2025 Publications
Tiedje, V.; Greenberg, J.; Qin, T.; Im, S. Y.; Krishnamoorthy, G. P.; Boucai, L.; Xu, B.; French, J. D.; Sherman, E. J.; Ho, A. L.; de Stanchina, E.; Socci, N. D.; Jin, J.; Ghossein, R. A.; Knauf, J. A.; Koche, R. P.; Fagin, J. A.* “Loss of tumor cell MHC class II drives MAPK inhibitor insensitivity of BRAF-mutant anaplastic thyroid cancers” The Journal of Clinical Investigation, 2025, 135(20). doi: 10.1172/JCI191781. PMCID: PMC12520682.
Xu, Z.; Pokushalov, D.; Kabir, M.; Lee, Y.; Chattopadhyay, M.; Jenkins, E. C.; Choo, C.; Kaniskan, H. Ü.; Germain, D.*; Jin, J.*“Targeting the Mitochondrial Protease ClpP for Anticancer Therapy” Journal of Medicinal Chemistry, 2025, doi: 10.1021/acs.jmedchem.5c01315.
Nelson, T.; Kemper, R.; Chiarella, A.; Gonzalez, T. S.; Carroll, M.; Tripathi, S.; Clarke, B.; Yu, X.; Hu, X.; Cooke, A.; Chirumamilla, B.; Chandler, A.; McGilvary, E.; Pattenden, S.; Jin, J.; Crona, D.*; Hathaway, N.* “A first-in-class chemical-induced proximity system achieves dose-dependent control of Tumor Protein 53 (TP53) gene activation in preclinical models of gastric cancer”, ACS Pharmacology & Translational Science, 2025, 8(10):3585-3599. PMCID: PMC12519258.
Atienza Párraga, A.; Nylund, P.; Diamanti, K.; Garrido-Zabala, B.; Tziola, S. I.; Vasquez, L.; Pyl, P. T.; Raykova, D.; Skaftason, A.; Ma, A.; Jin, J.; Martín-Subero, J. I.; Öberg, F.; De Bruyne, E.; Komorowski, J.; Jernberg Wiklund, H.*; Kalushkova, A.* “Combinatorial DNMTs and EZH2 inhibition reprograms the H3K27me3 and DNAme-mediated onco-epigenome to suppress multiple myeloma proliferation” Scientific Reports, 2025, 15(1):31568. PMCID: PMC12391466.
Dutta, R. P.; Lee, H. H.; Leshchenko, V. V.; Shukla, R. P.; Yan, F.; Liu, Y.; Kaniskan, H. Ü.; Qiu, X.; Jin, J.; Alinari, L.; Wang, M.; Parekh, S.* “SOX11 Modulates BCR Signaling Through the PAX5/CD19 Axis for Therapeutic Targeting in BTK Resistant Mantle Cell Lymphoma”, Blood Advances, 2025, DOI: 10.1182/bloodadvances.2025016801; PMID: 40845256.
Chen, L.; Deng, Z.; Xiong, Y.; Liu, J.; Huang, D.; Wang, J.; Chen, Y.; Inuzuka, H.; Xie, L.; Chen, X.; Jin, J.*; Wei, W.* “Deubiquitinase-Targeting Chimeras Mediated Stabilization of Tumor Suppressive E3 Ligase Proteins as a Strategy for Cancer Therapy” Journal of the American Chemical Society, 2025, 147, 29875-29883.
Hu, X.; Graciano, K.; Hu, J.; Liu, C.; Zhang, J.; Xie, L.; Chen, X.; Xiong, Y.; Jin, J.*; Xu, J.* “Discovery of the first-in-class Aurora B kinase selective degrader” European Journal of Medicinal Chemistry, 2025, 298, PMCID: PMC12379206.
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.* “Ketone drink enhances therapeutic efficacy in prostate cancer by targeting EZH2”, Oncogenesis, 2025, 14, 24. PMCID: PMC12255682.
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.* “G proteins of the G12 family expressed by POMC neurons regulate key metabolic functions” Science Advances, 2025, 11, eadu1670. PMCID: PMC12248387.
Zhu, S.; Gao, H.; Jiang, D.; Guo, G.; Hou, J.; Han, Y.; Zhang, C.; Hu, X.; Indulkar, S.; Kloeber, J. A.; Hu, Q.; Jiang, Y.; Zeng, X.; Ouyang, Y.; Lu, J.; Yin, P.; Luo, K.; Huang, J.; Wu, Z.; Chen, B.; Xiao, H.; Dragojevic, S.; Qin, H.; Zhou, X.; Jin, J.; Tu, X.; Wang, L.; Luo, Z.* “Isoform-Specific Function of NSD3 in DNA Replication Stress Confers Resistance to PARP Inhibitors in Prostate Cancer”, Molecular Cell, 2025, 85, 2673-2687.e8. PMCID: PMC12276998.
