Jin, Jian - Icahn School of Medicine at Mount Sinai -

个人简介

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 >25 years of experience in small-molecule drug discovery. His laboratory is a leader in discovering novel degraders targeting oncoproteins, selective inhibitors of histone methyltransferases, and biased ligands of G protein-coupled receptors. Dr. Jin has published >250 peer-reviewed papers and delivered >100 invited talks. He is also an inventor of >80 issued U.S. patents and published international patent applications. In particular, Dr. Jin is one of several inventors of Daprodustat, a hypoxia-inducible factor (HIF) prolyl hydroxylase small-molecule inhibitor, which has been approved in the U.S. and Japan as an oral medication for the treatment of anemia caused by chronic kidney disease. Dr. Jin has been inducted to the National Academy of Inventors (NAI) as an NAI Fellow. 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.

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Hu,X; Kabir, M; Lin, Y; Xiong Y; Parsons, R; Gu, W; Jin, J*. “Design, Synthesis, and Evaluation of p53Y220C Acetylation Targeting Chimeras (AceTACs)”, Journal of Medicinal Chemistry, August, 2024. Hu,X; Kabir, M; Lin, Y; Xiong Y; Parsons, R; Gu, W; Jin, J*“Design, Synthesis, and Evaluation of p53Y220C Acetylation Targeting Chimeras (AceTACs)”, Journal of Medicinal Chemistry, August, 2024. Wang, S, E.; Xiong, Y.; Jang, M, A,; Park, K, S.; Donahue, M.; Velez J.; Jin J.*; Jiang, Y, H.*, “Newly developed oral bioavailable EHMT2 inhibitor as a potential epigenetic therapy for Prader-Willi syndrome”, Molecular Therapy, 2024, doi: 10.1016/j.ymthe.2024.05.034. Kabir, M.; Qin, L.; Luo, K.; Xiong, Y.; Sidi, R. A.; Park, K.-S.*; Jin, J.*, Discovery and characterization of a novel Cereblon-recruiting PRC1 bridged PROTAC degrader. Journal of Medicinal Chemistry. 2024, 67:6880-6892. PMID: 38607318. Nigam, A. K.; Hurley, M. F. D.; Lid, F.; Konkoľováe, E.; Klímae, M.; Trylčováe, J.; Pollice, R.; Çinaroǧluh, S. S.; Levin-Konigsbergb, R.; Handjayafg, J.; Schapiradi, M.; Chaud, R.; Perveen, S.; Ho-Leung Ng, H.; Kaniskan, Ü.; Hank, Y.; Singhl, S.; Gorgullamno, C.; Kundajeab, A.; Jin, J.; Voelz, V. A.; Webere, J.; Nenckae, R.; Bourae, E.; Vedadi, M.*; Aspuru-Guzik, A.* “Application of established computational techniques to identify potential SARS-CoV-2 Nsp14-MTase inhibitors in low data regimes.” Digital Discovery, 2024, doi: 1039/D4DD00006D. Velez, J.; Han, Y.; Yim, H.; Yang, P.; Deng, Z.; Park, K.-s.; Kabir, M.; Kaniskan, H. Ü.; Xiong, Y.*; Jin, J.*, Discovery of the first-in-class G9a/GLP PROTAC degrader. Journal of Medicinal Chemistry. 2024, 67(8):6397-6409. PMID: 38607318. Kim, Y.; Gumpper, R. H.; Liu, Y.; Kocak, D. D.; Xiong, Y.; Cao, C.; Deng, Z.; Krumm, B. E.; Jain, M. K.; Zhang, S.; Jin, J.; Roth, B. L., Bitter taste receptor activation by cholesterol and an intracellular tastant. Nature 2024, 628(8008):664-671. PMID: 38600377. Liu, J.; Hu, X.; Luo, K.; Xiong, Y.; Chen, L.; Wang, Z.; Inuzuka, H.; Qian, C.; Yu, X.; Xie, L.; Muneer, A.; Zhang, D.; Paulo, J. A.; Chen, X.; Jin, J.*; Wei, W.*, USP7-based deubiquitinase-targeting chimeras stabilize AMPK. Journal of the American Chemical Society. 