{"id":24,"date":"2026-03-30T14:41:27","date_gmt":"2026-03-30T14:41:27","guid":{"rendered":"http:\/\/labs.icahn.mssm.edu\/center-for-therapeutics-discovery\/?page_id=24"},"modified":"2026-03-30T18:33:08","modified_gmt":"2026-03-30T18:33:08","slug":"publications","status":"publish","type":"page","link":"https:\/\/labs.icahn.mssm.edu\/center-for-therapeutics-discovery\/publications\/","title":{"rendered":"Publications"},"content":{"rendered":"<p style=\"text-align: center\"><strong>2026<\/strong><\/p>\n<p class=\"p1\">Chen, H.; Dutta, R. P.; Li, Z.; Zhong, Y.; Ma, A.; Park, K. S.; Kottur, J.; Park, A.; Babault, N.; Wang, K.; Wang, D.; Xiong, Y.; Kaniskan, H. \u00dc.; Luo, M.; Parekh, S.; Jin, J.*, \u201cDiscovery of a Potent, Selective, and In Vivo Efficacious Covalent Inhibitor for Lysine Methyltransferase SETD8\u201d,\u00a0<strong>Journal of Medicinal Chemistry<\/strong>, 2026, 69(4), 4255-4269. doi:<a href=\"https:\/\/doi.org\/https:\/\/doi.org\/10.1021\/acs.jmedchem.5c02958\">https:\/\/https:\/\/doi.org\/https:\/\/doi.org\/10.1021\/acs.jmedchem.5c02958<\/a><\/p>\n<p class=\"p1\">Yim, H.; Song, X.; Zhong, Y.; Hu, J.; Xiong, Y.; Jin, J.*, \u201cDiscovery of KRAS-G12D degraders via exploration of various E3 ligases\u201d,\u00a0<strong>European Journal of Medicinal Chemistry<\/strong>, 2026, 307, 118635.doi:<a href=\"https:\/\/doi.org\/10.1016\/j.ejmech.2026.118635\">https:\/\/https:\/\/doi.org\/10.1016\/j.ejmech.2026.118635<\/a><\/p>\n<p>PMID:<a href=\"https:\/\/pubmed.ncbi.nlm.nih.gov\/41679196\">41679196<\/a><\/p>\n<p class=\"p1\">Xia, Z.; Yang, X.; Samovich, S. N.; Tyurina, Y. Y.; Tyurin, V. A.; Kon, N.; Zhang, J.; Jiang, X.; Stockwell, B. R.; Jin, J.; Bayir, H.; Kagan, V. E.; Gu, W.*, \u201cA GPX1\u2013OSBPL8 Axis Mediates Noncanonical In Vivo Ferroptosis and Cancer Growth Suppression\u201d,\u00a0<strong>Cell\u00a0<\/strong>, 2026, Feb 19, doi:<a href=\"https:\/\/doi.org\/10.1016\/j.cell.2026.01.009\">https:\/\/https:\/\/doi.org\/10.1016\/j.cell.2026.01.009<\/a> PMCID: PMC12927606.<\/p>\n<p class=\"p1\">Gelles, J. D.; Chen, Y.; Luna-Vargas, M. P. A.; Viacava Follis, A.; Al Noman, M. A.; Kabir, M.; Bayiokos, S. G.; Mohammed, J. N.; Sebastian, T. M.; Pham, N. D.; Shi, Y.; Jin, J.; Kriwacki, R. W.; Chipuk, J. E.*, \u201cA gated hydrophobic funnel within BAX binds bioactive lipids to potentiate pro-apoptotic function\u201d,\u00a0<strong>Nature Communications\u00a0<\/strong>, 2026, Feb 25, doi: 10.1038\/s41467-026-69836-9.<\/p>\n<p class=\"p1\">Wang, Y.; Xiong, Y.; Liu, S.; Bao, L.; Qiu, X.; Korboukh, I.; Song, X.; Toffessi Tcheuyap, V.; Wu, S.; Chen, M.; Brugarolas, J.; Jin, J.; Wang, Y.; Luo, W.*, \u201cHIF-activated priming of TRAIL-induced cell death determines epigenetic vulnerability in kidney cancer\u201d,\u00a0<strong>Cell Reports Medicine<\/strong>, 2026, Feb 18, 102630. doi: 10.1016\/j.xcrm.2026.102630.<\/p>\n<p class=\"p1\">Yi, Y.; Li, Y.; Wang, R.; Yu, X.; Liu, Q.; Yum, C.; Zhang, Y.; Qiao, Y.; Szczepanski, A.; Wu, S.; Li, Q.; Fazli, L.; Shen, J.; Wang, X.; Li, X.; Mu, P.; Schaeffer, E. M.; Hundley, H. A.; Niu, H.; Chinnaiyan, A. M.; Wang, L.; Shi, J.; Jin, J.; Dong, X.; Zhao, W.; Chen, K.; Cao, Q.*, \u201cA dual role of EZH2 in regulating A-to-I RNA editing and mRNA stability through ADAR\u201d,\u00a0<strong>Nature Communications<\/strong>, 2026, find PMID.<\/p>\n<p class=\"p1\">Yi, Y.; Fry, J.; Yum, C.; Wang, R.; Wu, S.; Narayan, S.; Liu, Q.; Zhang, X.; Oo, H. Z.; Xie, N.; Li, Y.; Gao, X.; Yu, X.; Hu, X.; Li, Q.; Keseroglu, K.; \u00d6zbudak, E. M.; Abdulkadir, S. A.; Chen, K.; Jin, J.; Zhao, J. C.; Dong, X.; Arango, D.; Yang, R.; Cao, Q.