Hosseini, A.; Qiu, X.; Xiong, Y.*; Chiang, K. H. N.; Catlett, J.; Kaltheuner, I.; Deng, Z.; Ghosh, S.; Shi, Y.*; Jin, J.* ”Discovery of an LSD1 PROTAC Degrader”, Proceedings of the National Academy Sciences of the United States of America (PNAS), 2025, 122, e2425812122. doi:https://doi.org/10.1073/pnas.2425812122; PMCID: pending.
Qian, C.; Wang, Z.; Xiong, Y.; Zhang, D.; Zhong, Y.;Inuzuka, H.; Qi, Y.; Xie, L.; Chen, X.; Wei, W.* ; Jin, J.* , “Harnessing the Deubiquitinase USP1 for Targeted Protein Stabilization”. Journal of the American Chemical Society , April 19, 2025, doi: https://doi.org/https://doi.org/10.1021/jacs.5c01662
Zhong, Y.; Kim, H. S.; Qian, C.; Xie, L.; Chen, X.; Xiong, Y.; Hu, J.; Chen, M.; Guccione, E.; Shen, Y.*; Jin, J.* , “Discovery of A Potent and Selective Protein Arginine Methyltransferase 5 (PRMT5) PROTAC Degrader”. Journal of Medicinal Chemistry 68, 8, 8543–8563, April 15, 2025. doi: https://doi.org/https://doi.org/10.1021/acs.jmedchem.5c00198 .
Deng, Z.; Catlett, J.; Lee, Y.; Wu, Q.; Xu, Z.; Xie, L.; Chen, X.; Xiong, Y.; Kaniskan, H. U.*; Jin, J.*; “Harnessing the SPOP E3 Ubiquitin Ligase via Bridged Proteolysis Targeting Chimera (PROTAC) Strategy for Targeted Protein Degradation”, Journal of Medicinal Chemistry , April 9,2025, doi: https://doi.org/10.1021/acs.jmedchem.5c00295
Yim, H.; Sun, R.; Xu, Z.; Kim, H. S.; Kim, M.; Cao, T.; Xie, L.; Chen, X.; Kaniskan, H. U.*; Jin, J.*; “Discovery of the First-in-class DOT1L PROTAC Degrader” European Journal of Medicinal Chemistry , Volume 291, 5 July, 117595, 2025. doi:https://https://doi.org/10.1016/j.ejmech.2025.117595;
Qian,C.; Lee,Y.; Han,Y.; Zhong,Y.; Zhou,J.; Hrit, J.; Xie,L.; Chen, Q.; Kaniskan, H. U.; Chen, X.; Rothbart, S.; Cheng, X.; Xiong, Y.*; Jin, J.* , “Structure-activity Relationship Studies of DNA Methyltransferase 1 (DNMT1) Monovalent Degraders”. Journal of Medicinal Chemistry, 2025, 68, 3, 2903–2919 doi:https://doi.org/10.1021/acs.jmedchem.4c02161; PMID: 39905966
Deng, Z; Chen, L; Qian, C; Liu,J; Wu,Q; Song,X; Xiong,Y.; Wang, Z; Hu, X; Inuzuka, H; Zhong, Y; Lin; Y; Pham, N.D.; Shi,Y; Wei ;W.*; Jin,J.* Angewandte Chemie International Edition, “The First-in-class Deubiquitinase-targeting Chimera Stabilizes and Activates cGAS.”,2025 Jan 15;64(3):e202415168.; e202415168. doi: 10.1002/anie.202415168 PubMed PMID: 39150898.
Kabir. M.; Hu, X. Martin, T. C.; Pokushalov, D.; Kim, Y. J.; Chen, Y.; Zhong, Y.; Wu, Q; Chipuk, J. Y.; Shi, Y; Xiong, Y.; Gu, W.; Parsons, R. E.; and Jin, J.* , “Harnessing the TAF1 Acetyltransferase for Targeted Acetylation of the Tumor Suppressor p53”, Advanced Science, 2025, PMID: 39716936. PMCID: PMC11831463
doi: http://doi.org/10.1002/advs.202413377
Wang, Z.; Qian, C.; Xiong, Y.; Zhang, D.; Inuzuka, H.; Zhong, Y.; Xie, L.; Chen, X.; Jin, J.*; Wei, W.*, “USP28-Based Deubiquitinase-Targeting Chimeras for Cancer Treatment”, Journal of the American Chemical Society,2025, 147, 16, 13754–13763. doi:https://doi.org/https://doi.org/10.1021/jacs.5c01889; PMCID: PMC12105324.
