012.06.036  0.396
2012 Cheng CK, Gustafson WC, Charron E, Houseman BT, Zunder E, Goga A, Gray NS, Pollok B, Oakes SA, James CD, Shokat KM, Weiss WA, Fan QW. Dual blockade of lipid and cyclin-dependent kinases induces synthetic lethality in malignant glioma. Proceedings of the National Academy of Sciences of the United States of America. 109: 12722-7. PMID 22802621 DOI: 10.1073/Pnas.1202492109  0.618
2012 Duan Z, Zhang J, Choy E, Harmon D, Liu X, Nielsen P, Mankin H, Gray NS, Hornicek FJ. Systematic kinome shRNA screening identifies CDK11 (PITSLRE) kinase expression is critical for osteosarcoma cell growth and proliferation. Clinical Cancer Research : An Official Journal of the American Association For Cancer Research. 18: 4580-8. PMID 22791884 DOI: 10.1158/1078-0432.Ccr-12-1157  0.367
2012 Berry T, Luther W, Bhatnagar N, Jamin Y, Poon E, Sanda T, Pei D, Sharma B, Vetharoy WR, Hallsworth A, Ahmad Z, Barker K, Moreau L, Webber H, Wang W, ... ... Gray NS, et al. The ALK(F1174L) mutation potentiates the oncogenic activity of MYCN in neuroblastoma. Cancer Cell. 22: 117-30. PMID 22789543 DOI: 10.1016/J.Ccr.2012.06.001  0.737
2012 Deng X, Zhou W, Weisberg E, Wang J, Zhang J, Sasaki T, Nelson E, Griffin JD, Jänne PA, Gray NS. An amino-indazole scaffold with spectrum selective kinase inhibition of FLT3, PDGFRα and kit. Bioorganic & Medicinal Chemistry Letters. 22: 4579-84. PMID 22727638 DOI: 10.1016/J.Bmcl.2012.05.107  0.688
2012 Dzamko N, Inesta-Vaquera F, Zhang J, Xie C, Cai H, Arthur S, Tan L, Choi H, Gray N, Cohen P, Pedrioli P, Clark K, Alessi DR. The IkappaB kinase family phosphorylates the Parkinson's disease kinase LRRK2 at Ser935 and Ser910 during Toll-like receptor signaling. Plos One. 7: e39132. PMID 22723946 DOI: 10.1371/Journal.Pone.0039132  0.779
2012 Zhang Z, Kwiatkowski N, Zeng H, Lim SM, Gray NS, Zhang W, Yang PL. Leveraging kinase inhibitors to develop small molecule tools for imaging kinases by fluorescence microscopy. Molecular Biosystems. 8: 2523-6. PMID 22673640 DOI: 10.1039/C2Mb25099C  0.6
2012 Wang JC, Gray NE, Kuo T, Harris CA. Regulation of triglyceride metabolism by glucocorticoid receptor. Cell & Bioscience. 2: 19. PMID 22640645 DOI: 10.1186/2045-3701-2-19  0.357
2012 Ni J, Liu Q, Xie S, Carlson C, Von T, Vogel K, Riddle S, Benes C, Eck M, Roberts T, Gray N, Zhao J. Functional characterization of an isoform-selective inhibitor of PI3K-p110β as a potential anticancer agent. Cancer Discovery. 2: 425-33. PMID 22588880 DOI: 10.1158/2159-8290.Cd-12-0003  0.633
2012 Thoreen CC, Chantranupong L, Keys HR, Wang T, Gray NS, Sabatini DM. A unifying model for mTORC1-mediated regulation of mRNA translation. Nature. 485: 109-13. PMID 22552098 DOI: 10.1038/Nature11083  0.76
2012 Hellwig S, Miduturu CV, Kanda S, Zhang J, Filippakopoulos P, Salah E, Deng X, Choi HG, Zhou W, Hur W, Knapp S, Gray NS, Smithgall TE. Small-molecule inhibitors of the c-Fes protein-tyrosine kinase. Chemistry & Biology. 19: 529-40. PMID 22520759 DOI: 10.1016/J.Chembiol.2012.01.020  0.622
2012 Liu Q, Ren T, Fresques T, Oppliger W, Niles BJ, Hur W, Sabatini DM, Hall MN, Powers T, Gray NS. Selective ATP-competitive inhibitors of TOR suppress rapamycin-insensitive function of TORC2 in Saccharomyces cerevisiae. Acs Chemical Biology. 7: 982-7. PMID 22496512 DOI: 10.1021/Cb300058V  0.749
2012 Weisberg E, Liu Q, Nelson E, Kung AL, Christie AL, Bronson R, Sattler M, Sanda T, Zhao Z, Hur W, Mitsiades C, Smith R, Daley JF, Stone R, Galinsky I, ... ... Gray N, et al. Using combination therapy to override stromal-mediated chemoresistance in mutant FLT3-positive AML: synergism between FLT3 inhibitors, dasatinib/multi-targeted inhibitors and JAK inhibitors. Leukemia. 26: 2233-44. PMID 22469781 DOI: 10.1038/Leu.2012.96  0.703
2012 Garnett MJ, Edelman EJ, Heidorn SJ, Greenman CD, Dastur A, Lau KW, Greninger P, Thompson IR, Luo X, Soares J, Liu Q, Iorio F, Surdez D, Chen L, Milano RJ, ... ... Gray NS, et al. Systematic identification of genomic markers of drug sensitivity in cancer cells. Nature. 483: 570-5. PMID 22460902 DOI: 10.1038/Nature11005  0.661
2012 Zhang J, Deng X, Choi HG, Alessi DR, Gray NS. Characterization of TAE684 as a potent LRRK2 kinase inhibitor. Bioorganic & Medicinal Chemistry Letters. 22: 1864-9. PMID 22335897 DOI: 10.1016/J.Bmcl.2012.01.084  0.833
2012 Zhang T, Inesta-Vaquera F, Niepel M, Zhang J, Ficarro SB, Machleidt T, Xie T, Marto JA, Kim N, Sim T, Laughlin JD, Park H, LoGrasso PV, Patricelli M, Nomanbhoy TK, ... ... Gray NS, et al. Discovery of potent and selective covalent inhibitors of JNK. Chemistry & Biology. 19: 140-54. PMID 22284361 DOI: 10.1016/J.Chembiol.2011.11.010  0.849
2012 Gray NE, Lam LN, Yang K, Zhou AY, Koliwad S, Wang JC. Angiopoietin-like 4 (Angptl4) protein is a physiological mediator of intracellular lipolysis in murine adipocytes. The Journal of Biological Chemistry. 287: 8444-56. PMID 22267746 DOI: 10.1074/Jbc.M111.294124  0.384
