[7-31]Discovery of chemical probes for histone methyltransferases

报告题目：Discovery of chemical probes for histone methyltransferases

报 告 人：Prof. Jian Jin（Icahn School of Medicine at Mount Sinai ）

报告时间：2015年 7月31日（星期五）9：30 AM

报告地点：独墅湖校区二期云轩楼2301室

 Abstract

Mounting evidence suggests that post-translational modifications of histones play a critical role in diverse biological processes. Among the “writers”, “readers”, and “erasers” involved in chromatin regulation, histone methyltransferases (HMTs) have received great attention as a new class of potential therapeutic targets. Well-characterized chemical probes of HMTs will permit biological and disease hypotheses concerning these enzymes to be tested with high confidence in cell-based and/or animal models. To create high quality chemical probes of HMTs, my laboratory has pursued multiple complementary structure-based probe discovery approaches since 2008. Our discoveries of substrate-competitive inhibitors of G9a/GLP and SETD8, allosteric inhibitors of PRMT3, and cofactor-competitive inhibitors of EZH2/1 will be presented.

Introduction of the Speaker

Dr. Jian Jin received a B.S. degree in chemistry from University of Science and Technology of China in 1991 and a Ph.D. degree in synthetic organic chemistry from the Pennsylvania State University in 1997, and completed postdoctoral training at the Ohio State University. Dr. Jin joined GlaxoSmithKline as a medicinal chemist in 1998 and had been a manager of medicinal chemistry from 2003 to 2008. In 2008, Dr. Jin joined the Division of Chemical Biology and Medicinal Chemistry at the University of North Carolina at Chapel Hill as a faculty member and served as an associate director of medicinal chemistry in the Center for Integrative Chemical Biology and Drug Discovery. In 2014, Dr. Jin joined the Icahn School of Medicine at Mount Sinai as a Professor of Structural and Chemical Biology, Oncological Sciences, and Pharmacology and Systems Therapeutics. Since 2008, Dr. Jin’s laboratory has focused on discovering chemical probes of histone methyltransferases and functionally selective ligands of G protein-coupled receptors. To date, Dr. Jin has published 95 peer-reviewed papers and delivered 60 invited talks. He is also an inventor of 9 issued U.S. patents and 37 published PCT patent applications.