*, \u201cEZH2 crosstalk with RNA methylation promotes prostate cancer progression through modulation of the m6A autoregulation pathway\u201d\u00a0<strong>Journal of Clinical Investigation<\/strong>, 2026, 136(2). doi: 10.1172\/JCI195840. PMCID: PMC12807473.<\/p>\n<p style=\"text-align: center\"><strong>2025<\/strong><\/p>\n<p class=\"p1\">Hu, X.; Graciano, K.; Hu, J.; Liu, C.; Zhang, J.; Xie, L.; Chen, X.; Xiong, Y.; Jin, J.*; Xu, J.*, \u201cDiscovery of the first-in-class Aurora B kinase selective degrader&#8221;, <strong> European Journal of Medicinal Chemistry <\/strong>, 2025, 298, 118006. Volume 298,\u00a015 November 2025, 118006<br \/>\nDOI: <a href=\"https:\/\/doi.org\/10.1016\/j.molcel.2025.06.004\"> https:\/\/pubs.acs.org\/doi\/10.1021\/jacs.5c06306<\/a><\/p>\n<p class=\"p1\">Chen, L; Deng, Z.; Xiong, Y.; Liu, J.; Huang, D.; Wang, J.; Chen, Y.; Inuzuka, H.; Xie, L.; Chen, X.; Jin, J.*; Wei, W.*, \u201cDeubiquitinase-Targeting Chimeras Mediated Stabilization of Tumor Suppressive E3 Ligase Proteins as a Strategy for Cancer Therapy&#8221;, <strong>Journal of the American Chemical Society <\/strong>, 2025, 147,DOI: <a href=\"https:\/\/doi.org\/10.1021\/jacs.5c06306\"> https:\/\/doi.org\/10.1021\/jacs.5c06306<\/a><\/p>\n<p class=\"p1\"><u>Qian, C.; Wang, Z.; Xiong, Y.; Zhang, D.; Zhong, Y.;<\/u>Inuzuka, H.; Qi, Y.; Xie, L.; Chen, X.; Wei, W.* ; Jin, J.* , \u201cHarnessing the Deubiquitinase\u00a0USP1\u00a0for Targeted Protein Stabilization\u201d. <strong> Journal of the American Chemical Society ,<\/strong> 2025, 147, 17, 14564\u201314573, doi:<a href=\"https:\/\/doi.org\/https:\/\/doi.org\/10.1021\/jacs.5c01662\"> https:\/\/doi.org\/https:\/\/doi.org\/10.1021\/jacs.5c01662<\/a><\/p>\n<p class=\"p1\"><u>Zhong, Y.<\/u>; Kim, H. S.; Qian, C.; Xie, L.; Chen, X.; Xiong, Y.; Hu, J.; Chen, M.; Guccione, E.; Shen, Y.*; Jin, J.* , \u201cDiscovery of A Potent and Selective Protein Arginine Methyltransferase 5 (PRMT5) PROTAC Degrader\u201d. <strong>Journal of Medicinal Chemistry<\/strong>, 2025, 68, 8, 8543\u20138563. doi:<a href=\"https:\/\/doi.org\/https:\/\/doi.org\/10.1021\/acs.jmedchem.5c00198\"> https:\/\/doi.org\/https:\/\/doi.org\/10.1021\/acs.jmedchem.5c00198<\/a> .<\/p>\n<p class=\"p1\">Deng, Z.; Catlett, J.; Lee, Y.; Wu, Q.; Xu, Z.; Xie, L.; Chen, X.; Xiong, Y.; Kaniskan, H. U.*; Jin, J.*; \u201cHarnessing the SPOP E3 Ubiquitin Ligase via Bridged Proteolysis Targeting Chimera (PROTAC) Strategy for Targeted Protein Degradation\u201d, <strong> Journal of Medicinal Chemistry <\/strong>,\u00a02025, 68, 8634\u20138647, doi:<a href=\"https:\/\/doi.org\/10.1021\/acs.jmedchem.5c00295\"> https:\/\/doi.org\/10.1021\/acs.jmedchem.5c00295 <\/a><\/p>\n<p class=\"p1\"><u>Yim, H.; Sun, R.; Xu, Z.<\/u>; Kim, H. S.; Kim, M.; Cao, T.; Xie, L.; Chen, X.; Kaniskan, H. U.*; Jin, J.*; \u201cDiscovery of the First-in-class DOT1L PROTAC Degrader\u201d <strong> European Journal of Medicinal Chemistry <\/strong>, Volume 291,\u00a05 July, 117595, 2025. doi:<a href=\"https:\/\/doi.org\/10.1021\/acs.jmedchem.4c02161\">https:\/\/https:\/\/doi.org\/10.1016\/j.ejmech.2025.117595;<\/a><\/p>\n<p class=\"p1\"><u>Qian,C.; Lee,Y.; Han,Y.; Zhong,Y.<\/u>; Zhou,J.; Hrit, J.; Xie,L.; Chen, Q.; Kaniskan, H. U.; Chen, X.; Rothbart, S.; Cheng, X.; Xiong, Y.*; Jin, J.* , \u201cStructure-activity Relationship Studies of DNA Methyltransferase 1 (DNMT1) Monovalent Degraders\u201d. <strong> Journal of Medicinal Chemistry<\/strong>, 2025, 68, 3, 2903\u20132919,\u00a0 doi:<a href=\"https:\/\/doi.org\/10.1021\/acs.jmedchem.4c02161\">https:\/\/doi.org\/10.1021\/acs.jmedchem.4c02161;<\/a> PMID: <a href=\"https:\/\/pubmed.ncbi.nlm.nih.gov\/39905966\">39905966<\/a><\/p>\n<p class=\"p1\">Wang, S. E.; Cheng, Y.; Lim, J.; Jang, M.; Forrest, E.; Kim, Y.; Donahue, M.; Jo, S.; Qiao, S.; Lee, D. E.; Hong, J. Y.; Xiong, Y.; Jin, J.; Wang, S.; Jiang, Y. H.