GSK3368715(又称EPZ019997)是口服活性、可逆的SAM非竞争性I型蛋白精氨酸甲基转移酶(PRMTs)抑制剂,抗癌活性强,对PRMT8(1.7nM)、PRMT1(3.1nM)、PRMT6(5.7nM)、PRMT3(48nM)、PRMT4(1148nM)均有抑制作用,能诱导精氨酸甲基化状态转变、改变外显子使用模式,可用于相关癌症研究。
[1] Fedoriw A, Rajapurkar SR, O'Brien S, Gerhart SV, Mitchell LH, Adams ND, Rioux N, Lingaraj T, Ribich SA, Pappalardi MB, Shah N, Laraio J, Liu Y, Butticello M, Carpenter CL, Creasy C, Korenchuk S, McCabe MT, McHugh CF, Nagarajan R, Wagner C, Zappacosta F, Annan R, Concha NO, Thomas RA, Hart TK, Smith JJ, Copeland RA, Moyer MP, Campbell J, Stickland K, Mills J, Jacques-O'Hagan S, Allain C, Johnston D, Raimondi A, Porter Scott M, Waters N, Swinger K, Boriack-Sjodin A, Riera T, Shapiro G, Chesworth R, Prinjha RK, Kruger RG, Barbash O, Mohammad HP. Anti-tumor Activity of the Type I PRMT Inhibitor, GSK3368715, Synergizes with PRMT5 Inhibition through MTAP Loss. Cancer Cell. 2019 Jul 8;36(1):100-114.e25. doi: 10.1016/j.ccell.2019.05.014. Epub 2019 Jun 27. PMID: 31257072.





