James Bradner, MD - Publications

Affiliations: 
Dana-Farber Cancer Institute, Harvard Medical School, Boston, MA, United States 

247 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
2024 Souroullas GP, Jeck WR, Parker JS, Simon JM, Liu JY, Paulk J, Xiong J, Clark KS, Fedoriw Y, Qi J, Burd CE, Bradner JE, Sharpless NE. Author Correction: An oncogenic Ezh2 mutation induces tumors through global redistribution of histone 3 lysine 27 trimethylation. Nature Medicine. PMID 38383796 DOI: 10.1038/s41591-024-02867-1  0.727
2023 Hudson L, Mason JW, Westphal MV, Richter MJR, Thielman JR, Hua BK, Gerry CJ, Xia G, Osswald HL, Knapp JM, Tan ZY, Kokkonda P, Tresco BIC, Liu S, Reidenbach AG, ... ... Bradner JE, et al. Author Correction: Diversity-oriented synthesis encoded by deoxyoligonucleotides. Nature Communications. 14: 7589. PMID 37989745 DOI: 10.1038/s41467-023-43518-2  0.728
2023 Hudson L, Mason JW, Westphal MV, Richter MJR, Thielman JR, Hua BK, Gerry CJ, Xia G, Osswald HL, Knapp JM, Tan ZY, Kokkonda P, Tresco BIC, Liu S, Reidenbach AG, ... ... Bradner JE, et al. Diversity-oriented synthesis encoded by deoxyoligonucleotides. Nature Communications. 14: 4930. PMID 37582753 DOI: 10.1038/s41467-023-40575-5  0.767
2023 de Matos Simoes R, Shirasaki R, Downey-Kopyscinski SL, Matthews GM, Barwick BG, Gupta VA, Dupéré-Richer D, Yamano S, Hu Y, Sheffer M, Dhimolea E, Dashevsky O, Gandolfi S, Ishiguro K, Meyers RM, ... ... Bradner JE, et al. Genome-scale functional genomics identify genes preferentially essential for multiple myeloma cells compared to other neoplasias. Nature Cancer. 4: 754-773. PMID 37237081 DOI: 10.1038/s43018-023-00550-x  0.698
2023 Chory EJ, Wang M, Ceribelli M, Michalowska AM, Golas S, Beck E, Klumpp-Thomas C, Chen L, McKnight C, Itkin Z, Wilson KM, Holland D, Divakaran S, Bradner J, Khan J, et al. High-throughput Approaches to Uncover Synergistic Drug Combinations in Leukemia. Slas Discovery : Advancing Life Sciences R & D. PMID 37121274 DOI: 10.1016/j.slasd.2023.04.004  0.748
2022 Hess L, Moos V, Lauber AA, Reiter W, Schuster M, Hartl N, Lackner D, Boenke T, Koren A, Guzzardo PM, Gundacker B, Riegler A, Vician P, Miccolo C, Leiter S, ... ... Bradner J, et al. A toolbox for class I HDACs reveals isoform specific roles in gene regulation and protein acetylation. Plos Genetics. 18: e1010376. PMID 35994477 DOI: 10.1371/journal.pgen.1010376  0.363
2022 Zaiken MC, Flynn R, Paz KG, Rhee SY, Jin S, Mohamed FA, Saha A, Thangavelu G, Park PMC, Hemming ML, Sage PT, Sharpe AH, DuPage M, Bluestone JA, Panoskaltsis-Mortari A, ... ... Bradner JE, et al. BET-bromodomain and EZH2 inhibitor treated chronic GVHD mice have blunted germinal centers with distinct transcriptomes. Blood. PMID 35226736 DOI: 10.1182/blood.2021014557  0.48
2022 Liao Y, Chen CH, Xiao T, de la Peña Avalos B, Dray EV, Cai C, Gao S, Shah N, Zhang Z, Feit A, Xue P, Liu Z, Yang M, Lee JH, Xu H, ... ... Bradner JE, et al. Inhibition of EZH2 transactivation function sensitizes solid tumors to genotoxic stress. Proceedings of the National Academy of Sciences of the United States of America. 119. PMID 35031563 DOI: 10.1073/pnas.2105898119  0.363
2021 Gill T, Wang H, Bandaru R, Lawlor M, Lu C, Nieman LT, Tao J, Zhang Y, Anderson DG, Ting DT, Chen X, Bradner JE, Ott CJ. Selective targeting of MYC mRNA by stabilized antisense oligonucleotides. Oncogene. PMID 34650218 DOI: 10.1038/s41388-021-02053-4  0.681
2021 Hideshima T, Mazitschek R, Qi J, Mimura N, Tseng JC, Kung AL, Bradner JE, Anderson KC. Correction: HDAC6 inhibitor WT161 downregulates growth factor receptors in breast cancer. Oncotarget. 12: 1736. PMID 34434504 DOI: 10.18632/oncotarget.28051  0.405
2021 Kong W, Dimitri A, Wang W, Jung IY, Ott CJ, Fasolino M, Wang Y, Kulikovskaya I, Gupta M, Yoder T, DeNizio JE, Everett JK, Williams EF, Xu J, Scholler J, ... ... Bradner JE, et al. BET bromodomain protein inhibition reverses chimeric antigen receptor extinction and reinvigorates exhausted T cells in chronic lymphocytic leukemia. The Journal of Clinical Investigation. 131. PMID 34396987 DOI: 10.1172/JCI145459  0.636
2021 Yi JS, Sias-Garcia O, Nasholm N, Hu X, Iniguez AB, Hall MD, Davis M, Guha R, Moreno-Smith M, Barbieri E, Duong K, Koach J, Qi J, Bradner JE, Stegmaier K, et al. The synergy of BET inhibitors with aurora A kinase inhibitors in MYCN-amplified neuroblastoma is heightened with functional TP53. Neoplasia (New York, N.Y.). 23: 624-633. PMID 34107377 DOI: 10.1016/j.neo.2021.05.003  0.51
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, ... ... Bradner J, 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 Dowling CM, Hollinshead KER, Di Grande A, Pritchard J, Zhang H, Dillon ET, Haley K, Papadopoulos E, Mehta AK, Bleach R, Lindner AU, Mooney B, Düssmann H, O'Connor D, Prehn JHM, ... ... Bradner JE, et al. Multiple screening approaches reveal HDAC6 as a novel regulator of glycolytic metabolism in triple-negative breast cancer. Science Advances. 7. PMID 33523897 DOI: 10.1126/sciadv.abc4897  0.32
2021 Shirasaki R, Matthews GM, Gandolfi S, de Matos Simoes R, Buckley DL, Raja Vora J, Sievers QL, Brüggenthies JB, Dashevsky O, Poarch H, Tang H, Bariteau MA, Sheffer M, Hu Y, Downey-Kopyscinski SL, ... ... Bradner JE, et al. Functional Genomics Identify Distinct and Overlapping Genes Mediating Resistance to Different Classes of Heterobifunctional Degraders of Oncoproteins. Cell Reports. 34: 108532. PMID 33406420 DOI: 10.1016/j.celrep.2020.108532  0.714
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, ... ... Bradner JE, 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  0.528
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  0.488
2020 Antolic A, Wakimoto H, Jiao Z, Gorham JM, DePalma SR, Lemieux ME, Conner DA, Lee DY, Qi J, Seidman JG, Bradner JE, Brown JD, Haldar SM, Seidman CE, Burke MA. BET bromodomain proteins regulate transcriptional reprogramming in genetic dilated cardiomyopathy. Jci Insight. PMID 32603312 DOI: 10.1172/Jci.Insight.138687  0.438
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  0.44
2020 Shu S, Wu HJ, Ge JY, Zeid R, Harris IS, Jovanović B, Murphy K, Wang B, Qiu X, Endress JE, Reyes J, Lim K, Font-Tello A, Syamala S, Xiao T, ... ... Bradner J, et al. Synthetic Lethal and Resistance Interactions with BET Bromodomain Inhibitors in Triple-Negative Breast Cancer. Molecular Cell. PMID 32416067 DOI: 10.1016/J.Molcel.2020.04.027  0.543
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  0.475
2019 Tatetsu H, Gao C, Armant M, Wang F, Ueno S, Tian X, Federation A, Qi J, Bradner J, Tenen DG, Chai L. Maintenance and enhancement of human PBSC engraftment after ex vivo culture via an HDACi/SALL4 axis (3465). Experimental Hematology. PMID 31260717 DOI: 10.1016/J.Exphem.2019.06.473  0.507
2019 Bandopadhayay P, Piccioni F, O'Rourke R, Ho P, Gonzalez EM, Buchan G, Qian K, Gionet G, Girard E, Coxon M, Rees MG, Brenan L, Dubois F, Shapira O, Greenwald NF, ... ... Bradner JE, et al. Neuronal differentiation and cell-cycle programs mediate response to BET-bromodomain inhibition in MYC-driven medulloblastoma. Nature Communications. 10: 2400. PMID 31160565 DOI: 10.1038/S41467-019-10307-9  0.486
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, ... ... Bradner JE, et al. Small-molecule targeting of brachyury transcription factor addiction in chordoma. Nature Medicine. PMID 30664779 DOI: 10.1038/S41591-018-0312-3  0.823
2018 Fulciniti M, Lin CY, Samur MK, Lopez MA, Singh I, Lawlor MA, Szalat RE, Ott CJ, Avet-Loiseau H, Anderson KC, Young RA, Bradner JE, Munshi NC. Non-overlapping Control of Transcriptome by Promoter- and Super-Enhancer-Associated Dependencies in Multiple Myeloma. Cell Reports. 25: 3693-3705.e6. PMID 30590042 DOI: 10.1016/j.celrep.2018.12.016  0.658
2018 Ott CJ, Federation AJ, Schwartz LS, Kasar S, Klitgaard JL, Lenci R, Li Q, Lawlor M, Fernandes SM, Souza A, Polaski D, Gadi D, Freedman ML, Brown JR, Bradner JE. Enhancer Architecture and Essential Core Regulatory Circuitry of Chronic Lymphocytic Leukemia. Cancer Cell. PMID 30503705 DOI: 10.1016/J.Ccell.2018.11.001  0.666
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  0.633
2018 Michel BC, D'Avino AR, Cassel SH, Mashtalir N, McKenzie ZM, McBride MJ, Valencia AM, Zhou Q, Bocker M, Soares LMM, Pan J, Remillard DI, Lareau CA, Zullow HJ, Fortoul N, ... ... Bradner JE, et al. A non-canonical SWI/SNF complex is a synthetic lethal target in cancers driven by BAF complex perturbation. Nature Cell Biology. PMID 30397315 DOI: 10.1038/S41556-018-0221-1  0.435
2018 Paz K, Flynn R, Du J, Qi J, Luznik L, Maillard I, MacDonald KP, Hill GR, Serody JS, Murphy WJ, Sage PT, Sharpe AH, Miklos D, Culter CS, Koreth J, ... ... Bradner JE, et al. Small-molecule BCL6 inhibitor effectively treats mice with non-sclerodermatous chronic graft-versus-host disease. Blood. PMID 30279226 DOI: 10.1182/Blood-2018-03-839993  0.49
2018 Liu S, Yosief HO, Dai L, Huang H, Dhawan G, Zhang X, Muthengi AM, Roberts J, Buckley DL, Perry JA, Wu L, Bradner JE, Qi J, Zhang W. Structure-guided Design and Development of Potent and Selective Dual Bromodomain 4 (BRD4)/Polo-like Kinase 1 (PLK1) Inhibitors. Journal of Medicinal Chemistry. PMID 30125504 DOI: 10.1021/Acs.Jmedchem.8B00765  0.433
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, ... ... Bradner JE, 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  0.583
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  0.444