Zhu, Z.; Chen, H.; Qiu, X.; Kaniskan, H. Ü.; Xie, L.; Chen, X.; Jin, J.*; Liu, P.* “(GGAA)3-based TF-PROTACs enable targeted degradation of ETV6 to inhibit Ewing sarcoma growth”, Journal of the American Chemical Society, 2025, 147, 16, 13396–13404. doi: https://doi.org/https://doi.org/10.1021/jacs.4c18484
Teichman , E. M.; Hu , J.; 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.* , “Design and validation of novel brain-penetrant HCN channel inhibitors to ameliorate social stress-induced susceptible phenotype ”. Molecular Psychiatry 08 April, 2025.PMID: 40199995 doi: https://doi.org/10.1038/s41380-025-02972-8
Xie, L.; Sheehy, R. N.; Xiong, Y.; Muneer, A.; Wrobel, J. A.; Park, K. S. ; Velez, J.; Liu, J.; Luo, Y. J.; Li , Y.; Quintanilla, L.; Li, Y.; Xu, C.; Deshmukh, M.; Wen, Z., Jin, J.*; Song, J.*; Chen, X.* , “A brain-penetrant G9a methylase inhibitor blocks Alzheimer’s disease proteopathology for the disease therapeutics.” Nature Communications, Published on March 18, 2025
Yu, Y.; Yu, X.; Pan, B.; Chan, H. M.; Kaniskan, H. Ü.; Jin, J.; Cai, L.*; Wang, G. G.*, “Pharmacologic degradation of WDR5 suppresses oncogenic activities of SS18::SSX and provides a therapeutic of synovial sarcoma”. Science Advances , 2025, 11, eads7876. doi: https://doi.org/10.1126/sciadv.ads7876; PMCID: PMC12017321.
Martinez, Criseyda; Xiong, Yan; Bartkowski, Alison; Harada, Ibuki; Ren, Xiaoxiao; Byerly, Jessica; Port, Elisa; Jian Jin*; Irie, Hanna*. “A PROTAC degrader suppresses oncogenic functions of PTK6 inducing apoptosis of breast cancer cells”, Cell Chemical Biology, 2025, 32(2), 255-266.E8, PMID: 39541980
Gumpper, R. H.*; Jain, M. K.; Kim, K.; Sun, R.; Sun, N.; Xu, Z.; DiBerto, J. F.; Krumm, B. E.; Kapolka, N. J.; Kaniskan, H. U.; Nichols, D. E.; Jin, J.; Fay, J. F.; Roth, B. L.* “The Structural Diversity of Psychedelic Drug Actions Revealed”, Nature Communications, 2025, 16:2734. PMID: 40108183
H, Su; Sun, Y; Han, G; Chen, S; Liu, S; Gao, A; Zhao, R; Glen, R; Jin, J; Qu, C; Yu, M; Klug, C.; K., A.; Zheng, G., Y.; Ballinger, S.; Kutny, M.; Chen, Y.; Luo, M*; Zhao, X.*, “PRMT1-Mediated Metabolic Reprogramming Promotes Leukemogenesis”. eLife, Feb, 17, 2025, preprint. doi: https://doi.org/10.7554/eLife.105318.1
Bauer, L.G., Ward, J.A., Díaz-Sáez, L., Sundström, Y., Tolvanen, T., Barrera, J. C. A., Kostidis, S., Rogers, C.M., Panagakou, I., Singh, U., Rothweiler, E.M., Gonzalez, Orta A, Kaniskan, H. Ü., Hu, J., Jin, J., Sievers, S., Waldmann, H., Giera, M., Sundström, M., Berg, L., Huber, K., “Phenomics-based Discovery of Novel Orthosteric Choline Kinase Inhibitors”. Angewandte Chemie International Edition, 2025 Feb 10;64(7):e202420149. doi: 10.1002/anie.202420149. PMID:39740997
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.*. “Epigenomic Analysis Identifies DTP Subpopulation Using HOPX to Develop Targeted Therapy Resistance in Lung Adenocarcinoma ”, iScience , 2025, Volume 28, Issue 5, 112387.
Muneer, A.; Xie, L.; Xie, X.; Zhang, F.; Wrobel, J. A.; Xiong, Y.; Yu, X.; Wang. C.; Gheorghe, C.; Wu, P.; Song, J.; Ming, G. L.; Jin, J.; Song, H.; Shi, P. Y.; Chen, X.* “Targeting G9a-m6A translational mechanism of SARS-CoV-2 pathogenesis for multifaceted therapeutics of COVID-19 and its sequalae” , iScience , 2025, doi:https://doi.org/10.1016/j.isci.2025.112632