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Dr. Jian Jin is currently the Mount Sinai Endowed Professor in Therapeutics Discovery and Director of the Mount Sinai Center for Therapeutics Discovery at Icahn School of Medicine at Mount Sinai (Mount Sinai). He is also a tenured professor in Departments of Pharmacological Sciences, Oncological Sciences and Neuroscience, and a Co-Leader of the Cancer Clinical Investigation Program at The Tisch Cancer Institute at Mount Sinai. Dr. Jin is an internationally recognized medicinal chemist and chemical biologist with more than 20 years of experience in small-molecule drug discovery. His laboratory is a leader in discovering selective inhibitors of histone methyltransferases, biased ligands of G protein-coupled receptors, and novel degraders targeting oncogenic proteins. Dr. Jin has published more than 200 peer-reviewed papers and delivered >100 invited talks. He is also an inventor of >60 issued U.S. patents and published international patent applications. Dr. Jin received a Bachelor’s 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 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 Mount Sinai as a professor with tenure in 2014.


Discovery of Selective Inhibitors for Histone Methyltransferases Histone methyltransferases (HMTs, also known as protein methyltransferases (PMTs)) play critical roles in various human diseases including cancer. The Jin lab has taken a systematic approach to target HMTs for over a decade. By targeting the HMT substrate binding groove, cofactor binding site, and allosteric binding sites, the Jin lab has discovered numerous high quality selective inhibitors of HMTs, which have been widely used by the scientific community. Discovery of Biased Ligands for G Protein-coupled Receptors 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. Biased ligands of GPCRs preferentially engage either canonical or non-canonical signaling pathways and are extremely useful tools for elucidating the signal transduction pathways essential for both therapeutic actions and side-effects. The Jin lab has been actively engaged in discovering biased ligands of GPCRs for more than a decade. Discovery of Novel Degraders Targeting Oncogenic Proteins The Jin lab is a leader in developing novel degraders targeting oncogenic proteins. Since 2014, the lab has discovered a number of first-in-class degraders using the PROTAC (proteolysis targeting chimera) and hydrophobic tagging technologies. Our degrader program has resulted in multiple patent applications filed by Mount Sinai.


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Zhang, S.; Chen, H.; Zhang, C.; Yang, Y.; Popov, P.; Liu, J.; Krumm, B. E.; Cao, C.; Kim, K.; Xiong, Y.; Katritch, V.; Shoichet, B. K.; Jin, J.; Fay, J. F.*; Roth, B. L.*; Inactive and active state structures template selective tools for the human 5-HT5A receptor. Nat Struct Mol Biol. 2022, 29(7), 677-687. PMID: 35835867 Meng, F.; Xu, C.; Park, K. S.; Kaniskan, H. U.*; Wang, G. G.* Jin, J.