Format
Sort by
Items per page

Send to

Choose Destination

Search results

Items: 1 to 50 of 227

1.

Dual Inhibition of TAF1 and BET Bromodomains from the BI-2536 Kinase Inhibitor Scaffold.

Remillard D, Buckley DL, Seo HS, Ferguson FM, Dhe-Paganon S, Bradner JE, Gray NS.

ACS Med Chem Lett. 2019 Sep 13;10(10):1443-1449. doi: 10.1021/acsmedchemlett.9b00243. eCollection 2019 Oct 10.

PMID:
31620231
2.

High-fat diet fuels prostate cancer progression by rewiring the metabolome and amplifying the MYC program.

Labbé DP, Zadra G, Yang M, Reyes JM, Lin CY, Cacciatore S, Ebot EM, Creech AL, Giunchi F, Fiorentino M, Elfandy H, Syamala S, Karoly ED, Alshalalfa M, Erho N, Ross A, Schaeffer EM, Gibb EA, Takhar M, Den RB, Lehrer J, Karnes RJ, Freedland SJ, Davicioni E, Spratt DE, Ellis L, Jaffe JD, DʼAmico AV, Kantoff PW, Bradner JE, Mucci LA, Chavarro JE, Loda M, Brown M.

Nat Commun. 2019 Sep 25;10(1):4358. doi: 10.1038/s41467-019-12298-z.

3.

PAX8 activates metabolic genes via enhancer elements in Renal Cell Carcinoma.

Bleu M, Gaulis S, Lopes R, Sprouffske K, Apfel V, Holwerda S, Pregnolato M, Yildiz U, Cordoʹ V, Dost AFM, Knehr J, Carbone W, Lohmann F, Lin CY, Bradner JE, Kauffmann A, Tordella L, Roma G, Galli GG.

Nat Commun. 2019 Aug 20;10(1):3739. doi: 10.1038/s41467-019-11672-1.

4.

Neuronal differentiation and cell-cycle programs mediate response to BET-bromodomain inhibition in MYC-driven medulloblastoma.

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, Pages M, Balboni Iniguez A, Paolella BR, Meng A, Sinai C, Roti G, Dharia NV, Creech A, Tanenbaum B, Khadka P, Tracy A, Tiv HL, Hong AL, Coy S, Rashid R, Lin JR, Cowley GS, Lam FC, Goodale A, Lee Y, Schoolcraft K, Vazquez F, Hahn WC, Tsherniak A, Bradner JE, Yaffe MB, Milde T, Pfister SM, Qi J, Schenone M, Carr SA, Ligon KL, Kieran MW, Santagata S, Olson JM, Gokhale PC, Jaffe JD, Root DE, Stegmaier K, Johannessen CM, Beroukhim R.

Nat Commun. 2019 Jun 3;10(1):2400. doi: 10.1038/s41467-019-10307-9.

5.

MTHFD1 interaction with BRD4 links folate metabolism to transcriptional regulation.

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, Májek P, Parapatics K, Schmidl C, Schuster M, Penz T, Buckley DL, Hudecz O, Imre R, Wang SY, Maric HM, Kralovics R, Bennett KL, Müller AC, Mechtler K, Menche J, Bradner JE, Winter GE, Klavins K, Casanova E, Bock C, Zuber J, Kubicek S.

Nat Genet. 2019 Jun;51(6):990-998. doi: 10.1038/s41588-019-0413-z. Epub 2019 May 27.

PMID:
31133746
6.

The BET inhibitor JQ1 attenuates double-strand break repair and sensitizes models of pancreatic ductal adenocarcinoma to PARP inhibitors.

Miller AL, Fehling SC, Garcia PL, Gamblin TL, Council LN, van Waardenburg RCAM, Yang ES, Bradner JE, Yoon KJ.

EBioMedicine. 2019 Jun;44:419-430. doi: 10.1016/j.ebiom.2019.05.035. Epub 2019 May 22.

7.

Small-molecule targeting of brachyury transcription factor addiction in chordoma.

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, Zhang T, Gray NS, Clarke PA, Blagg J, Workman P, Sommer J, Hornicek F, Root DE, Hahn WC, Bradner JE, Wong KK, Clemons PA, Lin CY, Kotz JD, Schreiber SL.

Nat Med. 2019 Feb;25(2):292-300. doi: 10.1038/s41591-018-0312-3. Epub 2019 Jan 21.

8.

Enhancer Domains in Gastrointestinal Stromal Tumor Regulate KIT Expression and Are Targetable by BET Bromodomain Inhibition.

