Jin Lab Full Publication List

Dr. Jin Google Scholar Citations

2024

 

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 AL;Simpson JB; Pellock SJ; Mehta N; Creekmore BC; Ariyarathna Y ;Bhatt AP; Jariwala PB; Sekela JJ; Kowalewski ME; Barker NK; Mordant AL; Borlandelli VB; Overkleeft H; Herring LE,; Jin J*. ; I James L, Redinbo MR. PubMed Central “Advanced piperazine-containing inhibitors target microbial β-glucuronidases linked to gut toxicity.” RSC Chemical Biology. 2024 Aug 28;5(9):853-865. doi: 10.1039/d4cb00058g. eCollection 2024 Aug 28. PubMed PMID: 39211470; PubMed Central PMCID: PMC11353122.

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, 67, 14633−14648

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, 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, 67:6880-6892. PMID: 38607318.

Nigam, A. K.; Hurley, M. F. D.; Lid, F.; Konkoľováe, E.; Klímae, M.; Trylčováe, J.; Pollice, R.; Çinaroǧluh, S. S.; Levin-Konigsbergb, R.; Handjayafg, J.; Schapiradi, M.; Chaud, R.; Perveen, S.; Ho-Leung Ng, H.;  Kaniskan, Ü.; Hank, Y.; Singhl, S.; Gorgullamno, C.; Kundajeab, A.; Jin, J.;  Voelz, V. A.;  Webere, J.; Nenckae, R.; Bourae, E.; Vedadi, M.*; Aspuru-Guzik, A.* “Application of established computational techniques to identify potential SARS-CoV-2 Nsp14-MTase inhibitors in low data regimes.” Digital Discovery, 2024, doi: 1039/D4DD00006D.

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: 38607318.

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 Apr 10; 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.  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: 38295690.

2023

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. 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.  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. Current Opinion in Chemical Biology, 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 Chemical Biology, 2023, 30(7):753-765.e8. PMID: 37354907.

Kabir, M.; Yu, X.; Kaniskan, H. Ü.*; Jin, J.*; Chemically induced degradation of epigenetic targets. Chemical Society Reviews, 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 & Differentiation, 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. Journal of Medicinal Chemistry. 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. Advanced science (Weinheim, Baden-Württemberg, Germany). 2023, 10(10):e2205573. PMID: 36737841.

Sun, N.; Kabir, M.; Lee, Y.; Xie, L.; Hu, X.; Velez, J.; Chen, X.; Kaniskan, H. Ü.*; & Jin, J*; Discovery of the First Lactate Dehydrogenase Proteolysis Targeting Chimera Degrader for the Treatment of Pancreatic Cancer. Journal of Medicinal Chemistry. 2023, 66(1):596-610. PMID: 36538511.

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

 

2022

Jin, J.*; Dar, A. C.; Doroshow, D. “Advancing Cancer Precision Medicine by Creating a Better Toolbox for Cancer Therapy” in The Frontiers of Medical Research: Cancer (Science/AAAS, Washington, DC, 2022), pp. 10-12.

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. Journal of the American Chemical Society. 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.

Yu, X.; Xu, J.; Cahuzac, K. M.; Xie, L.; Shen, Y.; Chen, X.; Liu, J.*; Parsons, R. E; Jin, J*; Novel Allosteric Inhibitor-Derived AKT Proteolysis Targeting Chimeras (PROTACs) Enable Potent and Selective AKT Degradation in KRAS/BRAF Mutant Cells. Journal of Medicinal Chemistry, 2022, 65(20):14237-14260. PMID: 36197750.

Kurimchak, A. M.; Herrera-Montávez, C.; Montserrat-Sangrà, S.; Araiza-Olivera, D.; Hu, J.; Neumann-Domer, R.; Kuruvilla, M.; Bellacosa, A.; Testa, J. R.; Jin, J.; Duncan, J. S.*; The drug efflux pump MDR1 promotes intrinsic and acquired resistance to PROTACs in cancer cells. Science signaling, 2022, 15(749), eabn2707. PMID: 36041010.

Cai, W. L.; Chen, J. F.; Chen, H.; Wingrove, E.; Kurley, S. J.; Chan, L. H.; Zhang, M.; Arnal-Estape, A.; Zhao, M.; Balabaki, A.; Li, W.; Yu, X.; Krop, E. D.; Dou, Y.; Liu, Y.; Jin, J.; Westbrook, T. F.; Nguyen, D. X.; Yan, Q.; Human WDR5 promotes breast cancer growth and metastasis via KMT2-independent translation regulation. Elife, 2022, 11, e78163. PMID: 36043466.

Klima, M.; Khalili Yazdi, A.; Li, F.; Chau, I.; Hajian, T.; Bolotokova, A.; Kaniskan, H. Ü.; Han, Y.; Wang, K.; Li, D.; Luo, M.; Jin, J.; Boura, E.; Vedadi, M. Crystal structure of SARS-CoV-2 nsp10-nsp16 in complex with small molecule inhibitors, SS148 and WZ16. Protein Science. 2022, 31(9). PMID: 36040262.

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-HT_5A receptor. Nature Structural & Molecular Biology. 2022, 29(7), 677-687. PMID: 35835867.

Meng, F.; Xu, C.;  Park, K. S.; Kaniskan, H. U.*; Wang, G. G.* Jin, J.*; Discovery of a First-in-Class Degrader for Nuclear Receptor Binding SET Domain Protein 2 (NSD2) and Ikaros/Aiolos. Journal of Medicinal Chemistry. 2022, 65(15), 10611-10625. PMID: 35895319.

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 & Disease. 2022, 13(6), 551. PMID: 35710782

Park, K. S.; Xiong, Y.*; Yim, H.; Velez, J.; Babault, N.; Kumar, P.; Liu, J.; Jin, J.*; Discovery of the First-in-Class G9a/GLP Covalent Inhibitors. Journal of Medicinal Chemistry. 2022, 65(15), 10506-10522. PMID: 35763668.