* \u201cMechanism of EHMT2-mediated genomic imprinting associated with Prader-Willi syndrome\u201d. <strong>Nature Communications<\/strong>, 2025, 16:6125. PMCID: PMC12229668.<\/p>\n<p class=\"p1\">Zhu, S.; et al, Jin, J.; Luo, Z.* \u201cIsoform-Specific Function of NSD3 in DNA Replication Stress Confers Resistance to PARP Inhibitors in Prostate Cancer\u201d, <strong>Molecular Cell<\/strong>, 2025, DOI: <a href=\"https:\/\/doi.org\/10.1016\/j.molcel.2025.06.004\"> https:\/\/doi.org\/10.1016\/j.molcel.2025.06.004<\/a><\/p>\n<p class=\"p1\">Haspula, D.; Cui, Z.; Pittala, S.; Cui, Y.; Lu, H.; Xiong, Y.; Jin, J.; Gavrilova, O.; Hwang, E.; Ajwani, J.; Portillo, B.; Williams, K. W.; Inoue, A.; Weiss, J.* \u201cG proteins of the G12 family expressed by POMC neurons regulate key metabolic functions\u201d, <strong>Science Advances<\/strong>, in press.<\/p>\n<p class=\"p1\">Yum, C.; Schaefer, R.; Wang, R.; Wang, T.; Lu, X.; Liu, Q.; Ren, Y.; Meng, Q.; Yang, Y.; Zhang, X.; Xiong, Y.; Yu, X.; Zhang, X.; Jin, J.; Dong, X.; Yi, Y.; Yang, R.; Cao, Q.* &#8220;Ketone drink enhances therapeutic efficacy in prostate cancer by targeting EZH2&#8221;, <strong>Oncogenesis,<\/strong>. in press<\/p>\n<p class=\"p1\">Dutta, R. P.; et al, Jin, J.; Alinari, L.; Wang, M.; Parekh, S.* , \u201cSOX11 Modulates BCR Signaling Through the PAX5\/CD19 Axis for Therapeutic Targeting in BTK Resistant Mantle Cell Lymphoma&#8221;, <strong>Blood Advances<\/strong>, 2025, in press<\/p>\n<p class=\"p1\"><span style=\"color: #333300\"><u>Deng, Z; Chen, L; Qian, C; Liu,J; Wu,Q; Song,X; Xiong,Y.<\/u>; Wang, Z; Hu, X; Inuzuka, H; Zhong, Y; Lin; Y; Pham, N.D.; Shi,Y; Wei ;W.*;\u00a0Jin,J.* <em><strong>Angewandte Chemie International Edition<\/strong>,<\/em> \u201cThe First-in-class Deubiquitinase-targeting Chimera Stabilizes and Activates cGAS.&#8221;,2025 Jan 15;64(3):e202415168.; e202415168. doi: <a href=\"https:\/\/doi.org\/10.1002\/anie.202415168\"> 10.1002\/anie.202415168<\/a> PubMed PMID: <a href=\"https:\/\/pubmed.ncbi.nlm.nih.gov\/39150898\">39150898.<\/a><\/span><\/p>\n<p class=\"p1\"><span style=\"color: #333300\"> <u> Kabir. M.; Hu, X.<\/u> Martin, T. C.; Pokushalov, D.; Kim, Y. J.; Chen, Y.; Zhong, Y.;\u00a0Wu, Q; Chipuk, J. Y.; Shi, Y; Xiong, Y.; Gu, W.; Parsons, R. E.;\u00a0and\u00a0Jin, J.* , \u201cHarnessing the TAF1 Acetyltransferase for Targeted Acetylation of the Tumor Suppressor p53\u201d, <strong>Advanced Science<\/strong>, 2025, PMID: <a href=\"https:\/\/pubmed.ncbi.nlm.nih.gov\/39716936\">39716936.<\/a><\/span> \u00a0PMCID: PMC11831463, doi: <a href=\"http:\/\/doi.org\/10.1002\/advs.202413377\"> http:\/\/doi.org\/10.1002\/advs.202413377<\/a><\/p>\n<p class=\"p1\"><u>Wang, Z.; Qian, C.; Xiong, Y.; Zhang, D.<\/u>; Inuzuka, H.; Zhong, Y.; Xie, L.; Chen, X.; Jin, J.*; Wei, W.*, \u201cUSP28-Based Deubiquitinase-Targeting Chimeras for Cancer Treatment&#8221;, <strong> Journal of the American Chemical Society<\/strong>,2025, 147, 16, 13754\u201313763. Published\u00a0April 11, 2025.<br \/>\ndoi:<a href=\"https:\/\/doi.org\/https:\/\/doi.org\/10.1021\/jacs.5c01889\">https:\/\/doi.org\/https:\/\/doi.org\/10.1021\/jacs.5c01889<\/a><\/p>\n<p class=\"p1\">Zhu, Z.; Chen, H.; Qiu, X.; Kaniskan, H. \u00dc.; Xie, L.; Chen, X.; Jin, J.*; Liu, P.