2024 Apr 10; PMID: 38597345. Xiong, Y.; Greschik, H.; Johansson, C.; Seifert, L.; Gamble, V.; Park, K.-s.; Fagan, V.; Li, F.; Chau, I.; Vedadi, M.; Arrowsmith, C. H.; Brennan, P.; Fedorov, O.; Jung, M.; Farnie, G.; Liu, J.; Oppermann, U. *; Schüle, R. *; Jin, J. *, Discovery of a potent, selective, and cell-active SPIN1 inhibitor. Journal of Medicinal Chemistry. 2024, 67(7):5837-5853. PMID: 38533580. Nylund, P.; Garrido-Zabala, B.; Párraga, A. A.; Vasquez, L.; Pyl, P. T.; Harinck, G. M.; Ma, A.; Jin, J.; Öberg, F.; Kalushkova, A.; Wiklund, H. J.*, PVT1 interacts with polycomb repressive complex 2 to suppress genomic regions with pro-apoptotic and tumour suppressor functions in multiple myeloma. Haematologica 2024, 109 (2): 567-577. PMID: 37496441. Wang, Z.; Zhang, D.; Qiu, X.; Inuzuka, H.; Xiong, Y.; Liu, J.; Chen, L.; Chen, H.; Xie, L.; Kaniskan, H. Ü.; Chen, X.; Jin, J. *; Wei, W. *, Structurally specific Z-DNA proteolysis targeting chimera enables targeted degradation of adenosine deaminase acting on RNA. Journal of the American Chemical Society. 2024, 146 (11): 7584-7593. PMID: 38469801. Velez, J.; Dale, B.; Park, K.-S.; Kaniskan, H. Ü.; Yu, X. *; Jin, J. *, Discovery of a novel, highly potent EZH2 PROTAC degrader for targeting non-canonical oncogenic functions of EZH2. European Journal of Medicinal Chemistry. 2024, 267, 116154. PMID: 38295690. Dang, F.; Bai, L.; Dong, J.; Hu, X.; Wang, J.; Paulo, J. A.; Xiong, Y.; Liang, X.; Sun, Y.; Chen, Y.; Guo, M.; Wang, X.; Huang, Z.; Inuzuka, H.; Chen, L.; Chu, C.; Liu, J.; Zhang, T.; Rezaeian, A.-H.; Liu, J.; Kaniskan, H. Ü.; Zhong, B.; Zhang, J.; Letko, M.; Jin, J. *; Lan, K. *; Wei, W. *, USP2 inhibition prevents infection with ACE2-dependent coronaviruses in vitro and is protective against SARS-CoV-2 in mice. Science Translational Medicine. 2023, 15 (725): eadh7668. PMID: 38055802. Yu, X.; Li, D.; Kottur, J.; Kim, H. S.; Herring, L. E.; Yu, Y.; Xie, L.; Hu, X.; Chen, X.; Cai, L.; Liu, J.; Aggarwal, A. K.; Wang, G. G. *; Jin, J.*, Discovery of Potent and Selective WDR5 Proteolysis Targeting Chimeras as Potential Therapeutics for Pancreatic Cancer. Journal of Medicinal Chemistry. 2023, 66(23): 16168–16186. PMID: 38019706. Umaña, J.D.; Wasserman S.R.; Song L.; Goel A.A.; Yu X.; Jin J.; Hathaway N.A. *, Chemical Epigenetic Regulation of Adeno-Associated Virus Delivered Transgenes. Human Gene Therapy. 2023, 34(17-18): 947-957. PMID: 37624737. Pogorelov, V. M. *; Martini, M. L.; Jin, J.; Wetsel, W. C.;* Caron, M. G., Dopamine-Depleted Dopamine Transporter Knockout (DDD) Mice: Dyskinesia with L-DOPA and Dopamine D1 Agonists. Biomolecules, 2023, 13(11): 1658. PMID: 38002340. Muneer, A.; Wang, L.; Xie, L.; Zhang, F.; Wu, B.; Mei, L.; Lenarcic, E. M.; Feng, E. H.; Song, J.; Xiong, Y.; Yu, X.; Wang, C.; Jain, K.; Strahl, B.; Cook, J. G.; Wan, Y. Y.; Moorman, N. J.; Song, H.; Jin, J.; Chen, X. *, Non-canonical function of histone methyltransferase G9a in the translational regulation of chronic inflammation. Cell Chemical Biology, 2023, 30(12):1525-1541.e7. PMID: 37858336. Gray, Z. H.; Chakraborty, D.; Duttweiler, R. R.; Alekbaeva, G. D.; Murphy, S. E.; Chetal, K.; Ji, F.; Ferman, B. I.; Honer, M. A.; Wang, Z.; Myers, C.; Sun, R.; Kaniskan, H. Ü.; Toma, M. M.; Bondarenko, E. A.; Santoro, J. N.; Miranda, C.; Dillingham, M. E.; Tang, R.; Gozani, O.; Jin, J.; Skorski, T.; Duy, C.; Lee, H.; Sadreyev, R. I.; Whetstine, J. R.