2025 Publications

 

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, 68(20):21377-21393. PMID: 41032690.

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.

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(33):29875-29883. PMCID: PMC12395470.

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: 118006. 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(1):24. PMCID: PMC12255682.

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(14):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(20):e2425812122. PMCID: PMC12107161.

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 , 2025, 147(17):14564-14573. PMCID: PMC12077936.

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, 2025, 68(8): 8543–8563. PMCID: PMC12080994.

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, 2025, 68(8):8634-8647. PMCID: PMC12043353.

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 , 2025, 291:117595. PMCID: PMC12045715.

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.  PMCID: PMC11932022.

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, 64(3):e202415168. PMCID: PMC11738674.

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, 12(7):e2413377. PMCID: PMC11831463.

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. 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. PMID: 40215343.

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, 2025, 30(9):3937-3950.PMCID: PMC12339378.

Xie, L; Sheehy, RN; Muneer, A; Xiong, Y; Wrobel, JA; Zhang, F; Park, KS; Velez, J; Liu, J; Luo, YJ; Asrican, B; Dong, P; Li, YD; Damian, C; Quintanilla, L; Li, Y; Xu, C; Deshmukh, M; Coleman, LG Jr; Ming, GL; Song, H; Wen, Z; Jin, J*; Song, J*; Chen, X*. “Development of a brain-penetrant G9a methylase inhibitor to target Alzheimer’s disease-associated proteopathology”. Nature Communication,  2025. 16(1):4222. PMCID: PMC12056044.

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. PMCID: PMC12017321.

Wang, SE; Cheng, Y; Lim, J; Jang, MA; Forrest, EN; Kim, Y; Donahue, M; Jo, S; Qiao, SN; Lee, DE; Hong, JY; Xiong, Y; Jin, J; Wang, S; Jiang, YH. “Mechanism of EHMT2-mediated genomic imprinting associated with Prader-Willi syndrome”. Nature Communication, 2025, 16(1):6125. PMCID: PMC12229668.

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): e191781.  PMCID: PMC12520682.

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.

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(28):eadu1670. PMCID: PMC12248387.

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. PMCID: PMC11845306.

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,  2025, 14: RP105318. PMCID: PMC12349897.

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, 64(7):e202420149. 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, 28(5):112387. PMCID: PMC12063144.

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, 28(6):112632. PMCID: PMC12159498.