2012 Liu Q, Kirubakaran S, Hur W, Niepel M, Westover K, Thoreen CC, Wang J, Ni J, Patricelli MP, Vogel K, Riddle S, Waller DL, Traynor R, Sanda T, Zhao Z, ... ... Gray NS, et al. Kinome-wide selectivity profiling of ATP-competitive mammalian target of rapamycin (mTOR) inhibitors and characterization of their binding kinetics. The Journal of Biological Chemistry. 287: 9742-52. PMID 22223645 DOI: 10.1074/Jbc.M111.304485  0.869
2012 Liu Q, Kang SA, Thoreen CC, Hur W, Wang J, Chang JW, Markhard A, Zhang J, Sim T, Sabatini DM, Gray NS. Development of ATP-competitive mTOR inhibitors. Methods in Molecular Biology (Clifton, N.J.). 821: 447-60. PMID 22125084 DOI: 10.1007/978-1-61779-430-8_29  0.844
2012 Kwiatkowski N, Deng X, Wang J, Tan L, Villa F, Santaguida S, Huang HC, Mitchison T, Musacchio A, Gray N. Selective aurora kinase inhibitors identified using a taxol-induced checkpoint sensitivity screen. Acs Chemical Biology. 7: 185-96. PMID 21992004 DOI: 10.1021/Cb200305U  0.764
2012 Nonami A, Sattler M, Weisberg EL, Qingsong L, Zhang J, Adelmant G, Marto JA, Kohl N, Kung AL, Sim T, Gray NS, Griffin JD. Deciphering the Critical Pathways of Mutant N-RAS in AML Using Small Molecule Inhibitors. Blood. 120: 2455-2455. DOI: 10.1182/Blood.V120.21.2455.2455  0.639
2012 Azarova AM, Bhatnagar N, Olsen-Drake L, Ross K, Frumm S, Liu Q, Christie A, Sanda T, Rodig SJ, Christensen JG, Kung AL, Gray N, Stegmaier K, George RE. Abstract 2935: The ATP-competitive mTOR inhibitor Torin2 enhances sensitivity of the ALK F1174L mutation to crizotinib in neuroblastoma Cancer Research. 72: 2935-2935. DOI: 10.1158/1538-7445.Am2012-2935  0.657
2012 Liao R, Hammerman P, Sivachenko A, Greulich H, Getz G, Liu Q, Gray N, Meyerson M. Abstract 2: FGFR3 as a therapeutic target in squamous cell lung carcinoma Cancer Research. 72: 2-2. DOI: 10.1158/1538-7445.Am2012-2  0.582
2012 Liao RG, Hammerman P, Sivachencko A, Greulich H, Getz G, Liu Q, Gray N, Meyerson M. Abstract B13: FGFR2 as a therapeutic target in squamous cell lung carcinoma Clinical Cancer Research. 18: B13-B13. DOI: 10.1158/1078-0432.12Aacriaslc-B13  0.588
2012 Moroco J, Craigo J, Gray N, Smithgall T. 225 Diversity in Individual Src-family Kinase Regulation: Opportunities for Selective Inhibitor Discovery European Journal of Cancer. 48: 68. DOI: 10.1016/S0959-8049(12)72023-3  0.367
2012 Clark K, MacKenzie K, Zhang J, Kristariyanto Y, Petkevicius K, Peggie M, Arthur S, Pedrioli P, Gray N, McIver E, Cohen P. P089 Identification of the first protein kinase inhibitors that switch macrophages from pro-inflammatory to anti-inflammatory cytokine production Cytokine. 59: 547-548. DOI: 10.1016/J.Cyto.2012.06.177  0.715
2011 Hammerman PS, Sos ML, Ramos AH, Xu C, Dutt A, Zhou W, Brace LE, Woods BA, Lin W, Zhang J, Deng X, Lim SM, Heynck S, Peifer M, Simard JR, ... ... Gray NS, et al. Mutations in the DDR2 kinase gene identify a novel therapeutic target in squamous cell lung cancer. Cancer Discovery. 1: 78-89. PMID 22328973 DOI: 10.1158/2159-8274.Cd-11-0005  0.576
2011 Miduturu CV, Deng X, Kwiatkowski N, Yang W, Brault L, Filippakopoulos P, Chung E, Yang Q, Schwaller J, Knapp S, King RW, Lee JD, Herrgard S, Zarrinkar P, Gray NS. High-throughput kinase profiling: a more efficient approach toward the discovery of new kinase inhibitors. Chemistry & Biology. 18: 868-79. PMID 21802008 DOI: 10.1016/J.Chembiol.2011.05.010  0.671
2011 Sasaki T, Koivunen J, Ogino A, Yanagita M, Nikiforow S, Zheng W, Lathan C, Marcoux JP, Du J, Okuda K, Capelletti M, Shimamura T, Ercan D, Stumpfova M, Xiao Y, ... ... Gray NS, et al. A novel ALK secondary mutation and EGFR signaling cause resistance to ALK kinase inhibitors. Cancer Research. 71: 6051-60. PMID 21791641 DOI: 10.1158/0008-5472.Can-11-1340  0.331
2011 Patricelli MP, Nomanbhoy TK, Wu J, Brown H, Zhou D, Zhang J, Jagannathan S, Aban A, Okerberg E, Herring C, Nordin B, Weissig H, Yang Q, Lee JD, Gray NS, et al. In situ kinase profiling reveals functionally relevant properties of native kinases. Chemistry & Biology. 18: 699-710. PMID 21700206 DOI: 10.1016/J.Chembiol.2011.04.011  0.454
2011 Hsu PP, Kang SA, Rameseder J, Zhang Y, Ottina KA, Lim D, Peterson TR, Choi Y, Gray NS, Yaffe MB, Marto JA, Sabatini DM. The mTOR-regulated phosphoproteome reveals a mechanism of mTORC1-mediated inhibition of growth factor signaling. Science (New York, N.Y.). 332: 1317-22. PMID 21659604 DOI: 10.1126/Science.1199498  0.712
2011 Liu Q, Wang J, Kang SA, Thoreen CC, Hur W, Choi HG, Waller DL, Sim T, Sabatini DM, Gray NS. Discovery and optimization of potent and selective benzonaphthyridinone analogs as small molecule mTOR inhibitors with improved mouse microsome stability. Bioorganic & Medicinal Chemistry Letters. 21: 4036-40. PMID 21621413 DOI: 10.1016/J.Bmcl.2011.04.129  0.829
2011 Deng X, Wang J, Zhang J, Sim T, Kim ND, Sasaki T, Luther W, George RE, Jänne PA, Gray NS. Discovery of 3,5-Diamino-1,2,4-triazole Ureas as Potent Anaplastic Lymphoma Kinase Inhibitors. Acs Medicinal Chemistry Letters. 2: 379-384. PMID 21572589 DOI: 10.1021/Ml200002A  0.646