*, Epigenetic balance ensures mechanistic control of MLL amplification and rearrangement. Cell, 2023, 186(21):4528-4545.e18. PMID: 37788669. Wang Z.; Liu J.; Qiu X.; Zhang D.; Inuzuka H.; Chen L.; Chen H.; Xie L.; Kaniskan HÜ.; Chen X.; Jin J.* ; Wei W.* , Methylated Nucleotide-Based Proteolysis-Targeting Chimera Enables Targeted Degradation of Methyl-CpG-Binding Protein 2. J Am Chem Soc. 2023, 145(40): 21871–21878. PMID: 37774414. Salas-Estrada, L.; Provasi, D.; Qiu, X.; Kaniskan, H. Ü.; Huang, X. P.; DiBerto, J. F.; Lamim Ribeiro, J. M.; Jin, J.; Roth, B. L.; Filizola, M.; De Novo Design of κ-Opioid Receptor Antagonists Using a Generative Deep-Learning Framework. Journal of Chemical Information and Modeling, 63(16): 5056–5065. PMID: 37555591. Rialdi, A.; Duffy, M.; Scopton, A. P.; Fonseca, F.; Zhao, J. N.; Schwarz, M.; Molina-Sanchez, P.; Mzoughi, S.; Arceci, E.; Abril-Fornaguera, J.; Meadows, A.; Ruiz de Galarreta, M.; Torre, D.; Reyes, K.; Lim, Y. T.; Rosemann, F.; Khan, Z. M.; Mohammed, K.; Wang, X.; Yu, X.; Jin, J.; Guccione, E; Dar, A. C.; WNTinib is a multi-kinase inhibitor with specificity against β-catenin mutant hepatocellular carcinoma. Nature cancer, 2023, 4(8):1157-1175. PMID: 37537299. Gao, J.; Yang, L.; Lei, S.; Zhou, F.; Nie, H.; Peng, B.; Xu, T.; Chen, X.; Yang, X.; Sheng, C.; Rao, Y.; Pu, K.; Jin, J.; Xu, Z.; Yu, H.; Stimuli-activatable PROTACs for precise protein degradation and cancer therapy. Science bulletin, 2023, 68(10): 1069–1085. PMID: 37169612. Kabir, M.; Sun, N.; Hu, X.; Martin, T. C.; Yi, J.; Zhong, Y.; Xiong, Y.; Kaniskan, H. Ü.; Gu, W.; Parsons, R.; Jin, J.*; Acetylation Targeting Chimera Enables Acetylation of the Tumor Suppressor p53. J Am Chem Soc, 2023, 145(27):14932-14944. PMID: 37365684. Velez, J.; Kaniskan, H. Ü.*; Jin, J.*; Recent advances in developing degraders & inhibitors of lysine methyltransferases. Current Opinion in Chemical Biology, 2023, 76:102356. PMID: 37379717. Schwalm, M. P.; Krämer, A.; Dölle, A.; Weckesser, J.; Yu, X.; Jin, J.; Saxena, K.; Knapp, S.; Tracking the PROTAC degradation pathway in living cells highlights the importance of ternary complex measurement for PROTAC optimization. Cell Chemical Biology, 2023, 30(7):753-765.e8. PMID: 37354907. Kabir, M.; Yu, X.; Kaniskan, H. Ü.*; Jin, J.*; Chemically induced degradation of epigenetic targets. Chemical Society Reviews, 2023, 52(13):4313-4342. PMID: 37314393. Zhao, N.; Ho, J. S. Y.; Meng, F.; Zheng, S.; Kurland, A. P.; Tian, L.; Rea-Moreno, M.; Song, X.; Seo, J. S.; Kaniskan, H. Ü.; Te Velthuis, A. J. W.; Tortorella, D.; Chen, Y. W.; Johnson, J. R.; Jin, J.*; Marazzi, I.