Jian Jin, PhD
- PROFESSOR | Oncological Sciences
- PROFESSOR | Pharmacological Sciences
Research Topics:Cancer, Chromatin, Drug Design and Discovery, Membrane Proteins/Channels, Schizophrenia
Dr. Jian Jin is a world-renowned medicinal chemist with more than 20 years of experience in small-molecule drug discovery. He is currently the Mount Sinai Endowed Professor in Therapeutics Discovery, a Professor in Department of Pharmacological Sciences, a Professor in Department of Oncological Sciences, and the Director of the Mount Sinai Center for Therapeutics Discovery at Icahn School of Medicine at Mount Sinai. Dr. Jin’s laboratory is a leader in discovering selective inhibitors of histone methyltransferases and biased ligands of G protein-coupled receptors, and a pioneer in developing novel degraders targeting oncogenic proteins.Dr. Jian Jin received a Bachelor’s of Science degree in chemistry from University of Science and Technology of China in 1991 and a PhD in organic chemistry from the Pennsylvania State University in 1997. After completing a post-doctoral 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 (UNC) as an Associate Professor. He had also served as an Associate Director of Medicinal Chemistry in the Center for Integrative Chemical Biology and Drug Discovery at UNC from 2008 to 2014. Dr. Jin was recruited to Icahn School of Medicine at Mount Sinai as a professor with tenure in 2014. Dr. Jin has published well over 100 peer-reviewed original research papers and delivered >100 invited talks. He is also an inventor of 10 granted U.S. patents and 40 published PCT patent applications.
Multi-Disciplinary Training AreaPharmacology and Therapeutics Discovery [PTD]
BS, University of Science and Technology of China
PhD, Pennsylvania State University
Postdoc, Ohio State University
Discovery of Functionally Selective Ligands of GPCRs
G protein-coupled receptors (GPCRs) signal not only via canonical pathways involving heterotrimeric large G proteins, but also via non-canonical G protein-independent interactions with other signaling proteins including beta-arrestins. The process by which GPCR ligands differentially modulate canonical and non-canonical signal transduction pathways is a phenomenon known as “functional selectivity” (also knows as signaling bias). Such functionally selective ligands (also known as biased ligands) preferentially engage either canonical or non-canonical GPCR pathways. The discovery of ligands with discrete functional selectivity profiles will be extremely useful for elucidating the key signal transduction pathways essential for both the therapeutic actions and side-effects of drugs. The Jin lab has been actively engaged in generating functionally selective ligands of GPCRs.
Discovery of Selective Inhibitors for Histone Methyltransferases
Post-translational modifications (PTMs) of histones play a critical role in diverse biological processes including chromatin compaction, gene expression, transcriptional regulation, and cell differentiation. Among a myriad of PTMs, histone methylation catalyzed by histone methyltransferases (HMTs) has been increasingly recognized as a major signaling mechanism in eukaryotic cells. HMTs are divided into two categories: lysine methyltransferases (PKMTs) and arginine methyltransferases (PRMTs), More than 50 PKMTs and 9 PRMTs have been identified. Mounting evidence suggests that HMTs play crucial roles in various human diseases. To create high quality selective inhibitors of HMTs, the Jin lab has taken a systematic approach by targeting the HMT substrate binding groove, cofactor binding site, and potential allosteric binding site(s).