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Jian Jin

  • SENIOR FACULTY Structural and Chemical Biology
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  • B.S., University of Science and Technology of China

  • Ph.D., Pennsylvania State University
    Organic Chemistry

  • Postdoc, Ohio State University
    Organic Chemistry


    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. Over the last six years, Dr. Jin’s laboratory has focused on discovering chemical probes of protein methyltransferases and functionally selective ligands of G protein-coupled receptors. To date, Dr. Jin has published84 peer-reviewed papers (including 62 papers since 2008) and delivered more than 50 invited talks. He is also an inventor of 9 issued U.S. patents and 37 published PCT patent applications.


Discovery of Chemical Probes 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 chemical probes 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).

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 (AKA 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.


Ma A, Yu W, Xiong Y, Butler KV, Brown PJ, Jin J. Structure-activity Relationship Studies of SETD8 Inhibitors. MedChemComm 2014;: DOI: 10.1039/C4MD00317A.

Ma A, Yu W, Li F, Bleich RM, Herold JM, Butler KV, Norris JL, Korboukh V, Tripathy A, Janzen WP, Arrowsmith CH, Frye SV, Vedadi M, Brown PJ, Jin J. Discovery of a selective, substrate-competitive inhibitor of the lysine methyltransferase SETD8. Journal of medicinal chemistry 2014 Aug; 57(15).

Sundriyal S, Malmquist NA, Caron J, Blundell S, Liu F, Chen X, Srimongkolpithak N, Jin J, Charman SA, Scherf A, Fuchter MJ. Development of diaminoquinazoline histone lysine methyltransferase inhibitors as potent blood-stage antimalarial compounds. ChemMedChem 2014 Oct; 9(10).

Wright BD, Loo L, Street SE, Ma A, Taylor-Blake B, Stashko MA, Jin J, Janzen WP, Frye SV, Zylka MJ. The lipid kinase PIP5K1C regulates pain signaling and sensitization. Neuron 2014 May; 82(4).

Konze KD, Pattenden SG, Liu F, Barsyte-Lovejoy D, Li F, Simon JM, Davis IJ, Vedadi M, Jin J. A chemical tool for in vitro and in vivo precipitation of lysine methyltransferase G9a. ChemMedChem 2014 Mar; 9(3).

Lehnertz B, Pabst C, Su L, Miller M, Liu F, Yi L, Zhang R, Krosl J, Yung E, Kirschner J, Rosten P, Underhill TM, Jin J, Hébert J, Sauvageau G, Humphries RK, Rossi FM. The methyltransferase G9a regulates HoxA9-dependent transcription in AML. Genes & development 2014 Feb; 28(4).

Zhou B, Damrauer JS, Bailey ST, Hadzic T, Jeong Y, Clark K, Fan C, Murphy L, Lee CY, Troester MA, Miller CR, Jin J, Darr D, Perou CM, Levine RL, Diehn M, Kim WY. Erythropoietin promotes breast tumorigenesis through tumor-initiating cell self-renewal. The Journal of clinical investigation 2014 Feb; 124(2).

Industry Relationships

Physicians and scientists on the faculty of the Icahn School of Medicine at Mount Sinai often interact with pharmaceutical, device and biotechnology companies to improve patient care, develop new therapies and achieve scientific breakthroughs. In order to promote an ethical and transparent environment for conducting research, providing clinical care and teaching, Mount Sinai requires that salaried faculty inform the School of their relationships with such companies.

Dr. Jin did not report having any of the following types of financial relationships with industry during 2013 and/or 2014: consulting, scientific advisory board, industry-sponsored lectures, service on Board of Directors, participation on industry-sponsored committees, equity ownership valued at greater than 5% of a publicly traded company or any value in a privately held company. Please note that this information may differ from information posted on corporate sites due to timing or classification differences.

Mount Sinai's faculty policies relating to faculty collaboration with industry are posted on our website at Patients may wish to ask their physician about the activities they perform for companies.

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