Hae Ju Han, Woong Sub Byun, Gyu Ho Lee, Won Kyung Kim, Kyungkuk Jang, Sehun Yang, Jewon Yang, Min Woo Ha, Suckchang Hong, Jeeyeon Lee, Jongheon Shin, Ki Bong Oh, Sang Kook Lee, Hyeung-Geun Park
Disruptor of telomeric silencing-1 like (DOT1L) is a histone H3 methyltransferase which specifically catalyzes the methylation of histone H3 lysine-79 residue. Recent findings demonstrate that DOT1L is abnormally overexpressed and the upregulated DOT1L evokes the proliferation and metastasis in human breast cancer cells. Therefore, the DOT1L inhibitor is considered a promising strategy to treat breast cancers. Non-nucleoside DOT1L inhibitors, selenopsammaplin A and its analogues, were firstly reported in the present study...
February 11, 2021: Bioorganic & Medicinal Chemistry