Liu, J.; Yu, X.; Chen, H.; Kaniskan H. Ü.; Xie, L.; Chen, X.; Jin, J*.; Wei, W*.; TF-DUBTACs Stabilize Tumor Suppressor Transcription Factors. Journal of the American Chemical Society. 2022, 144(28), 12934-12941. PMID: 35786952.

Dale, B.; Anderson, C.; Park, K. S.; Kaniskan H. U.; Ma, A.; Shen Y.; Zhang, C.; Xie, L.; Chen, X.; Yu, X.*; Jin, J.*; Targeting Triple-Negative Breast Cancer by a Novel Proteolysis Targeting Chimera Degrader of Enhancer of Zeste Homolog 2. ACS Pharmacol. Transl. Sci. 2022, 5, 7, 491–507. PMID: 358337138.

Yu, X.; Cheng, M.; Lu, K.; Shen, Y.; Zhong, Y.; Liu, J.; Xiong, Y.; Jin, J.*; Exploring Degradation of Mutant and Wild-Type Epidermal Growth Factor Receptors Induced by Proteolysis-Targeting Chimeras. J. Med. Chem. 2022, 65(12), 8416-8443. PMID: 35675209.

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, 18(8), 821-830. PMID: 35578032.

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, 41(24), 3328-3340. PMID: 35525905.

Xu, C.;  Meng, F.;  Park, K. S.;  Storey, A. J.;  Gong, W.; Tsai, Y. H.;  Gibson, E.;  Byrum, S. D.; Li, D.;  Edmondson, R. D.;  Mackintosh, S. G.;  Vedadi, M.; Cai, L.;  Tackett, A. J.;  Kaniskan, H. U.;  Jin, J.*; Wang, G. G.* A NSD3-targeted PROTAC suppresses NSD3 and cMyc oncogenic nodes in cancer cells. Cell Chem. Biol. 2022, 29, 386-397.e9. PMID: 34469831.

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. PMID: 35217626

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.

Yu, X.; Xu, J.; Shen, Y.; Cahuzac, K.; Park, K.; Dale, B.; Liu, J.*; Parsons, R.*; Jin, J.* Discovery of potent, selective, and in vivo efficacious AKT kinase protein degraders via structure-activity relationship studies. J. Med. Chem. 2022, 65, 3644-3666. PMID: 35119851

Cao Tao, Martini Michael L., Park Kwang-Su, Kaniskan H. Ümit and Jin Jian, Pyrimidines and Their Benzo Derivatives. In: Black, David StC, Cossy, Janine and Stevens, Christian V. Eds., Comprehensive Heterocyclic Chemistry IV, Elsevier, 2022, 86-228.

 

2021

Yu, X.; Xu, J.; Xie, L.; Wang, L.; Shen, Y.; Cahuzac, K.; Chen, X.; Liu, J.*; Parsons, R.*; Jin, J.* Design, Synthesis and Evaluation of Potent, Selective and Bioavailable AKT Kinase Degraders. J. Med. Chem. 2021, 64, 18054-18081. PMID: 34855399.

Yang, X.;  Wang, X.;  Li, Z.;  Duan, S.;  Li, H.;  Jin, J.;  Zhang, Z.; Gu, W., An unexpected role for Dicer as a reader of the unacetylated DNA binding domain of p53 in transcriptional regulation. Sci. Adv. 2021, 7, eabi6684. PMID: 34705508, PMCID: PMC8550248.

Kusakabe, Y.;  Chiba, T.;  Oshima, M.;  Koide, S.;  Rizq, O.;  Aoyama, K.;  Ao, J.;  Kaneko, T.;  Kanzaki, H.;  Kanayama, K.;  Maeda, T.;  Saito, T.;  Nakagawa, R.;  Kobayashi, K.;  Kiyono, S.;  Nakamura, M.;  Ogasawara, S.;  Suzuki, E.;  Nakamoto, S.;  Yasui, S.;  Mikata, R.;  Muroyama, R.;  Kanda, T.;  Maruyama, H.;  Kato, J.;  Mimura, N.;  Ma, A.;  Jin, J.;  Zen, Y.;  Otsuka, M.;  Kaneda, A.;  Iwama, A.; Kato, N., EZH1/2 inhibition augments the anti-tumor effects of sorafenib in hepatocellular carcinoma. Sci. Rep. 2021, 11, 21396.  PMID: 34725436, PMCID: PMC8560765.

Herviou, L.;  Ovejero, S.;  Izard, F.;  Karmous-Gadacha, O.;  Gourzones, C.;  Bellanger, C.;  De Smedt, E.;  Ma, A.;  Vincent, L.;  Cartron, G.;  Jin, J.;  De Bruyne, E.;  Grimaud, C.;  Julien, E.; Moreaux, J., Targeting the methyltransferase SETD8 impairs tumor cell survival and overcomes drug resistance independently of p53 status in multiple myeloma. Clinical Epigenetics 2021, 13, 174. PMID:34530900, PMCID: PMC8447659.

Liu, L.;  Dattaroy, D.;  Simpson, K. F.;  Barella, L. F.;  Cui, Y.;  Xiong, Y.;  Jin, J.;  Konig, G. M.;  Kostenis, E.;  Roman, J. C.;  Kaestner, K. H.;  Doliba, N. M.; Wess, J., Gq signaling in alpha cells is critical for maintaining euglycemia. JCI Insight 2021, 6, e152852. PMID: 34752420.

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. PMCID: PMC8500670.

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.

Li, M. Y.;  Flora, P.; Pu, H.;  Bar, C.;  Silva, J.; Cohen, I.;  Galbo, P. M., Jr.;  Liu, H.;  Yu, X.; Jin, J.;  Koseki, H.;  D’Orazio, J. A.;  Zheng, D.; Ezhkova, E.* UV-induced reduction in Polycomb repression promotes epidermal pigmentation. Dev. Cell 2021, 56, 2547-2561.e8. PMID: 34473941.