* &#8220;(GGAA)3-based TF-PROTACs enable targeted degradation of ETV6 to inhibit Ewing sarcoma growth&#8221;, <strong>Journal of the American Chemical Society<\/strong>, April, 11, 2025, 147, 16, 13396\u201313404. doi:<a href=\"https:\/\/doi.org\/https:\/\/doi.org\/10.1021\/jacs.4c18484\"> https:\/\/doi.org\/https:\/\/doi.org\/10.1021\/jacs.4c18484<\/a><\/p>\n<p class=\"p1\"><u> Teichman , E. M.; Hu , J.;<\/u> in, H.; Fisher, R. F.; Blando, A.; Hu, X.; Kaniskan , H. U; Montgomery, S. E.; Cai, M.; Parise, L.; Wang, J.; Russo, S.; Han, M.*; Jin , J.*; Morel, C.* , \u201cDesign and validation of novel brain-penetrant HCN channel inhibitors to ameliorate social stress-induced susceptible phenotype \u201d. <strong> Molecular Psychiatry, <\/strong>April, 08,2025.PMID: <a href=\"https:\/\/pubmed.ncbi.nlm.nih.gov\/40199995\">40199995<\/a>, doi:<a href=\"https:\/\/doi.org\/10.1038\/s41380-025-02972-8\"> https:\/\/doi.org\/10.1038\/s41380-025-02972-8 <\/a><\/p>\n<p class=\"p1\">Xie, L.; Sheehy, R. N.; Xiong, Y.; Muneer, A.; Wrobel, J. A.; Park, K. S. ; Velez, J.;\u00a0 Liu, J.;\u00a0 Luo, Y. J.; Li , Y.; Quintanilla, L.; Li, Y.; Xu, C.; Deshmukh, M.; Wen, Z., Jin, J.*; Song, J.*; Chen, X.* , \u201cA brain-penetrant G9a methylase inhibitor blocks Alzheimer\u2019s disease proteopathology for the disease therapeutics.\u201d <strong> Nature Communications<\/strong>, <b data-test=\"journal-volume\">16<\/b>, Article\u00a0number:\u00a0<span data-test=\"article-number\">4222<\/span>\u00a0(<span data-test=\"article-publication-year\">2025<\/span>) , doi:<\/p>\n<p class=\"p1\">Yu, Y.; Yu, X.; Pan, B.; Chan, H. M.; Kaniskan, H. \u00dc.; Jin, J.; Cai, L.*; Wang, G. G.*, \u201cPharmacologic degradation of WDR5 suppresses oncogenic activities of SS18::SSX and provides a therapeutic of synovial sarcoma\u201d. <strong>Science Advances <\/strong>, Apr,23, 2025.Vol 11, Issue 17. doi:<a href=\"https:\/\/doi.org\/10.1126\/sciadv.ads7876\"> https:\/\/doi.org\/10.1126\/sciadv.ads7876<\/a><br \/>\nPMID:<a href=\"https:\/\/pubmed.ncbi.nlm.nih.gov\/23297491\">23297491<\/a><\/p>\n<p class=\"p1\">Bauer, L.G., Ward, J.A., D\u00edaz-S\u00e1ez, L., Sundstr\u00f6m, Y., Tolvanen, T., Barrera, J. C. A., Kostidis, S., Rogers, C.M., Panagakou, I., Singh, U., Rothweiler, E.M., Gonzalez, Orta A, Kaniskan, H. \u00dc., Hu, J., Jin, J., Sievers, S., Waldmann, H., Giera, M., Sundstr\u00f6m, M., Berg, L., Huber, K., \u201cPhenomics-based Discovery of Novel Orthosteric Choline Kinase Inhibitors\u201d<strong> * Angewandte Chemie International Edition <\/strong>, 2024 Dec 30; e202420149. doi: 10.1002\/anie.202420149. PMID:<a href=\"https:\/\/pubmed.ncbi.nlm.nih.gov\/39740997\/\">39740997<\/a><\/p>\n<p class=\"p1\">Tian, Y.; Bhattacharya, R.; Yoo, S.; Jiang, F.; Park, E.; Laragranados, G.; Shen, Y.; Park, K.-S.; Kaniskan, H. U,; Jin, J.; Hopkins, B.; Zhu, J.; Watanabe, H.* \u201cEpigenomic Analysis Identifies DTP Subpopulation Using HOPX to Develop Targeted Therapy Resistance in Lung Adenocarcinoma\u201d <strong>iScience<\/strong>, Volume 28,\u00a0Issue 5, 112387, May 16, 2025<\/p>\n<p style=\"text-align: center\"><strong>Selective 12 of total 15 of 2024 Publications<\/strong><\/p>\n<p class=\"p1\"><span style=\"color: #333300\"> <u> Kabir. M.; Hu, X.<\/u> Martin, T. C.; Pokushalov, D.; Kim, Y. J.; Chen, Y.; Zhong, Y.;\u00a0Wu, Q; Chipuk, J. Y.; Shi, Y; Xiong, Y.; Gu, W.; Parsons, R. E.;\u00a0and\u00a0Jin, J.* <strong>Advanced Science.