James Bradner, MD - Publications

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

151 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
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  0.32
2019 Sdelci S, Rendeiro AF, Rathert P, You W, Lin JG, Ringler A, Hofstätter G, Moll HP, Gürtl B, Farlik M, Schick S, Klepsch F, Oldach M, Buphamalai P, Schischlik F, ... ... Bradner JE, et al. MTHFD1 interaction with BRD4 links folate metabolism to transcriptional regulation. Nature Genetics. PMID 31133746 DOI: 10.1038/s41588-019-0413-z  0.36
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  0.36
2019 Hemming ML, Lawlor MA, Andersen JL, Hagan T, Chipashvili O, Scott TG, Raut CP, Sicinska E, Armstrong SA, Demetri GD, Bradner JE. Enhancer Domains in Gastrointestinal Stromal Tumor Regulate KIT Expression and are Targetable by BET Bromodomain Inhibition. Cancer Research. PMID 30630822 DOI: 10.1158/0008-5472.CAN-18-1888  0.36
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  0.36
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  0.36
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  0.4
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: 10.1021/acschembio.7b00638  0.4
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  0.36
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  0.4
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  0.4
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  0.4
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  0.36
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  0.36
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  0.36
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  0.4
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  0.4
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  0.36
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  0.32
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  0.36
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: 10.1084/jem.20151778  0.4
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  0.36
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  0.36
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  0.4
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  0.36
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  0.36
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  0.36
2017 Huang H, Liu S, Jean M, Simpson S, Huang H, Merkley M, Hayashi T, Kong W, Rodríguez-Sánchez I, Zhang X, Yosief HO, Miao H, Que J, Kobie JJ, Bradner J, et al. A Novel Bromodomain Inhibitor Reverses HIV-1 Latency through Specific Binding with BRD4 to Promote Tat and P-TEFb Association. Frontiers in Microbiology. 8: 1035. PMID 28638377 DOI: 10.3389/fmicb.2017.01035  0.4
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  0.36
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  0.36
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  0.36
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  0.4
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  0.4
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  0.36
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  0.4
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  0.4
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  0.36
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  0.32
2016 Saint-André V, Federation AJ, Lin CY, Abraham BJ, Reddy J, Lee TI, Bradner JE, Young RA. Models of human core transcriptional regulatory circuitries. Genome Research. PMID 26843070 DOI: 10.1101/gr.197590.115  0.36
2016 Lin CY, Erkek S, Tong Y, Yin L, Federation AJ, Zapatka M, Haldipur P, Kawauchi D, Risch T, Warnatz HJ, Worst BC, Ju B, Orr BA, Zeid R, Polaski DR, ... ... Bradner JE, et al. Active medulloblastoma enhancers reveal subgroup-specific cellular origins. Nature. PMID 26814967 DOI: 10.1038/nature16546  0.36
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  0.36
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  0.36
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: 10.1084/jem.20151317  0.36
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  0.36
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  0.36
