Publications

Xue Z; Qin L; Xuan H; Luo K; Huang M; Xie L; Su Y; Xu L; Harsh J; Dale B; Shi X; Chen X; Kaniskan HÜ; Jin J; *. , Wen H.*, “A potent and selective ENL degrader suppresses oncogenic gene expression and leukemia progression.”.
Science Advances, 2024 Aug 30;10(35):eado1432. doi: 10.1126/sciadv.ado1432. Epub 2024 Aug 28. PMID:39196923. PMCID: PMC11352836

Graboski, A.L.;Simpson,J.B.; 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.. RSC Chemical Biology Journal, “Advanced piperazine-containing inhibitors target microbial β-glucuronidases linked to gut toxicity.” PMID:39211470 ; PubMed Central PMCID: PMC11353122. RSC Chemical Biology. 2024 Jul 16;5(9):853-865

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, PMID:38796700. 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(8):6880-6892. PMID: 38607318.

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: 38295690.

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. 2024,146, 16, 11507–11514. 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 1. 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: 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. Journal of the American Chemical Society. 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. 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.

Wei, J.; Meng, F.;Park, K.; Yim, H.; Velez, J.; Kumar, P.; Wang, L.; Xie, L.; Chen, H.; Shen, Y.; Teichman, E.; Wang, G.; Chen, X.; Kaniskan, H.*; Jin, J.* Harnessing the E3 ligase KEAP1 for targeted protein degradation. J. Am. Chem. Soc.  2021, 143, 37, 15073–15083. PMID: 34520194，PMCID:PMC8480205.

Xu, J.;  Yu, X.;  Martin, T. C.;  Bansal, A.; Cheung, K.;  Lubin, A.;  Stratikopoulos, E.;  Cahuzac, K. M.;  Wang, L.; Xie, L.;  Zhou, R.;  Shen, Y.; Wu, X.;  Yao, S.;  Qiao, R.; Poulikakos, P. I.;  Chen, X.;  Liu, J.; Jin, J.*; Parsons, R.* AKT degradation selectively inhibits the growth of PI3K/PTEN pathway mutant cancers with wild-type KRAS and BRAF by destabilizing Aurora kinase B. Cancer Discovery 2021, 11, 3064-3089. PMID: 34301793.

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.

Li, J.; Galbo, P. M., Jr.; Gong, W.; Storey, A. J.; Tsai, Y. H.; Yu, X.; Ahn, J. H.;Guo, Y.; Mackintosh, S. G.; Edmondson, R. D.; Byrum, S. D.; Farrar, J. E.; He, S.; Cai, L.; Jin, J.; Tackett, A. J.; Zheng, D.; Wang, G. G.* ZMYND11-MBTD1 induces leukemogenesis through hijacking NuA4/TIP60 acetyltransferase complex and a PWWP-mediated chromatin association mechanism. Nat. Commun. 2021, 12, 1045. PMID: 33594072, PMCID: PMC7886901.

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.

Wang, M.;  Li, A.;  Sekiya, M.; Beckmann, N. D.;  Quan, X.;  Schrode, N.; Fernando, M. B.;  Yu, A.;  Zhu, L.; Cao, J.;  Lyu, L.;  Horgusluoglu, E.;  Wang, Q.; Guo, L.;  Wang, Y. S.;  Neff, R.; Song, W. M.;  Wang, E.;  Shen, Q.; Zhou, X.;  Ming, C.;  Ho, S. M.; Vatansever, S.;  Kaniskan, H. U.;  Jin, J.;  Zhou, M. M.; Ando, K.;  Ho, L.;  Slesinger, P. A.;  Yue, Z.; Zhu, J.;  Katsel, P.;  Gandy, S.; Ehrlich, M. E.;  Fossati, V.;  Noggle, S.; Cai, D.;  Haroutunian, V.;  Iijima, K. M.;  Schadt, E.; Brennand, K. J.; Zhang, B.* Transformative network modeling of multi-omics data reveals detailed circuits, key regulators, and potential therapeutics for alzheimer’s disease. Neuron 2020, 109, 257-272. PMID: 33238137, PMCID: PMC7855384.

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.

Nagai, Y.; Miyakawa, N.; Takuwa, H.; Hori, Y.; Oyama, K.; Ji, B.; Takahashi, M.; Huang, X. P.; Slocum, S. T.; DiBerto, J. F.; Xiong, Y.; Urushihata, T.; Hirabayashi, T.; Fujimoto, A.; Mimura, K.; English, J. G.; Liu, J.; Inoue, K. I.; Kumata, K.; Seki, C.; Ono, M.; Shimojo, M.; Zhang, M. R.; Tomita, Y.; Nakahara, J.; Suhara, T.; Takada, M.; Higuchi, M.; Jin, J.; Roth, B. L.; Minamimoto, T. Deschloroclozapine, a potent and selective chemogenetic actuator enables rapid neuronal and behavioral modulations in mice and monkeys. Nat Neurosci. 2020, 23, 1157-1167. PMID: 32632286, PMCID: In progress.