2011 Deng X, Yang Q, Kwiatkowski N, Sim T, McDermott U, Settleman JE, Lee JD, Gray NS. Discovery of a benzo[e]pyrimido-[5,4-b][1,4]diazepin-6(11H)-one as a Potent and Selective Inhibitor of Big MAP Kinase 1. Acs Medicinal Chemistry Letters. 2: 195-200. PMID 21412406 DOI: 10.1021/Ml100304B  0.615
2011 Deng X, Dzamko N, Prescott A, Davies P, Liu Q, Yang Q, Lee JD, Patricelli MP, Nomanbhoy TK, Alessi DR, Gray NS. Characterization of a selective inhibitor of the Parkinson's disease kinase LRRK2. Nature Chemical Biology. 7: 203-5. PMID 21378983 DOI: 10.1038/Nchembio.538  0.776
2011 Liu Q, Wang J, Kang SA, Thoreen CC, Hur W, Ahmed T, Sabatini DM, Gray NS. Discovery of 9-(6-aminopyridin-3-yl)-1-(3-(trifluoromethyl)phenyl)benzo[h][1,6]naphthyridin-2(1H)-one (Torin2) as a potent, selective, and orally available mammalian target of rapamycin (mTOR) inhibitor for treatment of cancer. Journal of Medicinal Chemistry. 54: 1473-80. PMID 21322566 DOI: 10.1021/Jm101520V  0.852
2011 Iacob RE, Zhang J, Gray NS, Engen JR. Allosteric interactions between the myristate- and ATP-site of the Abl kinase. Plos One. 6: e15929. PMID 21264348 DOI: 10.1371/Journal.Pone.0015929  0.34
2011 Zhou W, Ercan D, Jänne PA, Gray NS. Discovery of selective irreversible inhibitors for EGFR-T790M. Bioorganic & Medicinal Chemistry Letters. 21: 638-43. PMID 21208802 DOI: 10.1016/j.bmcl.2010.12.036  0.404
2011 Zhou W, Ercan D, Jänne PA, Gray NS. Discovery of selective irreversible inhibitors for EGFR-T790M. Bioorganic & Medicinal Chemistry Letters. 21: 638-43. PMID 21208802 DOI: 10.1016/j.bmcl.2010.12.036  0.404
2011 Sasaki T, Okuda K, Zheng W, Butrynski J, Capelletti M, Wang L, Gray N, Wilner KD, Christensen JG, Demetri GD, Shapiro GI, Rodig SJ, Eck MJ, Jänne PA. Abstract 1541: Secondary mutations in ALK and resistance to ALK kinase inhibitors Cancer Research. 71: 1541-1541. DOI: 10.1158/1538-7445.Am2011-1541  0.449
2010 Sasaki T, Okuda K, Zheng W, Butrynski J, Capelletti M, Wang L, Gray NS, Wilner K, Christensen JG, Demetri G, Shapiro GI, Rodig SJ, Eck MJ, Jänne PA. The neuroblastoma-associated F1174L ALK mutation causes resistance to an ALK kinase inhibitor in ALK-translocated cancers. Cancer Research. 70: 10038-43. PMID 21030459 DOI: 10.1158/0008-5472.Can-10-2956  0.37
2010 Chen Z, Sasaki T, Tan X, Carretero J, Shimamura T, Li D, Xu C, Wang Y, Adelmant GO, Capelletti M, Lee HJ, Rodig SJ, Borgman C, Park SI, Kim HR, ... ... Gray NS, et al. Inhibition of ALK, PI3K/MEK, and HSP90 in murine lung adenocarcinoma induced by EML4-ALK fusion oncogene. Cancer Research. 70: 9827-36. PMID 20952506 DOI: 10.1158/0008-5472.Can-10-1671  0.615
2010 Liu Q, Chang JW, Wang J, Kang SA, Thoreen CC, Markhard A, Hur W, Zhang J, Sim T, Sabatini DM, Gray NS. Discovery of 1-(4-(4-propionylpiperazin-1-yl)-3-(trifluoromethyl)phenyl)-9-(quinolin-3-yl)benzo[h][1,6]naphthyridin-2(1H)-one as a highly potent, selective mammalian target of rapamycin (mTOR) inhibitor for the treatment of cancer. Journal of Medicinal Chemistry. 53: 7146-55. PMID 20860370 DOI: 10.1021/Jm101144F  0.869
2010 Yang Q, Deng X, Lu B, Cameron M, Fearns C, Patricelli MP, Yates JR, Gray NS, Lee JD. Pharmacological inhibition of BMK1 suppresses tumor growth through promyelocytic leukemia protein. Cancer Cell. 18: 258-67. PMID 20832753 DOI: 10.1016/J.Ccr.2010.08.008  0.577
2010 Deng X, Okram B, Ding Q, Zhang J, Choi Y, Adrián FJ, Wojciechowski A, Zhang G, Che J, Bursulaya B, Cowan-Jacob SW, Rummel G, Sim T, Gray NS. Expanding the diversity of allosteric bcr-abl inhibitors. Journal of Medicinal Chemistry. 53: 6934-46. PMID 20828158 DOI: 10.1021/Jm100555F  0.845
2010 Weisberg E, Choi HG, Barrett R, Zhou W, Zhang J, Ray A, Nelson EA, Jiang J, Moreno D, Stone R, Galinsky I, Fox E, Adamia S, Kung AL, Gray NS, et al. Discovery and characterization of novel mutant FLT3 kinase inhibitors. Molecular Cancer Therapeutics. 9: 2468-77. PMID 20807780 DOI: 10.1158/1535-7163.Mct-10-0232  0.464
2010 Deng X, Nagle A, Wu T, Sakata T, Henson K, Chen Z, Kuhen K, Plouffe D, Winzeler E, Adrian F, Tuntland T, Chang J, Simerson S, Howard S, Ek J, ... ... Gray NS, et al. Discovery of novel 1H-imidazol-2-yl-pyrimidine-4,6-diamines as potential antimalarials. Bioorganic & Medicinal Chemistry Letters. 20: 4027-31. PMID 20610151 DOI: 10.1016/J.Bmcl.2010.05.095  0.757
2010 Choi HG, Ren P, Adrian F, Sun F, Lee HS, Wang X, Ding Q, Zhang G, Xie Y, Zhang J, Liu Y, Tuntland T, Warmuth M, Manley PW, Mestan J, ... Gray NS, et al. A type-II kinase inhibitor capable of inhibiting the T315I "gatekeeper" mutant of Bcr-Abl. Journal of Medicinal Chemistry. 53: 5439-48. PMID 20604564 DOI: 10.1021/Jm901808W  0.7
2010 Deng X, Lim SM, Zhang J, Gray NS. Broad spectrum alkynyl inhibitors of T315I Bcr-Abl. Bioorganic & Medicinal Chemistry Letters. 20: 4196-200. PMID 20541934 DOI: 10.1016/J.Bmcl.2010.05.043  0.599
2010 Hur W, Sun Z, Jiang T, Mason DE, Peters EC, Zhang DD, Luesch H, Schultz PG, Gray NS. A small-molecule inducer of the antioxidant response element. Chemistry & Biology. 17: 537-47. PMID 20534351 DOI: 10.1016/J.Chembiol.2010.03.013  0.631
