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Items: 1 to 50 of 210

1.

JAK2 is dispensable for maintenance of JAK2 mutant B-cell acute lymphoblastic leukemias.

Kim SK, Knight DA, Jones LR, Vervoort S, Ng AP, Seymour JF, Bradner JE, Waibel M, Kats L, Johnstone RW.

Genes Dev. 2018 Jun 15. doi: 10.1101/gad.307504.117. [Epub ahead of print]

PMID:
29907650
2.

Plasticity in binding confers selectivity in ligand-induced protein degradation.

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.

Nat Chem Biol. 2018 Jun 11. doi: 10.1038/s41589-018-0055-y. [Epub ahead of print]

PMID:
29892083
3.

Gastrointestinal stromal tumor enhancers support a transcription factor network predictive of clinical outcome.

Hemming ML, Lawlor MA, Zeid R, Lesluyes T, Fletcher JA, Raut CP, Sicinska ET, Chibon F, Armstrong SA, Demetri GD, Bradner JE.

Proc Natl Acad Sci U S A. 2018 Jun 4. pii: 201802079. doi: 10.1073/pnas.1802079115. [Epub ahead of print]

PMID:
29866822
4.

Targetable BET proteins- and E2F1-dependent transcriptional program maintains the malignancy of glioblastoma.

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, Dinh HQ, Kappei D, Winter GE, Ding LW, Ang BT, Berman BP, Bradner JE, Tang C, Koeffler HP.

Proc Natl Acad Sci U S A. 2018 May 29;115(22):E5086-E5095. doi: 10.1073/pnas.1712363115. Epub 2018 May 15.

PMID:
29764999
5.

NK cells mediate synergistic antitumor effects of combined inhibition of HDAC6 and BET in a SCLC preclinical model.

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, Quayle SN, Wong KK.

Cancer Res. 2018 May 14. pii: canres.0161.2018. doi: 10.1158/0008-5472.CAN-18-0161. [Epub ahead of print]

PMID:
29760044
6.

Dual Targeting of Oncogenic Activation and Inflammatory Signaling Increases Therapeutic Efficacy in Myeloproliferative Neoplasms.

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, Roberts J, Witkin M, Rapaport F, Teruya-Feldstein J, Qi J, Rampal R, Bernstein BE, Bradner JE, Levine RL.

Cancer Cell. 2018 Apr 9;33(4):785-787. doi: 10.1016/j.ccell.2018.03.024. No abstract available.

7.

The dTAG system for immediate and target-specific protein degradation.

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, Wong KK, Gray NS, Bradner JE.

Nat Chem Biol. 2018 May;14(5):431-441. doi: 10.1038/s41589-018-0021-8. Epub 2018 Mar 26.

PMID:
29581585
8.

Combined BET bromodomain and CDK2 inhibition in MYC-driven medulloblastoma.

Bolin S, Borgenvik A, Persson CU, Sundström A, Qi J, Bradner JE, Weiss WA, Cho YJ, Weishaupt H, Swartling FJ.

Oncogene. 2018 May;37(21):2850-2862. doi: 10.1038/s41388-018-0135-1. Epub 2018 Mar 7.

9.

Functional TRIM24 degrader via conjugation of ineffectual bromodomain and VHL ligands.

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, Gray NS, Bradner JE.

Nat Chem Biol. 2018 Apr;14(4):405-412. doi: 10.1038/s41589-018-0010-y. Epub 2018 Mar 5.

PMID:
29507391
10.

BET bromodomain proteins regulate enhancer function during adipogenesis.

Brown JD, Feldman ZB, Doherty SP, Reyes JM, Rahl PB, Lin CY, Sheng Q, Duan Q, Federation AJ, Kung AL, Haldar SM, Young RA, Plutzky J, Bradner JE.

Proc Natl Acad Sci U S A. 2018 Feb 27;115(9):2144-2149. doi: 10.1073/pnas.1711155115. Epub 2018 Feb 14.

11.

Enhancer invasion shapes MYCN-dependent transcriptional amplification in neuroblastoma.

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, Westbrook TF, Chesler L, Lin CY, Bradner JE.