 Chen, H.;  Liu, J.;  Kaniskan, H. U.;  Wei, W.*; Jin, J*. Folate-Guided Protein Degradation by Immunomodulatory Imide Drug-Based Molecular Glues and Proteolysis Targeting Chimeras. J. Med. Chem. 2021, 64,12273-12285. PMID: 34378936, PMCID: PMC8409242.

Su, H.;Jiang, M.;  Senevirathne, C.;  Aluri, S.; Zhang, T.;  Guo, H.;  Xavier-Ferrucio, J.;  Jin, S.; Tran, N. T.;  Liu, S. M.;  Sun, C. W.; Zhu, Y.;  Zhao, Q.;  Chen, Y.; Cable, L.;  Shen, Y.;  Liu, J.; Qu, C. K.;  Han, X.;  Klug, C. A.; Bhatia, R.;  Chen, Y.;  Nimer, S. D.; Zheng, Y. G.;  Iancu-Rubin, C.;  Jin, J.;  Deng, H.; Krause, D. S.;  Xiang, J.;  Verma, A.; Luo, M.; Zhao, X., Methylation of dual-specificity phosphatase 4 controls cell differentiation. Cell Reports 2021, 36, 109421. PMID: 34320342.

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.

Devkota, K., Schapira, M., Perveen, S., Khalili Yazdi, A., Li, F., Chau, I., Ghiabi, P., Hajian, T., Loppnau, P., Bolotokova, A., Satchell, K. J. F., Wang, K., Li, D., Liu, J., Smil, D., Luo, M., Jin, J., Fish, P. V., Brown, P. J., & Vedadi, M. Probing the SAM Binding Site of SARS-CoV-2 Nsp14 In Vitro Using SAM Competitive Inhibitors Guides Developing Selective Bisubstrate Inhibitors. SLAS DISCOVERY: Advancing the Science of Drug Discovery. 2021, 26, 1200-1211. PMID: 34192965, PMCID: PMC8458670

Pryce, K. D.; Kang, H. J.;  Sakloth, F.;  Liu, Y.; Khan, S.;  Toth, K.;  Kapoor, A.; Nicolais, A.;  Che, T.;  Qin, L.; Bertherat, F.;  Kaniskan, H. U.;  Jin, J.;  Cameron, M. D.;  Roth, B. L.; Zachariou, V.; Filizola, M., A promising chemical series of positive allosteric modulators of the mu-opioid receptor that enhance the antinociceptive efficacy of opioids but not their adverse effects. Neuropharmacology 2021, 195, 108673. PMID: 34153316.

Dale, B.; Cheng, M.; Park, K.-S.; Kaniskan, H. Ü.; Xiong, Y.*; Jin, J*. Advancing targeted protein degradation for cancer therapy. Nature Reviews Cancer 2021, 21, 638-654. PMID: 34131295, PMCID: PMC8463487.

Liu, J.;  Chen, H.;  Kaniskan, H. U.;  Xie, L.;  Chen, X.; Jin, J.*; Wei, W.* TF-PROTACs enable targeted degradation of transcription factors. J. Am. Chem. Soc. 2021, 143, 8902-8910. PMID: 34100597.

Luise, C.; Robaa, D.; Regenass, P.; Maurer, D.; Ostrovskyi, D.; Seifert, L.; Bacher, J.; Burgahn, T.; Wagner, T.; Seitz, J.; Greschik, H.; Park, K.-S.; Xiong, Y.; Jin, J.; Schüle, R.; Breit, B.; Jung, M.; Sippl, W. Structure-based design, docking and binding free energy calculations of A366 derivatives as spindlin1 inhibitors. Int. J. Mol. Sci.2021, 22, 5910. PMID: 34072837.

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.

Shen, Y.;  Li, F.;  Szewczyk, M. M.;  Halabelian, L.;  Chau, I.;  Eram, M. S.; Dela Sena, C.;  Park, K. S.;  Meng, F.; Chen, H.;  Zeng, H.;  McLeod, D.; Zepeda-Velazquez, C. A.; Campbell, R. M.;  Mader, M. M.;  Watson, B. M.;  Schapira, M.; Arrowsmith, C. H.;  Al-Awar, R.;  Barsyte-Lovejoy, D.;  Kaniskan, H. U.;  Brown, P. J.*;  Vedadi, M.*; Jin, J.* A First-in-Class, Highly Selective and Cell-Active Allosteric Inhibitor of Protein Arginine Methyltransferase 6. J. Med. Chem. 2021, 64, 3697-3796. PMID: 33591753, PMCID: PMC8035306.

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 2021, 109, 257-272. PMID:33238137, PMCID: PMC7855384.

Vatansever, S.; Schlessinger, A.; Wacker, D.; Kaniskan, H.; Jin, J.; Zhou, M.; Zhang, B.* Artificial intelligence and machine learning-aided drug discovery in central nervous system diseases: State-of-the-arts and future directions. Med. Res. Rev. 2021, 41, 1427-1473. PMID: 33295676, PMCID: PMC8043990.

 

2020

Hu, J.;  Wei, J.; Yim, H.;  Wang, L.;  Xie, L.; Jin, M. S.;  Kabir, M.;  Qin, L.; Chen, X.;  Liu, J.*; Jin, J.* Potent and selective mitogen-cctivated protein kinase kinase 1/2 (MEK1/2) heterobifunctional small-molecule degraders. J. Med. Chem. 2020, 63, 15883-15905. PMID: 33284613,  PMCID: PMC7770057.