2018 Xu L, Chen Y, Mayakonda A, Koh L, Chong YK, Buckley DL, Sandanaraj E, Lim SW, Lin RY, Ke XY, Huang ML, Chen J, Sun W, Wang LZ, Goh BC, ... ... Bradner JE, et al. Targetable BET proteins- and E2F1-dependent transcriptional program maintains the malignancy of glioblastoma. Proceedings of the National Academy of Sciences of the United States of America. PMID 29764999 DOI: 10.1073/Pnas.1712363115  0.34
2018 Liu Y, Li Y, Liu S, Adeegbe DO, Christensen CL, Quinn MM, Dries R, Han S, Buczkowski K, Wang X, Chen T, Gao P, Zhang H, Li F, Hammerman PS, ... Bradner JE, et al. NK cells mediate synergistic antitumor effects of combined inhibition of HDAC6 and BET in a SCLC preclinical model. Cancer Research. PMID 29760044 DOI: 10.1158/0008-5472.Can-18-0161  0.321
2018 Kleppe M, Koche R, Zou L, van Galen P, Hill CE, Dong L, De Groote S, Papalexi E, Hanasoge Somasundara AV, Cordner K, Keller M, Farnoud N, Medina J, McGovern E, Reyes J, ... ... Bradner JE, et al. Dual Targeting of Oncogenic Activation and Inflammatory Signaling Increases Therapeutic Efficacy in Myeloproliferative Neoplasms. Cancer Cell. 33: 785-787. PMID 29634952 DOI: 10.1016/j.ccell.2018.03.024  0.599
2018 Nabet B, Roberts JM, Buckley DL, Paulk J, Dastjerdi S, Yang A, Leggett AL, Erb MA, Lawlor MA, Souza A, Scott TG, Vittori S, Perry JA, Qi J, Winter GE, ... ... Bradner JE, et al. The dTAG system for immediate and target-specific protein degradation. Nature Chemical Biology. PMID 29581585 DOI: 10.1038/S41589-018-0021-8  0.813
2018 Bolin S, Borgenvik A, Persson CU, Sundström A, Qi J, Bradner JE, Weiss WA, Cho YJ, Weishaupt H, Swartling FJ. Combined BET bromodomain and CDK2 inhibition in MYC-driven medulloblastoma. Oncogene. PMID 29511348 DOI: 10.1038/S41388-018-0135-1  0.519
2018 Gechijian LN, Buckley DL, Lawlor MA, Reyes JM, Paulk J, Ott CJ, Winter GE, Erb MA, Scott TG, Xu M, Seo HS, Dhe-Paganon S, Kwiatkowski NP, Perry JA, Qi J, ... ... Bradner JE, et al. Functional TRIM24 degrader via conjugation of ineffectual bromodomain and VHL ligands. Nature Chemical Biology. PMID 29507391 DOI: 10.1038/S41589-018-0010-Y  0.813
2018 Zeid R, Lawlor MA, Poon E, Reyes JM, Fulciniti M, Lopez MA, Scott TG, Nabet B, Erb MA, Winter GE, Jacobson Z, Polaski DR, Karlin KL, Hirsch RA, Munshi NP, ... ... Bradner JE, et al. Enhancer invasion shapes MYCN-dependent transcriptional amplification in neuroblastoma. Nature Genetics. PMID 29379199 DOI: 10.1038/S41588-018-0044-9  0.581
2018 Ishoey M, Chorn S, Singh N, Jaeger MG, Brand M, Paulk J, Bauer S, Erb MA, Parapatics K, Müller AC, Bennett KL, Ecker GF, Bradner JE, Winter GE. The translation termination factor GSPT1 is a phenotypically relevant off-target of heterobifunctional phthalimide degraders. Acs Chemical Biology. PMID 29356495 DOI: 10.1021/Acschembio.7B00969  0.799
2018 Kalin JH, Wu M, Gomez AV, Song Y, Das J, Hayward D, Adejola N, Wu M, Panova I, Chung HJ, Kim E, Roberts HJ, Roberts JM, Prusevich P, Jeliazkov JR, ... ... Bradner JE, et al. Targeting the CoREST complex with dual histone deacetylase and demethylase inhibitors. Nature Communications. 9: 53. PMID 29302039 DOI: 10.1038/S41467-017-02242-4  0.328
2017 Zhao L, Dunne CE, Clausen DJ, Roberts JM, Paulk J, Liu H, Wiest OG, Bradner JE, Williams RM. Synthesis and Biochemical Evaluation of Biotinylated Conjugates of Largazole Analogues: Selective Class I Histone Deacetylase Inhibitors. Israel Journal of Chemistry. 57: 319-330. PMID 30760938 DOI: 10.1002/Ijch.201600130  0.739
2017 Mack SC, Pajtler KW, Chavez L, Okonechnikov K, Bertrand KC, Wang X, Erkek S, Federation A, Song A, Lee C, Wang X, McDonald L, Morrow JJ, Saiakhova A, Sin-Chan P, ... ... Bradner JE, et al. Therapeutic targeting of ependymoma as informed by oncogenic enhancer profiling. Nature. PMID 29258295 DOI: 10.1038/Nature25169  0.317
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, et al. Pharmacological perturbation of CDK9 using selective CDK9 inhibition or degradation. Nature Chemical Biology. PMID 29251720 DOI: 10.1038/Nchembio.2538  0.683
2017 Kleppe M, Koche R, Zou L, van Galen P, Hill CE, Dong L, De Groote S, Papalexi E, Hanasoge Somasundara AV, Cordner K, Keller M, Farnoud N, Medina J, McGovern E, Reyes J, ... ... Bradner JE, et al. Dual Targeting of Oncogenic Activation and Inflammatory Signaling Increases Therapeutic Efficacy in Myeloproliferative Neoplasms. Cancer Cell. PMID 29249691 DOI: 10.1016/J.Ccell.2017.11.009  0.637
2017 Su R, Dong L, Li C, Nachtergaele S, Wunderlich M, Qing Y, Deng X, Wang Y, Weng X, Hu C, Yu M, Skibbe J, Dai Q, Zou D, Wu T, ... ... Bradner JE, et al. R-2HG Exhibits Anti-tumor Activity by Targeting FTO/m6A/MYC/CEBPA Signaling. Cell. PMID 29249359 DOI: 10.1016/J.Cell.2017.11.031  0.423
2017 Weintraub AS, Li CH, Zamudio AV, Sigova AA, Hannett NM, Day DS, Abraham BJ, Cohen MA, Nabet B, Buckley DL, Guo YE, Hnisz D, Jaenisch R, Bradner JE, Gray NS, et al. YY1 Is a Structural Regulator of Enhancer-Promoter Loops. Cell. 171: 1573-1588.e28. PMID 29224777 DOI: 10.1016/J.Cell.2017.11.008  0.418
2017 Chen L, Alexe G, Dharia NV, Ross L, Iniguez AB, Conway AS, Wang EJ, Veschi V, Lam N, Qi J, Gustafson WC, Nasholm N, Vazquez F, Weir BA, Cowley GS, ... ... Bradner JE, et al. CRISPR-Cas9 screen reveals a MYCN-amplified neuroblastoma dependency on EZH2. The Journal of Clinical Investigation. PMID 29202477 DOI: 10.1172/Jci90793  0.545
2017 Erwin GS, Grieshop MP, Ali A, Qi J, Lawlor M, Kumar D, Ahmad I, McNally A, Teider N, Worringer K, Sivasankaran R, Syed DN, Eguchi A, Ashraf M, Jeffery J, ... ... Bradner JE, et al. Synthetic transcription elongation factors license transcription across repressive chromatin. Science (New York, N.Y.). PMID 29192133 DOI: 10.1126/Science.Aan6414  0.503
2017 Roti G, Qi J, Kitara S, Sanchez-Martin M, Saur Conway A, Varca AC, Su A, Wu L, Kung AL, Ferrando AA, Bradner JE, Stegmaier K. Leukemia-specific delivery of mutant NOTCH1 targeted therapy. The Journal of Experimental Medicine. PMID 29158376 DOI: 10.1182/Blood.V128.22.889.889  0.495
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, ... ... Bradner JE, 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  0.766
2017 Hideshima T, Mazitschek R, Qi J, Mimura N, Tseng JC, Kung AL, Bradner JE, Anderson KC. HDAC6 inhibitor WT161 downregulates growth factor receptors in breast cancer. Oncotarget. 8: 80109-80123. PMID 29113288 DOI: 10.18632/Oncotarget.19019  0.491
2017 Bhattacharyya S, Pradhan K, Campbell N, Mazdo J, Vasantkumar A, Maqbool S, Bhagat TD, Gupta S, Suzuki M, Yu Y, Greally JM, Steidl U, Bradner J, Dawlaty M, Godley L, et al. Altered hydroxymethylation is seen at regulatory regions in pancreatic cancer and regulates oncogenic pathways. Genome Research. PMID 28986391 DOI: 10.1101/Gr.222794.117  0.385
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, et al. MELK is not necessary for the proliferation of basal-like breast cancer cells. Elife. 6. PMID 28926338 DOI: 10.7554/Elife.26693  0.785
2017 Dai X, Gan W, Li X, Wang S, Zhang W, Huang L, Liu S, Zhong Q, Guo J, Zhang J, Chen T, Shimizu K, Beca F, Blattner M, Vasudevan D, ... ... Bradner JE, et al. Prostate cancer-associated SPOP mutations confer resistance to BET inhibitors through stabilization of BRD4. Nature Medicine. PMID 28805820 DOI: 10.1038/Nm.4378  0.486
2017 Breindel JL, Skibinski A, Sedic M, Wronski-Campos A, Zhou W, Keller PJ, Mills J, Bradner J, Onder T, Kuperwasser C. Epigenetic Reprogramming of Lineage-Committed Human Mammary Epithelial Cells Requires DNMT3A and Loss of DOT1L. Stem Cell Reports. PMID 28781076 DOI: 10.1016/J.Stemcr.2017.06.019  0.345
2017 Chakraborty AA, Nakamura E, Qi J, Creech A, Jaffe JD, Paulk J, Novak JS, Nagulapalli K, McBrayer SK, Cowley GS, Pineda J, Song J, Wang YE, Carr SA, Root DE, ... ... Bradner JE, et al. HIF activation causes synthetic lethality between the VHL tumor suppressor and the EZH1 histone methyltransferase. Science Translational Medicine. 9. PMID 28701475 DOI: 10.1126/Scitranslmed.Aal5272  0.784
2017 Ayoub AM, Hawk LML, Herzig RJ, Jiang J, Wisniewski AJ, Gee CT, Zhao P, Zhu JY, Berndt N, Offei-Addo NK, Scott TG, Qi J, Bradner JE, Ward TR, Schönbrunn E, et al. Correction to BET Bromodomain Inhibitors with One-Step Synthesis Discovered from Virtual Screen. Journal of Medicinal Chemistry. PMID 28696689 DOI: 10.1021/Acs.Jmedchem.7B00943  0.452
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, ... ... Bradner JE, 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  0.82
2017 Ayoub AM, Hawk LML, Herzig RJ, Jiang J, Wisniewski AJ, Gee CT, Zhao P, Zhu JY, Berndt N, Offei-Addo NK, Scott TG, Qi J, Bradner JE, Ward TR, Schönbrunn E, et al. BET Bromodomain Inhibitors With One-step Synthesis Discovered from Virtual Screen. Journal of Medicinal Chemistry. PMID 28535045 DOI: 10.1021/Acs.Jmedchem.6B01336  0.532
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, ... ... Bradner J, 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  0.691
2017 Remillard D, Buckley DL, Paulk J, Brien GL, Sonnett M, Seo HS, Dastierdi S, Wühr M, Dhe-Paganon S, Armstrong SA, Bradner JE. Degradation of the BAF Complex Factor BRD9 by Heterobifunctional Ligands. Angewandte Chemie (International Ed. in English). PMID 28418626 DOI: 10.1002/Anie.201611281  0.745
2017 Adeegbe D, Liu Y, Lizotte PH, Kamihara Y, Aref AR, Almonte C, Dries R, Li Y, Liu S, Wang X, Warner-Hatten T, Castrillon J, Yuan GC, Poudel-Neupane N, Zhang H, ... ... Bradner JE, et al. Synergistic Immunostimulatory Effects and Therapeutic Benefit of Combined Histone Deacetylase and Bromodomain Inhibition in Non-small Cell Lung Cancer. Cancer Discovery. PMID 28408401 DOI: 10.1158/2159-8290.Cd-16-1020  0.401