Nat Genet. 2018 Apr;50(4):515-523. doi: 10.1038/s41588-018-0044-9. Epub 2018 Jan 29.

PMID:
29379199
12.

Translation Termination Factor GSPT1 Is a Phenotypically Relevant Off-Target of Heterobifunctional Phthalimide Degraders.

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.

ACS Chem Biol. 2018 Mar 16;13(3):553-560. doi: 10.1021/acschembio.7b00969. Epub 2018 Jan 29.

PMID:
29356495
13.

Targeting the CoREST complex with dual histone deacetylase and demethylase inhibitors.

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, Roy Burman SS, Fairall L, Milano C, Eroglu A, Proby CM, Dinkova-Kostova AT, Hancock WW, Gray JJ, Bradner JE, Valente S, Mai A, Anders NM, Rudek MA, Hu Y, Ryu B, Schwabe JWR, Mattevi A, Alani RM, Cole PA.

Nat Commun. 2018 Jan 4;9(1):53. doi: 10.1038/s41467-017-02242-4.

14.

Therapeutic targeting of ependymoma as informed by oncogenic enhancer profiling.

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, Wu Q, Michaelraj KA, Miller TE, Hubert CG, Ryzhova M, Garzia L, Donovan L, Dombrowski S, Factor DC, Luu B, Valentim CLL, Gimple RC, Morton A, Kim L, Prager BC, Lee JJY, Wu X, Zuccaro J, Thompson Y, Holgado BL, Reimand J, Ke SQ, Tropper A, Lai S, Vijayarajah S, Doan S, Mahadev V, Miñan AF, Gröbner SN, Lienhard M, Zapatka M, Huang Z, Aldape KD, Carcaboso AM, Houghton PJ, Keir ST, Milde T, Witt H, Li Y, Li CJ, Bian XW, Jones DTW, Scott I, Singh SK, Huang A, Dirks PB, Bouffet E, Bradner JE, Ramaswamy V, Jabado N, Rutka JT, Northcott PA, Lupien M, Lichter P, Korshunov A, Scacheri PC, Pfister SM, Kool M, Taylor MD, Rich JN.

Nature. 2018 Jan 4;553(7686):101-105. doi: 10.1038/nature25169. Epub 2017 Dec 20.

PMID:
29258295
15.

Pharmacological perturbation of CDK9 using selective CDK9 inhibition or degradation.

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, Winter GE, Gray NS.

Nat Chem Biol. 2018 Feb;14(2):163-170. doi: 10.1038/nchembio.2538. Epub 2017 Dec 18.

PMID:
29251720
16.

Dual Targeting of Oncogenic Activation and Inflammatory Signaling Increases Therapeutic Efficacy in Myeloproliferative Neoplasms.

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, Roberts J, Witkin M, Rapaport F, Teruya-Feldstein J, Qi J, Rampal R, Bernstein BE, Bradner JE, Levine RL.

Cancer Cell. 2018 Jan 8;33(1):29-43.e7. doi: 10.1016/j.ccell.2017.11.009. Epub 2017 Dec 14. Erratum in: Cancer Cell. 2018 Apr 9;33(4):785-787.

PMID:
29249691
17.

R-2HG Exhibits Anti-tumor Activity by Targeting FTO/m6A/MYC/CEBPA Signaling.

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, Yu K, Weng H, Huang H, Ferchen K, Qin X, Zhang B, Qi J, Sasaki AT, Plas DR, Bradner JE, Wei M, Marcucci G, Jiang X, Mulloy JC, Jin J, He C, Chen J.

Cell. 2018 Jan 11;172(1-2):90-105.e23. doi: 10.1016/j.cell.2017.11.031. Epub 2017 Dec 14.

PMID:
29249359
18.

YY1 Is a Structural Regulator of Enhancer-Promoter Loops.

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, Young RA.

Cell. 2017 Dec 14;171(7):1573-1588.e28. doi: 10.1016/j.cell.2017.11.008. Epub 2017 Dec 7.

19.

CRISPR-Cas9 screen reveals a MYCN-amplified neuroblastoma dependency on EZH2.