Shen, Y.;  Gao, G.; Yu, X.;  Kim, H. S.;  Wang, L.;  Xie, L.;  Schwarz, M.;  Chen, X.;  Guccione, E.;  Liu, J.*;  Bedford, M. T.*; Jin, J.* Discovery of First-in-class Protein Arginine Methyltransferase 5 (PRMT5) Degraders. J. Med. Chem. 2020, 63, 9977-9989. PMID: 32787082,  PMCID: PMC7486226.

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, 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.

Shen, Y.;Li, F.;Szewczyk, M.; Halabelian, L.; Park, K –S.; Chau, L.; Dong, A.; Zeng, H.; Chen, H.; Meng, F.; Barsyte-Lovejoy, D.; Arrowsmith, C.; Brown, P.; Liu, J.*; Vedadi, M.*; Jin, J.* Discovery of a First-in-class Protein Arginine Methyltransferase 6 (PRMT6) Covalent Inhibitor. J. Med. Chem. 2020, 63, 10, 5477–5487. PMID: 32367723, PMCID: PMC7286362.

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.

Cheng, M.; Yu, X.*; Lu, K.; Xie, L.; Wang, L.; Meng, F.; Han, X.; Chen, X.; Liu, J.; Xiong, Y.*; Jin, J.* Discovery of Potent and Selective Epidermal Growth Factor Receptor (EGFR) Bifunctional Small-molecule Degraders. J. Med. Chem. 2020, 63, 3, 1216-1232. PMID: 31895569, PMCID: PMC7318554.

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.

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(2), 306-325. PMID:31776131, PMCID: PMC7271978.

 

2019

Wei, J.; Hu, J.; Wang, L.; Xie, L.; Jin, M. S.; Chen, X.; Liu, J.* and Jin, J.* Discovery of a First-in-Class Mitogen-Activated Protein Kinase Kinase 1/2 Degrader. J. Med. Chem. 2019, 62(23), 10897-10911. PMID: 31712774, PMCID: In progress.

Bott, A. J.; Shen, J.; Tonelli, C.; Zhan, L.; Sivaram, N.; Jiang, Y. P.; Yu, X.; Bhatt, V.; Chiles, E.; Zhong, H.; Maimouni, S.; Dai, W.; Velasquez, S.; Pan, J. A.; Muthalagu, N.; Morton, J.; Anthony, T. G.; Feng, H.; Lamers, W. H.; Murphy, D. J.; Guo, J. Y.; Jin, J.; Crawford, H. C.; Zhang, L.; White, E.; Lin, R. Z.; Su, X.; Tuveson, D. A.; Zong, W. X.* Glutamine Anabolism Plays a Critical Role in Pancreatic Cancer by Coupling Carbon and Nitrogen Metabolism. Cell Reports 2019, 29(5):1287-1298.e6. PMID: 31665640, PMCID: PMC6886125.

Martini, M. L.*; Neifert, S. N.; Mocco, J.; Panov, F.; Tse, W.; Walker, R. H.; Jin, J.; Gupta, F. Recent Advances in the Development of Experimental Therapeutics for Levodopa-Induced Dyskinesia. J Mov Disord. 2019, 12(3): 161–165. PMID: 31556261, PMCID: PMC6763722.

Rizk, M.; Rizq, O.; Oshima, M.; Nakajima-Takagi, Y.; Koide, S.; Saraya, A.; Isshiki, Y.; Chiba, T.; Yamazaki, S.; Ma, A.; Jin, J.; Iwama, A.*; Mimura, N.* Akt Inhibition Synergizes with PRC2 Inhibition in the Treatment of Multiple Myeloma. Cancer Science 2019, 00, 1-13. PMID: 31571328, PMCID: PMC6890440.

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.

Fagan, V.; Johansson, C.; Gileadi, C.; Monteiro, O.; Dunford, J. E.; Nibhani, R.; Philpott, M.; Malzahn, J.; Wells, G.; Farham, R.; Cribbs, A.; Halidi, N.; Li, F.; Chau, I.; Greschik, H.; Velupillai, S.; Allali-Hassani, A.; Bennett, J. M.; Christott, T.; Giroud, C.; Lewis, A. M.; Huber, K. V. M.; Athanasou, N.; Bountra, C.; Jung, M.; Schüle, R.; Vedadi, M.; Arrowsmith, C. H.; Xiong, Y.; Jin, J.; Fedorov, O.; Farnie, G.; Brennan, P. E.*; Oppermann, U. C. T.* A Chemical Probe for Tudor Domain Protein Spindlin1 to Investigate Chromatin Function. J. Med. Chem. 2019. 62, 20, 9008-9025. PMID: 31550156, PMCID: in progress.

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.

Wrobel, J. A.; Xie, L.; Wang, L.; Liu, C.; Rashid, N.; Gallagher, K. K.; Xiong ,Y.; Konze, K. D.; Jin, J.; Gatza, M. L.; Chen, X.* Multi-omic Dissection of Oncogenically Active Epiproteomes Identifies Drivers of Proliferative and Invasive Breast Tumors. iScience 2019, 17, 359-378. PMID: 31336272, PMCID: PMC6660457

Ren, Z.; Ahn, J. H.; Liu, H.; Tsai, Y. H.; Bhanu, N. V.; Koss, B.; Allison, D. F.; Ma, A.; Storey, A. J.; Wang, P.; Mackintosh, S. G.; Edmondson, R. D.; Groen, R. W. J.; Martens, A. C.; Garcia, B. A.; Tackett, A. J.; Jin, J.; Cai, L.; Zheng, D.; Wang, G. G.* PHF19 promotes multiple myeloma tumorigenicity through PRC2 activation. Blood 2019, 134, 1176-1189. PMID: 31383640. PMCID: : PMC6776795.