2015 Clausen DJ, Smith WB, Haines BE, Wiest O, Bradner JE, Williams RM. Modular synthesis and biological activity of pyridyl-based analogs of the potent Class I Histone Deacetylase Inhibitor Largazole. Bioorganic & Medicinal Chemistry. 23: 5061-74. PMID 26054247 DOI: 10.1016/j.bmc.2015.03.063  0.36
2015 Marcsisin SR, Liptak C, Marineau J, Bradner JE, Engen JR. Tag and Capture Flow Hydrogen Exchange Mass Spectrometry with a Fluorous-Immobilized Probe. Analytical Chemistry. 87: 6349-56. PMID 26023704 DOI: 10.1021/acs.analchem.5b01220  0.36
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  0.36
2015 Pefanis E, Wang J, Rothschild G, Lim J, Kazadi D, Sun J, Federation A, Chao J, Elliott O, Liu ZP, Economides AN, Bradner JE, Rabadan R, Basu U. RNA exosome-regulated long non-coding RNA transcription controls super-enhancer activity. Cell. 161: 774-89. PMID 25957685 DOI: 10.1016/j.cell.2015.04.034  0.36
2015 Fowler T, Ghatak P, Price DH, Conaway R, Conaway J, Chiang CM, Bradner JE, Shilatifard A, Roy AL. Correction: Regulation of MYC Expression and Differential JQ1 Sensitivity in Cancer Cells. Plos One. 10: e0126328. PMID 25902070 DOI: 10.1371/journal.pone.0126328  0.36
2015 Bradner JE. Cancer: An essential passenger with p53 Nature. 520: 626-627. PMID 25901678 DOI: 10.1038/nature14390  0.36
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  0.36
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  0.36
2015 Wu Q, Madany P, Akech J, Dobson JR, Douthwright S, Browne G, Colby JL, Winter GE, Bradner JE, Pratap J, Sluder G, Bhargava R, Chiosea S, van Wijnen AJ, Stein JL, et al. The SWI/SNF ATPases are Required for Triple Negative Breast Cancer Cell Proliferation. Journal of Cellular Physiology. PMID 25808524 DOI: 10.1002/jcp.24991  0.36
2015 Hnisz D, Schuijers J, Lin CY, Weintraub AS, Abraham BJ, Lee TI, Bradner JE, Young RA. Convergence of developmental and oncogenic signaling pathways at transcriptional super-enhancers. Molecular Cell. 58: 362-70. PMID 25801169 DOI: 10.1016/j.molcel.2015.02.014  0.36
2015 Ji X, Dadon DB, Abraham BJ, Lee TI, Jaenisch R, Bradner JE, Young RA. Chromatin proteomic profiling reveals novel proteins associated with histone-marked genomic regions. Proceedings of the National Academy of Sciences of the United States of America. 112: 3841-6. PMID 25755260 DOI: 10.1073/pnas.1502971112  0.36
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  0.36
2015 Alinari L, Mahasenan KV, Yan F, Karkhanis V, Chung JH, Smith EM, Quinion C, Smith PL, Kim L, Patton JT, Lapalombella R, Yu B, Wu Y, Roy S, De Leo A, ... ... Bradner JE, et al. Selective inhibition of protein arginine methyltransferase 5 blocks initiation and maintenance of B-cell transformation. Blood. 125: 2530-43. PMID 25742700 DOI: 10.1182/blood-2014-12-619783  0.36
2015 Pilon JL, Clausen DJ, Hansen RJ, Lunghofer PJ, Charles B, Rose BJ, Thamm DH, Gustafson DL, Bradner JE, Williams RM. Comparative pharmacokinetic properties and antitumor activity of the marine HDACi Largazole and Largazole peptide isostere. Cancer Chemotherapy and Pharmacology. 75: 671-82. PMID 25616967 DOI: 10.1007/s00280-015-2675-1  0.36
2015 Kühn MW, Hadler MJ, Daigle SR, Koche RP, Krivtsov AV, Olhava EJ, Caligiuri MA, Huang G, Bradner JE, Pollock RM, Armstrong SA. MLL partial tandem duplication leukemia cells are sensitive to small molecule DOT1L inhibition. Haematologica. 100: e190-3. PMID 25596271 DOI: 10.3324/haematol.2014.115337  0.36
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  0.36
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  0.36
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  0.36
2015 Trabucco SE, Gerstein RM, Evens AM, Bradner JE, Shultz LD, Greiner DL, Zhang H. Inhibition of bromodomain proteins for the treatment of human diffuse large B-cell lymphoma Clinical Cancer Research. 21: 113-122. DOI: 10.1158/1078-0432.CCR-13-3346  0.36
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  0.36
2014 Meng FL, Du Z, Federation A, Hu J, Wang Q, Kieffer-Kwon KR, Meyers RM, Amor C, Wasserman CR, Neuberg D, Casellas R, Nussenzweig MC, Bradner JE, Liu XS, Alt FW. Convergent transcription at intragenic super-enhancers targets AID-initiated genomic instability. Cell. 159: 1538-48. PMID 25483776 DOI: 10.1016/j.cell.2014.11.014  0.36