2010 Weisberg E, Deng X, Choi HG, Barrett R, Adamia S, Ray A, Moreno D, Kung AL, Gray N, Griffin JD. Beneficial effects of combining a type II ATP competitive inhibitor with an allosteric competitive inhibitor of BCR-ABL for the treatment of imatinib-sensitive and imatinib-resistant CML. Leukemia. 24: 1375-8. PMID 20508612 DOI: 10.1038/Leu.2010.107  0.614
2010 Kwiatkowski N, Jelluma N, Filippakopoulos P, Soundararajan M, Manak MS, Kwon M, Choi HG, Sim T, Deveraux QL, Rottmann S, Pellman D, Shah JV, Kops GJ, Knapp S, Gray NS. Small-molecule kinase inhibitors provide insight into Mps1 cell cycle function. Nature Chemical Biology. 6: 359-68. PMID 20383151 DOI: 10.1038/Nchembio.345  0.444
2010 Zhou W, Hur W, McDermott U, Dutt A, Xian W, Ficarro SB, Zhang J, Sharma SV, Brugge J, Meyerson M, Settleman J, Gray NS. A structure-guided approach to creating covalent FGFR inhibitors. Chemistry & Biology. 17: 285-95. PMID 20338520 DOI: 10.1016/J.Chembiol.2010.02.007  0.475
2010 Weisberg E, Choi HG, Ray A, Barrett R, Zhang J, Sim T, Zhou W, Seeliger M, Cameron M, Azam M, Fletcher JA, Debiec-Rychter M, Mayeda M, Moreno D, Kung AL, ... ... Gray N, et al. Discovery of a small-molecule type II inhibitor of wild-type and gatekeeper mutants of BCR-ABL, PDGFRalpha, Kit, and Src kinases: novel type II inhibitor of gatekeeper mutants. Blood. 115: 4206-16. PMID 20299508 DOI: 10.1182/Blood-2009-11-251751  0.499
2010 Fabbro D, Manley PW, Jahnke W, Liebetanz J, Szyttenholm A, Fendrich G, Strauss A, Zhang J, Gray NS, Adrian F, Warmuth M, Pelle X, Grotzfeld R, Berst F, Marzinzik A, et al. Inhibitors of the Abl kinase directed at either the ATP- or myristate-binding site. Biochimica Et Biophysica Acta. 1804: 454-62. PMID 20152788 DOI: 10.1016/j.bbapap.2009.12.009  0.427
2010 McDermott U, Pusapati RV, Christensen JG, Gray NS, Settleman J. Acquired resistance of non-small cell lung cancer cells to MET kinase inhibition is mediated by a switch to epidermal growth factor receptor dependency. Cancer Research. 70: 1625-34. PMID 20124471 DOI: 10.1158/0008-5472.CAN-09-3620  0.368
2010 Zhang J, Adrián FJ, Jahnke W, Cowan-Jacob SW, Li AG, Iacob RE, Sim T, Powers J, Dierks C, Sun F, Guo GR, Ding Q, Okram B, Choi Y, Wojciechowski A, ... ... Gray NS, et al. Targeting Bcr-Abl by combining allosteric with ATP-binding-site inhibitors. Nature. 463: 501-6. PMID 20072125 DOI: 10.1038/Nature08675  0.823
2010 Ding S, Gray NS, Ding Q, Schultz PG. ChemInform Abstract: Expanding the Diversity of Purine Libraries. Cheminform. 33: no-no. DOI: 10.1002/chin.200210137  0.342
2009 Speake G, Klinowska T, Hickinson M, Marshall G, Smith P, Vincent J, Anderton J, Gray N, Smith I, Ogilvie D. Characterization of AZD8931, a potent reversible small molecule inhibitor against epidermal growth factor receptor (EGFR), erythroblastic leukemia viral oncogene homolog 2 (HER2) and 3 (HER3) with a unique and balanced pharmacological profile. Journal of Clinical Oncology : Official Journal of the American Society of Clinical Oncology. 27: 11072. PMID 27963188 DOI: 10.1200/Jco.2009.27.15_Suppl.11072  0.45
2009 Liu Q, Thoreen C, Wang J, Sabatini D, Gray NS. mTOR Mediated Anti-Cancer Drug Discovery. Drug Discovery Today. Therapeutic Strategies. 6: 47-55. PMID 20622997 DOI: 10.1016/J.Ddstr.2009.12.001  0.843
2009 Zhou W, Ercan D, Chen L, Yun CH, Li D, Capelletti M, Cortot AB, Chirieac L, Iacob RE, Padera R, Engen JR, Wong KK, Eck MJ, Gray NS, Jänne PA. Novel mutant-selective EGFR kinase inhibitors against EGFR T790M. Nature. 462: 1070-4. PMID 20033049 DOI: 10.1038/Nature08622  0.401
2009 Emery CM, Vijayendran KG, Zipser MC, Sawyer AM, Niu L, Kim JJ, Hatton C, Chopra R, Oberholzer PA, Karpova MB, MacConaill LE, Zhang J, Gray NS, Sellers WR, Dummer R, et al. MEK1 mutations confer resistance to MEK and B-RAF inhibition. Proceedings of the National Academy of Sciences of the United States of America. 106: 20411-6. PMID 19915144 DOI: 10.1073/Pnas.0905833106  0.349
2009 Wu T, Nagle A, Sakata T, Henson K, Borboa R, Chen Z, Kuhen K, Plouffe D, Winzeler E, Adrian F, Tuntland T, Chang J, Simerson S, Howard S, Ek J, ... ... Gray NS, et al. Cell-based optimization of novel benzamides as potential antimalarial leads. Bioorganic & Medicinal Chemistry Letters. 19: 6970-4. PMID 19879133 DOI: 10.1016/J.Bmcl.2009.10.050  0.805
2009 Zhang G, Ren P, Gray NS, Sim T, Wang X, Liu Y, Che J, Dong W, Tian SS, Sandberg ML, Spalding TA, Romeo R, Iskandar M, Wang Z, Seidel HM, et al. Discovery of pyrimidine benzimidazoles as Src-family selective Lck inhibitors. Part II. Bioorganic & Medicinal Chemistry Letters. 19: 6691-5. PMID 19854052 DOI: 10.1016/J.Bmcl.2009.09.123  0.545
2009 Choi Y, Seeliger MA, Panjarian SB, Kim H, Deng X, Sim T, Couch B, Koleske AJ, Smithgall TE, Gray NS. N-myristoylated c-Abl tyrosine kinase localizes to the endoplasmic reticulum upon binding to an allosteric inhibitor. The Journal of Biological Chemistry. 284: 29005-14. PMID 19679652 DOI: 10.1074/Jbc.M109.026633  0.618
2009 Jänne PA, Gray N, Settleman J. Factors underlying sensitivity of cancers to small-molecule kinase inhibitors. Nature Reviews. Drug Discovery. 8: 709-23. PMID 19629074 DOI: 10.1038/Nrd2871  0.464