Zhu, Y.; He, X.; Lin, Y. C.; Dong, H.; Zhang, L.; Chen, X.; Wang, Z.; Shen, Y.; Li, M.; Wang, H.; Sun, J.; Nguyen, L. X.; Zhang, H.; Jiang, W.; Yang, Y.; Chen, J.; Müschen, M.; Chen, C. W.; Konopleva, M. Y.; Sun, W.; Jin, J.; Carlesso, N.; Marcucci, G.; Luo, Y.; Li, L.* Targeting PRMT1-Mediated FLT3 Methylation Disrupts Maintenance of MLL- rearranged Acute Lymphoblastic Leukemia. Blood 2019, 134(15), 1257-1268. PMID: 31395602. PMCID: PMC6788006.

Martini, M. L.; Ray, C.; Yu, X.; Liu, J.; Pogorelov, V.; Wetsel, W. C.; Huang, X. P.; McCorvy, J.*; Caron, M. G.*; Jin, J.* Designing Functionally Selective Non-Catechol Dopamine D1 Receptor Agonists with Potent In Vivo Antiparkinsonian Activity. ACS Chem Neurosci 2019, 10, 4160-4182. PMID: 31387346. PMCID: PMC6785188.

Li, M. T.; Liang, J. Y.; Sun, Y.P.; Jin, J.; Xiong, Y.; Guan, K. L.; Yuan, H. X.* ELP3 acetyltransferase is phosphorylated and regulated by the oncogenic anaplastic lymphoma kinase (ALK). Biochem J, 2019, 476(15), 2239-2254. PMID: 31341009. PMCID: in progress.

Yu, X.; Huang, X. -P.; Kenakin, T.;  Slocum, S.; Chen, X.; Martini, M.; Liu, J.*; Jin, J.* Design, Synthesis and Characterization of Ogerin-Based Positive Allosteric Modulators for G Protein-Coupled Receptor 68 (GPR68). J. Med. Chem. 2019, 62(16), 7557-7574. PMID: 31298539, PMCID: PMC6923801.

Gao, Y.; Haren, M.; Moret, E. E.; Rood, J. J. M.; Sartini, D.; Salvucci, A.; Emanuelli, M.; Carveur, P.; Babault, N.; Jin, J.; Martin, N. I.* Bisubstrate Inhibitors of Nicotinamide N- Methyltransferase (NNMT) with Enhanced Activity. J. Med. Chem. 2019, 62(14), 6597-6614. PMID: 31265285, PMCID:PMC6713424.

Xiong, Y.; Greschik, H.; Johansson, C.; Seifert, L.; Bacher, J.; Park, K. -S.; Babault, N.; Martini, M.; Fagan, V.; Li, F.; Chau, I.; Christott, T.; Dilworth, D.; Barsyte-Lovejoy, D.; Vedadi, M.; Arrowsmith, C.; Brennan, P.; Fedorov, O.; Jung, M.; Farnie, G.; Liu, J.; Oppermann, U.*; Schüle, R.*; Jin, J.* Discovery of a Potent and Selective Fragment-like Inhibitor of Methyllysine Reader Protein Spindlin 1 (SPIN1). J. Med. Chem. 2019, 62(20), 8996-9007. PMID: 31260300, PMCID: in progress.

He, X.; Zhu, Y.; Lin, Y. -C.; Li, M.; Du, J.; Dong, H.; Sun, D. J.; Zhu, L.; Wang, H.; Ding, Z.; Zhang, Lei.; Zhang, Lianjun.; Zhao, D.; Wang, Z.; Wu, H.; Zhang, H.; Jiang, W.; Xu, Y.; Jin, J.; Shen, Y.; Perry, J.; Zhao, X.; Zhang, B.; Liu, S.; Xue, S. -L.; Shen, B.; Chen, C. -W.; Chen, J.; Khaled, S.; Kuo, Y. -H.; Marcucci, G.; Luo, Y.; Li, L.* PRMT1-mediated FLT3 arginine methylation promotes maintenance of FLT3-ITD+ Acute Myeloid Leukemia. Blood 2019, 134(6), 548-560. PMID: 31217189, PMCID: PMC6688430.

MacDonald, I. A.; Butler, K. V.; Herring, L. E.; Clinkscales, S. E.; Yelagandula, R.; Stecher, K.; Bell, O.; Graves, L. M.; Jin, J.; Hathaway, N. A.* Pathway-Based High-Throughput Chemical Screen Identifies Compounds That Decouple Heterochromatin Transformations. SLAS DISCOVERY: Advancing Life Sciences R&D. May 2019. PMID:31145866, PMCID: PMC6893849.

Chen, S.; Wiewiora, R. P.; Meng, F.; Babault, N.; Ma, A.; Yu, W.; Qian, K.; Hu, H.; Zou, H.; Wang, J.; Fan, S.; Blum, G.; Pittella-Silva, F.; Beauchamp, K. A.; Tempel, W.; Jiang, H.; Chen, K.; Skene, R. J.; Zheng, Y. G.; Brown, P. J.; Jin, J.; Luo, C.*; Chodera, J. D.*; Luo, M.* The Dynamic Conformational Landscape of the Protein Methyltransferase SETD8. eLife 2019, 8, e45403. PMID : 31081496, PMCID:PMC6579520.

MacNevin, C. J.; Watanabe, T.; Weitzman, M.; Gulyani, A.; Fuehrer, S.; Pinkin, N. K.; Tian, X.; Liu, F.; Jin, J.; Hahn, K. M.* Membrane-permeant, environment-sensitive dyes generate biosensors within living cells. J. Am. Chem. Soc. 2019, 141(18), 7275-7282. PMID:30994345, PMCID:PMC6572722.

Shen, Y.; McCorvy, J. D.; Martini, M. L.; Rodriguiz, R. M.; Progorelov, V. M.; Ward, K. M.; Wetsel, W. C.; Liu, J.*; Roth, B. L.*; Jin, J.* D2 Dopamine Receptor G protein-biased Partial Agonists Based on Cariprazine. J. Med. Chem. 2019, 62(9), 4755-4771. PMID:30964661, PMCID: PMC6509010.