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, Ali LD, Pantel S, Jiang G, Harrington WF, Lee Y, Goodale A, Lubonja R, Krill-Burger JM, Meyers RM, Tsherniak A, Root DE, Bradner JE, Golub TR, Roberts CW, Hahn WC, Weiss WA, Thiele CJ, Stegmaier K.

J Clin Invest. 2018 Jan 2;128(1):446-462. doi: 10.1172/JCI90793. Epub 2017 Dec 4.

20.

Synthetic transcription elongation factors license transcription across repressive chromatin.

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, Xu M, Park PMC, Mukhtar H, Srivastava AK, Faruq M, Bradner JE, Ansari AZ.

Science. 2017 Dec 22;358(6370):1617-1622. doi: 10.1126/science.aan6414. Epub 2017 Nov 30.

PMID:
29192133
21.

Diminished microRNA-29b level is associated with BRD4-mediated activation of oncogenes in cutaneous T-cell lymphoma.

Kohnken R, Wen J, Mundy-Bosse B, McConnell K, Keiter A, Grinshpun L, Hartlage A, Yano M, McNeil B, Chakravarti N, William B, Bradner JE, Caligiuri MA, Porcu P, Mishra A.

Blood. 2018 Feb 15;131(7):771-781. doi: 10.1182/blood-2017-09-805663. Epub 2017 Nov 27.

PMID:
29180399
22.

Leukemia-specific delivery of mutant NOTCH1 targeted therapy.

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.

J Exp Med. 2018 Jan 2;215(1):197-216. doi: 10.1084/jem.20151778. Epub 2017 Nov 20.

PMID:
29158376
23.

JQ1 Induces DNA Damage and Apoptosis, and Inhibits Tumor Growth in a Patient-Derived Xenograft Model of Cholangiocarcinoma.

Garcia PL, Miller AL, Gamblin TL, Council LN, Christein JD, Arnoletti JP, Heslin MJ, Reddy S, Richardson JH, Cui X, van Waardenburg RCAM, Bradner JE, Yang ES, Yoon KJ.

Mol Cancer Ther. 2018 Jan;17(1):107-118. doi: 10.1158/1535-7163.MCT-16-0922. Epub 2017 Nov 15.

PMID:
29142067
24.

A Chemoproteomic Approach to Query the Degradable Kinome Using a Multi-kinase Degrader.

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, Fischer ES, Bradner JE, Tan L, Gray NS.

Cell Chem Biol. 2018 Jan 18;25(1):88-99.e6. doi: 10.1016/j.chembiol.2017.10.005. Epub 2017 Nov 9.

PMID:
29129717
25.

HDAC6 inhibitor WT161 downregulates growth factor receptors in breast cancer.

Hideshima T, Mazitschek R, Qi J, Mimura N, Tseng JC, Kung AL, Bradner JE, Anderson KC.

Oncotarget. 2017 Jul 5;8(46):80109-80123. doi: 10.18632/oncotarget.19019. eCollection 2017 Oct 6.

26.

Merkel cell polyomavirus recruits MYCL to the EP400 complex to promote oncogenesis.

Cheng J, Park DE, Berrios C, White EA, Arora R, Yoon R, Branigan T, Xiao T, Westerling T, Federation A, Zeid R, Strober B, Swanson SK, Florens L, Bradner JE, Brown M, Howley PM, Padi M, Washburn MP, DeCaprio JA.

PLoS Pathog. 2017 Oct 13;13(10):e1006668. doi: 10.1371/journal.ppat.1006668. eCollection 2017 Oct.

27.

MELK is not necessary for the proliferation of basal-like breast cancer cells.

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, Eck MJ, Dhe-Paganon S, Zhao JJ, Gray NS.

Elife. 2017 Sep 19;6. pii: e26693. doi: 10.7554/eLife.26693.

28.

Bromodomain inhibition shows antitumoral activity in mice and human luminal breast cancer.

Pérez-Salvia M, Simó-Riudalbas L, Llinàs-Arias P, Roa L, Setien F, Soler M, de Moura MC, Bradner JE, Gonzalez-Suarez E, Moutinho C, Esteller M.

Oncotarget. 2017 May 29;8(31):51621-51629. doi: 10.18632/oncotarget.18255. eCollection 2017 Aug 1.