2017 Shortt J, Ott CJ, Johnstone RW, Bradner JE. A chemical probe toolbox for dissecting the cancer epigenome. Nature Reviews. Cancer. 17: 268. PMID 28332503 DOI: 10.1038/nrc.2017.26  0.595
2017 Bian B, Bigonnet M, Gayet O, Loncle C, Maignan A, Gilabert M, Moutardier V, Garcia S, Turrini O, Delpero JR, Giovannini M, Grandval P, Gasmi M, Ouaissi M, Secq V, ... ... Bradner JE, et al. Gene expression profiling of patient-derived pancreatic cancer xenografts predicts sensitivity to the BET bromodomain inhibitor JQ1: implications for individualized medicine efforts. Embo Molecular Medicine. PMID 28275007 DOI: 10.15252/Emmm.201606975  0.495
2017 Hogg SJ, Vervoort SJ, Deswal S, Ott CJ, Li J, Cluse LA, Beavis PA, Darcy PK, Martin BP, Spencer A, Traunbauer AK, Sadovnik I, Bauer K, Valent P, Bradner JE, et al. BET-Bromodomain Inhibitors Engage the Host Immune System and Regulate Expression of the Immune Checkpoint Ligand PD-L1. Cell Reports. 18: 2162-2174. PMID 28249162 DOI: 10.1016/j.celrep.2017.02.011  0.61
2017 Wan L, Wen H, Li Y, Lyu J, Xi Y, Hoshii T, Joseph JK, Wang X, Loh YE, Erb MA, Souza AL, Bradner JE, Shen L, Li W, Li H, et al. ENL links histone acetylation to oncogenic gene expression in acute myeloid leukaemia. Nature. PMID 28241141 DOI: 10.1038/Nature21687  0.623
2017 Erb MA, Scott TG, Li BE, Xie H, Paulk J, Seo HS, Souza A, Roberts JM, Dastjerdi S, Buckley DL, Sanjana NE, Shalem O, Nabet B, Zeid R, Offei-Addo NK, ... ... Bradner JE, et al. Transcription control by the ENL YEATS domain in acute leukaemia. Nature. PMID 28241139 DOI: 10.1038/Nature21688  0.807
2017 Shortt J, Ott CJ, Johnstone RW, Bradner JE. A chemical probe toolbox for dissecting the cancer epigenome. Nature Reviews. Cancer. 17: 160-183. PMID 28228643 DOI: 10.1038/nrc.2016.148  0.651
2017 Gechijian LN, Buckley D, Lawlor M, Scott T, Paulk J, Reyes J, Winter G, Erb M, Ott C, Dhe-Paganon S, Bradner J. Abstract 981: The design and characterization of a selective TRIM24 degrader Cancer Research. 77: 981-981. DOI: 10.1158/1538-7445.Am2017-981  0.783
2017 Dowling CM, Hemann M, Bradner J, Letai A, Chonghaile TN. Abstract 2326: A high-throughput screen identified cancer selective small molecules that kill independent of mitochondrial apoptosis Cancer Research. 77: 2326-2326. DOI: 10.1158/1538-7445.Am2017-2326  0.414
2017 Bolin S, Borgenvik A, Persson C, Sundström A, Qi J, Bradner J, Weiss W, Cho Y, Weishaupt H, Swartling F. PDTM-34. COMBINED BET BROMODOMAIN AND CDK2 INHIBITION IN MYC-DRIVEN MEDULLOBLASTOMA Neuro-Oncology. 19: vi197-vi197. DOI: 10.1093/Neuonc/Nox168.797  0.528
2016 Cappel D, Hall ML, Lenselink EB, Beuming T, Qi J, Bradner J, Sherman W. Relative Binding Free Energy Calculations Applied to Protein Homology Models. Journal of Chemical Information and Modeling. 56: 2388-2400. PMID 28024402 DOI: 10.1021/Acs.Jcim.6B00362  0.473
2016 Koblan LW, Buckley DL, Ott CJ, Fitzgerald ME, Ember SW, Zhu JY, Liu S, Roberts JM, Remillard D, Vittori S, Zhang W, Schonbrunn E, Bradner JE. Assessment of Bromodomain Target Engagement by a Series of BI2536 Analogues with Miniaturized BET-BRET. Chemmedchem. PMID 27862999 DOI: 10.1002/Cmdc.201600502  0.675
2016 Yokoyama Y, Zhu H, Lee JH, Kossenkov AV, Wu SY, Wickramasinghe JM, Yin X, Palozola KC, Gardini A, Showe LC, Zaret KS, Liu Q, Speicher D, Conejo-Garcia JR, Bradner JE, et al. BET Inhibitors Suppress ALDH Activity by Targeting ALDH1A1 Super-Enhancer in Ovarian Cancer. Cancer Research. 76: 6320-6330. PMID 27803105 DOI: 10.1158/0008-5472.Can-16-0854  0.347
2016 Hideshima T, Qi J, Paranal RM, Tang W, Greenberg E, West N, Colling ME, Estiu G, Mazitschek R, Perry JA, Ohguchi H, Cottini F, Mimura N, Görgün G, Tai YT, ... ... Bradner JE, et al. Discovery of selective small-molecule HDAC6 inhibitor for overcoming proteasome inhibitor resistance in multiple myeloma. Proceedings of the National Academy of Sciences of the United States of America. PMID 27799547 DOI: 10.1073/Pnas.1608067113  0.72
2016 Tanaka M, Roberts JM, Seo HS, Souza A, Paulk J, Scott TG, DeAngelo SL, Dhe-Paganon S, Bradner JE. Design and characterization of bivalent BET inhibitors. Nature Chemical Biology. PMID 27775715 DOI: 10.1038/Nchembio.2209  0.757
2016 Ingham OJ, Paranal RM, Smith WB, Escobar RA, Yueh H, Snyder T, Porco JA, Bradner JE, Beeler AB. Development of a Potent and Selective HDAC8 Inhibitor. Acs Medicinal Chemistry Letters. 7: 929-932. PMID 27774131 DOI: 10.1021/acsmedchemlett.6b00239  0.56
2016 Sahni JM, Gayle SS, Weber-Bonk KL, Cuellar Vite L, Yori JL, Webb B, Ramos EK, Seachrist DD, Landis MD, Chang JC, Bradner JE, Keri RA. Bromodomain and extraterminal protein inhibition blocks growth of triple-negative breast cancers through the suppression of Aurora kinases. The Journal of Biological Chemistry. PMID 27650498 DOI: 10.1074/Jbc.M116.738666  0.323
2016 Xie H, Peng C, Huang J, Li BE, Kim W, Smith EC, Fujiwara Y, Qi J, Cheloni G, Das PP, Nguyen M, Li S, Bradner JE, Orkin SH. Chronic myelogenous leukemia initiating cells require Polycomb group protein EZH2. Cancer Discovery. PMID 27630126 DOI: 10.1158/2159-8290.Cd-15-1439  0.468
2016 Koo SJ, Fernández-Montalván AE, Badock V, Ott CJ, Holton SJ, von Ahsen O, Toedling J, Vittori S, Bradner JE, Gorjánácz M. ATAD2 is an epigenetic reader of newly synthesized histone marks during DNA replication. Oncotarget. PMID 27612420 DOI: 10.18632/oncotarget.11855  0.636
2016 Kühn MW, Song E, Feng Z, Sinha A, Chen CW, Deshpande AJ, Cusan M, Farnoud N, Mupo A, Grove C, Koche R, Bradner JE, de Stanchina E, Vassiliou GS, Hoshii T, et al. Targeting Chromatin Regulators Inhibits Leukemogenic Gene Expression in NPM1 Mutant Leukemia. Cancer Discovery. PMID 27535106 DOI: 10.1158/2159-8290.Cd-16-0237  0.328
2016 Xiang M, Kim H, Ho VT, Walker SR, Bar-Natan M, Anahtar M, Liu S, Toniolo PA, Kroll Y, Jones N, Giaccone ZT, Heppler LN, Ye DQ, Marineau JJ, Shaw D, ... Bradner JE, et al. Gene expression-based discovery of atovaquone as a STAT3 inhibitor and anti-cancer agent. Blood. PMID 27531676 DOI: 10.1182/blood-2015-07-660506  0.341
2016 Zhao Y, Liu Q, Acharya P, Stengel KR, Sheng Q, Zhou X, Kwak H, Fischer MA, Bradner JE, Strickland SA, Mohan SR, Savona MR, Venters BJ, Zhou MM, Lis JT, et al. High-Resolution Mapping of RNA Polymerases Identifies Mechanisms of Sensitivity and Resistance to BET Inhibitors in t(8;21) AML. Cell Reports. PMID 27498870 DOI: 10.1016/J.Celrep.2016.07.032  0.316
2016 Mishra A, La Perle K, Kwiatkowski S, Sullivan LA, Sams GH, Johns J, Curphey DP, Wen J, McConnell K, Qi J, Wong H, Russo G, Zhang J, Marcucci G, Bradner JE, et al. Mechanism, consequences and therapeutic targeting of abnormal IL-15 signaling in cutaneous T-cell lymphoma. Cancer Discovery. PMID 27422033 DOI: 10.1158/2159-8290.Cd-15-1297  0.394
2016 Zhang H, Qi J, Reyes JM, Li L, Rao PK, Li F, Lin CY, Perry JA, Lawlor MA, Federation A, De Raedt T, Li YY, Liu Y, Duarte MA, Zhang Y, ... ... Bradner JE, et al. Oncogenic deregulation of EZH2 as an opportunity for targeted therapy in lung cancer. Cancer Discovery. PMID 27312177 DOI: 10.1158/2159-8290.Cd-16-0164  0.754
2016 Spangle JM, Dreijerink KM, Groner AC, Cheng H, Ohlson CE, Reyes J, Lin CY, Bradner J, Zhao JJ, Roberts TM, Brown M. PI3K/AKT Signaling Regulates H3K4 Methylation in Breast Cancer. Cell Reports. PMID 27292631 DOI: 10.1016/J.Celrep.2016.05.046  0.411
2016 Jiang X, Bugno J, Hu C, Yang Y, Herold T, Qi J, Chen P, Gurbuxani S, Arnovitz S, Strong J, Ferchen K, Ulrich B, Weng H, Wang Y, Huang H, ... ... Bradner JE, et al. Eradication of acute myeloid leukemia with FLT3 ligand-targeted miR-150 nanoparticles. Cancer Research. PMID 27280396 DOI: 10.1158/0008-5472.Can-15-2949  0.411
2016 Paoluzzi L, Hanniford D, Sokolova E, Osman I, Darvishian F, Wang J, Bradner JE, Hernando E. BET and BRAF inhibitors act synergistically against BRAF-mutant melanoma. Cancer Medicine. PMID 27169980 DOI: 10.1002/Cam4.667  0.305
2016 Souroullas GP, Jeck WR, Parker JS, Simon JM, Liu JY, Paulk J, Xiong J, Clark KS, Fedoriw Y, Qi J, Burd CE, Bradner JE, Sharpless NE. An oncogenic Ezh2 mutation induces tumors through global redistribution of histone 3 lysine 27 trimethylation. Nature Medicine. PMID 27135738 DOI: 10.1038/Nm.4092  0.76
2016 Jacques C, Lamoureux F, Baud'huin M, Rodriguez Calleja L, Quillard T, Amiaud J, Tirode F, Rédini F, Bradner JE, Heymann D, Ory B. Targeting the epigenetic readers in Ewing sarcoma inhibits the oncogenic transcription factor EWS/Fli1. Oncotarget. 7: 24125-40. PMID 27006472 DOI: 10.18632/oncotarget.8214  0.346
2016 Kryukov GV, Wilson FH, Ruth JR, Paulk J, Tsherniak A, Marlow SE, Vazquez F, Weir BA, Fitzgerald ME, Tanaka M, Bielski CM, Scott JM, Dennis C, Cowley GS, Boehm JS, ... ... Bradner JE, et al. MTAP deletion confers enhanced dependency on the PRMT5 arginine methyltransferase in cancer cells. Science (New York, N.Y.). PMID 26912360 DOI: 10.1126/Science.Aad5214  0.752
2016 Bandopadhayay P, Ramkissoon LA, Jain P, Bergthold G, Wala J, Zeid R, Schumacher SE, Urbanski L, O'Rourke R, Gibson WJ, Pelton K, Ramkissoon SH, Han HJ, Zhu Y, Choudhari N, ... ... Bradner JE, et al. MYB-QKI rearrangements in angiocentric glioma drive tumorigenicity through a tripartite mechanism. Nature Genetics. PMID 26829751 DOI: 10.1038/Ng.3500  0.473