*; Discovery of a First-in-Class Degrader for Nuclear Receptor Binding SET Domain Protein 2 (NSD2) and Ikaros/Aiolos. J. Med. Chem. 2022 Montanaro, A.; Kitara, S.; Cerretani, E.; Marchesini. M.; Rompietti, C.; Pagliaro, L.; Gherli, A.; Su, A.; Minchillo, M. L.; Caputi, M.; Fioretzaki, R.; Lorusso, B.; Ross, L.; Alexe, G.; Masselli, E.; Marozzi, M.; Rizzi, F. M. A.; La Starza, R.; Mecucci, C.; Xiong, Y.; Jin, J.; Falco, A.; Knoechel, B.; Aversa, F.; Candini, O.; Quaini, F.; Sportoletti, P.; Stegmaier, K.; Roti, G.*; Identification of an Epi-metabolic dependency on EHMT2/G9a in T-cell acute lymphoblastic leukemia. Cell Death Dis. 2022, 13(6), 551. PMID: 35710782 Park, K. S.; Xiong, Y.*; Yim, H.; Velez, J.; Babault, N.; Kumar, P.; Liu, J.; Jin, J.*; Discovery of the First-in-Class G9a/GLP Covalent Inhibitors. J. Med. Chem. 2022, Epub ahead of print. PMID: 35763668. Liu, J.; Yu, X.; Chen, H.; Kaniskan H. Ü.; Xie, L.; Chen, X.; Jin, J*.; Wei, W*.; TF-DUBTACs Stabilize Tumor Suppressor Transcription Factors. J. Am. Chem. Soc. 2022, Epub ahead of print. PMID: 35786952. Dale, B.; Anderson, C.; Park, K. S.; Kaniskan H. U.; Ma, A.; Shen Y.; Zhang, C.; Xie, L.; Chen, X.; Yu, X.*; Jin, J.*; Targeting Triple-Negative Breast Cancer by a Novel Proteolysis Targeting Chimera Degrader of Enhancer of Zeste Homolog 2, ACS Pharmacol. Transl. Sci. 2022, 5, 7, 491–507 Yu, X.; Cheng, M.; Lu, K.; Shen, Y.; Zhong, Y.; Liu, J.; Xiong, Y.; Jin, J.*; Exploring Degradation of Mutant and Wild-Type Epidermal Growth Factor Receptors Induced by Proteolysis-Targeting Chimeras. J. Med. Chem. 2022, 65(12), 8416-8443. PMID: 35675209. Wu, Q.; Nie, D. Y.; Ba-Alawi, W.; Ji, Y.; Zhang, Z.; Cruickshank, J.; Haight J.; Ciamponi F. E.; Chen, J.; Duan, S.; Shen, Y.; Liu, J.; Marhon, S. A..; Mehdipour, P.; Szewczyk, M. M.; Dogan-Artun, N.; Chen, W.; Zhang, L. X.; Deblois, G.; Prinos, P.; Massirer, K. B.; Barsyte-Lovejoy, D.; Jin, J.; De Carvalho, D. D.; Haibe-Kains, B.; Wang, X.; Cescon, D. W.; Lupien, M.*.; Arrowsmith, C .H.*. PRMT inhibition induces a viral mimicry response in triple-negative breast cancer. Nat. Chem. Biol. 2022, Epub ahead of print. PMID: 35578032. Li, D.; Yu, X.; Kottur, J.; Gong, W.; Zhang, Z.; Storey, A. J.; Tsai, Y. H.; Uryu, H.; Shen, Y.; Byrum, S. D.; Edmondson, R. D.; Mackintosh, S. G.; Cai, L.; Liu, Z.; Aggarwal, A. K.; Tackett, A. J.; Liu, J.; Jin, J.*; Wang, G. G.* Discovery of a dual WDR5 and Ikaros PROTAC degrader as an anti-cancer therapeutic. Oncogene. 2022, Epub ahead of print. PMID: 35525905. Xu, C.; Meng, F.; Park, K. S.; Storey, A. J.; Gong, W.; Tsai, Y. H.; Gibson, E.; Byrum, S. D.; Li, D.; Edmondson, R. D.; Mackintosh, S. G.; Vedadi, M.; Cai, L.; Tackett, A. J.; Kaniskan, H. U.; Jin, J.*; Wang, G. G.* A NSD3-targeted PROTAC suppresses NSD3 and cMyc oncogenic nodes in cancer cells. Cell Chem. Biol. 2022, 29, 386-397.e9. PMID: 34469831. Ren, Z.; Kim, A.; Huang, Y. T.; Pi, W. C.; Gong, W.; Yu, X.; Qi, J.; Jin, J.; Cai, L.; Roeder, R. G.; Chen, W. Y.; Wang, G. G. A PRC2-Kdm5b axis sustains tumorigenicity of acute myeloid leukemia. Proc. Natl. Acad. Sci. U S A 2022, 119, e2122940119. Wang, J.; Yu, X.; Gong, W.; Liu, X.; Park, K.