29.

Prostate cancer-associated SPOP mutations confer resistance to BET inhibitors through stabilization of BRD4.

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, Buckley DL, Qi J, Buser L, Liu P, Inuzuka H, Beck AH, Wang L, Wild PJ, Garraway LA, Rubin MA, Barbieri CE, Wong KK, Muthuswamy SK, Huang J, Chen Y, Bradner JE, Wei W.

Nat Med. 2017 Sep;23(9):1063-1071. doi: 10.1038/nm.4378. Epub 2017 Aug 14.

30.

HIF activation causes synthetic lethality between the VHL tumor suppressor and the EZH1 histone methyltransferase.

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, Signoretti S, Bradner JE, Kaelin WG Jr.

Sci Transl Med. 2017 Jul 12;9(398). pii: eaal5272. doi: 10.1126/scitranslmed.aal5272.

PMID:
28701475
31.

Correction to BET Bromodomain Inhibitors with One-Step Synthesis Discovered from Virtual Screen.

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, Georg GI, Pomerantz WCK.

J Med Chem. 2017 Jul 27;60(14):6458. doi: 10.1021/acs.jmedchem.7b00943. Epub 2017 Jul 11. No abstract available.

PMID:
28696689
32.

BET Bromodomain Proteins Function as Master Transcription Elongation Factors Independent of CDK9 Recruitment.

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, Olson CM, Dastjerdi S, Bauer S, Lin CY, Gray NS, Kelliher MA, Churchman LS, Bradner JE.

Mol Cell. 2017 Jul 6;67(1):5-18.e19. doi: 10.1016/j.molcel.2017.06.004. Epub 2017 Jun 29.

PMID:
28673542
33.

BET Bromodomain Inhibitors with One-Step Synthesis Discovered from Virtual Screen.

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, Georg GI, Pomerantz WCK.

J Med Chem. 2017 Jun 22;60(12):4805-4817. doi: 10.1021/acs.jmedchem.6b01336. Epub 2017 Jun 7.

34.

BET bromodomain inhibition suppresses innate inflammatory and profibrotic transcriptional networks in heart failure.

Duan Q, McMahon S, Anand P, Shah H, Thomas S, Salunga HT, Huang Y, Zhang R, Sahadevan A, Lemieux ME, Brown JD, Srivastava D, Bradner JE, McKinsey TA, Haldar SM.

Sci Transl Med. 2017 May 17;9(390). pii: eaah5084. doi: 10.1126/scitranslmed.aah5084.

35.

Degradation of the BAF Complex Factor BRD9 by Heterobifunctional Ligands.

Remillard D, Buckley DL, Paulk J, Brien GL, Sonnett M, Seo HS, Dastjerdi S, Wühr M, Dhe-Paganon S, Armstrong SA, Bradner JE.

Angew Chem Int Ed Engl. 2017 May 15;56(21):5738-5743. doi: 10.1002/anie.201611281. Epub 2017 Apr 18.

36.

A chemical probe toolbox for dissecting the cancer epigenome.

Shortt J, Ott CJ, Johnstone RW, Bradner JE.

Nat Rev Cancer. 2017 Mar 23;17(4):268. doi: 10.1038/nrc.2017.26. No abstract available.

PMID:
28332503
37.

Gene expression profiling of patient-derived pancreatic cancer xenografts predicts sensitivity to the BET bromodomain inhibitor JQ1: implications for individualized medicine efforts.

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, Poizat F, Nicolle R, Blum Y, Marisa L, Rubis M, Raoul JL, Bradner JE, Qi J, Lomberk G, Urrutia R, Saul A, Dusetti N, Iovanna J.

EMBO Mol Med. 2017 Apr;9(4):482-497. doi: 10.15252/emmm.201606975.

38.

BET-Bromodomain Inhibitors Engage the Host Immune System and Regulate Expression of the Immune Checkpoint Ligand PD-L1.

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, Zuber J, Shortt J, Johnstone RW.

Cell Rep. 2017 Feb 28;18(9):2162-2174. doi: 10.1016/j.celrep.2017.02.011.