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. Nature Communications 2019, 10(1), 1436. PMID: 30926792, PMCID : PMC6441108.

Veo, B.; Danis, E.; Pierce, A.; Sola, I.; Wang, D.; Foreman, N. K.; Jin, J.; Ma, A.; Serkova, N.; Venkataraman, S.; Vibhakar, R.* Combined functional genomic and chemical screens identify SETD8 as a therapeutic target in MYC-driven medulloblastoma. JCI Insight 2019, 4(1), e122933. PMID: 30626740, PMCID:PMC6485357.

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. Nature Communications 2019, 10, 19. PMID:30604761, PMCID:PMC6318333.

Allen, D. C.; Carlson, T. L.; Xiong, Y.; Jin, J.; Grant, K. A.; Cuzon Carlson, V. C.* A comparative study of the pharmacokinetics of clozapine N-oxide and clozapine N-oxide hydrochloride salt in rhesus macaques. Journal of Pharmacology and Experimental Therapeutics 2019, 368(2), 199-207, PMID: 30523062, PMCID:PMC6337003.

2018

Chiarella, A. M.; Wang, T. A.; Butler, K. V.; Jin, J.; Hathaway, N. A.* Repressing Gene Transcription by Redirecting Cellular Machinery with Chemical Epigenetic Modifiers. J Vis Exp 2018, 139, e58222. PMID: 30295665, PMCID: PMC6235244

Zhao, N.; Sebastiano, V.; Moshkina, N.; Mena, N.; Hultquist, J.; Jimenez-Morales, D.; Ma, Y.; Rialdi, A.; Albrecht, R.; Fenouil, R.; Sánchez-Aparicio, M. T.; Ayllon, J.; Ravisankar, S.; Haddad, B.; Ho, J. S. Y.; Low, D.; Jin, J.; Yurchenko, V.; Prinjha, R. K.; Tarakhovsky, A.; Squatrito, M.; Pinto, D.; Allette, K.; Byun, M.; Smith, M. L.; Sebra, R.; Guccione, E.; Tumpey, T.; Krogan, N.; Greenbaum, B.; van Bakel, H.; García-Sastre, A.; Marazzi, I.* Influenza virus infection causes global RNAPII termination defects. Nature Structural & Molecular Biology 2018, 25, 885-893. PMID: 30177761,  PMCID: in progress.

McCorvy, J. D.*; Wacker, D.; Wang, S.; Agegnehu, B.; Liu, J.; Lansu, K.; Tribo, A. R.; Olsen, R. H. J.; Che, T.; Jin, J.; Roth, B. L.* Structural determinants of 5-HT2B receptor activation and biased agonism. Nature Structural & Molecular Biology 2018, 25, 787-796. PMID: 30127358,  PMCID: PMC6237183.

Thompson, K. J.; Khajehali, E.; Bradley, S. J.; Navarrete, J. S.; Huang, X.-P.; Slocum, S.; Jin, J.; Liu, J.; Xiong, Y.; Olsen, R.; DiBerto, J.; Boyt, K. M.; Pina, M. M.; Pati, D.; Molloy, C.; Bundgaard, C.; Sexton, P. M.; Kash, T. L.; Krashes, M. J.; Christopoulos, A.; Roth, B. L.*; Tobin, A. B.* DREADD Agonist 21 Is an Effective Agonist for Muscarinic-Based DREADDs in Vitro and in Vivo ACS Pharmacology & Translational Science 2018, 1, 61-72. PMID:30868140, PMCID:PMC6407913.

Pellock, S. J.; Creekmore, B. C.; Walton, W. G.; Mehta, N.; Biernat, K. A.; Cesmat, A. P.; Ariyarathna, Y.; Dunn, Z. D.; Li, B.; Jin, J.; James, L. I.; Redinbo, M. R.* Gut Microbial β-Glucuronidase Inhibition via Catalytic Cycle Interception. ACS Central Science 2018, 4, 868-879. PMID:30062115, PMCID: PMC6062831.

Zhang, C.; Han, X.-R.; Yang, X.; Jiang, B.; Liu, J.*; Xiong, Y.*; Jin, J.* Proteolysis Targeting Chimeras (PROTACs) of Anaplastic Lymphoma Kinase (ALK). European Journal of Medicinal Chemistry 2018, 151, 304-314. PMID: 29627725,  PMCID: PMC5924614.

Zhang, T.; Wu, J.; Ungvijanpunya, N.; Jackson-Weaver, O.; Gou, Y.; Feng, J.; Ho, T. V.; Shen, Y.; Liu, J.; Richard, S.; Jin, J.; Hajishengallis, G.; Chai, Y.; Xu, J.* Smad6 Methylation Represses NFκB Activation and Periodontal Inflammation. Journal of Dental Research 2018, 7, 810-819. PMID: 29420098, PMCID: PMC6728583.

Wang, D.-y.; Kosowan, J.; Samsom, J.; Leung, L.; Zhang, K.-l.; Li, Y.-x.; Xiong, Y.; Jin, J.; Petronis, A.; Oh, G.; Wong, A. H. C.* Inhibition of the G9a/GLP histone methyltransferase complex modulates anxiety-related behavior in mice. Acta Pharmacologica Sinica 2018, 39, 866-874. PMID: 29417943,  PMCID: PMC5943902.

Babault, N.; Allali-Hassani, A.; Li, F.; Fan, J.; Yue, A.; Ju, K.; Liu, F.*; Vedadi, M.*; Liu, J.*; Jin, J.* Discovery of Bisubstrate Inhibitors of Nicotinamide N-Methyltransferase (NNMT). Journal of Medicinal Chemistry 2018, 61, 1541-1551. PMID: 29320176, PMCID: PMC5823789.