2009 Choi Y, Syeda F, Walker JR, Finerty PJ, Cuerrier D, Wojciechowski A, Liu Q, Dhe-Paganon S, Gray NS. Discovery and structural analysis of Eph receptor tyrosine kinase inhibitors. Bioorganic & Medicinal Chemistry Letters. 19: 4467-70. PMID 19553108 DOI: 10.1016/J.Bmcl.2009.05.029  0.646
2009 Weisberg E, Barrett R, Liu Q, Stone R, Gray N, Griffin JD. FLT3 inhibition and mechanisms of drug resistance in mutant FLT3-positive AML. Drug Resistance Updates : Reviews and Commentaries in Antimicrobial and Anticancer Chemotherapy. 12: 81-9. PMID 19467916 DOI: 10.1016/J.Drup.2009.04.001  0.683
2009 Peterson TR, Laplante M, Thoreen CC, Sancak Y, Kang SA, Kuehl WM, Gray NS, Sabatini DM. DEPTOR is an mTOR inhibitor frequently overexpressed in multiple myeloma cells and required for their survival. Cell. 137: 873-86. PMID 19446321 DOI: 10.1016/J.Cell.2009.03.046  0.791
2009 Iacob RE, Pene-Dumitrescu T, Zhang J, Gray NS, Smithgall TE, Engen JR. Conformational disturbance in Abl kinase upon mutation and deregulation. Proceedings of the National Academy of Sciences of the United States of America. 106: 1386-91. PMID 19164531 DOI: 10.1073/Pnas.0811912106  0.306
2009 Thoreen CC, Kang SA, Chang JW, Liu Q, Zhang J, Gao Y, Reichling LJ, Sim T, Sabatini DM, Gray NS. An ATP-competitive mammalian target of rapamycin inhibitor reveals rapamycin-resistant functions of mTORC1. The Journal of Biological Chemistry. 284: 8023-32. PMID 19150980 DOI: 10.1074/Jbc.M900301200  0.852
2009 Zhang J, Yang PL, Gray NS. Targeting cancer with small molecule kinase inhibitors. Nature Reviews. Cancer. 9: 28-39. PMID 19104514 DOI: 10.1038/Nrc2559  0.677
2009 Klinowska T, Hickinson M, Speake G, Marshall G, Beck S, Smith P, Vincent J, Anderton J, Gray N, Ogilvie D. 1225 AZD8931, an equipotent, reversible inhibitor of erbB1, erbB2 and erbB3 receptor signalling: characterisation of pharmacological profile European Journal of Cancer Supplements. 7: 127-128. DOI: 10.1016/S1359-6349(09)70437-9  0.374
2009 Liu Q, Thoreen C, Wang J, Sabatini D, Gray NS. MTOR mediated anti-cancer drug discovery Drug Discovery Today: Therapeutic Strategies. 6: 47-55. DOI: 10.1016/j.ddstr.2009.12.001  0.479
2008 George RE, Sanda T, Hanna M, Fröhling S, Luther W, Zhang J, Ahn Y, Zhou W, London WB, McGrady P, Xue L, Zozulya S, Gregor VE, Webb TR, Gray NS, et al. Activating mutations in ALK provide a therapeutic target in neuroblastoma. Nature. 455: 975-8. PMID 18923525 DOI: 10.1038/Nature07397  0.349
2008 Azam M, Seeliger MA, Gray NS, Kuriyan J, Daley GQ. Activation of tyrosine kinases by mutation of the gatekeeper threonine Nature Structural and Molecular Biology. 15: 1109-1118. PMID 18794843 DOI: 10.1038/Nsmb.1486  0.409
2008 Zhang G, Ren P, Gray NS, Sim T, Liu Y, Wang X, Che J, Tian SS, Sandberg ML, Spalding TA, Romeo R, Iskandar M, Chow D, Martin Seidel H, Karanewsky DS, et al. Discovery of pyrimidine benzimidazoles as Lck inhibitors: part I. Bioorganic & Medicinal Chemistry Letters. 18: 5618-21. PMID 18793846 DOI: 10.1016/J.Bmcl.2008.08.104  0.543
2008 Hur W, Velentza A, Kim S, Flatauer L, Jiang X, Valente D, Mason DE, Suzuki M, Larson B, Zhang J, Zagorska A, Didonato M, Nagle A, Warmuth M, Balk SP, ... ... Gray NS, et al. Clinical stage EGFR inhibitors irreversibly alkylate Bmx kinase. Bioorganic & Medicinal Chemistry Letters. 18: 5916-9. PMID 18667312 DOI: 10.1016/J.Bmcl.2008.07.062  0.769
2008 Koivunen JP, Mermel C, Zejnullahu K, Murphy C, Lifshits E, Holmes AJ, Choi HG, Kim J, Chiang D, Thomas R, Lee J, Richards WG, Sugarbaker DJ, Ducko C, Lindeman N, ... ... Gray NS, et al. EML4-ALK fusion gene and efficacy of an ALK kinase inhibitor in lung cancer. Clinical Cancer Research : An Official Journal of the American Association For Cancer Research. 14: 4275-83. PMID 18594010 DOI: 10.1158/1078-0432.Ccr-08-0168  0.331
2008 Plouffe D, Brinker A, McNamara C, Henson K, Kato N, Kuhen K, Nagle A, Adrián F, Matzen JT, Anderson P, Nam TG, Gray NS, Chatterjee A, Janes J, Yan SF, et al. In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen. Proceedings of the National Academy of Sciences of the United States of America. 105: 9059-64. PMID 18579783 DOI: 10.1073/Pnas.0802982105  0.815
2008 Kato N, Sakata T, Breton G, Le Roch KG, Nagle A, Andersen C, Bursulaya B, Henson K, Johnson J, Kumar KA, Marr F, Mason D, McNamara C, Plouffe D, Ramachandran V, ... ... Gray N, et al. Gene expression signatures and small-molecule compounds link a protein kinase to Plasmodium falciparum motility. Nature Chemical Biology. 4: 347-56. PMID 18454143 DOI: 10.1038/Nchembio.87  0.807
2008 McDermott U, Iafrate AJ, Gray NS, Shioda T, Classon M, Maheswaran S, Zhou W, Choi HG, Smith SL, Dowell L, Ulkus LE, Kuhlmann G, Greninger P, Christensen JG, Haber DA, et al. Genomic alterations of anaplastic lymphoma kinase may sensitize tumors to anaplastic lymphoma kinase inhibitors. Cancer Research. 68: 3389-95. PMID 18451166 DOI: 10.1158/0008-5472.Can-07-6186  0.398
2008 Goldstein DM, Gray NS, Zarrinkar PP. High-throughput kinase profiling as a platform for drug discovery. Nature Reviews. Drug Discovery. 7: 391-7. PMID 18404149 DOI: 10.1038/nrd2541  0.43
