Jian Jin, PhD
- PROFESSOR | Pharmacological Sciences
- PROFESSOR | Oncological Sciences
Research Topics:Cancer, Chromatin, Drug Design and Discovery, Epigenetics, Membrane Proteins/Channels, Neuroscience, Structural Biology
Jian Jin, PhD, is the Mount Sinai Endowed Professor in Therapeutics Discovery, Director of the Mount Sinai Center for Therapeutics Discovery, and Co-Leader of the Cancer Clinical Investigation Program at The Tisch Cancer Institute.
Dr. Jin is an internationally recognized medicinal chemist with more than 20 years of experience in small-molecule drug discovery. His laboratory is a leader in developing novel small-molecule degraders using heterobifunctional technologies including the proteolysis targeting chimera (PROTAC) technology. Since 2014, Dr. Jin’s lab has generated numerous first-in-class degraders targeting oncogenic proteins and studied their anti-tumor activities. For example, they discovered first-in-class degraders of the lysine methyltransferase EZH2, a key oncogenic driver for breast cancer, prostate cancer, lymphoma, leukemia and several other cancers. Dr. Jin is an inventor of more than 50 U.S. patents and published international patent applications. As the Director of the Mount Sinai Center for Therapeutics Discovery, he leads Mount Sinai’s research effort on discovering innovative small-molecule therapeutics for the treatment of human diseases including cancer.
Dr. Jin has mentored more than 25 MD/PhD and PhD students and postdoctoral fellows in his lab. He has served as co-director of the Multidisciplinary Training Area in Pharmacology and Therapeutics Discovery for the Graduate School of biomedical sciences at Mount Sinai.
Dr. Jian Jin received a Bachelor of Science degree in chemistry from the University of Science and Technology of China in 1991 and a PhD in organic chemistry from the Pennsylvania State University in 1997. After completing post-doctoral training at the Ohio State University, Dr. Jin joined GlaxoSmithKline as a medicinal chemist. In 2008, he joined the Division of Chemical Biology and Medicinal Chemistry at the University of North Carolina at Chapel Hill as an associate professor; he also served as Associate Director of Medicinal Chemistry in the Center for Integrative Chemical Biology and Drug Discovery. Dr. Jin was recruited to the Icahn School of Medicine at Mount Sinai as a professor with tenure in 2014.
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).