2016 Drier Y, Cotton MJ, Williamson KE, Gillespie SM, Ryan RJ, Kluk MJ, Carey CD, Rodig SJ, Sholl LM, Afrogheh AH, Faquin WC, Queimado L, Qi J, Wick MJ, El-Naggar AK, ... Bradner JE, et al. An oncogenic MYB feedback loop drives alternate cell fates in adenoid cystic carcinoma. Nature Genetics. PMID 26829750 DOI: 10.1038/Ng.3502  0.643
2016 Shu S, Lin CY, He HH, Witwicki RM, Tabassum DP, Roberts JM, Janiszewska M, Jin Huh S, Liang Y, Ryan J, Doherty E, Mohammed H, Guo H, Stover DG, Ekram MB, ... ... Bradner JE, et al. Response and resistance to BET bromodomain inhibitors in triple-negative breast cancer. Nature. PMID 26735014 DOI: 10.1038/Nature16508  0.731
2016 Shahbazi J, Liu PY, Atmadibrata B, Bradner JE, Marshall GM, Lock RB, Liu T. The bromodomain inhibitor JQ1 and the histone deacetylase inhibitor panobinostat synergistically reduce N-Myc expression and induce anticancer effects. Clinical Cancer Research : An Official Journal of the American Association For Cancer Research. PMID 26733615 DOI: 10.1158/1078-0432.Ccr-15-1666  0.335
2016 Zurnic I, Hütter S, Lehmann U, Stanke N, Reh J, Kern T, Lindel F, Gerresheim G, Hamann M, Müllers E, Lesbats P, Cherepanov P, Serrao E, Engelman A, Lindemann D, ... ... Bradner J, et al. Proceedings of the Frontiers of Retrovirology Conference 2016 Retrovirology. 13. DOI: 10.1186/S12977-016-0294-5  0.437
2016 Chen CD, Delaney C, Xu H, Koche R, Lujambio Goizueta A, Hoshii T, Cusan M, Chabon J, Valerio DG, Kuehn M, Wang X, Cai S, Chu SH, Chen YK, He J, ... ... Bradner JE, et al. An Epigenetic Regulator Screen Identifies Novel Targets That Sensitize MLL-Rearranged Leukemia to DOT1L Inhibition Blood. 128: 571-571. DOI: 10.1182/Blood.V128.22.571.571  0.548
2016 Matthews GM, Gandolfi S, Bruggentheis J, De Matos Simoes R, Buckley DL, Hu Y, Sheffer M, Poarch H, Bradner JE, Mitsiades CS. BET Bromodomain Degradation As a Therapeutic Strategy in Multiple Myeloma Blood. 128: 1062-1062. DOI: 10.1182/Blood.V128.22.1062.1062  0.319
2016 Shu S, Lin C, He HH, Witwicki R, Roberts J, Tabassum D, Liang Y, Ekram M, Doherty E, Brown J, Mohammed H, D'Santos C, McKeown M, Ott C, Qi J, ... ... Bradner J, et al. Abstract B16: Response and resistance to BET bromodomain inhibitors in triple-negative breast cancer Molecular Cancer Research. 14. DOI: 10.1158/1557-3125.Advbc15-B16  0.758
2016 Stahlhut CE, Ambrico AJ, Watrud KE, Cho H, Wang L, Qi J, Cantley LC, Bradner J, Trotman L. Abstract 4165: Myc vs. Akt therapy in RapidCap, a GEM model for metastatic prostate cancer Cancer Research. 76: 4165-4165. DOI: 10.1158/1538-7445.Am2016-4165  0.494
2016 Winter G, Buckley D, Mayer A, Roderick J, Kelliher M, Churchman S, Bradner J. Global disruption of productive transcriptional elongation via targeted BET protein degradation European Journal of Cancer. 69: S90. DOI: 10.1016/S0959-8049(16)32866-0  0.378
2016 Koblan LW, Buckley DL, Ott CJ, Fitzgerald ME, Ember SWJ, Zhu J, Liu S, Roberts JM, Remillard D, Vittori S, Zhang W, Schonbrunn E, Bradner JE. Back Cover: Assessment of Bromodomain Target Engagement by a Series of BI2536 Analogues with Miniaturized BET-BRET (ChemMedChem 23/2016) Chemmedchem. 11: 2638-2638. DOI: 10.1002/Cmdc.201600587  0.62
2015 Roberts JM, Bradner JE. A Bead-Based Proximity Assay for BRD4 Ligand Discovery. Current Protocols in Chemical Biology. 7: 263-78. PMID 26629616 DOI: 10.1002/9780470559277.ch150024  0.306
2015 Seashore-Ludlow B, Rees MG, Cheah JH, Cokol M, Price EV, Coletti ME, Jones V, Bodycombe NE, Soule CK, Gould J, Alexander B, Li A, Montgomery P, Wawer MJ, Kuru N, ... ... Bradner JE, et al. Harnessing Connectivity in a Large-Scale Small-Molecule Sensitivity Dataset. Cancer Discovery. 5: 1210-23. PMID 26482930 DOI: 10.1158/2159-8290.Cd-15-0235  0.76
2015 Viny AD, Ott CJ, Spitzer B, Rivas M, Meydan C, Papalexi E, Yelin D, Shank K, Reyes J, Chiu A, Romin Y, Boyko V, Thota S, Maciejewski JP, Melnick A, ... Bradner JE, et al. Dose-dependent role of the cohesin complex in normal and malignant hematopoiesis. The Journal of Experimental Medicine. 212: 1819-32. PMID 26438361 DOI: 10.1182/Blood.V126.23.435.435  0.638
2015 Mazur PK, Herner A, Mello SS, Wirth M, Hausmann S, Sánchez-Rivera FJ, Lofgren SM, Kuschma T, Hahn SA, Vangala D, Trajkovic-Arsic M, Gupta A, Heid I, Noël PB, Braren R, ... ... Bradner JE, et al. Combined inhibition of BET family proteins and histone deacetylases as a potential epigenetics-based therapy for pancreatic ductal adenocarcinoma. Nature Medicine. PMID 26390243 DOI: 10.1038/Nm.3952  0.37
2015 Sun B, Shah B, Fiskus W, Qi J, Rajapakshe K, Coarfa C, Li L, Devaraj SG, Sharma S, Zhang L, Wang ML, Saenz DT, Krieger S, Bradner JE, Bhalla KN. Synergistic activity of BET protein antagonist-based combinations in mantle cell lymphoma cells sensitive or resistant to ibrutinib. Blood. PMID 26254443 DOI: 10.1182/Blood-2015-04-639542  0.505
2015 Tanaka M, Roberts JM, Qi J, Bradner JE. Inhibitors of emerging epigenetic targets for cancer therapy: a patent review (2010-2014). Pharmaceutical Patent Analyst. 4: 261-84. PMID 26174566 DOI: 10.4155/Ppa.15.16  0.537
2015 Devaraj SG, Fiskus W, Shah B, Qi J, Sun B, Iyer SP, Sharma S, Bradner JE, Bhalla KN. HEXIM1 induction is mechanistically involved in mediating anti-AML activity of BET protein bromodomain antagonist. Leukemia. PMID 26148704 DOI: 10.1038/Leu.2015.142  0.435
2015 Hu YJ, Belaghzal H, Hsiao WY, Qi J, Bradner JE, Guertin DA, Sif S, Imbalzano AN. Transcriptional and post-transcriptional control of adipocyte differentiation by Jumonji domain-containing protein 6. Nucleic Acids Research. PMID 26117538 DOI: 10.1093/Nar/Gkv645  0.455
2015 Wedeh G, Cerny-Reiterer S, Eisenwort G, Herrmann H, Blatt K, Hadzijusufovic E, Sadovnik I, Müllauer L, Schwaab J, Hoffmann T, Bradner JE, Radia D, Sperr WR, Hoermann G, Reiter A, et al. Identification of bromodomain-containing protein-4 as a novel marker and epigenetic target in mast cell leukemia. Leukemia. PMID 26055303 DOI: 10.1038/leu.2015.138  0.334
2015 Winter GE, Buckley DL, Paulk J, Roberts JM, Souza A, Dhe-Paganon S, Bradner JE. DRUG DEVELOPMENT. Phthalimide conjugation as a strategy for in vivo target protein degradation. Science (New York, N.Y.). 348: 1376-81. PMID 25999370 DOI: 10.1126/Science.Aab1433  0.763
2015 Garcia PL, Miller AL, Kreitzburg KM, Council LN, Gamblin TL, Christein JD, Heslin MJ, Arnoletti JP, Richardson JH, Chen D, Hanna CA, Cramer SL, Yang ES, Qi J, Bradner JE, et al. The BET bromodomain inhibitor JQ1 suppresses growth of pancreatic ductal adenocarcinoma in patient-derived xenograft models. Oncogene. PMID 25961927 DOI: 10.1038/Onc.2015.126  0.459
2015 Zhou X, Fan LX, Peters DJ, Trudel M, Bradner JE, Li X. Therapeutic targeting of BET bromodomain protein, Brd4, delays cyst growth in ADPKD. Human Molecular Genetics. 24: 3982-93. PMID 25877301 DOI: 10.1093/hmg/ddv136  0.318
2015 Chen CW, Koche RP, Sinha AU, Deshpande AJ, Zhu N, Eng R, Doench JG, Xu H, Chu SH, Qi J, Wang X, Delaney C, Bernt KM, Root DE, Hahn WC, ... Bradner JE, et al. DOT1L inhibits SIRT1-mediated epigenetic silencing to maintain leukemic gene expression in MLL-rearranged leukemia. Nature Medicine. 21: 335-43. PMID 25822366 DOI: 10.1038/Nm.3832  0.531
2015 Schölz C, Weinert BT, Wagner SA, Beli P, Miyake Y, Qi J, Jensen LJ, Streicher W, McCarthy AR, Westwood NJ, Lain S, Cox J, Matthias P, Mann M, Bradner JE, et al. Acetylation site specificities of lysine deacetylase inhibitors in human cells. Nature Biotechnology. 33: 415-23. PMID 25751058 DOI: 10.1038/Nbt.3130  0.522
2015 Stubbs MC, Kim W, Bariteau M, Davis T, Vempati S, Minehart J, Witkin M, Qi J, Krivtsov AV, Bradner JE, Kung AL, Armstrong SA. Selective Inhibition of HDAC1 and HDAC2 as a Potential Therapeutic Option for B-ALL. Clinical Cancer Research : An Official Journal of the American Association For Cancer Research. 21: 2348-58. PMID 25688158 DOI: 10.1158/1078-0432.CCR-14-1290  0.571
2015 Baratta MG, Schinzel AC, Zwang Y, Bandopadhayay P, Bowman-Colin C, Kutt J, Curtis J, Piao H, Wong LC, Kung AL, Beroukhim R, Bradner JE, Drapkin R, Hahn WC, Liu JF, et al. An in-tumor genetic screen reveals that the BET bromodomain protein, BRD4, is a potential therapeutic target in ovarian carcinoma. Proceedings of the National Academy of Sciences of the United States of America. 112: 232-7. PMID 25535366 DOI: 10.1073/Pnas.1422165112  0.32
2015 Yi JS, Federation AJ, Qi J, Dhe-Paganon S, Hadler M, Xu X, St Pierre R, Varca AC, Wu L, Marineau JJ, Smith WB, Souza A, Chory EJ, Armstrong SA, Bradner JE. Structure-guided DOT1L probe optimization by label-free ligand displacement. Acs Chemical Biology. 10: 667-74. PMID 25397901 DOI: 10.1021/Cb500796D  0.789
2015 Lee DH, Qi J, Bradner JE, Said JW, Doan NB, Forscher C, Yang H, Koeffler HP. Synergistic effect of JQ1 and rapamycin for treatment of human osteosarcoma. International Journal of Cancer. Journal International Du Cancer. 136: 2055-64. PMID 25307878 DOI: 10.1002/Ijc.29269  0.546
2015 Wang H, Cheng F, Cheng J, Villagra A, Tao J, Bradner JE, Sotomayor EM. JQ1, a Selective Bromodomain Inhibitor, Augment the Immunogenicity of Mantle Cell Lymphoma By Influencing the Expression of PD-L1 Blood. 126: 822-822. DOI: 10.1182/Blood.V126.23.822.822  0.308
2015 Mishra A, Hartlage A, Sullivan L, Grinshpun L, Kwiatkowski S, Qi J, Bradner JE, Porcu P, Caligiuri MA. Genome-Wide Mapping Reveals BRD4 in Regulation of Tumor-Driver Genes in Cutaneous T-Cell Lymphoma Blood. 126: 589-589. DOI: 10.1182/Blood.V126.23.589.589  0.474