<\/strong>, \u201cHarnessing the TAF1 Acetyltransferase for Targeted Acetylation of the Tumor Suppressor p53\u201d, 2024, doi: <a href=\"http:\/\/doi.org\/10.1002\/advs.202413377\"> http:\/\/doi.org\/10.1002\/advs.202413377<\/a> <\/span><\/p>\n<p class=\"p1\"><span style=\"color: #333300\"> <u> Martinez, Criseyda; Xiong, Yan;<\/u> Bartkowski, Alison; Harada, Ibuki; Ren, Xiaoxiao; Byerly, Jessica; Port, Elisa; Jian\u00a0Jin*; Irie, Hanna*. <strong>Cell Chemical Biology<\/strong>, \u201cA PROTAC degrader suppresses oncogenic functions of PTK6 inducing apoptosis of breast cancer cells\u201d, 2024, doi: <a href=\"https:\/\/doi.org\/10.1016\/j.chembiol.2024.10.008\"> https:\/\/doi.org\/10.1016\/j.chembiol.2024.10.008<\/a><br \/>\nPMID: <a href=\"https:\/\/pubmed.ncbi.nlm.nih.gov\/39541980\/\">39541980<\/a> <\/span><\/p>\n<p class=\"p1\"><span style=\"color: #333300\"> <u> Inuzuka, H; Qian, Chao; Qi,Y; <\/u> Xiong, Y; Wang, C;Wang,Z; Zhang, D;Zhang, C; Jin, J*; Wei, W*; <strong> ACS Pharmacology &amp; Translational Science <\/strong>, \u201cTargeted Degradation of Receptor-Interacting Protein Kinase 1 to Modulate the Necroptosis Pathway\u201d, <a href=\"https:\/\/doi.org\/10.1021\/acsptsci.4c00421\">https:\/\/doi.org\/10.1021\/acsptsci.4c00421<\/a> 2024, 7, 3518-3526.<\/span><\/p>\n<p class=\"p1\"><span style=\"color: #333300\"> Corbin, J.; Yu, X.; Cai, L.; Jin, J.; Wang, G. G.* <strong> Oncogene <\/strong>, \u201cEZH2 PROTACs target EZH2- and FOXM1-associated oncogenic nodes, suppressing breast cancer cell growth\u201d, 2024, 43, 2722-2736. PMID:<a href=\"https:\/\/pubmed.ncbi.nlm.nih.gov\/39112519\/\">39112519<\/a> <\/span><\/p>\n<p class=\"p1\"><u>Xue Z;\u00a0Qin L; Xuan H; Luo K<\/u>; Huang M; Xie L; Su Y; Xu L; Harsh J; Dale B; Shi X; Chen X; Kaniskan H\u00dc; Jin J;\u00a0<b>*.\u00a0<\/b>, Wen H.*, \u201cA potent and selective ENL degrader suppresses oncogenic gene expression and leukemia progression.\u201d.<br \/>\n<strong>Science Advances<\/strong>, 2024 Aug 30;10(35):eado1432. doi: 10.1126\/sciadv.ado1432. Epub 2024 Aug 28. PMID:<a href=\"https:\/\/pubmed.ncbi.nlm.nih.gov\/39196923\/\">39196923<\/a>.\u00a0PMCID:\u00a0PMC11352836<\/p>\n<p><u>Graboski, A.L.;Simpson,J.B.;<\/u> Pellock;S.J.; Mehta, N.; Creekmore, B.C.; Ariyarathna; Y. ;Bhatt, A.P.; Jariwala,P.B.; Sekela, J.J.; Kowalewski, M.E.; Barker, N.K.; Mordant, A.L.; Borlandelli, V.B.; Overkleeft, H.; Herring, L.E.; Jin, J.*. ; I James L, Redinbo,M.R.. <strong>RSC Chemical Biology Journal<\/strong>, \u201cAdvanced piperazine-containing inhibitors target microbial \u03b2-glucuronidases linked to gut toxicity.\u201d PMID:<a href=\"https:\/\/pubmed.ncbi.nlm.nih.gov\/39211470\/\">39211470<\/a> ; PubMed Central PMCID: PMC11353122. RSC Chemical Biology. 2024 Jul 16;5(9):853-865<\/p>\n<p class=\"p1\"><u>Hu,X; Kabir, M;<\/u> Lin, Y; Xiong Y; Parsons, R;<span class=\"Apple-converted-space\">\u00a0\u00a0<\/span>Gu, W; Jin, J<b>*<\/b>\u201cDesign, Synthesis, and Evaluation of p53Y220C Acetylation Targeting Chimeras (AceTACs)\u201d,\u00a0<a class=\"customize-unpreviewable\" href=\"https:\/\/pubs.acs.org\/journal\/jmcmar\"><i><strong>Journal of Medicinal Chemistry<\/strong><\/i><\/a><i>, August, 2024.<\/i><\/p>\n<p><u>Wang, S, E.; Xiong, Y.<\/u>; Jang, M, A,; Park, K, S.; Donahue, M.; Velez J.; Jin J.*; Jiang, Y, H.*, \u201cNewly developed oral bioavailable EHMT2 inhibitor as a potential epigenetic therapy for Prader-Willi syndrome\u201d,\u00a0<strong>Molecular Therapy<\/strong>, 2024, PMID:<a href=\"https:\/\/pubmed.ncbi.nlm.nih.gov\/38796700\/\">38796700<\/a>. doi: 10.1016\/j.ymthe.2024.05.034.<\/p>\n<p><u>Kabir, M.<\/u>;\u00a0 <u>Qin, L.<\/u>;\u00a0 Luo, K.;\u00a0 Xiong, Y.;\u00a0 Sidi, R. A.;\u00a0 Park, K.-S.*; Jin, J.*, Discovery and characterization of a novel Cereblon-recruiting PRC1 bridged PROTAC degrader.\u00a0<em><strong>Journal of Medicinal Chemistry<\/strong>. <\/em>2024,\u00a0<span class=\"volume\">67<\/span><span class=\"issue\">(8)<\/span><span class=\"pages\">:6880-6892. <\/span><span class=\"pmid\">PMID: <a href=\"https:\/\/pubmed.ncbi.nlm.nih.gov\/38607318\/\">38607318<\/a>.