2014 Deshpande AJ, Deshpande A, Sinha AU, Chen L, Chang J, Cihan A, Fazio M, Chen CW, Zhu N, Koche R, Dzhekieva L, Ibáñez G, Dias S, Banka D, Krivtsov A, ... ... Bradner JE, et al. AF10 regulates progressive H3K79 methylation and HOX gene expression in diverse AML subtypes. Cancer Cell. 26: 896-908. PMID 25464900 DOI: 10.1016/j.ccell.2014.10.009  0.36
2014 Kawasumi M, Bradner JE, Tolliday N, Thibodeau R, Sloan H, Brummond KM, Nghiem P. Identification of ATR-Chk1 pathway inhibitors that selectively target p53-deficient cells without directly suppressing ATR catalytic activity. Cancer Research. 74: 7534-45. PMID 25336189 DOI: 10.1158/0008-5472.CAN-14-2650  0.36
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  0.36
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  0.36
2014 Schubbert S, Cardenas A, Chen H, Garcia C, Guo W, Bradner J, Wu H. Targeting the MYC and PI3K pathways eliminates leukemia-initiating cells in T-cell acute lymphoblastic leukemia. Cancer Research. 74: 7048-59. PMID 25287161 DOI: 10.1158/0008-5472.CAN-14-1470  0.36
2014 McKeown MR, Bradner JE. Therapeutic strategies to inhibit MYC. Cold Spring Harbor Perspectives in Medicine. 4. PMID 25274755 DOI: 10.1101/cshperspect.a014266  0.36
2014 Brown JD, Lin CY, Duan Q, Griffin G, Federation AJ, Paranal RM, Bair S, Newton G, Lichtman AH, Kung AL, Yang T, Wang H, Luscinskas FW, Croce KJ, Bradner JE, et al. NF-κB directs dynamic super enhancer formation in inflammation and atherogenesis. Molecular Cell. 56: 219-31. PMID 25263595 DOI: 10.1016/j.molcel.2014.08.024  0.36
2014 Rajagopalan V, Vaidyanathan M, Janardhanam VAr, Bradner JE. Pre-clinical analysis of changes in intra-cellular biochemistry of glioblastoma multiforme (GBM) cells due to c-Myc silencing Cellular and Molecular Neurobiology. 34: 1059-1069. PMID 25056450 DOI: 10.1007/s10571-014-0083-4  0.36
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  0.36
2014 D'Erasmo MP, Smith WB, Munoz A, Mohandas P, Au AS, Marineau JJ, Quadri LE, Bradner JE, Murelli RP. 7,9-Diaryl-1,6,8-trioxaspiro[4.5]dec-3-en-2-ones: readily accessible and highly potent anticancer compounds. Bioorganic & Medicinal Chemistry Letters. 24: 4035-8. PMID 25011911 DOI: 10.1016/j.bmcl.2014.05.102  0.36
2014 Vogl DT, Stadtmauer EA, Tan KS, Heitjan DF, Davis LE, Pontiggia L, Rangwala R, Piao S, Chang YC, Scott EC, Paul TM, Nichols CW, Porter DL, Kaplan J, Mallon G, ... Bradner JE, et al. Combined autophagy and proteasome inhibition: a phase 1 trial of hydroxychloroquine and bortezomib in patients with relapsed/refractory myeloma. Autophagy. 10: 1380-90. PMID 24991834 DOI: 10.4161/auto.29264  0.36
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  0.36
2014 Ichida JK, TCW J, T C W J, Williams LA, Carter AC, Shi Y, Moura MT, Ziller M, Singh S, Amabile G, Bock C, Umezawa A, Rubin LL, Bradner JE, Akutsu H, et al. Notch inhibition allows oncogene-independent generation of iPS cells. Nature Chemical Biology. 10: 632-9. PMID 24952596 DOI: 10.1038/nchembio.1552  0.36
2014 Chen C, Liu Y, Rappaport AR, Kitzing T, Schultz N, Zhao Z, Shroff AS, Dickins RA, Vakoc CR, Bradner JE, Stock W, LeBeau MM, Shannon KM, Kogan S, Zuber J, et al. MLL3 is a haploinsufficient 7q tumor suppressor in acute myeloid leukemia Cancer Cell. 25: 652-665. PMID 24794707 DOI: 10.1016/j.ccr.2014.03.016  0.36
2014 Lane AA, Chapuy B, Lin CY, Tivey T, Li H, Townsend EC, van Bodegom D, Day TA, Wu SC, Liu H, Yoda A, Alexe G, Schinzel AC, Sullivan TJ, Malinge S, ... ... Bradner JE, et al. Triplication of a 21q22 region contributes to B cell transformation through HMGN1 overexpression and loss of histone H3 Lys27 trimethylation. Nature Genetics. 46: 618-23. PMID 24747640 DOI: 10.1038/ng.2949  0.36
2014 Wang R, Liu W, Helfer CM, Bradner JE, Hornick JL, Janicki SM, French CA, You J. Activation of SOX2 expression by BRD4-NUT oncogenic fusion drives neoplastic transformation in NUT midline carcinoma Cancer Research. 74: 3332-3343. PMID 24736545 DOI: 10.1158/0008-5472.CAN-13-2658  0.36
2014 Gröschel S, Sanders MA, Hoogenboezem R, De Wit E, Bouwman BAM, Erpelinck C, Van Der Velden VHJ, Havermans M, Avellino R, Van Lom K, Rombouts EJ, Van Duin M, Döhner K, Beverloo HB, Bradner JE, et al. A single oncogenic enhancer rearrangement causes concomitant EVI1 and GATA2 deregulation in Leukemia Cell. 157: 369-381. PMID 24703711 DOI: 10.1016/j.cell.2014.02.019  0.36