2015 Ott CJ, Federation AJ, Kasar S, Klitgaard JL, Fernandes SM, Brown JR, Bradner JE. Enhancer Landscapes Reveal Transcription Factor Network Dependencies in Chronic Lymphocytic Leukemia Blood. 126: 436-436. DOI: 10.1182/Blood.V126.23.436.436  0.666
2015 Jiang X, Bugno J, Hu C, Yang Y, Herold T, Qi J, Chen P, Gurbuxani S, Arnovitz S, Ulrich B, Weng H, Wang Y, Huang H, Li S, Strong J, ... ... Bradner JE, et al. Targeted Treatment of FLT3 -Overexpressing Acute Myeloid Leukemia with MiR-150 Nanoparticles Guided By Conjugated FLT3 Ligand Peptides Blood. 126: 3784-3784. DOI: 10.1182/Blood.V126.23.3784.3784  0.397
2015 Will CM, Scholle M, St. Pierre R, Schiltz G, Bradner JE, Mrksich M, Licht JD. High Throughput Screening Identifies Potential Inhibitors of WHSC1/MMSET, a Histone Methyltransferase Oncoprotein in Multiple Myeloma and Acute Lymphocytic Leukemia Blood. 126: 3251-3251. DOI: 10.1182/Blood.V126.23.3251.3251  0.353
2015 Zhang X, Francis J, Lin C, Rahl P, Bradner J, Young R. Abstract A38: The role of MGA loss-of-function mutations in lung adenocarcinomas Molecular Cancer Research. 13. DOI: 10.1158/1557-3125.Myc15-A38  0.31
2015 Bradner J. Abstract IA11: Targeting enhancers in CNS tumors Brain. 75. DOI: 10.1158/1538-7445.Brain15-Ia11  0.431
2015 Stahlhut CE, Watrud KE, Ambrico AJ, Cho H, Wang L, Qi J, Cantley LC, Bradner J, Trotman LC. Abstract 2636: Myc vs. Akt therapy in RapidCap, a GEM model for metastatic prostate cancer Cancer Research. 75: 2636-2636. DOI: 10.1158/1538-7445.Am2015-2636  0.492
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, ... ... Bradner JE, 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  0.537
2014 Chan CT, Qi J, Smith W, Paranol R, Mazitschek R, West N, Reeves R, Chiosis G, Schreiber SL, Bradner JE, Paulmurugan R, Gambhir SS. Syntheses and discovery of a novel class of cinnamic hydroxamates as histone deacetylase inhibitors by multimodality molecular imaging in living subjects. Cancer Research. 74: 7475-86. PMID 25320008 DOI: 10.1158/0008-5472.Can-14-0197  0.596
2014 McKeown MR, Shaw DL, Fu H, Liu S, Xu X, Marineau JJ, Huang Y, Zhang X, Buckley DL, Kadam A, Zhang Z, Blacklow SC, Qi J, Zhang W, Bradner JE. Biased multicomponent reactions to develop novel bromodomain inhibitors. Journal of Medicinal Chemistry. 57: 9019-27. PMID 25314271 DOI: 10.1021/Jm501120Z  0.522
2014 De Raedt T, Beert E, Pasmant E, Luscan A, Brems H, Ortonne N, Helin K, Hornick JL, Mautner V, Kehrer-Sawatzki H, Clapp W, Bradner J, Vidaud M, Upadhyaya M, Legius E, et al. PRC2 loss amplifies Ras-driven transcription and confers sensitivity to BRD4-based therapies. Nature. 514: 247-51. PMID 25119042 DOI: 10.1038/Nature13561  0.349
2014 Fiskus W, Sharma S, Qi J, Shah B, Devaraj SG, Leveque C, Portier BP, Iyer S, Bradner JE, Bhalla KN. BET protein antagonist JQ1 is synergistically lethal with FLT3 tyrosine kinase inhibitor (TKI) and overcomes resistance to FLT3-TKI in AML cells expressing FLT-ITD. Molecular Cancer Therapeutics. 13: 2315-27. PMID 25053825 DOI: 10.1158/1535-7163.Mct-14-0258  0.476
2014 Tang Y, Gholamin S, Schubert S, Willardson MI, Lee A, Bandopadhayay P, Bergthold G, Masoud S, Nguyen B, Vue N, Balansay B, Yu F, Oh S, Woo P, Chen S, ... ... Bradner JE, et al. Epigenetic targeting of Hedgehog pathway transcriptional output through BET bromodomain inhibition. Nature Medicine. 20: 732-40. PMID 24973920 DOI: 10.1038/Nm.3613  0.549
2014 Feng Q, Zhang Z, Shea MJ, Creighton CJ, Coarfa C, Hilsenbeck SG, Lanz R, He B, Wang L, Fu X, Nardone A, Song Y, Bradner J, Mitsiades N, Mitsiades CS, et al. An epigenomic approach to therapy for tamoxifen-resistant breast cancer. Cell Research. 24: 809-19. PMID 24874954 DOI: 10.1038/Cr.2014.71  0.351
2014 Knoechel B, Roderick JE, Williamson KE, Zhu J, Lohr JG, Cotton MJ, Gillespie SM, Fernandez D, Ku M, Wang H, Piccioni F, Silver SJ, Jain M, Pearson D, Kluk MJ, ... ... Bradner JE, et al. An epigenetic mechanism of resistance to targeted therapy in T cell acute lymphoblastic leukemia. Nature Genetics. 46: 364-70. PMID 24584072 DOI: 10.1038/Ng.2913  0.748
2014 Reynolds C, Roderick JE, LaBelle JL, Bird G, Mathieu R, Bodaar K, Colon D, Pyati U, Stevenson KE, Qi J, Harris M, Silverman LB, Sallan SE, Bradner JE, Neuberg DS, et al. Repression of BIM mediates survival signaling by MYC and AKT in high-risk T-cell acute lymphoblastic leukemia. Leukemia. 28: 1819-27. PMID 24552990 DOI: 10.1038/Leu.2014.78  0.418
2014 Bhagwat N, Koppikar P, Keller M, Marubayashi S, Shank K, Rampal R, Qi J, Kleppe M, Patel HJ, Shah SK, Taldone T, Bradner JE, Chiosis G, Levine RL. Improved targeting of JAK2 leads to increased therapeutic efficacy in myeloproliferative neoplasms. Blood. 123: 2075-83. PMID 24470592 DOI: 10.1182/Blood-2014-01-547760  0.502
2014 Fowler T, Ghatak P, Price DH, Conaway R, Conaway J, Chiang CM, Bradner JE, Shilatifard A, Roy AL. Regulation of MYC expression and differential JQ1 sensitivity in cancer cells. Plos One. 9: e87003. PMID 24466310 DOI: 10.1371/Journal.Pone.0087003  0.318
2014 Cho H, Herzka T, Zheng W, Qi J, Wilkinson JE, Bradner JE, Robinson BD, Castillo-Martin M, Cordon-Cardo C, Trotman LC. RapidCaP, a novel GEM model for metastatic prostate cancer analysis and therapy, reveals myc as a driver of Pten-mutant metastasis. Cancer Discovery. 4: 318-333. PMID 24444712 DOI: 10.1158/2159-8290.Cd-13-0346  0.404
2014 Liu S, Walker SR, Nelson EA, Cerulli R, Xiang M, Toniolo PA, Qi J, Stone RM, Wadleigh M, Bradner JE, Frank DA. Targeting STAT5 in hematologic malignancies through inhibition of the bromodomain and extra-terminal (BET) bromodomain protein BRD2. Molecular Cancer Therapeutics. 13: 1194-205. PMID 24435449 DOI: 10.1158/1535-7163.Mct-13-0341  0.549
2014 Fiskus W, Sharma S, Qi J, Valenta JA, Schaub LJ, Shah B, Peth K, Portier BP, Rodriguez M, Devaraj SG, Zhan M, Sheng J, Iyer SP, Bradner JE, Bhalla KN. Highly active combination of BRD4 antagonist and histone deacetylase inhibitor against human acute myelogenous leukemia cells. Molecular Cancer Therapeutics. 13: 1142-54. PMID 24435446 DOI: 10.1158/1535-7163.Mct-13-0770  0.512
2014 Gutierrez A, Pan L, Groen RWJ, Baleydier F, Kentsis A, Marineau J, Grebliunaite R, Kozakewich E, Reed C, Pflumio F, Poglio S, Uzan B, Clemons P, VerPlank L, An F, ... ... Bradner JE, et al. Phenothiazines induce PP2A-mediated apoptosis in T cell acute lymphoblastic leukemia Journal of Clinical Investigation. 124: 644-655. PMID 24401270 DOI: 10.1172/Jci65093  0.595
2014 Roderick JE, Tesell J, Shultz LD, Brehm MA, Greiner DL, Harris MH, Silverman LB, Sallan SE, Gutierrez A, Look AT, Qi J, Bradner JE, Kelliher MA. c-Myc inhibition prevents leukemia initiation in mice and impairs the growth of relapsed and induction failure pediatric T-ALL cells Blood. 123: 1040-1050. PMID 24394663 DOI: 10.1182/Blood-2013-08-522698  0.444
2014 Anders L, Guenther MG, Qi J, Fan ZP, Marineau JJ, Rahl PB, Lovén J, Sigova AA, Smith WB, Lee TI, Bradner JE, Young RA. Genome-wide localization of small molecules. Nature Biotechnology. 32: 92-6. PMID 24336317 DOI: 10.1038/Nbt.2776  0.454
2014 Bandopadhayay P, Bergthold G, Nguyen B, Schubert S, Gholamin S, Tang Y, Bolin S, Schumacher SE, Zeid R, Masoud S, Yu F, Vue N, Gibson WJ, Paolella BR, Mitra SS, ... ... Bradner JE, et al. BET bromodomain inhibition of MYC-amplified medulloblastoma. Clinical Cancer Research : An Official Journal of the American Association For Cancer Research. 20: 912-25. PMID 24297863 DOI: 10.1158/1078-0432.Ccr-13-2281  0.663
2014 Lu G, Middleton RE, Sun H, Naniong M, Ott CJ, Mitsiades CS, Wong KK, Bradner JE, Kaelin WG. The myeloma drug lenalidomide promotes the cereblon-dependent destruction of Ikaros proteins. Science (New York, N.Y.). 343: 305-9. PMID 24292623 DOI: 10.1126/Science.1244917  0.664
2014 Wienerroither S, Rauch I, Rosebrock F, Jamieson AM, Bradner J, Muhar M, Zuber J, Müller M, Decker T. Regulation of NO synthesis, local inflammation, and innate: Immunity to pathogens by BET family proteins Molecular and Cellular Biology. 34: 415-427. PMID 24248598 DOI: 10.1128/Mcb.01353-13  0.348
2014 Zou Z, Huang B, Wu X, Zhang H, Qi J, Bradner J, Nair S, Chen LF. Brd4 maintains constitutively active NF-κB in cancer cells by binding to acetylated RelA Oncogene. 33: 2395-2404. PMID 23686307 DOI: 10.1038/Onc.2013.179  0.541
2014 Paoluzzi L, Hanniford D, Sokolova E, Dolgalev I, Heguy A, Osman I, Darvishian F, Wang J, Bradner JE, Hernando E. Preclinical testing supports combined BET and BRAF inhibition as a promising therapeutic strategy for melanoma. Journal of Clinical Oncology. 32: 9072-9072. DOI: 10.1200/Jco.2014.32.15_Suppl.9072  0.309
2014 Sun B, Fiskus W, Shah B, Qi J, Devaraj SGT, Iyer SP, Sharma S, Bradner J, Zu Y, Bhalla KN. Superior Pre-Clinical Activity of BET (Bromodomain and Extra terminal) Protein Antagonist Combined with Ibrutinib, Panobinostat or Carfilzomib Against Human Mantle Cell Lymphoma (MCL) Cells Blood. 124: 918-918. DOI: 10.1182/Blood.V124.21.918.918  0.559
2014 Xie H, Peng C, Qi J, Cheloni G, Das P, Huang J, Nguyen M, Li S, Bradner JE, Orkin SH. Eradication of Chronic Myelogenous Leukemia By Inactivation of the Polycomb Group Protein EZH2 Blood. 124: 778-778. DOI: 10.1182/Blood.V124.21.778.778  0.491
2014 Flynn RP, Goodman K, Qi J, Jing D, Panoskaltsis-Mortari A, Yi Z, Dong C, Liu X, MacDonald KPA, Hill GR, Serody JS, Murphy WJ, Luznik L, Maillard I, Koreth J, ... ... Bradner JE, et al. Targeting BCL6 and Germinal Centers (GCs) in Chronic Graft-Versus-Host Disease (cGVHD) Using Direct and Epigenomic Therapies Blood. 124: 535-535. DOI: 10.1182/Blood.V124.21.535.535  0.518