<\/span><\/p>\n<p><u>Velez, J.<\/u>;\u00a0 <u>Han, Y.<\/u>;\u00a0 Yim, H.;\u00a0 Yang, P.;\u00a0 Deng, Z.;\u00a0 Park, K.-s.;\u00a0 Kabir, M.;\u00a0 Kaniskan, H. \u00dc.;\u00a0 Xiong, Y.*; Jin, J.*, Discovery of the first-in-class G9a\/GLP PROTAC degrader. <strong>Journal of Medicinal Chemistry<em>.<\/em><\/strong> 2024<strong>,<\/strong>\u00a0<i><span class=\"volume\">67<\/span><span class=\"issue\">(8)<\/span><span class=\"pages\">:6397-6409.<\/span><\/i>\u00a0PMID: <a href=\"https:\/\/pubmed.ncbi.nlm.nih.gov\/38295690\/\">38295690.<\/a><\/p>\n<p><u>Kim, Y.<\/u>;\u00a0 Gumpper, R. H.;\u00a0 <u>Liu, Y.<\/u>;\u00a0 Kocak, D. D.;\u00a0 Xiong, Y.;\u00a0 Cao, C.;\u00a0 Deng, Z.;\u00a0 Krumm, B. E.;\u00a0 Jain, M. K.;\u00a0 Zhang, S.;\u00a0 Jin, J.; Roth, B. L., Bitter taste receptor activation by cholesterol and an intracellular tastant. <strong><em>Nature <\/em>2024<\/strong>, <span class=\"volume\">628<\/span><span class=\"issue\">(8008)<\/span><span class=\"pages\">:664-671<\/span>. PMID: <a href=\"https:\/\/pubmed.ncbi.nlm.nih.gov\/38600377\/\">38600377.<\/a><\/p>\n<p><u>Liu, J.<\/u>;\u00a0 <u>Hu, X.;<\/u>\u00a0 <u>Luo, K<\/u>.;\u00a0 <u>Xiong, Y.<\/u>;\u00a0 <u>Chen, L.<\/u>;\u00a0 Wang, Z.;\u00a0 Inuzuka, H.;\u00a0 Qian, C.;\u00a0 Yu, X.;\u00a0 Xie, L.;\u00a0 Muneer, A.;\u00a0 Zhang, D.;\u00a0 Paulo, J. A.;\u00a0 Chen, X.;\u00a0 Jin, J.*; Wei, W.*, USP7-based deubiquitinase-targeting chimeras stabilize AMPK. <strong>Journal of the American Chemical Society<em>. <\/em><\/strong>2024,146, 16, 11507\u201311514. PMID:<a href=\"https:\/\/pubmed.ncbi.nlm.nih.gov\/38597345\/\">38597345.<\/a><\/p>\n<p><u>Xiong, Y.<\/u>;\u00a0 <u>Greschik, H.<\/u>;\u00a0 Johansson, C.;\u00a0 Seifert, L.;\u00a0 Gamble, V.;\u00a0 Park, K.-s.;\u00a0 Fagan, V.;\u00a0 Li, F.;\u00a0 Chau, I.;\u00a0 Vedadi, M.;\u00a0 Arrowsmith, C. H.;\u00a0 Brennan, P.;\u00a0 Fedorov, O.;\u00a0 Jung, M.;\u00a0 Farnie, G.;\u00a0 Liu, J.;\u00a0 Oppermann, U. *;\u00a0 Sch\u00fcle, R. *; Jin, J. *, Discovery of a potent, selective, and cell-active SPIN1 inhibitor. <strong>Journal of Medicinal Chemistry<\/strong><em>.<\/em> 2024, 67(7):5837-5853. <span class=\"identifier pubmed\"><span class=\"id-label\">PMID:<strong>\u00a0<\/strong><\/span><a href=\"https:\/\/pubmed.ncbi.nlm.nih.gov\/38533580\/\">38533580.<\/a><\/span><\/p>\n<p><u>Nylund, P. <\/u>;\u00a0, Garrido-Zabala, B.;\u00a0 P\u00e1rraga, A. A.;\u00a0 Vasquez, L.;\u00a0 Pyl, P. T.;\u00a0 Harinck, G. M.;\u00a0 Ma, A.; \u00a0Jin, J.;\u00a0 \u00d6berg, F.;\u00a0 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.\u00a0 <strong><em>Haematologica<\/em><\/strong> 2024, <em>109<\/em> (2): 567-577. PMID: <a href=\"https:\/\/pubmed.ncbi.nlm.nih.gov\/37496441\/\">37496441.<\/a><\/p>\n<p><u>Wang, Z.<\/u>;\u00a0 Zhang, D.;\u00a0 Qiu, X.;\u00a0 Inuzuka, H.;\u00a0 Xiong, Y.;\u00a0 Liu, J.;\u00a0 Chen, L.;\u00a0 Chen, H.;\u00a0 Xie, L.;\u00a0 Kaniskan, H. \u00dc.;\u00a0 Chen, X.;\u00a0 Jin, J. *; Wei, W. *, Structurally specific Z-DNA proteolysis targeting chimera enables targeted degradation of adenosine deaminase acting on RNA 1. <strong>Journal of the American Chemical Society<em>.<\/em> <\/strong>2024,\u00a0 <em>146<\/em> (11): 7584-7593. <span class=\"identifier pubmed\"><span class=\"id-label\">PMID:\u00a0<\/span><a href=\"https:\/\/pubmed.ncbi.nlm.nih.gov\/38469801\/\">38469801.<\/a><\/span><\/p>\n<p><u>Velez, J.;\u00a0 Dale, B.;\u00a0 Park, K.-S.;\u00a0 Kaniskan, H. \u00dc.<\/u>;\u00a0 Yu, X. *; Jin, J. *, Discovery of a novel, highly potent EZH2 PROTAC degrader for targeting non-canonical oncogenic functions of EZH2. <strong><em>European Journal of Medicinal Chemistry<\/em><\/strong>.