Hemming ML, Lawlor MA, Andersen JL, Hagan T, Chipashvili O, Scott TG, Raut CP, Sicinska E, Armstrong SA, Demetri GD, Bradner JE.

Cancer Res. 2019 Mar 1;79(5):994-1009. doi: 10.1158/0008-5472.CAN-18-1888. Epub 2019 Jan 10.

PMID:
30630822
9.

Non-overlapping Control of Transcriptome by Promoter- and Super-Enhancer-Associated Dependencies in Multiple Myeloma.

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.

Cell Rep. 2018 Dec 26;25(13):3693-3705.e6. doi: 10.1016/j.celrep.2018.12.016.

10.

Enhancer Architecture and Essential Core Regulatory Circuitry of Chronic Lymphocytic Leukemia.

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.

Cancer Cell. 2018 Dec 10;34(6):982-995.e7. doi: 10.1016/j.ccell.2018.11.001. Epub 2018 Nov 29.

PMID:
30503705
11.

Targeted degradation of BRD9 reverses oncogenic gene expression in synovial sarcoma.

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, Vakoc CR, Armstrong SA.

Elife. 2018 Nov 15;7. pii: e41305. doi: 10.7554/eLife.41305.

12.

A non-canonical SWI/SNF complex is a synthetic lethal target in cancers driven by BAF complex perturbation.

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, Gray NS, Bradner JE, Chan HM, Kadoch C.

Nat Cell Biol. 2018 Dec;20(12):1410-1420. doi: 10.1038/s41556-018-0221-1. Epub 2018 Nov 5.

13.

Small-molecule BCL6 inhibitor effectively treats mice with nonsclerodermatous chronic graft-versus-host disease.

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, Cutler CS, Koreth J, Antin JH, Soiffer RJ, Ritz J, Bradner JE, Melnick AM, Blazar BR.

Blood. 2019 Jan 3;133(1):94-99. doi: 10.1182/blood-2018-03-839993. Epub 2018 Oct 2.

PMID:
30279226
14.

Structure-Guided Design and Development of Potent and Selective Dual Bromodomain 4 (BRD4)/Polo-like Kinase 1 (PLK1) Inhibitors.

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.

J Med Chem. 2018 Sep 13;61(17):7785-7795. doi: 10.1021/acs.jmedchem.8b00765. Epub 2018 Aug 30.

15.

Structural and Atropisomeric Factors Governing the Selectivity of Pyrimido-benzodiazipinones as Inhibitors of Kinases and Bromodomains.

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, Becht K, Kim ND, McKeown MR, Roberts JM, Zhang J, Sim T, Alessi DR, Bradner JE, Lizcano JM, Blacklow SC, Qi J, Xu X, Gray NS.

ACS Chem Biol. 2018 Sep 21;13(9):2438-2448. doi: 10.1021/acschembio.7b00638. Epub 2018 Aug 31.

16.

BET Bromodomain Inhibition Cooperates with PD-1 Blockade to Facilitate Antitumor Response in Kras-Mutant Non-Small Cell Lung Cancer.

Adeegbe DO, Liu S, Hattersley MM, Bowden M, Zhou CW, Li S, Vlahos R, Grondine M, Dolgalev I, Ivanova EV, Quinn MM, Gao P, Hammerman PS, Bradner JE, Diehl JA, Rustgi AK, Bass AJ, Tsirigos A, Freeman GJ, Chen H, Wong KK.

Cancer Immunol Res. 2018 Oct;6(10):1234-1245. doi: 10.1158/2326-6066.CIR-18-0077. Epub 2018 Aug 7.

17.

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 1;32(11-12):849-864. doi: 10.1101/gad.307504.117. Epub 2018 Jun 15.

18.

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 Jul;14(7):706-714. doi: 10.1038/s41589-018-0055-y. Epub 2018 Jun 11.

19.

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 19;115(25):E5746-E5755. doi: 10.1073/pnas.1802079115. Epub 2018 Jun 4.

20.

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.

21.

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 Jul 1;78(13):3709-3717. doi: 10.1158/0008-5472.CAN-18-0161. Epub 2018 May 14.

22.

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.

23.

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.

24.

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.

25.

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.

26.

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.

27.

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.

28.

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
29.

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.

30.

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.

31.

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.

32.

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.

33.

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.

34.

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.

35.

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.

36.

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.

37.

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.

38.

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.

39.

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.

40.

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.

41.

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.

42.

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.

43.

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.

44.

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.

45.

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.

46.

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.

47.

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
48.

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.

49.

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. Erratum in: J Med Chem. 2017 Jul 27;60(14):6458.

50.

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.

Supplemental Content

Loading ...
Support Center