2008 Andersen CB, Wan Y, Chang JW, Riggs B, Lee C, Liu Y, Sessa F, Villa F, Kwiatkowski N, Suzuki M, Nallan L, Heald R, Musacchio A, Gray NS. Discovery of selective aminothiazole aurora kinase inhibitors. Acs Chemical Biology. 3: 180-92. PMID 18307303 DOI: 10.1021/Cb700200W  0.539
2008 Supekova L, Supek F, Lee J, Chen S, Gray N, Pezacki JP, Schlapbach A, Schultz PG. Identification of human kinases involved in hepatitis C virus replication by small interference RNA library screening. The Journal of Biological Chemistry. 283: 29-36. PMID 17951261 DOI: 10.1074/Jbc.M703988200  0.797
2008 McMillin DW, Negri J, Delmore J, Ooi MG, Jakubikova J, Wright R, Gray N, Kung A, Anderson KC, Mitsiades CS. Activity of Plk Inhibitor BI2536 on Myeloma Cells Blood. 112: 2764-2764. DOI: 10.1182/Blood.V112.11.2764.2764  0.443
2007 McDermott U, Sharma SV, Dowell L, Greninger P, Montagut C, Lamb J, Archibald H, Raudales R, Tam A, Lee D, Rothenberg SM, Supko JG, Sordella R, Ulkus LE, Iafrate AJ, ... ... Gray NS, et al. Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. Proceedings of the National Academy of Sciences of the United States of America. 104: 19936-41. PMID 18077425 DOI: 10.1073/pnas.0707498104  0.448
2007 Peters EC, Gray NS. Chemical proteomics identifies unanticipated targets of clinical kinase inhibitors. Acs Chemical Biology. 2: 661-4. PMID 18041816 DOI: 10.1021/cb700203j  0.46
2007 Jansma A, Zhang Q, Li B, Ding Q, Uno T, Bursulaya B, Liu Y, Furet P, Gray NS, Geierstanger BH. Verification of a designed intramolecular hydrogen bond in a drug scaffold by nuclear magnetic resonance spectroscopy Journal of Medicinal Chemistry. 50: 5875-5877. PMID 17975906 DOI: 10.1021/jm700983a  0.752
2007 Hong J, Lee J, Min KH, Walker JR, Peters EC, Gray NS, Cho CY, Schultz PG. Identification and characterization of small-molecule inducers of epidermal keratinocyte differentiation. Acs Chemical Biology. 2: 171-5. PMID 17348628 DOI: 10.1021/Cb600435T  0.764
2007 Galkin AV, Melnick JS, Kim S, Hood TL, Li N, Li L, Xia G, Steensma R, Chopiuk G, Jiang J, Wan Y, Ding P, Liu Y, Sun F, Schultz PG, ... Gray NS, et al. Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. Proceedings of the National Academy of Sciences of the United States of America. 104: 270-5. PMID 17185414 DOI: 10.1073/Pnas.0609412103  0.846
2007 Azam M, Seeliger M, Gray NS, Kuriyan J, Daley GQ. A Unified Mechanism of Tyrosine Kinase Regulation by the Gatekeeper Residue. Blood. 110: 223-223. DOI: 10.1182/Blood.V110.11.223.223  0.418
2007 Powers JT, Azam M, Gray NS, Daley GQ. Dissection of Bcr-abl Structural Domains Relating to Kinase Auto-Inhibition Using a Forward Mutational Screen with the Non-ATP Competitive Inhibitor GNF-2. Blood. 110: 1021-1021. DOI: 10.1182/Blood.V110.11.1021.1021  0.399
2006 Pan S, Mi Y, Pally C, Beerli C, Chen A, Guerini D, Hinterding K, Nuesslein-Hildesheim B, Tuntland T, Lefebvre S, Liu Y, Gao W, Chu A, Brinkmann V, Bruns C, ... ... Gray N, et al. A monoselective sphingosine-1-phosphate receptor-1 agonist prevents allograft rejection in a stringent rat heart transplantation model. Chemistry & Biology. 13: 1227-34. PMID 17114004 DOI: 10.1016/J.Chembiol.2006.09.017  0.431
2006 Okram B, Nagle A, Adrián FJ, Lee C, Ren P, Wang X, Sim T, Xie Y, Wang X, Xia G, Spraggon G, Warmuth M, Liu Y, Gray NS. A general strategy for creating "inactive-conformation" abl inhibitors. Chemistry & Biology. 13: 779-86. PMID 16873026 DOI: 10.1016/J.Chembiol.2006.05.015  0.824
2006 Liu Y, Gray NS. Rational design of inhibitors that bind to inactive kinase conformations. Nature Chemical Biology. 2: 358-64. PMID 16783341 DOI: 10.1038/nchembio799  0.524
2006 Choi HS, Wang Z, Richmond W, He X, Yang K, Jiang T, Karanewsky D, Gu XJ, Zhou V, Liu Y, Che J, Lee CC, Caldwell J, Kanazawa T, Umemura I, ... ... Gray N, et al. Design and synthesis of 7H-pyrrolo[2,3-d]pyrimidines as focal adhesion kinase inhibitors. Part 2. Bioorganic & Medicinal Chemistry Letters. 16: 2689-92. PMID 16524731 DOI: 10.1016/j.bmcl.2006.02.032  0.503
2006 Nagle A, Hur W, Gray NS. Antimitotic agents of natural origin. Current Drug Targets. 7: 305-26. PMID 16515529 DOI: 10.2174/138945006776054933  0.709
2006 Melnick JS, Janes J, Kim S, Chang JY, Sipes DG, Gunderson D, Jarnes L, Matzen JT, Garcia ME, Hood TL, Beigi R, Xia G, Harig RA, Asatryan H, Yan SF, ... ... Gray NS, et al. An efficient rapid system for profiling the cellular activities of molecular libraries. Proceedings of the National Academy of Sciences of the United States of America. 103: 3153-8. PMID 16492761 DOI: 10.1073/Pnas.0511292103  0.848
2006 Zhang Q, Liu Y, Gao F, Ding Q, Cho C, Hur W, Jin Y, Uno T, Joazeiro CA, Gray N. Discovery of EGFR selective 4,6-disubstituted pyrimidines from a combinatorial kinase-directed heterocycle library. Journal of the American Chemical Society. 128: 2182-3. PMID 16478150 DOI: 10.1021/Ja0567485  0.851
