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The SUV4-20 inhibitor A-196 verifies a role for epigenetics in genomic integrity.
Bromberg KD, Mitchell TR, Upadhyay AK, Jakob CG, Jhala MA, Comess KM, Lasko LM, Li C, Tuzon CT, Dai Y, Li F, Eram MS, Nuber A, Soni NB, Manaves V, Algire MA, Sweis RF, Torrent M, Schotta G, Sun C, Michaelides MR, Shoemaker AR, Arrowsmith CH, Brown PJ, Santhakumar V, Martin A, Rice JC, Chiang GG, Vedadi M, Barsyte-Lovejoy D, Pappano WN. Bromberg KD, et al. Among authors: upadhyay ak. Nat Chem Biol. 2017 Mar;13(3):317-324. doi: 10.1038/nchembio.2282. Epub 2017 Jan 23. Nat Chem Biol. 2017. PMID: 28114273
Turning a Substrate Peptide into a Potent Inhibitor for the Histone Methyltransferase SETD8.
Judge RA, Zhu H, Upadhyay AK, Bodelle PM, Hutchins CW, Torrent M, Marin VL, Yu W, Vedadi M, Li F, Brown PJ, Pappano WN, Sun C, Petros AM. Judge RA, et al. Among authors: upadhyay ak. ACS Med Chem Lett. 2016 Oct 11;7(12):1102-1106. doi: 10.1021/acsmedchemlett.6b00303. eCollection 2016 Dec 8. ACS Med Chem Lett. 2016. PMID: 27994746 Free PMC article.
Novel Modes of Inhibition of Wild-Type Isocitrate Dehydrogenase 1 (IDH1): Direct Covalent Modification of His315.
Jakob CG, Upadhyay AK, Donner PL, Nicholl E, Addo SN, Qiu W, Ling C, Gopalakrishnan SM, Torrent M, Cepa SP, Shanley J, Shoemaker AR, Sun CC, Vasudevan A, Woller KR, Shotwell JB, Shaw B, Bian Z, Hutti JE. Jakob CG, et al. Among authors: upadhyay ak. J Med Chem. 2018 Aug 9;61(15):6647-6657. doi: 10.1021/acs.jmedchem.8b00305. Epub 2018 Jul 30. J Med Chem. 2018. PMID: 30004704
185 results