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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. Nat Commun. 2012;3:1288. doi: 10.1038/ncomms2304. Nat Commun. 2012. PMID: 23250418 Free article.
Bromo-deaza-SAH: a potent and selective DOT1L inhibitor.
Yu W, Smil D, Li F, Tempel W, Fedorov O, Nguyen KT, Bolshan Y, Al-Awar R, Knapp S, Arrowsmith CH, Vedadi M, Brown PJ, Schapira M. Yu W, et al. Bioorg Med Chem. 2013 Apr 1;21(7):1787-1794. doi: 10.1016/j.bmc.2013.01.049. Epub 2013 Jan 30. Bioorg Med Chem. 2013. PMID: 23433670 Free PMC article.
A scintillation proximity assay for histone demethylases.
Yu W, Eram MS, Hajian T, Szykowska A, Burgess-Brown N, Vedadi M, Brown PJ. Yu W, et al. Anal Biochem. 2014 Oct 15;463:54-60. doi: 10.1016/j.ab.2014.06.023. Epub 2014 Jul 8. Anal Biochem. 2014. PMID: 25010373
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: yu w. 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.
The dynamic conformational landscape of the protein methyltransferase SETD8.
Chen S, Wiewiora RP, Meng F, Babault N, Ma A, Yu W, Qian K, Hu H, Zou H, Wang J, Fan S, Blum G, Pittella-Silva F, Beauchamp KA, Tempel W, Jiang H, Chen K, Skene RJ, Zheng YG, Brown PJ, Jin J, Luo C, Chodera JD, Luo M. Chen S, et al. Among authors: yu w. Elife. 2019 May 13;8:e45403. doi: 10.7554/eLife.45403. Elife. 2019. PMID: 31081496 Free PMC article.
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