2006 Choi HS, Wang Z, Richmond W, He X, Yang K, Jiang T, Sim T, Karanewsky D, Gu XJ, Zhou V, Liu Y, Ohmori O, Caldwell J, Gray N, He Y. Design and synthesis of 7H-pyrrolo[2,3-d]pyrimidines as focal adhesion kinase inhibitors. Part 1. Bioorganic & Medicinal Chemistry Letters. 16: 2173-6. PMID 16458503 DOI: 10.1016/J.Bmcl.2006.01.053  0.555
2006 Adrián FJ, Ding Q, Sim T, Velentza A, Sloan C, Liu Y, Zhang G, Hur W, Ding S, Manley P, Mestan J, Fabbro D, Gray NS. Allosteric inhibitors of Bcr-abl-dependent cell proliferation Nature Chemical Biology. 2: 95-102. PMID 16415863 DOI: 10.1038/Nchembio760  0.711
2005 Han S, Zhou V, Pan S, Liu Y, Hornsby M, McMullan D, Klock HE, Haugen J, Lesley SA, Gray N, Caldwell J, Gu XJ. Identification of coumarin derivatives as a novel class of allosteric MEK1 inhibitors. Bioorganic & Medicinal Chemistry Letters. 15: 5467-73. PMID 16199156 DOI: 10.1016/J.Bmcl.2005.08.097  0.731
2005 Tang L, Li MH, Cao P, Wang F, Chang WR, Bach S, Reinhardt J, Ferandin Y, Galons H, Wan Y, Gray N, Meijer L, Jiang T, Liang DC. Crystal structure of pyridoxal kinase in complex with roscovitine and derivatives. The Journal of Biological Chemistry. 280: 31220-9. PMID 15985434 DOI: 10.1074/Jbc.M500805200  0.394
2005 Bach S, Knockaert M, Reinhardt J, Lozach O, Schmitt S, Baratte B, Koken M, Coburn SP, Tang L, Jiang T, Liang DC, Galons H, Dierick JF, Pinna LA, Meggio F, ... ... Gray N, et al. Roscovitine targets, protein kinases and pyridoxal kinase. The Journal of Biological Chemistry. 280: 31208-19. PMID 15975926 DOI: 10.1074/Jbc.M500806200  0.52
2005 Luesch H, Wu TY, Ren P, Gray NS, Schultz PG, Supek F. A genome-wide overexpression screen in yeast for small-molecule target identification. Chemistry & Biology. 12: 55-63. PMID 15664515 DOI: 10.1016/J.Chembiol.2004.10.015  0.777
2004 Li B, Liu Y, Uno T, Gray N. Creating chemical diversity to target protein kinases. Combinatorial Chemistry & High Throughput Screening. 7: 453-72. PMID 15320712 DOI: 10.2174/1386207043328580  0.604
2004 Wan Y, Hur W, Cho CY, Liu Y, Adrian FJ, Lozach O, Bach S, Mayer T, Fabbro D, Meijer L, Gray NS. Synthesis and target identification of hymenialdisine analogs. Chemistry & Biology. 11: 247-59. PMID 15123286 DOI: 10.1016/j.chembiol.2004.01.015  0.746
2004 Wignall SM, Gray NS, Chang YT, Juarez L, Jacob R, Burlingame A, Schultz PG, Heald R. Identification of a novel protein regulating microtubule stability through a chemical approach. Chemistry & Biology. 11: 135-46. PMID 15113003 DOI: 10.1016/J.Chembiol.2003.12.019  0.623
2004 Wu X, Ding S, Ding Q, Gray NS, Schultz PG. Small molecules that induce cardiomyogenesis in embryonic stem cells. Journal of the American Chemical Society. 126: 1590-1. PMID 14871063 DOI: 10.1021/Ja038950I  0.64
2004 Sanna MG, Liao J, Jo E, Alfonso C, Ahn MY, Peterson MS, Webb B, Lefebvre S, Chun J, Gray N, Rosen H. Sphingosine 1-phosphate (S1P) receptor subtypes S1P1 and S1P3, respectively, regulate lymphocyte recirculation and heart rate. The Journal of Biological Chemistry. 279: 13839-48. PMID 14732717 DOI: 10.1074/Jbc.M311743200  0.556
2003 Warmuth M, Damoiseaux R, Liu Y, Fabbro D, Gray N. SRC family kinases: potential targets for the treatment of human cancer and leukemia. Current Pharmaceutical Design. 9: 2043-59. PMID 14529415 DOI: 10.2174/1381612033454126  0.591
2003 Ding S, Wu TY, Brinker A, Peters EC, Hur W, Gray NS, Schultz PG. Synthetic small molecules that control stem cell fate. Proceedings of the National Academy of Sciences of the United States of America. 100: 7632-7. PMID 12794184 DOI: 10.1073/Pnas.0732087100  0.803
2003 Ruetz S, Fabbro D, Zimmermann J, Meyer T, Gray N. Chemical and biological profile of dual Cdk1 and Cdk2 inhibitors. Current Medicinal Chemistry. Anti-Cancer Agents. 3: 1-14. PMID 12678910 DOI: 10.2174/1568011033353605  0.499
2002 Wu X, Ding S, Ding Q, Gray NS, Schultz PG. A small molecule with osteogenesis-inducing activity in multipotent mesenchymal progenitor cells. Journal of the American Chemical Society. 124: 14520-1. PMID 12465946 DOI: 10.1021/Ja0283908  0.65
2002 Knockaert M, Lenormand P, Gray N, Schultz P, Pouysségur J, Meijer L. p42/p44 MAPKs are intracellular targets of the CDK inhibitor purvalanol. Oncogene. 21: 6413-24. PMID 12226745 DOI: 10.1038/Sj.Onc.1205908  0.599
2002 Chang YT, Choi G, Bae YS, Burdett M, Moon HS, Lee JW, Gray NS, Schultz PG, Meijer L, Chung SK, Choi KY, Suh PG, Ryu SH. Purine-based inhibitors of inositol-1,4,5-trisphosphate-3-kinase. Chembiochem : a European Journal of Chemical Biology. 3: 897-901. PMID 12210991 DOI: 10.1002/1439-7633(20020902)3:9<897::Aid-Cbic897>3.0.Co;2-B  0.732
2002 Ding S, Gray NS, Ding Q, Wu X, Schultz PG. Resin-capture and release strategy toward combinatorial libraries of 2,6,9-substituted purines. Journal of Combinatorial Chemistry. 4: 183-6. PMID 11886295 DOI: 10.1021/Cc010080I  0.602
2002 Ding S, Gray NS, Wu X, Ding Q, Schultz PG. A combinatorial scaffold approach toward kinase-directed heterocycle libraries. Journal of the American Chemical Society. 124: 1594-6. PMID 11853431 DOI: 10.1021/Ja0170302  0.677