Kaniskan, H. Ü.; Eram, M. S.; Zhao, K.; Szewczyk, M. M.; Yang, X.; Schmidt, K.; Luo, X.; Xiao, S.; Dai, M.; He, F.; Zang, I.; Lin, Y.; Li, F.; Dobrovetsky, E.; Smil, D.; Min, S.-J.; Lin-Jones, J.; Schapira, M.; Atadja, P.; Li, E.; Barsyte-Lovejoy, D.; Arrowsmith, C. H.; Brown, P. J.; Liu, F.*; Yu, Z.*; Vedadi, M.*; Jin, J.* Discovery of Potent and Selective Allosteric Inhibitors of Protein Arginine Methyltransferase 3 (PRMT3). Journal of Medicinal Chemistry 2018, 61, 1204-1217. PMID: 29244490, PMCID: PMC5808361.

Morini, M. F.; Giampietro, C.; Corada, M.; Pisati, F.; Lavarone, E.; Cunha, S. I.; Conze, L. L.; O’Reilly, N. J.; Joshi, D.; Kjaer, S.; George, R.; Nye, E.; Ma, A.; Jin, J.; Mitter, R.; Lupia, M.; Cavallaro, U.; Pasini, D.; Calado, D. P.; Dejana, E.*; Taddei, A.* VE-Cadherin-Mediated Epigenetic Regulation of Endothelial Gene Expression. Circulation Research 2018, 122, 231-245. PMID: 29233846, PMCID: PMC5771688.

McCorvy, J. D.; Butler, K. V.; Kelly, B.; Rechsteiner, K.; Karpiak, J.; Betz, R. M.; Kormos, B. L.; Shoichet, B. K.; Dror, R. O.*; Jin, J.*; Roth, B. L.* Structure-inspired design of β-arrestin-biased ligands for aminergic GPCRs. Nature Chemical Biology 2018, 14, 126-134. PMID: 29227473, PMCID: PMC5771956.

Butler, K. V.;  Chiarella, A. M.; Jin, J. *; Hathaway N. A.* Targeted Gene Repression Using Novel Bifunctional Molecules to Harness Endogenous Histone Deacetylation Activity ACS Synth. Biol. 2018, 7, 38-45. PMID: 29073761, PMCID: PMC5775041.

Kaniskan, H. Ü.*; Martini, M. L.; Jin, J.* Inhibitors of Protein Methyltransferases and Demethylases. Chemical Reviews 2018, 118, 989-1068. PMID: 28338320, PMCID: PMC5610952.

 2017

Alzrigat, M.*; Párraga, A. A.; Majumder, M. M.; Ma, A.; Jin, J.; Österborg, A.; Nahi, H.; Nilsson, K.; Heckman, C. A.; Öberg, F.; Kalushkova A.; Jernberg-Wiklund H.* The polycomb group protein BMI-1 inhibitor PTC-209 is a potent anti-myeloma agent alone or in combination with epigenetic inhibitors targeting EZH2 and the BET bromodomains Oncotarget 2017, 8, 103731–103743. PMID: 2829262596  PMCID: PMC5732762

Butler, K. V.; MacDonald, I. A.; Hathaway, N. A.; Jin, J.* Report And Application Of A Tool Compound Dataset. Journal of Chemical Information and Modeling 2017, 57, 2699–2706. PMID: 29035535  PMCID: PMC5705340

Xiong, Y.; Li, F.; Babault, N.; Wu, H.; Dong, A.; Zeng, H.; Chen, X.; Arrowsmith, C. H.; Brown, P. J.; Liu, J.; Vedadi, M.*; Jin, J.* Structure-Activity Relationship studies of G9a-Like protein (GLP) inhibitors. Bioorganic & Medicinal Chemistry 2017, 25, 4414-4423. PMID: 28662962  PMCID: PMC5562403

Kaniskan, H. Ü.*; Jin, J.* Recent progress in developing selective inhibitors of protein methyltransferases. Current Opinion in Chemical Biology 2017, 39, 100-108. PMID: 28662389  PMCID: PMC5624721

Rizq, O.; Mimura, N.*; Oshima, M.; Saraya, A.; Koide, S.; Kato, Y.; Aoyama, K.; Nakajima-Takagi, Y.; Wang, C.; Chiba, T.; Ma, A.; Jin, J.; Iseki, T.; Nakaseko, C.; Iwama, A.* Dual inhibition of EZH2 and EZH1 sensitizes PRC2-dependent tumors to proteasome inhibition. Clinical Cancer Research 2017, 23, 4817-4830. PMID: 28490465 PMCID: PMC5562278

Jain, R.; Butler, K. V.; Coloma, J.; Jin, J.; Aggarwal, A. K.* Development of a S-adenosylmethionine analog that intrudes the RNA-cap binding site of Zika methyltransferase. Scientific Reports 2017, 7, 1632. PMID: 28487506  PMCID: PMC5431627

Lansu, K.; Karpiak, J.; Liu, J.; Huang, X.-P.; McCorvy, J. D.; Kroeze, W. K.; Che, T.; Nagase, H.; Carroll, F. I.; Jin, J.; Shoichet, B. K.; Roth, B. L.* In silico design of novel probes for the atypical opioid receptor MRGPRX2. Nat. Chem. Biol. 2017, 13, 529-536. PMID: 28288109  PMCID: PMC5391270

Beak, J. Y.; Huang, W.; Parker, J. S.; Hicks, S. T.; Patterson, C.; Simpson, P. C.; Ma, A.; Jin, J.; Jensen, B. C.* An Oral Selective Alpha-1A Adrenergic Receptor Agonist Prevents Doxorubicin Cardiotoxicity. JACC: Basic to Translational Science 2017, 2, 39-53. PMID: 28286875  PMCID: PMC5343290