*; Generation of host-directed and virus-specific antivirals using targeted protein degradation promoted by small molecules and viral RNA mimics. Cell Host Microbe, 2023, 31(7):1154-1169.e10. PMID: 37339625. Yi, J.; Li, H.; Chu, B.; Kon, N.; Hu, X.; Hu, J.; Xiong, Y.; Kaniskan, H. U.; Jin, J.; Gu, W*; Inhibition of USP7 induces p53-independent tumor growth suppression in triple-negative breast cancers by destabilizing FOXM1. Cell Death & Differentiation, 2023, 30(7):1799-1810. PMID: 37291217. Singh, I.; Li, F.; Fink, E. A.; Chau, I.; Li, A.; Rodriguez-Hernández, A.; Glenn, I.; Zapatero-Belinchón, F. J.; Rodriguez, M. L.; Devkota, K.; Deng, Z.; White, K.; Wan, X.; Tolmachova, N. A.; Moroz, Y. S.; Kaniskan, H. Ü.; Ott, M.; García-Sastre, A.; Jin, J.; Fujimori, D. G.; … Shoichet, B. K.*; Structure-Based Discovery of Inhibitors of the SARS-CoV-2 Nsp14 N7-Methyltransferase. J. Med. Chem, 2023, 66(12):7785-7803. PMID: 37294077. Wang, Z.; Liu, J.; Chen, H.; Qiu, X.; Xie, L.; Kaniskan, H. Ü.; Chen, X.; Jin, J.*; Wei, W.*; Telomere Targeting Chimera Enables Targeted Destruction of Telomeric Repeat-Binding Factor Proteins. Journal of Medicinal Chemistry. 2023, 145(19):10872-10879. PMID: 37141574. Qiang, N.; Ao, J.; Nakamura, M.*; Chiba, T.; Kusakabe, Y.; Kaneko, T.; Kurosugi, A.; Kogure, T.; Ma, Y.; Zhang, J.; Ogawa, K.; Kan, M.; Iwanaga, T.; Sakuma, T.; Kanayama, K.; Kanzaki, H.; Kojima, R.; Nakagawa, R.; Kondo, T.; Nakamoto, S.; … Jin, J.; Kato, N.; Alteration of the tumor microenvironment by pharmacological inhibition of EZH2 in hepatocellular carcinoma. Int immunopharmacol. 2023, 118:110068. PMID: 37001386. Vital, T.; Wali, A.; Butler, K. V.; Xiong, Y.; Foster, J. P.; Marcel, S. S.; McFadden, A. W.; Nguyen, V. U.; Bailey, B. M.; Lamb, K. N.; James, L. I.; Frye, S. V.; Mosely, A. L.; Jin, J.; Pattenden, S. G.; Davis, I. J.*; MS0621, a novel small-molecule modulator of Ewing sarcoma chromatin accessibility, interacts with an RNA-associated macromolecular complex and influences RNA splicing. Frontiers in Oncology, 2023, 13:1099550. PMID: 36793594. Yu, X.; Wang, J.; Gong, W.; Ma, A.; Shen, Y.; Zhang, C.; Liu, X.; Cai, L.; Liu, J.; Wang, G. G.*; Jin, J.*; Dissecting and targeting noncanonical functions of EZH2 in multiple myeloma via an EZH2 degrader. Oncogene, 2023, 42(13):994-1009. PMID: 36747009. Park, K. S.; Qin, L.; Kabir, M.; Luo, K.; Dale, B.; Zhong, Y.; Kim, A.; Wang, G. G.; Kaniskan, H. Ü.; Jin, J*; Targeted Degradation of PRC1 Components, BMI1 and RING1B, via a Novel Protein Complex Degrader Strategy. Advanced science (Weinheim, Baden-Württemberg, Germany). 2023, 10(10):e2205573. PMID: 36737841. Sun, N.; Kabir, M.; Lee, Y.; Xie, L.; Hu, X.; Velez, J.; Chen, X.; Kaniskan, H. Ü.*; & Jin, J*; Discovery of the First Lactate Dehydrogenase Proteolysis Targeting Chimera Degrader for the Treatment of Pancreatic Cancer. Journal of Medicinal Chemistry. 2023, 66(1):596-610. PMID: 36538511. Marcellino, B. K.; Yang, X.; Ümit Kaniskan, H.; Brady, C.; Chen, H.; Chen, K.; Qiu, X.; Clementelli, C.; Herschbein, L.; Li, Z.; Elghaity-Beckley, S.; Arandela, J.; Kelly, B.; Hoffman, R.; Liu, J.; Xiong, Y.; Jin, J.*; Shih, A. H.*; An MDM2 degrader for treatment of acute leukemias. Leukemia, 2023, 37(2):370-378. PMID: 36309559 Jin, J.*; Dar, A. C.; Doroshow, D. “Advancing Cancer Precision Medicine by Creating a Better Toolbox for Cancer Therapy” in The Frontiers of Medical Research: Cancer (Science/AAAS, Washington, DC, 2022), pp. 10-12. Xiong, Y.; Zhong, Y.; Yim, H.; Yang, X.; Park, K. S.; Xie, L.; Poulikakos, P. I.; Han, X.; Xiong, Y.; Chen, X.; Liu, J.; Jin, J.