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Page 1
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. Wang J, et al. Among authors: bradner je. ACS Chem Biol. 2018 Sep 21;13(9):2438-2448. doi: 10.1021/acschembio.7b00638. Epub 2018 Aug 31. ACS Chem Biol. 2018. PMID: 30102854 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.
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.
Targeting MYCN in neuroblastoma by BET bromodomain inhibition.
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, Stegmaier K. Puissant A, et al. Among authors: bradner je. Cancer Discov. 2013 Mar;3(3):308-23. doi: 10.1158/2159-8290.CD-12-0418. Epub 2013 Feb 21. Cancer Discov. 2013. PMID: 23430699 Free PMC article.
PFI-1, a highly selective protein interaction inhibitor, targeting BET Bromodomains.
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, Stankovic T, Knapp S. Picaud S, et al. Among authors: bradner je. Cancer Res. 2013 Jun 1;73(11):3336-46. doi: 10.1158/0008-5472.CAN-12-3292. Epub 2013 Apr 10. Cancer Res. 2013. PMID: 23576556 Free PMC article.
Selective HDAC1/HDAC2 inhibitors induce neuroblastoma differentiation.
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, Tolliday N, Stegmaier K. Frumm SM, et al. Among authors: bradner je. Chem Biol. 2013 May 23;20(5):713-25. doi: 10.1016/j.chembiol.2013.03.020. Chem Biol. 2013. PMID: 23706636 Free PMC article.
260 results