2014 Lamoureux F, Baud'huin M, Rodriguez Calleja L, Jacques C, Berreur M, Rédini F, Lecanda F, Bradner JE, Heymann D, Ory B. Selective inhibition of BET bromodomain epigenetic signalling interferes with the bone-associated tumour vicious cycle. Nature Communications. 5: 3511. PMID 24646477 DOI: 10.1038/ncomms4511  0.36
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  0.36
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  0.36
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  0.36
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  0.36
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  0.36
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  0.36
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  0.36
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  0.36
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  0.36
2014 Anderson NM, Harrold I, Mansour MR, Sanda T, McKeown M, Nagykary N, Bradner JE, Lan Zhang G, Look AT, Feng H. BCL2-specific inhibitor ABT-199 synergizes strongly with cytarabine against the early immature LOUCY cell line but not more-differentiated T-ALL cell lines. Leukemia. 28: 1145-8. PMID 24342948 DOI: 10.1038/leu.2013.377  0.36
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  0.36
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  0.36
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  0.36
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  0.36
2014 Federation AJ, Bradner JE, Meissner A. The use of small molecules in somatic-cell reprogramming. Trends in Cell Biology. 24: 179-87. PMID 24183602 DOI: 10.1016/j.tcb.2013.09.011  0.36
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  0.36
2014 Grayson AR, Walsh EM, Cameron MJ, Godec J, Ashworth T, Ambrose JM, Aserlind AB, Wang H, Evan GI, Kluk MJ, Bradner JE, Aster JC, French CA. MYC, a downstream target of BRD-NUT, is necessary and sufficient for the blockade of differentiation in NUT midline carcinoma Oncogene. 33: 1736-1742. PMID 23604113 DOI: 10.1038/onc.2013.126  0.36
2014 Bradner JE. From transcriptional regulation to drugging the cancer epigenome Genome Medicine. 6. DOI: 10.1186/s13073-014-0123-1  0.36
2014 Patel H, Chuckowree I, Coxhead P, Guille M, Wang M, Zuckermann A, Williams RSB, Librizzi M, Paranal RM, Bradner JE, Spencer J. Synthesis of hybrid anticancer agents based on kinase and histone deacetylase inhibitors Medchemcomm. 5: 1829-1833. DOI: 10.1039/c4md00211c  0.36
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. DOI: 10.1038/nature13561  0.36
2014 Orlando DA, Chen MW, Brown VE, Solanki S, Choi YJ, Olson ER, Fritz CC, Bradner JE, Guenther MG. Quantitative ChIP-Seq normalization reveals global modulation of the epigenome Cell Reports. 9: 1163-1170. DOI: 10.1016/j.celrep.2014.10.018  0.36
2013 Bradner J. New targets for hematologic malignancies Clinical Advances in Hematology and Oncology. 11: 375-376. PMID 24472807  0.36
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  0.36
2013 Lwin T, Zhao X, Cheng F, Zhang X, Huang A, Shah B, Zhang Y, Moscinski LC, Choi YS, Kozikowski AP, Bradner JE, Dalton WS, Sotomayor E, Tao J. A microenvironment-mediated c-Myc/miR-548m/HDAC6 amplification loop in non-Hodgkin B cell lymphomas. The Journal of Clinical Investigation. 123: 4612-26. PMID 24216476 DOI: 10.1172/JCI64210  0.36
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  0.36
2013 Chen C, Liu Y, Lu C, Cross JR, Morris JP, Shroff AS, Ward PS, Bradner JE, Thompson C, Lowe SW. Cancer-associated IDH2 mutants drive an acute myeloid leukemia that is susceptible to Brd4 inhibition. Genes & Development. 27: 1974-85. PMID 24065765 DOI: 10.1101/gad.226613.113  0.36
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  0.36
2013 Guerra-Bubb JM, Bowers AA, Smith WB, Paranal R, Estiu G, Wiest O, Bradner JE, Williams RM. Synthesis and HDAC inhibitory activity of isosteric thiazoline-oxazole largazole analogs. Bioorganic & Medicinal Chemistry Letters. 23: 6025-8. PMID 24035339 DOI: 10.1016/j.bmcl.2013.06.012  0.36
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  0.36
2013 Bradner JE. Interview: Interview with James Bradner Future Medicinal Chemistry. 5: 1373-1376. PMID 23919548 DOI: 10.4155/fmc.13.124  0.36
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  0.36