2001 Chang YT, Wignall SM, Rosania GR, Gray NS, Hanson SR, Su AI, Merlie J, Moon HS, Sangankar SB, Perez O, Heald R, Schultz PG. Synthesis and biological evaluation of myoseverin derivatives: microtubule assembly inhibitors. Journal of Medicinal Chemistry. 44: 4497-500. PMID 11741468 DOI: 10.1021/Jm010451+  0.812
2001 Ding S, Gray NS, Ding Q, Schultz PG. A concise and traceless linker strategy toward combinatorial libraries of 2,6,9-substituted purines. The Journal of Organic Chemistry. 66: 8273-6. PMID 11722241 DOI: 10.1021/Jo016010F  0.563
2001 Wu TY, Ding S, Gray NS, Schultz PG. Solid-phase synthesis of 2,3,5-trisubstituted indoles. Organic Letters. 3: 3827-30. PMID 11720546 DOI: 10.1021/Ol016525T  0.623
2001 Lin Q, Jiang F, Schultz PG, Gray NS. Design of allele-specific protein methyltransferase inhibitors Journal of the American Chemical Society. 123: 11608-11613. PMID 11716715 DOI: 10.1021/Ja011423J  0.785
2001 Gray NS. Combinatorial libraries and biological discovery Current Opinion in Neurobiology. 11: 608-614. PMID 11595496 DOI: 10.1016/S0959-4388(00)00257-9  0.315
2001 Verdugo DE, Cancilla MT, Ge X, Gray NS, Chang YT, Schultz PG, Negishi M, Leary JA, Bertozzi CR. Discovery of estrogen sulfotransferase inhibitors from a purine library screen. Journal of Medicinal Chemistry. 44: 2683-6. PMID 11495578 DOI: 10.1021/Jm010171U  0.593
2001 Harmse L, van Zyl R, Gray N, Schultz P, Leclerc S, Meijer L, Doerig C, Havlik I. Structure-activity relationships and inhibitory effects of various purine derivatives on the in vitro growth of Plasmodium falciparum. Biochemical Pharmacology. 62: 341-8. PMID 11434907 DOI: 10.1016/S0006-2952(01)00644-X  0.578
2001 Ding S, Gray NS, Ding Q, Schultz PG. Expanding the diversity of purine libraries Tetrahedron Letters. 42: 8751-8755. DOI: 10.1016/S0040-4039(01)01925-6  0.543
2000 Bishop AC, Ubersax JA, Petsch DT, Matheos DP, Gray NS, Blethrow J, Shimizu E, Tsien JZ, Schultz PG, Rose MD, Wood JL, Morgan DO, Shokat KM. A chemical switch for inhibitor-sensitive alleles of any protein kinase. Nature. 407: 395-401. PMID 11014197 DOI: 10.1038/35030148  0.699
2000 Knockaert M, Gray N, Damiens E, Chang YT, Grellier P, Grant K, Fergusson D, Mottram J, Soete M, Dubremetz JF, Le Roch K, Doerig C, Schultz P, Meijer L. Intracellular targets of cyclin-dependent kinase inhibitors: identification by affinity chromatography using immobilised inhibitors. Chemistry & Biology. 7: 411-22. PMID 10873834 DOI: 10.1016/S1074-5521(00)00124-1  0.657
2000 Armstrong JI, Portley AR, Chang YT, Nierengarten DM, Cook BN, Bowman KG, Bishop A, Gray NS, Shokat KM, Schultz PG, Bertozzi CR. Discovery of Carbohydrate Sulfotransferase Inhibitors from a Kinase-Directed Library We thank Sharon Long and Dave Keating for providing both the NodH sulfotransferase and APS Kinase during our preliminary experiments and Jack Kirsch for numerous helpful conversations. J.I.A. and K.G.B were supported by NIH Molecular Biophysics Training Grant (No. T32GM0895). This research was funded by grants to C.R.B. from the Pew Scholars Program, the W. M. Keck Foundation and the American Cancer Society (Grant No. RPG9700501BE). Angewandte Chemie (International Ed. in English). 39: 1303-1306. PMID 10767039 DOI: 10.1002/(Sici)1521-3773(20000403)39:7<1303::Aid-Anie1303>3.0.Co;2-0  0.671
1999 Chang YT, Gray NS, Rosania GR, Sutherlin DP, Kwon S, Norman TC, Sarohia R, Leost M, Meijer L, Schultz PG. Synthesis and application of functionally diverse 2,6,9-trisubstituted purine libraries as CDK inhibitors. Chemistry & Biology. 6: 361-75. PMID 10375538 DOI: 10.1016/S1074-5521(99)80048-9  0.853
1999 Rosania GR, Merlie J, Gray N, Chang YT, Schultz PG, Heald R. A cyclin-dependent kinase inhibitor inducing cancer cell differentiation: biochemical identification using Xenopus egg extracts. Proceedings of the National Academy of Sciences of the United States of America. 96: 4797-802. PMID 10220373 DOI: 10.1073/Pnas.96.9.4797  0.756
1999 Gohil K, Packer L, Gray N, Rosania GR, Moy RK, Maguire J, Schultz PG. mRNA expression profile of a human cancer cell line in response to a phytochemical extract with antioxidant properties Nature Genetics. 23: 47-47. DOI: 10.1038/14313  0.466
1998 Gray NS, Wodicka L, Thunnissen AM, Norman TC, Kwon S, Espinoza FH, Morgan DO, Barnes G, LeClerc S, Meijer L, Kim SH, Lockhart DJ, Schultz PG. Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors. Science (New York, N.Y.). 281: 533-8. PMID 9677190 DOI: 10.1126/Science.281.5376.533  0.796
1997 Brooks EE, Gray NS, Joly A, Kerwar SS, Lum R, Mackman RL, Norman TC, Rosete J, Rowe M, Schow SR, Schultz PG, Wang X, Wick MM, Shiffman D. CVT-313, a specific and potent inhibitor of CDK2 that prevents neointimal proliferation. The Journal of Biological Chemistry. 272: 29207-11. PMID 9360999 DOI: 10.1074/Jbc.272.46.29207  0.764
1996 Patten PA, Gray NS, Yang PL, Marks CB, Wedemayer GJ, Boniface JJ, Stevens RC, Schultz PG. The immunological evolution of catalysis. Science (New York, N.Y.). 271: 1086-91. PMID 8599084 DOI: 10.1126/Science.271.5252.1086  0.772
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