39.

ENL links histone acetylation to oncogenic gene expression in acute myeloid leukaemia.

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, Allis CD, Armstrong SA, Shi X.

Nature. 2017 Mar 9;543(7644):265-269. doi: 10.1038/nature21687. Epub 2017 Mar 1.

40.

Transcription control by the ENL YEATS domain in acute leukaemia.

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, Dhe-Paganon S, Zhang F, Orkin SH, Winter GE, Bradner JE.

Nature. 2017 Mar 9;543(7644):270-274. doi: 10.1038/nature21688. Epub 2017 Mar 1.

41.

A chemical probe toolbox for dissecting the cancer epigenome.

Shortt J, Ott CJ, Johnstone RW, Bradner JE.

Nat Rev Cancer. 2017 Feb 23;17(3):160-183. doi: 10.1038/nrc.2016.148. Review. Erratum in: Nat Rev Cancer. 2017 Mar 23;17 (4):268.

PMID:
28228643
42.

Transcriptional Addiction in Cancer.

Bradner JE, Hnisz D, Young RA.

Cell. 2017 Feb 9;168(4):629-643. doi: 10.1016/j.cell.2016.12.013. Review.

43.

Hotspots of aberrant enhancer activity punctuate the colorectal cancer epigenome.

Cohen AJ, Saiakhova A, Corradin O, Luppino JM, Lovrenert K, Bartels CF, Morrow JJ, Mack SC, Dhillon G, Beard L, Myeroff L, Kalady MF, Willis J, Bradner JE, Keri RA, Berger NA, Pruett-Miller SM, Markowitz SD, Scacheri PC.

Nat Commun. 2017 Feb 7;8:14400. doi: 10.1038/ncomms14400.

44.

Assessment of Bromodomain Target Engagement by a Series of BI2536 Analogues with Miniaturized BET-BRET.

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.

ChemMedChem. 2016 Dec 6;11(23):2575-2581. doi: 10.1002/cmdc.201600502. Epub 2016 Nov 15.

PMID:
27862999
45.

Chronic Myelogenous Leukemia- Initiating Cells Require Polycomb Group Protein EZH2.

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.

Cancer Discov. 2016 Nov;6(11):1237-1247. Epub 2016 Sep 14.

46.

BET Inhibitors Suppress ALDH Activity by Targeting ALDH1A1 Super-Enhancer in Ovarian Cancer.

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, Zhang Z, Sood AK, Ordog T, Bitler BG, Zhang R.

Cancer Res. 2016 Nov 1;76(21):6320-6330.

47.

Inhibition of BET proteins and epigenetic signaling as a potential treatment for osteoporosis.

Baud'huin M, Lamoureux F, Jacques C, Rodriguez Calleja L, Quillard T, Charrier C, Amiaud J, Berreur M, Brounais-LeRoyer B, Owen R, Reilly GC, Bradner JE, Heymann D, Ory B.

Bone. 2017 Jan;94:10-21. doi: 10.1016/j.bone.2016.09.020. Epub 2016 Sep 23.

PMID:
27669656
48.

Discovery of selective small-molecule HDAC6 inhibitor for overcoming proteasome inhibitor resistance in multiple myeloma.

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, Richardson PG, Carrasco RD, Wiest O, Schreiber SL, Anderson KC, Bradner JE.

Proc Natl Acad Sci U S A. 2016 Nov 15;113(46):13162-13167. Epub 2016 Oct 31.

49.

Design and characterization of bivalent BET inhibitors.

Tanaka M, Roberts JM, Seo HS, Souza A, Paulk J, Scott TG, DeAngelo SL, Dhe-Paganon S, Bradner JE.

Nat Chem Biol. 2016 Dec;12(12):1089-1096. doi: 10.1038/nchembio.2209. Epub 2016 Oct 24.

50.

Development of a Potent and Selective HDAC8 Inhibitor.

Ingham OJ, Paranal RM, Smith WB, Escobar RA, Yueh H, Snyder T, Porco JA Jr, Bradner JE, Beeler AB.

ACS Med Chem Lett. 2016 Sep 1;7(10):929-932. eCollection 2016 Oct 13.

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