2013 Floyd SR, Pacold ME, Huang Q, Clarke SM, Lam FC, Cannell IG, Bryson BD, Rameseder J, Lee MJ, Blake EJ, Fydrych A, Ho R, Greenberger BA, Chen GC, Maffa A, ... ... Bradner JE, et al. The bromodomain protein Brd4 insulates chromatin from DNA damage signalling. Nature. 498: 246-50. PMID 23728299 DOI: 10.1038/nature12147  0.36
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  0.36
2013 Amin J, Puglisi A, Clarke J, Milton J, Wang M, Paranal RM, Bradner JE, Spencer J. A cyclodextrin-capped histone deacetylase inhibitor. Bioorganic & Medicinal Chemistry Letters. 23: 3346-8. PMID 23591111 DOI: 10.1016/j.bmcl.2013.03.084  0.36
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  0.36
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  0.36
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  0.36
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  0.36
2013 Boehm D, Calvanese V, Dar RD, Xing S, Schroeder S, Martins L, Aull K, Li PC, Planelles V, Bradner JE, Zhou MM, Siliciano RF, Weinberger L, Verdin E, Ott M. BET bromodomain-targeting compounds reactivate HIV from latency via a Tat-independent mechanism. Cell Cycle (Georgetown, Tex.). 12: 452-62. PMID 23255218 DOI: 10.4161/cc.23309  0.36
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  0.36
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  0.36
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  0.36
2012 Herrmann H, Blatt K, Shi J, Gleixner KV, Cerny-Reiterer S, Müllauer L, Vakoc CR, Sperr WR, Horny HP, Bradner JE, Zuber J, Valent P. Small-molecule inhibition of BRD4 as a new potent approach to eliminate leukemic stem- and progenitor cells in acute myeloid leukemia (AML) Oncotarget. 3: 1588-1599. PMID 23249862  0.36
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  0.36
2012 Lin CY, Lovén J, Rahl PB, Paranal RM, Burge CB, Bradner JE, Lee TI, Young RA. Transcriptional amplification in tumor cells with elevated c-Myc. Cell. 151: 56-67. PMID 23021215 DOI: 10.1016/j.cell.2012.08.026  0.36
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  0.36
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  0.36
2012 Bauer DE, Mitchell CM, Strait KM, Lathan CS, Stelow EB, Lüer SC, Muhammed S, Evans AG, Sholl LM, Rosai J, Giraldi E, Oakley RP, Rodriguez-Galindo C, London WB, Sallan SE, ... Bradner JE, et al. Clinicopathologic features and long-term outcomes of NUT midline carcinoma. Clinical Cancer Research : An Official Journal of the American Association For Cancer Research. 18: 5773-9. PMID 22896655 DOI: 10.1158/1078-0432.CCR-12-1153  0.36
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  0.36
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  0.36
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  0.36
2012 Weigert O, Lane AA, Bird L, Kopp N, Chapuy B, van Bodegom D, Toms AV, Marubayashi S, Christie AL, McKeown M, Paranal RM, Bradner JE, Yoda A, Gaul C, Vangrevelinghe E, et al. Genetic resistance to JAK2 enzymatic inhibitors is overcome by HSP90 inhibition. The Journal of Experimental Medicine. 209: 259-73. PMID 22271575 DOI: 10.1084/jem.20111694  0.36
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  0.36
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  0.36
2011 Kawasumi M, Lemos B, Bradner JE, Thibodeau R, Kim YS, Schmidt M, Higgins E, Koo SW, Angle-Zahn A, Chen A, Levine D, Nguyen L, Heffernan TP, Longo I, Mandinova A, et al. Protection from UV-induced skin carcinogenesis by genetic inhibition of the ataxia telangiectasia and Rad3-related (ATR) kinase. Proceedings of the National Academy of Sciences of the United States of America. 108: 13716-21. PMID 21844338 DOI: 10.1073/pnas.1111378108  0.36
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  0.36
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  0.36
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  0.36
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  0.36
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  0.36
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  0.36
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  0.36
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  0.36
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  0.36
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  0.36
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  0.36
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  0.36
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