\u00a0<span class=\"pubdate\">2024, <\/span><span class=\"pages\"><em>267<\/em>, 116154\u00a0<span class=\"pmid\">PMID: <a href=\"https:\/\/pubmed.ncbi.nlm.nih.gov\/PMID: 38295690\/\">PMID: 38295690.<\/a><\/span><\/span><\/p>\n<p style=\"text-align: center\"><strong>Selective 9 of total 24 of 2023 Publications<\/strong><\/p>\n<p><u>Dang, F.;<\/u> <u>Bai, L.;<\/u> <u>Dong, J.;<\/u> <u>Hu, X.;<\/u> 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. \u00dc.; 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.\u00a0 <strong>Science Translational Medicine<\/strong>. 2023<strong>,<\/strong> <em>15<\/em> (725): eadh7668. PMID:<a href=\"https:\/\/pubmed.ncbi.nlm.nih.gov\/38055802\/\"> 38055802<\/a>.<\/p>\n<p class=\"p1\"><span style=\"color: #333300\"> <u>Yu, X.; Li, D.; Kottur, J.<\/u>; 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. <em><strong>Journal of Medicinal Chemistry<\/strong><strong><em>. <\/em><\/strong>2023<strong>, <\/strong><\/em>66(23): 16168\u201316186. PMID:<a href=\"https:\/\/pubmed.ncbi.nlm.nih.gov\/38019706\/\"> 38019706.<\/a><\/span><\/p>\n<p><span style=\"color: #333300\">Wang Z.; Liu J.; Qiu X.; Zhang D.; Inuzuka H.; Chen L.; Chen H.; Xie L.; Kaniskan H\u00dc.; Chen X.; Jin J.* ; Wei W.* , Methylated Nucleotide-Based Proteolysis-Targeting Chimera Enables Targeted Degradation of Methyl-CpG-Binding Protein 2. <em><strong>Journal of the American Chemical Society <\/strong><\/em>. 2023, 145(40): 21871\u201321878. PMID: <a href=\"https:\/\/pubmed.ncbi.nlm.nih.gov\/37774414\/\">37774414<\/a>.<\/span><\/p>\n<p><span style=\"text-decoration: underline\">Kabir, M.; Sun, N.; Hu, X.;<\/span> Martin, T. C.; Yi, J.; Zhong, Y.; Xiong, Y.; Kaniskan, H. \u00dc.; Gu, W.; Parsons, R.; Jin, J.*; Acetylation Targeting Chimera Enables Acetylation of the Tumor Suppressor p53. <strong><em>Journal of the American Chemical Society<\/em><\/strong>\u00a02023,\u00a0145(27):14932-14944. PMID:<a href=\"https:\/\/pubmed.ncbi.nlm.nih.gov\/37365684\/\"><span style=\"color: #0000ff\"> 37365684.<\/span><\/a><\/p>\n<p>Velez, J.; Kaniskan, H. \u00dc.*; Jin, J.*; Recent advances in developing degraders &amp; inhibitors of lysine methyltransferases. <strong>Current Opinion in Chemical Biology,<\/strong>\u00a02023, 76:102356. PMID: <a href=\"https:\/\/pubmed.ncbi.nlm.nih.gov\/37379717\/\"><span style=\"color: #0000ff\">37379717.<\/span><\/a><\/p>\n<p class=\"p1\"><span style=\"color: #333300\">Kabir, M.; Yu, X.; Kaniskan, H. \u00dc.*; Jin, J.*; Chemically induced degradation of epigenetic targets. <strong><em>Chemical Society Reviews,<\/em><\/strong><em><strong>\u00a0<\/strong><\/em>2023, 52(13):4313-4342. <span class=\"identifier pubmed\"><span class=\"id-label\">PMID:\u00a0<\/span><a href=\"https:\/\/pubmed.ncbi.nlm.nih.gov\/37314393\/\"><span style=\"color: #0000ff\">37314393.<\/span><\/a><\/span><\/span><\/p>\n<p><span style=\"text-decoration: underline\">Zhao, N.; Ho, J. S. Y.; Meng, F.;<\/span> Zheng, S.; Kurland, A. P.; Tian, L.; Rea-Moreno, M.; Song, X.; Seo, J. S.; Kaniskan, H. \u00dc.; 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. <em><strong>Cell Host Microbe,<\/strong><\/em>\u00a02023, 31(7):1154-1169.e10. PMID:<a href=\"https:\/\/pubmed.ncbi.nlm.nih.gov\/37339625\/\"><span style=\"color: #0000ff\"> 37339625.<\/span><\/a><\/p>\n<p><span style=\"text-decoration: underline\">Yu, X.; Wang, J.;<\/span> 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. <strong><i>Oncogene<\/i><\/strong>, 2023, 42(13):994-1009. <span class=\"identifier pubmed\"><span class=\"id-label\">PMID:\u00a0<\/span><a href=\"https:\/\/pubmed.ncbi.nlm.nih.gov\/36747009\/\"><span style=\"text-decoration: underline\"><span style=\"color: #0000ff;text-decoration: underline\">36747009.