2014 Yi JS, Federation A, Qi J, Dhe-Paganon S, Hadler M, Xu X, Varca A, St. Pierre R, Armstrong SA, Bradner JE. Structure-Guided Design of DOT1L Methyltransferase Inhibitors By a Novel, Label Free Assay Platform Blood. 124: 4811-4811. DOI: 10.1182/Blood.V124.21.4811.4811  0.558
2014 Ott CJ, Lu G, Reyes J, Lin CY, Kaelin WG, Bradner JE. Disruption of the Ikaros-Mediated Gene Expression Program in Multiple Myeloma with Immunomodulatory Agents Blood. 124: 420-420. DOI: 10.1182/Blood.V124.21.420.420  0.308
2014 Devaraj SGT, Fiskus W, Shah B, Sharma S, Qi J, Sun B, Saha S, Iyer SP, Zu Y, Bradner J, Bhalla KN. Mechanistic Role of HEXIM1 Induction in BRD4-Antagonist Mediated Growth Inhibition, Differentiation and in Vivo Lethal Activity Against Human AML Blast Progenitor Cells Blood. 124: 3534-3534. DOI: 10.1182/Blood.V124.21.3534.3534  0.598
2014 Roti G, Qi J, Su A, Varca A, Aster JC, Bradner JE, Stegmaier K. Selectively Targeting Mutated NOTCH1 with a Folate-Thapsigargin Derivative Blood. 124: 2158-2158. DOI: 10.1182/Blood.V124.21.2158.2158  0.501
2014 Tatetsu H, Wang F, Gao C, Ueno S, Tian X, Armant M, Federation A, Qi J, Bradner JE, Tenen DG, Chai L. SALL4 Is a Key Factor in HDAC Inhibitor Mediated Ex Vivo Expansion of Human Peripheral Blood Mobilized Stem/Progenitor CD34+CD90+ Cells Blood. 124: 1566-1566. DOI: 10.1182/Blood.V124.21.1566.1566  0.375
2014 Chen Z, Weisberg E, Cheng K, Kung AL, Bradner J, Griffin J, Wong K. Abstract B01: Improve MEK/ERK targeting in mutant KRAS lung cancer Molecular Cancer Research. 12. DOI: 10.1158/1557-3125.Rasonc14-B01  0.386
2014 Raedt TD, Beert E, Pasmant E, Luscan A, Brems H, Ortonne N, Helin K, Mautner V, Kehrer-Sawatski H, Clapp W, Bradner J, Upadhyaya M, Vidaud M, Legius E, Cichowski K. Abstract LB-79: PRC2 loss amplifies Ras-driven transcription and sensitizes cancers to bromodomain inhibitor-based combination therapies Cancer Research. 74. DOI: 10.1158/1538-7445.Am2014-Lb-79  0.34
2014 Knoechel B, Roderick J, Williamson K, Zhu J, Lohr J, Cotton M, Gillespie S, Fernandez D, Ku M, Wang H, Piccioni F, Silver S, Jain M, Pearson D, Kluk M, ... ... Bradner J, et al. Abstract 4782: Epigenetic resistance to Notch inhibition in T cell acute lymphoblastic leukemia Cancer Research. 74: 4782-4782. DOI: 10.1158/1538-7445.Am2014-4782  0.771
2014 Lee DHT, Qi J, Bradner J, Said J, Doan N, Forscher C, Koeffler HP. Abstract 1689: Synergistic effect of JQ1 and rapamycin for treatment of human osteosarcoma Cancer Research. 74: 1689-1689. DOI: 10.1158/1538-7445.Am2014-1689  0.569
2014 Cho Y, Tang Y, Schubert S, Willardson M, Bandopadhayay P, Bergthold G, Nguyen B, Masoud S, Vue N, Balansay B, Gholamin S, Cheshier SH, Atwood SX, Whitson RJ, Lee A, ... ... Bradner JE, et al. EPIGENETIC TARGETING OF HEDGEHOG PATHWAY TRANSCRIPTIONAL OUTPUT Neuro-Oncology. 16: iii25-iii25. DOI: 10.1093/Neuonc/Nou208.9  0.551
2014 Deshpande A, Deshpande A, Sinha A, Chen L, Chang J, Chen D, Koche R, Krivtsov A, Luo M, Bradner J, Bernt K, Armstrong S. Regulation of HOX gene expression by AF10-mediated conversion of H3K79me1 to H3K79me2 Experimental Hematology. 42: S30. DOI: 10.1016/J.Exphem.2014.07.107  0.302
2013 Chapuy B, McKeown MR, Lin CY, Monti S, Roemer MG, Qi J, Rahl PB, Sun HH, Yeda KT, Doench JG, Reichert E, Kung AL, Rodig SJ, Young RA, Shipp MA, ... Bradner JE, et al. Discovery and characterization of super-enhancer-associated dependencies in diffuse large B cell lymphoma. Cancer Cell. 24: 777-90. PMID 24332044 DOI: 10.1016/J.Ccr.2013.11.003  0.505
2013 Wu X, Qi J, Bradner JE, Xiao G, Chen LF. Bromodomain and extraterminal (BET) protein inhibition suppresses human T cell leukemia virus 1 (HTLV-1) Tax protein-mediated tumorigenesis by inhibiting nuclear factor κB (NF-κB) signaling. The Journal of Biological Chemistry. 288: 36094-105. PMID 24189064 DOI: 10.1074/Jbc.M113.485029  0.502
2013 Shimamura T, Chen Z, Soucheray M, Carretero J, Kikuchi E, Tchaicha JH, Gao Y, Cheng KA, Cohoon TJ, Qi J, Akbay E, Kimmelman AC, Kung AL, Bradner JE, Wong KK. Efficacy of BET bromodomain inhibition in Kras-mutant non-small cell lung cancer. Clinical Cancer Research : An Official Journal of the American Association For Cancer Research. 19: 6183-92. PMID 24045185 DOI: 10.1158/1078-0432.Ccr-12-3904  0.47
2013 Spiltoir JI, Stratton MS, Cavasin MA, Demos-Davies K, Reid BG, Qi J, Bradner JE, McKinsey TA. BET acetyl-lysine binding proteins control pathological cardiac hypertrophy Journal of Molecular and Cellular Cardiology. 63: 175-179. PMID 23939492 DOI: 10.1016/J.Yjmcc.2013.07.017  0.46
2013 Anand P, Brown JD, Lin CY, Qi J, Zhang R, Artero PC, Alaiti MA, Bullard J, Alazem K, Margulies KB, Cappola TP, Lemieux M, Plutzky J, Bradner JE, Haldar SM. BET bromodomains mediate transcriptional pause release in heart failure Cell. 154: 569-582. PMID 23911322 DOI: 10.1016/J.Cell.2013.07.013  0.457
2013 Frumm SM, Fan ZP, Ross KN, Duvall JR, Gupta S, VerPlank L, Suh BC, Holson E, Wagner FF, Smith WB, Paranal RM, Bassil CF, Qi J, Roti G, Kung AL, ... Bradner JE, et al. Selective HDAC1/HDAC2 inhibitors induce neuroblastoma differentiation. Chemistry & Biology. 20: 713-25. PMID 23706636 DOI: 10.1016/J.Chembiol.2013.03.020  0.542
2013 Lovén J, Hoke HA, Lin CY, Lau A, Orlando DA, Vakoc CR, Bradner JE, Lee TI, Young RA. Selective inhibition of tumor oncogenes by disruption of super-enhancers. Cell. 153: 320-34. PMID 23582323 DOI: 10.1016/J.Cell.2013.03.036  0.334
2013 Picaud S, Da Costa D, Thanasopoulou A, Filippakopoulos P, Fish PV, Philpott M, Fedorov O, Brennan P, Bunnage ME, Owen DR, Bradner JE, Taniere P, O'Sullivan B, Müller S, Schwaller J, et al. PFI-1, a highly selective protein interaction inhibitor, targeting BET Bromodomains. Cancer Research. 73: 3336-46. PMID 23576556 DOI: 10.1158/0008-5472.Can-12-3292  0.395
2013 Puissant A, Frumm SM, Alexe G, Bassil CF, Qi J, Chanthery YH, Nekritz EA, Zeid R, Gustafson WC, Greninger P, Garnett MJ, Mcdermott U, Benes CH, Kung AL, Weiss WA, ... Bradner JE, et al. Targeting MYCN in neuroblastoma by BET bromodomain inhibition Cancer Discovery. 3: 309-323. PMID 23430699 DOI: 10.1158/2159-8290.Cd-12-0418  0.553
2013 Gao C, Dimitrov T, Yong KJ, Tatetsu H, Jeong HW, Luo HR, Bradner JE, Tenen DG, Chai L. Targeting transcription factor SALL4 in acute myeloid leukemia by interrupting its interaction with an epigenetic complex Blood. 121: 1413-1421. PMID 23287862 DOI: 10.1182/blood-2012-04-424275  0.301
2013 Barroilhet L, Yang J, Hasselblatt K, Paranal RM, Ng SK, Rauh-Hain JA, Welch WR, Bradner JE, Berkowitz RS, Ng SW. C-terminal binding protein-2 regulates response of epithelial ovarian cancer cells to histone deacetylase inhibitors Oncogene. 32: 3896-3903. PMID 22945647 DOI: 10.1038/Onc.2012.380  0.459
2013 David Chen C, Sinha AU, Qi J, Deshpande AJ, Zhu N, Koche R, Eng R, Chang J, Hahn WC, Bradner JE, Armstrong SA. Genome-Wide RNAi Screen Identifies The Mechanistic Role For DOT1L In MLL-Rearranged Leukemia Blood. 122: 598-598. DOI: 10.1182/Blood.V122.21.598.598  0.55
2013 Fiskus W, Sharma S, Qi J, Valenta JA, Schaub LJ, Shah B, Peth K, Jakkula LU, Rodriguez M, Devaraj S, Padmanabhan Iyer S, Bradner JE, Bhalla KN. BRD4 Antagonist and Histone Deacetylase Inhibitor: A Novel Synergistic Combination Against Human Acute Myeloid Leukemia (AML) Cells Blood. 122: 485-485. DOI: 10.1182/Blood.V122.21.485.485  0.495
2013 Rodriguez M, Fiskus W, Sharma S, Qi J, Valenta JA, Schaub LJ, Shah B, Devaraj S, Iyer SP, Bradner JE, Bhalla KN. Combined Therapy With BRD4 Antagonist and FLT3 Inhibitor Exerts Synergistic Activity Against Cultured and Primary AML Blast Progenitors Expressing FLT-ITD Blood. 122: 3821-3821. DOI: 10.1182/Blood.V122.21.3821.3821  0.499
2013 Wedeh G, Hadzijusufovic E, Cerny-Reiterer S, Herrmann H, Blatt K, Eisenwort G, Hoermann G, Sperr WR, Müllauer L, Vakoc CR, Bradner JE, Horny H, Willmann M, Zuber J, Arock M, et al. Bromodomain-Containing Protein 4 (BRD4): A Novel Marker and Drug Target Expressed In Neoplastic Cells In Advanced Mast Cell Neoplasms Blood. 122: 3747-3747. DOI: 10.1182/Blood.V122.21.3747.3747  0.321
2013 Chapuy B, Michael M, Lin CY, Monti S, Roemer MG, Qi J, Rahl PB, Sun H, Yeda KT, Kung AL, Rodig SJ, Young RA, Shipp MA, Bradner JE. Disruption Of Super Enhancer-Driven Cancer Dependencies In Diffuse Large B-Cell Lymphoma Blood. 122: 3021-3021. DOI: 10.1182/Blood.V122.21.3021.3021  0.569
2013 Valenta JA, Fiskus W, Manshouri T, Sharma S, Qi J, Schaub LJ, Shah B, Rodriguez M, Devaraj S, Iyer SP, Verstovsek S, Bradner JE, Bhalla KN. Combined Therapy With BRD4 Antagonist and JAK Inhibitor Is Synergistically Lethal Against Human Myeloproliferative Neoplasm (MPN) Cells Blood. 122: 2842-2842. DOI: 10.1182/Blood.V122.21.2842.2842  0.526
2013 Mishra A, La Perle KM, Sullivan L, Sams GH, Curphey DP, McConnell K, Qi J, Wong HK, Kulp SK, Fernandez S, Bradner JE, Marcucci G, Chen C, Porcu P, Caligiuri MA. Increased Expression Of IL-15 Promotes Cutaneous T-Cell Lymphomagenesis Via The Upregulation Of Histone Deacetylases: Evidence For Successful Preclinical Targeting Blood. 122: 1826-1826. DOI: 10.1182/Blood.V122.21.1826.1826  0.378
2013 Kühn MW, Hadler M, Daigle SR, Chen C, Sinha AU, Krivtsov AV, Olhava EJ, Caligiuri MA, Bradner JE, Pollock RM, Armstrong SA. Myeloid Leukemia Cells With MLL partial Tandem Duplication Are Sensitive To Pharmacological Inhibition Of The H3K79 Methyltransferase DOT1L Blood. 122: 1256-1256. DOI: 10.1182/Blood.V122.21.1256.1256  0.36