*; Bridged Proteolysis Targeting Chimera (PROTAC) Enables Degradation of Undruggable Targets. Journal of the American Chemical Society. 2022, 144(49):22622-22632. PMID: 36448571. Wang, J.; Park, K. S.; Yu, X.; Gong, W.; Earp, H. S.; Wang, G. G.*; Jin, J.; * Cai, L.*; A cryptic transactivation domain of EZH2 binds AR and AR’s splice variant, promoting oncogene activation and tumorous transformation. Nucleic acids research, 2022, 50(19):10929-10946. PMID: 36300627. Yu, X.; Xu, J.; Cahuzac, K. M.; Xie, L.; Shen, Y.; Chen, X.; Liu, J.*; Parsons, R. E; Jin, J*; Novel Allosteric Inhibitor-Derived AKT Proteolysis Targeting Chimeras (PROTACs) Enable Potent and Selective AKT Degradation in KRAS/BRAF Mutant Cells. Journal of Medicinal Chemistry, 2022, 65(20):14237-14260. PMID: 36197750. Kurimchak, A. M.; Herrera-Montávez, C.; Montserrat-Sangrà, S.; Araiza-Olivera, D.; Hu, J.; Neumann-Domer, R.; Kuruvilla, M.; Bellacosa, A.; Testa, J. R.; Jin, J.; Duncan, J. S.*; The drug efflux pump MDR1 promotes intrinsic and acquired resistance to PROTACs in cancer cells. Science signaling, 2022, 15(749), eabn2707. PMID: 36041010. Cai, W. L.; Chen, J. F.; Chen, H.; Wingrove, E.; Kurley, S. J.; Chan, L. H.; Zhang, M.; Arnal-Estape, A.; Zhao, M.; Balabaki, A.; Li, W.; Yu, X.; Krop, E. D.; Dou, Y.; Liu, Y.; Jin, J.; Westbrook, T. F.; Nguyen, D. X.; Yan, Q.; Human WDR5 promotes breast cancer growth and metastasis via KMT2-independent translation regulation. Elife, 2022, 11, e78163. PMID: 36043466. Klima, M.; Khalili Yazdi, A.; Li, F.; Chau, I.; Hajian, T.; Bolotokova, A.; Kaniskan, H. Ü.; Han, Y.; Wang, K.; Li, D.; Luo, M.; Jin, J.; Boura, E.; Vedadi, M. Crystal structure of SARS-CoV-2 nsp10-nsp16 in complex with small molecule inhibitors, SS148 and WZ16. Protein Science. 2022, 31(9). PMID: 36040262. 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. Nature Structural & Molecular Biology. 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. Journal of Medicinal Chemistry. 2022, 65(15), 10611-10625. PMID: 35895319. 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 & Disease. 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. Journal of Medicinal Chemistry. 2022, 65(15), 10506-10522. 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. Journal of the American Chemical Society. 2022, 144(28), 12934-12941. 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. PMID: 358337138. 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, 18(8), 821-830. 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, 41(24), 3328-3340. 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. PMID: 35217626 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 Cao Tao, Martini Michael L., Park Kwang-Su, Kaniskan H. Ümit and Jin Jian, Pyrimidines and Their Benzo Derivatives. In: Black, David StC, Cossy, Janine and Stevens, Christian V. Eds., Comprehensive Heterocyclic Chemistry IV, Elsevier, 2022, 86-228. 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. 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