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. J. Med. Chem. 2024. Published online.
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. J. Med. Chem. 2024. Published online.
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. Published online.
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. J. Am. Chem. Soc. 2024. Published online.
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. J. Med. Chem. 2024, 67(7):5837-5853.
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.
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 1. J. Am. Chem. Soc. 2024, 146 (11): 7584-7593.
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. E. J. Med. Chem. 2024, 267, 116154.
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. Sci. Transl. Med. 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. Hum Gene Ther. 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 chem Biol, 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. J Chem Inf Model, 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. Curr Opin Chem Biol, 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 Chem Biol, 2023, 30(7):753-765.e8. PMID: 37354907.
Kabir, M.; Yu, X.; Kaniskan, H. Ü.*; Jin, J.*; Chemically induced degradation of epigenetic targets. Chem Soc Rev. 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 Differ, 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. J Am Chem Soc. 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. Adv Sci (Weinh), 2023, 10(10):e2205573. PMID: 36737841
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
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. J. Am. Chem. Soc. 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
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
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.
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.
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.
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.
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.
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.
Yu, X.; Li, D.; Kottur, J.; Shen, Y.; Kim, H. S.; Park, K. S.; et al, Kaniskan, H. Ü.; Cai, L.; Jain, R.; Liu, J.; Aggarwal, A. K.; Wang, G. G.*; Jin, J.* A Selective WDR5 Degrader Inhibits Acute Myeloid Leukemia in Patient-Derived Mouse Models. Science Translational Medicine 2021, 13, eabj1578. PMID:34586829.
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Lu, S. X.; De Neef, E.; Thomas, J. D.; Sabio, E.; Rousseau, B.; Gigoux, M.; Knorr, D. A.; Greenbaum, B.; Elhanati, Y.; Hogg, S. J.; Chow, A.; Ghosh, A.; Xie, A.; Zamarin, D.; Cui, D.; Erickson, C.; Singer, M.; Cho, H.; Wang, E.; Lu, B.; Durham, B. H.; Shah, H.; Chowell, D.; Gabel, A. M.; Shen, Y.; Liu, J.; Jin, J.; Rhodes, M. C.; Taylor, R. E.; Molina, H.; Wolchok, J. D.; Merghoub, T.; Diaz, L. A.; Abdel-Wahab, O.*; Bradley, R. K.* Pharmacologic modulation of RNA splicing enhances anti-tumor immunity. Cell2021, 184, 4032-4047. PMID: 34171309
Dale, B.; Cheng, M.; Park, K.-S.; Kaniskan, H. Ü.; Xiong, Y.*; Jin, J*. Advancing targeted protein degradation for cancer therapy. Nature Reviews Cancer2021, 21, 638-654. PMID: 34131295, PMCID: PMC8463487.
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Wu, X.; Yang, X.; Xiong, Y.; Li, R.; Ito, T.; Ahmed, T. A.; Karoulia, Z.; Adamopoulos, C.; Wang, H.; Wang, L.; Xie, L.; Liu, J.; Ueberheide, B.; Aaronson, S. A.; Chen, X.; Buchanan, S. G.; Sellers, W.R.; Jin, J.; Poulikakos, P. I.* Distinct CDK6 complexes determine tumor cell response to CDK4/6 inhibitors and degraders. Nature Cancer 2021, 2, 429-443.
Bhat, K. P.; Ümit Kaniskan, H.; Jin, J.*; Gozani, O.* Epigenetics and beyond: targeting writers of protein lysine methylation to treat disease. Nat. Rev. Drug Discov. 2021, 20, 265-286. PMID: 33469207, PMCID: PMC8035146.
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Clarke, T. L.; Tang, R.; Chakraborty, D.; Rechem, C. V.; Ji, F.; Mishra, S.; Ma, A.; Kaniskan, H. U.; Jin, J.; Lawrence, M. S.; Sadreyev, R. I.; and Whetstine, J. R.* Histone Lysine Methylation Dynamics Control EGFR DNA Copy Number Amplification. Cancer Discovery 2020, 10, 306-325. PMID: 31776131, PMCID: PMC7271978.
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Liu, J.; Chen, H.; Ma, L.; He, Z.; Wang, D.; Liu, Y.; Lin, Q.; Zhang, T.; Gray, N.; Kaniskan, H. U.; Jin, J.*; Wei, W.*Light-induced control of protein destruction by opto-PROTAC. Sci. Adv., 2020, 6, eaay5154. PMID: 32128407, PMCID: PMC7034987.
Ma, A.; Stratikopoulos, E.; Park, K –S.; Wei, J.; Martin, T. C.; Yang, X.; Schwarz, M.; Leshchenko, V.; Rialdi, A.; Dale, B.; Lagana, A.; Guccione, E.; Parekh, S.; Parsons, R.* and Jin, J.* Discovery of a first-in-class EZH2 selective degrader. Nature Chemical Biology 2020,16, 214–222.PMID: 31730343, PMCID: PMC6982609.
Chiarella, A. M.; Butler, K. V.; Gryder, B. E.; Lu, D.; Wang, T. A.; Yu, X.; Pomella, S.; Khan, J.; Jin, J.*; Hathaway, N. A.* Dose-dependent activation of gene expression is achieved using CRISPR and small molecules that recruit endogenous chromatin machinery. Nature Biotechnology 2020, 38, 50–55. PMID: 31712774, PMCID: PMC6954327.
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