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Page 1
Mutation of A677 in histone methyltransferase EZH2 in human B-cell lymphoma promotes hypertrimethylation of histone H3 on lysine 27 (H3K27).
McCabe MT, Graves AP, Ganji G, Diaz E, Halsey WS, Jiang Y, Smitheman KN, Ott HM, Pappalardi MB, Allen KE, Chen SB, Della Pietra A 3rd, Dul E, Hughes AM, Gilbert SA, Thrall SH, Tummino PJ, Kruger RG, Brandt M, Schwartz B, Creasy CL. McCabe MT, et al. Among authors: ott hm. Proc Natl Acad Sci U S A. 2012 Feb 21;109(8):2989-94. doi: 10.1073/pnas.1116418109. Epub 2012 Feb 8. Proc Natl Acad Sci U S A. 2012. PMID: 22323599 Free PMC article.
EZH2 inhibition as a therapeutic strategy for lymphoma with EZH2-activating mutations.
McCabe MT, Ott HM, Ganji G, Korenchuk S, Thompson C, Van Aller GS, Liu Y, Graves AP, Della Pietra A 3rd, Diaz E, LaFrance LV, Mellinger M, Duquenne C, Tian X, Kruger RG, McHugh CF, Brandt M, Miller WH, Dhanak D, Verma SK, Tummino PJ, Creasy CL. McCabe MT, et al. Among authors: ott hm. Nature. 2012 Dec 6;492(7427):108-12. doi: 10.1038/nature11606. Epub 2012 Oct 10. Nature. 2012. PMID: 23051747
Long residence time inhibition of EZH2 in activated polycomb repressive complex 2.
Van Aller GS, Pappalardi MB, Ott HM, Diaz E, Brandt M, Schwartz BJ, Miller WH, Dhanak D, McCabe MT, Verma SK, Creasy CL, Tummino PJ, Kruger RG. Van Aller GS, et al. Among authors: ott hm. ACS Chem Biol. 2014 Mar 21;9(3):622-9. doi: 10.1021/cb4008748. Epub 2013 Dec 31. ACS Chem Biol. 2014. PMID: 24304166
A687V EZH2 is a driver of histone H3 lysine 27 (H3K27) hypertrimethylation.
Ott HM, Graves AP, Pappalardi MB, Huddleston M, Halsey WS, Hughes AM, Groy A, Dul E, Jiang Y, Bai Y, Annan R, Verma SK, Knight SD, Kruger RG, Dhanak D, Schwartz B, Tummino PJ, Creasy CL, McCabe MT. Ott HM, et al. Mol Cancer Ther. 2014 Dec;13(12):3062-73. doi: 10.1158/1535-7163.MCT-13-0876. Epub 2014 Sep 24. Mol Cancer Ther. 2014. PMID: 25253781
Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2.
Verma SK, Tian X, LaFrance LV, Duquenne C, Suarez DP, Newlander KA, Romeril SP, Burgess JL, Grant SW, Brackley JA, Graves AP, Scherzer DA, Shu A, Thompson C, Ott HM, Aller GS, Machutta CA, Diaz E, Jiang Y, Johnson NW, Knight SD, Kruger RG, McCabe MT, Dhanak D, Tummino PJ, Creasy CL, Miller WH. Verma SK, et al. Among authors: ott hm. ACS Med Chem Lett. 2012 Oct 19;3(12):1091-6. doi: 10.1021/ml3003346. eCollection 2012 Dec 13. ACS Med Chem Lett. 2012. PMID: 24900432 Free PMC article.
EZH2 is required for germinal center formation and somatic EZH2 mutations promote lymphoid transformation.
Béguelin W, Popovic R, Teater M, Jiang Y, Bunting KL, Rosen M, Shen H, Yang SN, Wang L, Ezponda T, Martinez-Garcia E, Zhang H, Zheng Y, Verma SK, McCabe MT, Ott HM, Van Aller GS, Kruger RG, Liu Y, McHugh CF, Scott DW, Chung YR, Kelleher N, Shaknovich R, Creasy CL, Gascoyne RD, Wong KK, Cerchietti L, Levine RL, Abdel-Wahab O, Licht JD, Elemento O, Melnick AM. Béguelin W, et al. Among authors: ott hm. Cancer Cell. 2013 May 13;23(5):677-92. doi: 10.1016/j.ccr.2013.04.011. Cancer Cell. 2013. PMID: 23680150 Free PMC article.
Identification of a CARM1 Inhibitor with Potent In Vitro and In Vivo Activity in Preclinical Models of Multiple Myeloma.
Drew AE, Moradei O, Jacques SL, Rioux N, Boriack-Sjodin AP, Allain C, Scott MP, Jin L, Raimondi A, Handler JL, Ott HM, Kruger RG, McCabe MT, Sneeringer C, Riera T, Shapiro G, Waters NJ, Mitchell LH, Duncan KW, Moyer MP, Copeland RA, Smith J, Chesworth R, Ribich SA. Drew AE, et al. Among authors: ott hm. Sci Rep. 2017 Dec 21;7(1):17993. doi: 10.1038/s41598-017-18446-z. Sci Rep. 2017. PMID: 29269946 Free PMC article.
12 results