<\/span><\/span><\/a><\/span><\/p>\n<p class=\"p1\"><span style=\"color: #333300\">Park, K. S.; Qin, L.; Kabir, M.; Luo, K.; Dale, B.; Zhong, Y.; Kim, A.; Wang, G. G.; Kaniskan, H. \u00dc.; Jin, J*; Targeted Degradation of PRC1 Components, BMI1 and RING1B, via a Novel Protein Complex Degrader Strategy. <strong>Advanced science (Weinheim, Baden-W\u00fcrttemberg, Germany)<\/strong><i><strong>.<\/strong><\/i>\u00a02023, 10(10):e2205573. <span class=\"identifier pubmed\"><span class=\"id-label\">PMID:<span style=\"color: #0000ff\"><a style=\"color: #0000ff\" href=\"https:\/\/pubmed.ncbi.nlm.nih.gov\/36737841\/\">\u00a0<\/a><\/span><\/span><a href=\"https:\/\/pubmed.ncbi.nlm.nih.gov\/36737841\/\"><span style=\"color: #0000ff\">36737841.<\/span><\/a><\/span><\/span><\/p>\n<p><span style=\"text-decoration: underline\">Sun, N.; Kabir, M.;<\/span> Lee, Y.; Xie, L.; Hu, X.; Velez, J.; Chen, X.; Kaniskan, H. \u00dc.*; &amp; Jin, J*; Discovery of the First Lactate Dehydrogenase Proteolysis Targeting Chimera Degrader for the Treatment of Pancreatic Cancer. <strong>Journal of Medicinal Chemistry<i>. <\/i><\/strong>2023, 66(1):596-610. <span class=\"identifier pubmed\"><span class=\"id-label\">PMID:\u00a0<\/span><a href=\"https:\/\/pubmed.ncbi.nlm.nih.gov\/36538511\/\"><span style=\"color: #0000ff\">36538511.<\/span><\/a><\/span><\/p>\n<p><span style=\"text-decoration: underline\">Marcellino, B. K.; Yang, X.; \u00dcmit Kaniskan, H.;<\/span> 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.<strong> <i>Leukemia<\/i><\/strong>, 2023, 37(2):370-378. <span class=\"identifier pubmed\"><span class=\"id-label\">PMID:\u00a0<\/span><span style=\"color: #0000ff\"><a style=\"color: #0000ff\" href=\"https:\/\/pubmed.ncbi.nlm.nih.gov\/36309559\/\">36309559<\/a><\/span><\/span><\/p>\n","protected":false},"excerpt":{"rendered":"<p>2026 Chen, H.; Dutta, R. P.; Li, Z.; Zhong, Y.; Ma, A.; Park, K. S.; Kottur, J.; Park, A.; Babault, N.; Wang, K.; Wang, D.; Xiong, Y.; Kaniskan, H. \u00dc.; Luo, M.; Parekh, S.; Jin, J.*, \u201cDiscovery of a Potent, Selective, and In Vivo Efficacious Covalent Inhibitor for Lysine Methyltransferase SETD8\u201d,\u00a0Journal of Medicinal Chemistry, 2026, [&hellip;]<\/p>\n","protected":false},"author":43,"featured_media":0,"parent":0,"menu_order":0,"comment_status":"closed","ping_status":"closed","template":"","meta":{"footnotes":""},"class_list":["post-24","page","type-page","status-publish","hentry"],"aioseo_notices":[],"_links":{"self":[{"href":"https:\/\/labs.icahn.mssm.edu\/center-for-therapeutics-discovery\/wp-json\/wp\/v2\/pages\/24","targetHints":{"allow":["GET"]}}],"collection":[{"href":"https:\/\/labs.icahn.mssm.edu\/center-for-therapeutics-discovery\/wp-json\/wp\/v2\/pages"}],"about":[{"href":"https:\/\/labs.icahn.mssm.edu\/center-for-therapeutics-discovery\/wp-json\/wp\/v2\/types\/page"}],"author":[{"embeddable":true,"href":"https:\/\/labs.icahn.mssm.edu\/center-for-therapeutics-discovery\/wp-json\/wp\/v2\/users\/43"}],"replies":[{"embeddable":true,"href":"https:\/\/labs.icahn.mssm.edu\/center-for-therapeutics-discovery\/wp-json\/wp\/v2\/comments?post=24"}],"version-history":[{"count":163,"href":"https:\/\/labs.icahn.mssm.edu\/center-for-therapeutics-discovery\/wp-json\/wp\/v2\/pages\/24\/revisions"}],"predecessor-version":[{"id":389,"href":"https:\/\/labs.icahn.mssm.edu\/center-for-therapeutics-discovery\/wp-json\/wp\/v2\/pages\/24\/revisions\/389"}],"wp:attachment":[{"href":"https:\/\/labs.icahn.mssm.edu\/center-for-therapeutics-discovery\/wp-json\/wp\/v2\/media?parent=24"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}