2013 Yu W, Chory EJ, Wernimont AK, Tempel W, Scopton A, Federation A, Marineau JJ, Qi J, Barsyte-Lovejoy D, Yi J, Marcellus R, Iacob RE, Engen JR, Griffin C, Aman A, ... ... Bradner JE, et al. Corrigendum: Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors Nature Communications. 4. DOI: 10.1038/Ncomms2845  0.758
2013 Pineda J, Marineau J, Estiu G, Bradner J. Molecular Dynamics of DOT1L and Modeling of EZH2 Biophysical Journal. 104: 403a. DOI: 10.1016/J.Bpj.2012.11.2248  0.369
2012 Yu W, Chory EJ, Wernimont AK, Tempel W, Scopton A, Federation A, Marineau JJ, Qi J, Barsyte-Lovejoy D, Yi J, Marcellus R, Iacob RE, Engen JR, Griffin C, Aman A, ... ... Bradner JE, et al. Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors. Nature Communications. 3: 1288. PMID 23250418 DOI: 10.1038/Ncomms2304  0.812
2012 Lockwood WW, Zejnullahu K, Bradner JE, Varmus H. Sensitivity of human lung adenocarcinoma cell lines to targeted inhibition of BET epigenetic signaling proteins Proceedings of the National Academy of Sciences of the United States of America. 109: 19408-19413. PMID 23129625 DOI: 10.1073/Pnas.1216363109  0.419
2012 Ott CJ, Kopp N, Bird L, Paranal RM, Qi J, Bowman T, Rodig SJ, Kung AL, Bradner JE, Weinstock DM. BET bromodomain inhibition targets both c-Myc and IL7R in high-risk acute lymphoblastic leukemia. Blood. 120: 2843-52. PMID 22904298 DOI: 10.1182/Blood-2012-02-413021  0.714
2012 Matzuk MM, McKeown MR, Filippakopoulos P, Li Q, Ma L, Agno JE, Lemieux ME, Picaud S, Yu RN, Qi J, Knapp S, Bradner JE. Small-molecule inhibition of BRDT for male contraception. Cell. 150: 673-84. PMID 22901802 DOI: 10.1016/J.Cell.2012.06.045  0.495
2012 Deshpande AJ, Bradner J, Armstrong SA. Chromatin modifications as therapeutic targets in MLL-rearranged leukemia. Trends in Immunology. 33: 563-70. PMID 22867873 DOI: 10.1016/J.It.2012.06.002  0.478
2012 Wen Q, Goldenson B, Silver SJ, Schenone M, Dancik V, Huang Z, Wang LZ, Lewis TA, An WF, Li X, Bray MA, Thiollier C, Diebold L, Gilles L, Vokes MS, ... ... Bradner JE, et al. Identification of regulators of polyploidization presents therapeutic targets for treatment of AMKL. Cell. 150: 575-89. PMID 22863010 DOI: 10.1016/J.Cell.2012.06.032  0.69
2012 Banerjee C, Archin N, Michaels D, Belkina AC, Denis GV, Bradner J, Sebastiani P, Margolis DM, Montano M. BET bromodomain inhibition as a novel strategy for reactivation of HIV-1 Journal of Leukocyte Biology. 92: 1147-1154. PMID 22802445 DOI: 10.1189/Jlb.0312165  0.35
2012 Santo L, Hideshima T, Kung AL, Tseng JC, Tamang D, Yang M, Jarpe M, van Duzer JH, Mazitschek R, Ogier WC, Cirstea D, Rodig S, Eda H, Scullen T, Canavese M, ... Bradner J, et al. Preclinical activity, pharmacodynamic, and pharmacokinetic properties of a selective HDAC6 inhibitor, ACY-1215, in combination with bortezomib in multiple myeloma. Blood. 119: 2579-89. PMID 22262760 DOI: 10.1182/Blood-2011-10-387365  0.388
2012 Bradner JE. Targeting Bromodomains in Myeloma Blood. 120: SCI-6-SCI-6. DOI: 10.1182/blood.v120.21.sci-6.sci-6  0.41
2012 Liu S, Walker S, Nelson E, Cirulli R, Xiang M, Qi J, Bradner JE, Frank D. Targeting STAT5 in Leukemia Through Inhibition of Bromodomain Proteins Blood. 120: 399-399. DOI: 10.1182/Blood.V120.21.399.399  0.548
2012 Shearstone JR, van Duzer JH, Bradner JE, Mazitschek R, Jones SS, Jarpe M. Induction of Human Fetal Hemoglobin Expression by Selective Inhibitors of Histone Deacetylase 1 and 2 (HDAC1/2) Blood. 120: 3259-3259. DOI: 10.1182/blood.v120.21.3259.3259  0.337
2012 Kopp N, Ott CJ, Bird L, Paranal R, Qi J, Bowman T, Rodig SJ, Kung AL, Bradner JE, Weinstock D. BET Bromodomain Inhibition Targets Both c-Myc and IL7R in Acute Lymphoblastic Leukemia Blood. 120: 672-672. DOI: 10.1016/S0959-8049(12)72336-5  0.698
2011 Delmore JE, Issa GC, Lemieux ME, Rahl PB, Shi J, Jacobs HM, Kastritis E, Gilpatrick T, Paranal RM, Qi J, Chesi M, Schinzel AC, McKeown MR, Heffernan TP, Vakoc CR, ... ... Bradner JE, et al. BET bromodomain inhibition as a therapeutic strategy to target c-Myc. Cell. 146: 904-17. PMID 21889194 DOI: 10.1016/J.Cell.2011.08.017  0.554
2011 Zuber J, Shi J, Wang E, Rappaport AR, Herrmann H, Sison EA, Magoon D, Qi J, Blatt K, Wunderlich M, Taylor MJ, Johns C, Chicas A, Mulloy JC, Kogan SC, ... ... Bradner JE, et al. RNAi screen identifies Brd4 as a therapeutic target in acute myeloid leukaemia. Nature. 478: 524-8. PMID 21814200 DOI: 10.1038/Nature10334  0.569
2011 Aldana-Masangkay GI, Rodriguez-Gonzalez A, Lin T, Ikeda AK, Hsieh YT, Kim YM, Lomenick B, Okemoto K, Landaw EM, Wang D, Mazitschek R, Bradner JE, Sakamoto KM. Tubacin suppresses proliferation and induces apoptosis of acute lymphoblastic leukemia cells. Leukemia & Lymphoma. 52: 1544-55. PMID 21699378 DOI: 10.3109/10428194.2011.570821  0.308
2011 Kemp MM, Wang Q, Fuller JH, West N, Martinez NM, Morse EM, Weïwer M, Schreiber SL, Bradner JE, Koehler AN. A novel HDAC inhibitor with a hydroxy-pyrimidine scaffold. Bioorganic & Medicinal Chemistry Letters. 21: 4164-9. PMID 21696956 DOI: 10.1016/J.Bmcl.2011.05.098  0.777
2011 de Zoeten EF, Wang L, Butler K, Beier UH, Akimova T, Sai H, Bradner JE, Mazitschek R, Kozikowski AP, Matthias P, Hancock WW. Histone deacetylase 6 and heat shock protein 90 control the functions of Foxp3+ T-regulatory cells Molecular and Cellular Biology. 31: 2066-2078. PMID 21444725 DOI: 10.1128/Mcb.05155-11  0.327
2011 Tang W, Luo T, Greenberg EF, Bradner JE, Schreiber SL. Discovery of histone deacetylase 8 selective inhibitors. Bioorganic & Medicinal Chemistry Letters. 21: 2601-5. PMID 21334896 DOI: 10.1016/J.Bmcl.2011.01.134  0.739
2011 Esrick EB, Xu J, Lin K, McConkey ME, Frisbee A, Poveromo L, Orkin SH, Bradner JE, Ebert BL. Induction of Fetal Hemoglobin by Inactivation of HDAC1 or HDAC2 without Altering Cellular Proliferation Blood. 118: 354-354. DOI: 10.1182/Blood.V118.21.354.354  0.336
2011 Herrmann H, Blatt K, Shi J, Rappaport AR, Gleixner KV, Cerny-Reiterer S, Peter B, Wang E, Sperr WR, Bradner JE, Lowe SW, Vakoc CR, Zuber J, Valent P. Small-Molecule Inhibition of BRD4 Is a Novel Promising Approach to Therapeutically Target Leukemia Stem Cells in AML, Blood. 118: 3484-3484. DOI: 10.1182/Blood.V118.21.3484.3484  0.356
2011 Santo L, Hideshima T, Kung AL, Tseng J, Tamang D, Yang M, Jarpe M, van Duzer JH, Mazitschek R, Ogier WC, Cirstea DD, Rodig S, Eda H, Scullen TA, Canavese M, ... Bradner JE, et al. Pharmacodynamic and Pharmacokinetic Properties of a Novel and Selective HDAC6 Inhibitor, ACY-1215, in Combination with Bortezomib in Multiple Myeloma Blood. 118: 2912-2912. DOI: 10.1182/Blood.V118.21.2912.2912  0.306
2011 Santo L, Hideshima T, Kung AL, Tseng J, Tamang D, Yang M, Jarpe M, van Duzer JH, Mazitschek R, Cirstea D, Eda H, Scullen TA, Rodig S, Canavese M, Bradner J, et al. Selective HDAC6 Inhibition Via ACY-1215, Either Alone or in Combination with Bortezomib, Restores Osteoblast Function and Suppresses Osteoclast Differentiation in Multiple Myeloma Blood. 118: 2908-2908. DOI: 10.1182/Blood.V118.21.2908.2908  0.375
2011 Issa GC, Delmore JE, McKeown MR, Lemieux ME, Rahl PB, Jacobs HM, Kastritis E, Gilpatrick T, Paranal RM, Qi J, Shi J, Chesi M, Schinzel AC, Vakoc CR, Bergsagel P, ... ... Bradner JE, et al. Inhibition of c-Myc Expression and Function in Hematologic Malignancies Blood. 118: 1409-1409. DOI: 10.1182/Blood.V118.21.1409.1409  0.482
2011 Schwartz B, Hofer M, Lemieux M, Bauer D, Cameron M, West N, Agoston E, Ince T, Christie A, Aster J, Sallan S, Kung A, Bradner J, French CA. Abstract 2575: Differentiation of NUT midline carcinoma by epigenomic reprogramming Cancer Research. 71: 2575-2575. DOI: 10.1158/1538-7445.Am2011-2575  0.417
2010 Filippakopoulos P, Qi J, Picaud S, Shen Y, Smith WB, Fedorov O, Morse EM, Keates T, Hickman TT, Felletar I, Philpott M, Munro S, McKeown MR, Wang Y, Christie AL, ... ... Bradner JE, et al. Selective inhibition of BET bromodomains. Nature. 468: 1067-73. PMID 20871596 DOI: 10.1038/Nature09504  0.528
2010 Bradner JE, Mak R, Tanguturi SK, Mazitschek R, Haggarty SJ, Ross K, Chang CY, Bosco J, West N, Morse E, Lin K, Shen JP, Kwiatkowski NP, Gheldof N, Dekker J, et al. Chemical genetic strategy identifies histone deacetylase 1 (HDAC1) and HDAC2 as therapeutic targets in sickle cell disease. Proceedings of the National Academy of Sciences of the United States of America. 107: 12617-22. PMID 20616024 DOI: 10.1073/Pnas.1006774107  0.681
2010 Estiu G, West N, Mazitschek R, Greenberg E, Bradner JE, Wiest O. On the inhibition of histone deacetylase 8. Bioorganic & Medicinal Chemistry. 18: 4103-10. PMID 20472442 DOI: 10.1016/J.Bmc.2010.03.080  0.343
2010 Bradner JE, West N, Grachan ML, Greenberg EF, Haggarty SJ, Warnow T, Mazitschek R. Chemical phylogenetics of histone deacetylases. Nature Chemical Biology. 6: 238-243. PMID 20139990 DOI: 10.1038/Nchembio.313  0.604
2010 Santo L, Hideshima T, Kung AL, Jarpe M, Cirstea D, Patel K, Pozzi S, Tseng JC, Rodig SJ, Bradner J, Anderson KC, Jones S, Raje N. Selective Inhibition of HDAC6 with a New Prototype Inhibitor (ACY-1215) Overcomes Bortezomib Resistance In Multiple Myeloma (MM) Blood. 116: 2997-2997. DOI: 10.1182/Blood.V116.21.2997.2997  0.426
2010 Rao R, Fiskus W, Balusu R, Ma H, Bradner J, Tao J, Sotomayor EM, Bhalla KN. Treatment with Histone Deacetylase 6-Specific Inhibitor WT-161 Disrupts hsp90 Function, Abrogates Aggresome Formation and Sensitizes Human Mantle Cell Lymphoma Cells to Lethal ER Stress Induced by Proteasome Inhibitor Carfilzomib Blood. 116: 2856-2856. DOI: 10.1182/Blood.V116.21.2856.2856  0.412
