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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. Ayoub AM, et al. Among authors: bradner je. J Med Chem. 2017 Jun 22;60(12):4805-4817. doi: 10.1021/acs.jmedchem.6b01336. Epub 2017 Jun 7. J Med Chem. 2017. PMID: 28535045 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.
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.
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.
BET acetyl-lysine binding proteins control pathological cardiac hypertrophy.
Spiltoir JI, Stratton MS, Cavasin MA, Demos-Davies K, Reid BG, Qi J, Bradner JE, McKinsey TA. Spiltoir JI, et al. Among authors: bradner je. J Mol Cell Cardiol. 2013 Oct;63:175-9. doi: 10.1016/j.yjmcc.2013.07.017. Epub 2013 Aug 9. J Mol Cell Cardiol. 2013. PMID: 23939492 Free PMC article.
260 results