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Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors.
Yu W, Chory EJ, Wernimont AK, Tempel W, Scopton A, Federation A, Marineau JJ, Qi J, Barsyte-Lovejoy D, Yi J, Marcellus R, Iacob RE, Engen JR, Griffin C, Aman A, Wienholds E, Li F, Pineda J, Estiu G, Shatseva T, Hajian T, Al-Awar R, Dick JE, Vedadi M, Brown PJ, Arrowsmith CH, Bradner JE, Schapira M. Yu W, et al. Among authors: bradner je. Nat Commun. 2012;3:1288. doi: 10.1038/ncomms2304. Nat Commun. 2012. PMID: 23250418 Free article.
On the inhibition of histone deacetylase 8.
Estiu G, West N, Mazitschek R, Greenberg E, Bradner JE, Wiest O. Estiu G, et al. Among authors: bradner je. Bioorg Med Chem. 2010 Jun 1;18(11):4103-10. doi: 10.1016/j.bmc.2010.03.080. Epub 2010 Apr 3. Bioorg Med Chem. 2010. PMID: 20472442 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.
The use of small molecules in somatic-cell reprogramming.
Federation AJ, Bradner JE, Meissner A. Federation AJ, et al. Among authors: bradner je. Trends Cell Biol. 2014 Mar;24(3):179-87. doi: 10.1016/j.tcb.2013.09.011. Epub 2013 Oct 31. Trends Cell Biol. 2014. PMID: 24183602 Free PMC article. Review.
Genome-wide localization of small molecules.
Anders L, Guenther MG, Qi J, Fan ZP, Marineau JJ, Rahl PB, Lovén J, Sigova AA, Smith WB, Lee TI, Bradner JE, Young RA. Anders L, et al. Among authors: bradner je. Nat Biotechnol. 2014 Jan;32(1):92-6. doi: 10.1038/nbt.2776. Epub 2013 Dec 15. Nat Biotechnol. 2014. PMID: 24336317 Free PMC article.
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.
Structure-guided DOT1L probe optimization by label-free ligand displacement.
Yi JS, Federation AJ, Qi J, Dhe-Paganon S, Hadler M, Xu X, St Pierre R, Varca AC, Wu L, Marineau JJ, Smith WB, Souza A, Chory EJ, Armstrong SA, Bradner JE. Yi JS, et al. Among authors: bradner je. ACS Chem Biol. 2015 Mar 20;10(3):667-74. doi: 10.1021/cb500796d. Epub 2015 Jan 15. ACS Chem Biol. 2015. PMID: 25397901 Free PMC article.
260 results