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Page 1
Biased multicomponent reactions to develop novel bromodomain inhibitors.
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. McKeown MR, et al. Among authors: bradner je. J Med Chem. 2014 Nov 13;57(21):9019-27. doi: 10.1021/jm501120z. Epub 2014 Oct 31. J Med Chem. 2014. PMID: 25314271 Free PMC article.
Direct inhibition of the NOTCH transcription factor complex.
Moellering RE, Cornejo M, Davis TN, Del Bianco C, Aster JC, Blacklow SC, Kung AL, Gilliland DG, Verdine GL, Bradner JE. Moellering RE, et al. Among authors: bradner je. Nature. 2009 Nov 12;462(7270):182-8. doi: 10.1038/nature08543. Nature. 2009. PMID: 19907488 Free PMC article.
Selective inhibition of BET bromodomains.
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, West N, Cameron MJ, Schwartz B, Heightman TD, La Thangue N, French CA, Wiest O, Kung AL, Knapp S, Bradner JE. Filippakopoulos P, et al. Among authors: bradner je. Nature. 2010 Dec 23;468(7327):1067-73. doi: 10.1038/nature09504. Epub 2010 Sep 24. Nature. 2010. PMID: 20871596 Free PMC article.
A novel HDAC inhibitor with a hydroxy-pyrimidine scaffold.
Kemp MM, Wang Q, Fuller JH, West N, Martinez NM, Morse EM, Weïwer M, Schreiber SL, Bradner JE, Koehler AN. Kemp MM, et al. Among authors: bradner je. Bioorg Med Chem Lett. 2011 Jul 15;21(14):4164-9. doi: 10.1016/j.bmcl.2011.05.098. Epub 2011 Jun 2. Bioorg Med Chem Lett. 2011. PMID: 21696956 Free PMC article.
BET bromodomain inhibition as a therapeutic strategy to target c-Myc.
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, Bergsagel PL, Ghobrial IM, Richardson PG, Young RA, Hahn WC, Anderson KC, Kung AL, Bradner JE, Mitsiades CS. Delmore JE, et al. Among authors: bradner je. Cell. 2011 Sep 16;146(6):904-17. doi: 10.1016/j.cell.2011.08.017. Epub 2011 Sep 1. Cell. 2011. PMID: 21889194 Free PMC article.
Genetic resistance to JAK2 enzymatic inhibitors is overcome by HSP90 inhibition.
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, Romanet V, Murakami M, Tiedt R, Ebel N, Evrot E, De Pover A, Régnier CH, Erdmann D, Hofmann F, Eck MJ, Sallan SE, Levine RL, Kung AL, Baffert F, Radimerski T, Weinstock DM. Weigert O, et al. Among authors: bradner je. J Exp Med. 2012 Feb 13;209(2):259-73. doi: 10.1084/jem.20111694. Epub 2012 Jan 23. J Exp Med. 2012. PMID: 22271575 Free PMC article.
Small-molecule inhibition of BRDT for male contraception.
Matzuk MM, McKeown MR, Filippakopoulos P, Li Q, Ma L, Agno JE, Lemieux ME, Picaud S, Yu RN, Qi J, Knapp S, Bradner JE. Matzuk MM, et al. Among authors: bradner je. Cell. 2012 Aug 17;150(4):673-84. doi: 10.1016/j.cell.2012.06.045. Cell. 2012. PMID: 22901802 Free PMC article.
260 results