-S.; Ma, A.; Tsai, Y.-H.; Shen, Y.; Onikubo, T.; Pi, W.-C.; Allison, D. F.; Liu, J.; Chen, W.-Y.; Cai, L.; Roeder, R. G.; Jin, J.*; Wang, G. G.* EZH2 noncanonically binds cMyc and p300 through a cryptic transactivation domain to mediate gene activation and promote oncogenesis. Nature Cell Biology 2022, 24, 384-399. PMID: 35210568 Esposito, D.; Pant, I.; Shen, Y.; Qiao, R. F.; Yang, X.; Bai, Y.; Jin, J.; Poulikakos, P. I.; Aaronson, S. A. ROCK1 mechano-signaling dependency of human malignancies driven by TEAD/YAP activation. Nat Commun 2022, 13, 703. PMID: 35121738. Yu, X.; Xu, J.; Shen, Y.; Cahuzac, K.; Park, K.; Dale, B.; Liu, J.*; Parsons, R.*; Jin, J.* Discovery of potent, selective, and in vivo efficacious AKT kinase protein degraders via structure-activity relationship studies. J. Med. Chem. 2022, 65, 3644-3666. PMID: 35119851 Yu, X.; Xu, J.; Xie, L.; Wang, L.; Shen, Y.; Cahuzac, K.; Chen, X.; Liu, J.*; Parsons, R.*; Jin, J.* Design, Synthesis and Evaluation of Potent, Selective and Bioavailable AKT Kinase Degraders. J. Med. Chem. 2021, 64, 18054-18081. PMID: 34855399. Yang, X.; Wang, X.; Li, Z.; Duan, S.; Li, H.; Jin, J.; Zhang, Z.; Gu, W., An unexpected role for Dicer as a reader of the unacetylated DNA binding domain of p53 in transcriptional regulation. Sci. Adv. 2021, 7, eabi6684. PMID: 34705508, PMCID: PMC8550248. Kusakabe, Y.; Chiba, T.; Oshima, M.; Koide, S.; Rizq, O.; Aoyama, K.; Ao, J.; Kaneko, T.; Kanzaki, H.; Kanayama, K.; Maeda, T.; Saito, T.; Nakagawa, R.; Kobayashi, K.; Kiyono, S.; Nakamura, M.; Ogasawara, S.; Suzuki, E.; Nakamoto, S.; Yasui, S.; Mikata, R.; Muroyama, R.; Kanda, T.; Maruyama, H.; Kato, J.; Mimura, N.; Ma, A.; Jin, J.; Zen, Y.; Otsuka, M.; Kaneda, A.; Iwama, A.; Kato, N., EZH1/2 inhibition augments the anti-tumor effects of sorafenib in hepatocellular carcinoma. Sci. Rep. 2021, 11, 21396. PMID: 34725436, PMCID: PMC8560765. Herviou, L.; Ovejero, S.; Izard, F.; Karmous-Gadacha, O.; Gourzones, C.; Bellanger, C.; De Smedt, E.; Ma, A.; Vincent, L.; Cartron, G.; Jin, J.; De Bruyne, E.; Grimaud, C.; Julien, E.; Moreaux, J., Targeting the methyltransferase SETD8 impairs tumor cell survival and overcomes drug resistance independently of p53 status in multiple myeloma. Clinical Epigenetics 2021, 13, 174. PMID:34530900, PMCID: PMC8447659. Liu, L.; Dattaroy, D.; Simpson, K. F.; Barella, L. F.; Cui, Y.; Xiong, Y.; Jin, J.; Konig, G. M.; Kostenis, E.; Roman, J. C.; Kaestner, K. H.; Doliba, N. M.; Wess, J., Gq signaling in alpha cells is critical for maintaining euglycemia. JCI Insight 2021, 6, e152852. PMID: 34752420. Cao, C.; Kang, H. J.; Singh, I.; Chen, H.; Zhang, C.; Ye, W.; Hayes, B. W.; Liu, J.; Gumpper, R. H.; Bender, B. J.; Slocum, S. T.; Krumm, B. E.; Lansu, K.; McCorvy, J. D.; Kroeze, W. K.; English, J. G.; DiBerto, J. F.; Olsen, R. H. J.; Huang, X. P.; Zhang, S.; Liu, Y.; Kim, K.; Karpiak, J.; Jan, L. Y.; Abraham, S. N.; Jin, J.; Shoichet, B. K.; Fay, J. F.; Roth, B. L., Structure, function and pharmacology of human itch GPCRs. Nature 2021, 600, 170-175. PMID: 34789874.