NSC636819通过竞争性结合 H3K9me3,选择性抑制 KDM4A/KDM4B 的去甲基活性。作为一种竞争性抑制剂,它有望用于研究由 KDM4A/KDM4B 驱动的癌症,特别是前列腺癌。
[1] Chu CH, Wang LY, Hsu KC, Chen CC, Cheng HH, Wang SM, Wu CM, Chen TJ, Li LT, Liu R, Hung CL, Yang JM, Kung HJ, Wang WC. KDM4B as a target for prostate cancer: structural analysis and selective inhibition by a novel inhibitor. J Med Chem. 2014 Jul 24;57(14):5975-85. doi: 10.1021/jm500249n. Epub 2014 Jul 9. PMID: 24971742; PMCID: PMC4216216.[2]Wang J, Wang H, Wang LY, Cai D, Duan Z, Zhang Y, Chen P, Zou JX, Xu J, Chen X, Kung HJ, Chen HW. Silencing the epigenetic silencer KDM4A for TRAIL and DR5 simultaneous induction and antitumor therapy. Cell Death Differ. 2016 Nov 1;23(11):1886-1896. doi: 10.1038/cdd.2016.92. Epub 2016 Sep 9. PMID: 27612013; PMCID: PMC5071577.