Kato, S.; Weng, Q. Y.; Insco, M. L.; Chen, K. Y.; Muralidhar, S.; Pozniak, J.; Diaz, J.; Drier, Y.; Nguyen, N.; Lo, J. A.; van Rooijen, E.; Kemeny, L. V.; Zhan, Y.; Feng, Y.; Silkworth, W.; Powell, C. T.; Liau, B. B.; Xiong, Y.; Jin, J.; Newton-Bishop, J.; Zon, L. I.; Bernstein, B. E.; Fisher, D. E.* Gain-of-function genetic alterations of G9a drive oncogenesis. Cancer discovery 2020, 10, 7, 980-997. PMID: 32269030, PMCID: PMC7334057.

Li, T.; Li, X.; Zamani, A.; Wang, W.; Lee, C –N.; Li, M.; Luo, G.; Eiler, E.; Sun, H.; Ghosh, S.; Jin, J.; Murali, R.; Ruan, Q.; Shi, W.; & Chen. Y. H.* c-Rel is a myeloid checkpoint for cancer immunotherapy. Nature Cancer, 2020, 1, 507-517. PMID: 33458695, PMCID: PMC7808269.

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.

Qadeer, Z. A.; Valle-Garcia, D.; Hasson, D.; Sun, Z.; Cook, A.; Nguyen, C.; Soriano, A.; Ma, A.; Griffiths, L. M.; Zeineldin, M.; Filipescu, D.; Jubierre, L.; Chowdhury, A.; Deevy, O.; Chen, X.; Finkelstein, D. B.; Bahrami, A.; Stewart, E.; Federico, S.; Gallego, S.; Dekio, F.; Fowkes, M.; Meni, D.; Maris, J. M.; Weiss, W. A.; Roberts, S. S.; Cheung, N. V.; Jin, J.; Segura, M. F.; Dyer, M. A.; Bernstein, E. ATRX In-Frame Fusion Neuroblastoma Is Sensitive to EZH2 Inhibition via Modulation of Neuronal Gene Signatures. Cancer Cell 2019, 36, 1–16. PMID: 31631027, PMCID: PMC6851493.

Fong, J. Y.; Pignata, L.; Goy, P. A.; Kawabata, K. C.; Lee, S. C.; Koh, C. M.; Musiani, D.; Massignani, E.; Kotini, A. G.; Penson, A.; Wun, C. M.; Shen, Y.; Schwarz, M.; Low, D. H.; Rialdi, A.; Ki, M.; Wollmann, H.; Mzoughi, S.; Gay, F.; Thompson, C.; Hart, T.; Barbash, O.; Luciani, G. M.; Szewczyk, M. M.; Wouters, B. J.; Delwel, R.; Papapetrou, E. P.; Barsyte-Lovejoy, D.; Arrowsmith, C. H.; Minden, M. D.; Jin, J.; Melnick, A.; Bonaldi, T.; Abdel-Wahab, O.*; Guccione, E.* Therapeutic Targeting of RNA Splicing Catalysis through Inhibition of Protein Arginine Methylation. Cancer Cell 2019, 36, 194-209. e9. PMID: 31408619, PMCID: in progress.

Lima-Fernandes, E.; Murison, A.; Medina, T.S.; Wang, Y.; Ma, A.; Leung, C.; Luciani, G. M.; Haynes, J.; Pollett, A.; Zeller, C.; Duan, S.; Kreso, A.; Barsyte-Lovejoy, D.; Wouters, B. G.; Jin, J.; De Carvalho, D. D.; Lupien, M.; Arrowsmith, C. H.*; O’Brien, C. A.* Targeting bivalency de-represses Indian Hedgehog and inhibits self-renewal of colorectal cancer-initiating cells. Nat. Commun. 2019, 10(1), 1436. PMID: 30926792, PMCID : PMC6441108.

Scheer, S.; Ackloo, S.; Medina, T. S.; Schapira, M.; Li, F.; Ward, J. A.; Lewis, A. M.; Northrop, J. P.; Richardson, P. L.; Kaniskan, H. Ü.; Shen, Y.; Liu, J.; Smil, D.; McLeod, D.; Zepeda-Velazquez, C. A.; Luo, M.; Jin, J.; Barsyte-Lovejoy, D.; Huber, K. V. M.; De Carvalho, D. D.; Vedadi, M.; Zaph, C.; Brown, P. J.; Arrowsmith, C. H.  A chemical biology toolbox to study protein methyltransferases and epigenetic signaling. Nat. Commun. 2019, 10, 19. PMID:<a style=”color: #0000ff;%