2010 Pop M, Doug K, Bradner J, Koehler A, Garraway L. Abstract 3693: Small molecule microarray screens for inhibitors of oncogenic ETS factors Cancer Research. 70: 3693-3693. DOI: 10.1158/1538-7445.Am10-3693  0.714
2009 Mühlenberg T, Zhang Y, Wagner AJ, Grabellus F, Bradner J, Taeger G, Lang H, Taguchi T, Schuler M, Fletcher JA, Bauer S. Inhibitors of deacetylases suppress oncogenic KIT signaling, acetylate HSP90, and induce apoptosis in gastrointestinal stromal tumors Cancer Research. 69: 6941-6950. PMID 19706776 DOI: 10.1158/0008-5472.Can-08-4004  0.446
2009 Guan JS, Haggarty SJ, Giacometti E, Dannenberg JH, Joseph N, Gao J, Nieland TJ, Zhou Y, Wang X, Mazitschek R, Bradner JE, DePinho RA, Jaenisch R, Tsai LH. HDAC2 negatively regulates memory formation and synaptic plasticity. Nature. 459: 55-60. PMID 19424149 DOI: 10.1038/Nature07925  0.509
2009 Patel V, Mazitschek R, Coleman B, Nguyen C, Urgaonkar S, Cortese J, Barker RH, Greenberg E, Tang W, Bradner JE, Schreiber SL, Duraisingh MT, Wirth DF, Clardy J. Identification and characterization of small molecule inhibitors of a class I histone deacetylase from Plasmodium falciparum. Journal of Medicinal Chemistry. 52: 2185-7. PMID 19317450 DOI: 10.1021/Jm801654Y  0.656
2009 Bowers AA, West N, Newkirk TL, Troutman-Youngman AE, Schreiber SL, Wiest O, Bradner JE, Williams RM. Synthesis and histone deacetylase inhibitory activity of largazole analogs: alteration of the zinc-binding domain and macrocyclic scaffold. Organic Letters. 11: 1301-4. PMID 19239241 DOI: 10.1021/Ol900078K  0.414
2009 Bowers AA, Greshock TJ, West N, Estiu G, Schreiber SL, Wiest O, Williams RM, Bradner JE. Synthesis and conformation-activity relationships of the peptide isosteres of FK228 and largazole. Journal of the American Chemical Society. 131: 2900-5. PMID 19193120 DOI: 10.1021/Ja807772W  0.407
2009 Wen Q, Huang Z, Small S, Bubna N, An F, Bliss-Moreau M, Verplank L, Lewis T, Schenone M, Tolliday N, Moore C, Carpenter A, Mercher T, Levine RL, Izraeli S, ... ... Bradner JE, et al. Identification of Inducers of Megakaryocyte Polyploidization and Their Use as Targeted Differentiation Therapy for Acute Megakaryocytic Leukemia. Blood. 114: 792-792. DOI: 10.1182/Blood.V114.22.792.792  0.348
2009 Li Z, Hu M, Leung C, Steinberg JA, Shen J, Li M, Wang CS, Sanchez E, Bowers A, Greshock T, Miller K, Newkirk T, West N, Bradner JE, Williams RM, et al. Largazole, a Novel Cyclic Peptide Histone Deacetylase Inhibitor, Demonstrates Anti-MM Effects Alone and Increases the Anti-MM Effects of Bortezomib. Blood. 114: 4925-4925. DOI: 10.1182/Blood.V114.22.4925.4925  0.301
2009 West N, Yoda A, Chiaretti S, Mani K, Foà R, Bradner J, Weinstock DM. CRLF2/JAK Signaling Confers Susceptibility to JAK Inhibitors and Small Molecule Inhibitors of Protein Kinase C. Blood. 114: 3767-3767. DOI: 10.1182/Blood.V114.22.3767.3767  0.429
2009 Jia X, Roccaro A, Azab A, Ngo H, Sacco A, Melhem, Azab F, Runnels J, Burwick N, Quang P, Husu E, Leleu X, Anderson K, Bradner J, Ghobrial I. B525 Regulation of Histone Deacetylase in Waldenström Macroglobulinemia Clinical Lymphoma, Myeloma & Leukemia. 9. DOI: 10.1016/S1557-9190(11)70757-0  0.301
2008 Bazzaro M, Lin Z, Santillan A, Lee MK, Wang MC, Chan KC, Bristow RE, Mazitschek R, Bradner J, Roden RB. Ubiquitin proteasome system stress underlies synergistic killing of ovarian cancer cells by bortezomib and a novel HDAC6 inhibitor. Clinical Cancer Research : An Official Journal of the American Association For Cancer Research. 14: 7340-7. PMID 19010849 DOI: 10.1158/1078-0432.Ccr-08-0642  0.413
2008 Bowers A, West N, Taunton J, Schreiber SL, Bradner JE, Williams RM. Total synthesis and biological mode of action of largazole: a potent class I histone deacetylase inhibitor. Journal of the American Chemical Society. 130: 11219-22. PMID 18642817 DOI: 10.1021/Ja8033763  0.64
2008 Ponduru S, Moellering R, Greenberg E, Shen JPY, Stanton BZ, Bradner JE. Discovery and Characterization of Macrocyclic Thiopeptide Proteasome Inhibitors for Hematologic Malignancies Blood. 112: 3669-3669. DOI: 10.1182/Blood.V112.11.3669.3669  0.4
2008 Shen JPY, Divakaran S, Ponduru S, Vogl DT, Amaravadi RK, Bradner JE. The Rationale for Combined Proteasome and Autophagy Inhibition in Multiple Myeloma Established Using Novel Translational Platforms Blood. 112: 2755-2755. DOI: 10.1182/blood.v112.11.2755.2755  0.334
2008 Jia X, Roccaro AM, Azab AK, Ngo HT, Sacco A, Melhem MR, Azab F, Runnels J, Burwick N, Quang P, Husu EN, Leleu X, Anderson KC, Bradner J, Ghobrial IM. Regulation of Histone Deacetylase in Waldenström Macroglobulinemia Blood. 112: 2617-2617. DOI: 10.1182/Blood.V112.11.2617.2617  0.407
2007 Vegas AJ, Bradner JE, Tang W, McPherson OM, Greenberg EF, Koehler AN, Schreiber SL. Fluorous-based small-molecule microarrays for the discovery of histone deacetylase inhibitors. Angewandte Chemie (International Ed. in English). 46: 7960-4. PMID 17868168 DOI: 10.1002/Anie.200703198  0.813
2007 Duan Z, Bradner J, Greenberg E, Mazitschek R, Foster R, Mahoney J, Seiden MV. 8-benzyl-4-oxo-8-azabicyclo[3.2.1]oct-2-ene-6,7-dicarboxylic acid (SD-1008), a novel janus kinase 2 inhibitor, increases chemotherapy sensitivity in human ovarian cancer cells. Molecular Pharmacology. 72: 1137-45. PMID 17675586 DOI: 10.1124/Mol.107.038117  0.481
2007 Bradner J, Greenberg E, Ponduru S, Patel V, Schreiber S, Rich B, Mazitschek R. A Soft-Drug Histone Deacetylase Inhibitor for Cutaneous T-Cell Lymphoma. Blood. 110: 800-800. DOI: 10.1182/Blood.V110.11.800.800  0.554
2007 Moellering R, Cornejo M, Rocknik J, Hancock M, DelBianco C, Blacklow S, Gilliland G, Verdine G, Bradner J. Direct Inhibition of the Notch Transactivation Complex with Synthetic Constrained Peptides in T-Cell Acute Lymphoblastic Leukemia. Blood. 110: 2819-2819. DOI: 10.1182/Blood.V110.11.2819.2819  0.428
2007 Shen JP, Divakaran S, Kuai L, Wang X, Ong S, Amaravadi R, Wood J, Carr S, Schreiber S, Haggarty S, Bradner J. Autophagy as a Target Pathway in Multiple Myeloma: A Forward Chemical Genetic Approach. Blood. 110: 2510-2510. DOI: 10.1182/Blood.V110.11.2510.2510  0.775
2007 Rodriguez-Gonzalez A, Ch’ng J, Ikeda AK, Lin T, Bahrami B, Mazitschek R, Bradner JE, Fu C, Sakamoto KM. Targeting Histone Deacetylase 6 and the Aggresome Pathway in Acute Lymphoblastic Leukemia Cells. Blood. 110: 1602-1602. DOI: 10.1182/Blood.V110.11.1602.1602  0.31
2006 Bradner JE, McPherson OM, Koehler AN. A method for the covalent capture and screening of diverse small molecules in a microarray format. Nature Protocols. 1: 2344-52. PMID 17406478 DOI: 10.1038/Nprot.2006.282  0.654
2006 Duan Z, Bradner JE, Greenberg E, Levine R, Foster R, Mahoney J, Seiden MV. SD-1029 inhibits signal transducer and activator of transcription 3 nuclear translocation Clinical Cancer Research. 12: 6844-6852. PMID 17121906 DOI: 10.1158/1078-0432.Ccr-06-1330  0.328
2006 Bradner JE, McPherson OM, Mazitschek R, Barnes-Seeman D, Shen JP, Dhaliwal J, Stevenson KE, Duffner JL, Park SB, Neuberg DS, Nghiem P, Schreiber SL, Koehler AN. A robust small-molecule microarray platform for screening cell lysates. Chemistry & Biology. 13: 493-504. PMID 16720270 DOI: 10.1016/J.Chembiol.2006.03.004  0.698
2006 Bradner JE, Greenberg EF, Schreiber SL, Mazitschek R. Design and Characterization of a Novel, Reverse Prodrug Histone Deacetylase Inhibitor for Cutaneous T-Cell Lymphoma. Blood. 108: 4759-4759. DOI: 10.1182/Blood.V108.11.4759.4759  0.458
2006 Hideshima T, Bradner JE, Yasui H, Raje N, Chauhan D, Podar K, Tai Y, Mitsiades C, Richardson PG, Mazitschek R, Schreiber SL, Anderson KC. Histone Deacetylase-6 (HDAC6) Modulates Akt and STAT3 Activity Via Heat Shock Protein (Hsp) 90 in Human Multiple Myeloma (MM) Cells. Blood. 108: 3426-3426. DOI: 10.1182/blood.V108.11.3426.3426  0.484
2006 Bradner JE, Shen JP, Perlstein EO, Divakaran S, Greenberg EF, Amaravadi R, Schreiber SL. Discovery and Characterization of Small Molecule Inhibitors of Autophagy for Cancer Therapy. Blood. 108: 2606-2606. DOI: 10.1182/Blood.V108.11.2606.2606  0.794
2005 Bali P, Pranpat M, Bradner J, Balasis M, Fiskus W, Guo F, Rocha K, Kumaraswamy S, Boyapalle S, Atadja P, Seto E, Bhalla K. Inhibition of histone deacetylase 6 acetylates and disrupts the chaperone function of heat shock protein 90: a novel basis for antileukemia activity of histone deacetylase inhibitors. The Journal of Biological Chemistry. 280: 26729-34. PMID 15937340 DOI: 10.1074/Jbc.C500186200  0.425
2005 Hideshima T, Bradner JE, Wong J, Chauhan D, Richardson P, Schreiber SL, Anderson KC. Small-molecule inhibition of proteasome and aggresome function induces synergistic antitumor activity in multiple myeloma. Proceedings of the National Academy of Sciences of the United States of America. 102: 8567-72. PMID 15937109 DOI: 10.1073/Pnas.0503221102  0.648
2005 Bradner J, Shen JP, Greenberg E, Hideshima T, Anderson KC, Schreiber SL. Targeting the Protein Degradation Pathway in Multiple Myeloma with Synergistic, Selective Small Molecules. Blood. 106: 2471-2471. DOI: 10.1182/Blood.V106.11.2471.2471  0.605
2004 Bradner J, Kim Y, Koehler A, Kawasumi M, Li X, Schreiber SL, Nghiem P. Identification and Characterization of Novel Small-Molecule Inhibitors of the Replication Checkpoint. Blood. 104: 763-763. DOI: 10.1182/Blood.V104.11.763.763  0.779
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