Huang, Q.; He, S.; Tian, Y.; Gu, Y.; Chen, P.; Li, C.; Huang, J.; Liu, Y.; Yu, H.; Jin, M.; Hu, S.; Tong, Q.; Ma, A.; Jin, J.; Hexner, E.; Fung, H.; Reshef, R.; Zhang, Y.*; Zhang, Y.* Hsp90 inhibition destabilizes Ezh2 protein in alloreactive T cells and reduces graft-versus-host disease in mice. Blood 2017, 129, 2737-2748. PMID:28246193  PMCID: PMC5437825

Xiong, Y.; Li, F.; Babault, N.; Dong, A.; Zeng, H.; Wu, H.; Chen, X.; Arrowsmith, C. H.; Brown, P. J.; Liu, J.; Vedadi, M.*; Jin, J.* Discovery of Potent and Selective Inhibitors for G9a-Like Protein (GLP) Lysine Methyltransferase. J. Med. Chem. 2017, 60, 1876-1891. PMID: 28135087  PMCID: PMC5352984

Veschi, V.; Liu, Z.; Voss, T. C.; Ozbun, L.; Gryder, B.; Yan, C.; Hu, Y.; Ma, A.; Jin, J.; Mazur, S. J.; Lam, N.; Souza, B. K.; Giannini, G.; Hager, G. L.; Arrowsmith, C. H.; Khan, J.; Appella, E.; Thiele, C. J.* Epigenetic siRNA and Chemical Screens Identify SETD8 Inhibition as a Therapeutic Strategy for p53 Activation in High-Risk Neuroblastoma. Cancer Cell 2017, 31, 50-63. PMID: 28073004  PMCID: PMC5233415

Alzrigat, M.*; Párraga, A. A.; Agarwal, P.; Zureigat, H.; Österborg, A.; Nahi, H.; Ma, A.; Jin, J.; Nilsson, K.; Öberg, F.; Kalushkova, A.; Jernberg-Wiklund, H.* EZH2 inhibition in multiple myeloma downregulates myeloma associated oncogenes and upregulates microRNAs with potential tumor suppressor functions. Oncotarget 2017, 8, 10213-10224. PMID: 28052011  PMCID: PMC5354653

Kim, Y.; Lee, H.-M.; Xiong, Y.; Sciaky, N.; Hulbert, S. W.; Cao, X.; Everitt, J. I.; Jin, J.; Roth, B. L.*; Jiang, Y.-h.* Targeting the histone methyltransferase G9a activates imprinted genes and improves survival of a mouse model of Prader-Willi syndrome. Nat. Med. 2017, 23, 213-222. PMID: 28024084  PMCID: PMC5589073

2016

Urs, N. M.; Gee, S. M.; Pack, T. F.; McCorvy, J. D.; Evron, T.; Snyder, J. C.; Yang, X.; Rodriguiz, R. M.; Borrelli, E.; Wetsel, W. C.; Jin, J.; Roth, B. L.; O’Donnell, P.; Caron, M. G.* Distinct cortical and striatal actions of a β-arrestin–biased dopamine D2 receptor ligand reveal unique antipsychotic-like properties. Proceedings of the National Academy of Sciences 2016, 113, E8178-E8186. PMID: 27911814  PMCID: PMC5167191

Chen, X.; McCorvy, J. D.; Fischer, M. G.; Butler, K. V.; Shen, Y.; Roth, B. L.*; Jin, J.* Discovery of G Protein-biased D2 Dopamine Receptor Partial Agonists. J. Med. Chem. 2016, 59, 10601-10618. PMID: 27805392  PMCID: PMC5148701

Butler, K. V.; Ma, A.; Yu, W.; Li, F.; Tempel, W.; Babault, N.; Pittella-Silva, F.; Shao, J.; Wang, J.; Luo, M.; Vedadi, M.; Brown, P. J.; Arrowsmith, C. H.; Jin, J.* Structure-Based Design of a Covalent Inhibitor of the SET Domain-Containing Protein 8 (SETD8) Lysine Methyltransferase. J. Med. Chem. 2016, 59, 9881-9889. PMID: 27804297  PMCID: PMC5148670

Shen, Y.; Szewczyk, M. M.; Eram, M. S.; Smil, D.; Kaniskan, H. Ü.; de Freitas, R. F.; Senisterra, G.; Li, F.; Schapira, M.; Brown, P. J.; Arrowsmith, C. H.; Barsyte-Lovejoy, D.; Liu, J.*; Vedadi, M.*; Jin, J.* Discovery of a Potent, Selective and Cell-active Dual Inhibitor of Protein Arginine Methyltransferase 4 and Protein Arginine Methyltransferase 6. J. Med. Chem. 2016, 59, 9124-9139. PMID: 27584694  PMCID: PMC5063716

Yang, X.; Li, F.; Konze, K. D.; Meslamani, J.; Ma, A.; Brown, P. J.; Zhou, M.-M.; Arrowsmith, C. H.; Kaniskan, H. Ü.; Vedadi, M.*; Jin, J.* Structure–Activity Relationship Studies for Enhancer of Zeste Homologue 2 (EZH2) and Enhancer of Zeste Homologue 1 (EZH1) Inhibitors. J. Med. Chem. 2016, 59, 7617-7633. PMID: 27468126  PMCID: PMC5003625

Kaniskan, H. U.; Eram, M. S.; Liu, J.; Smil, D.; Martini, M. L.; Shen, Y.; Santhakumar, V.; Brown, P. J.; Arrowsmith, C. H.; Vedadi, M.*; Jin, J.* Design and synthesis of selective, small molecule inhibitors of coactivator-associated arginine methyltransferase 1 (CARM1). MedChemComm 2016, 7, 1793-1796. PMID: 28042453  PMCID: PMC5198778

Rialdi, A., Campisi, L., Zhao, N., Lagda, A. C., Pietzsch, C., Ho, J. S. Y., Martinez-Gil1, L., Fenouil, R., Chen, X., Edwards, M., Metreveli, G., Jordan, S., Peralta, Z., Munoz-Fontela, C., Bouvier, N., Merad, M., Jin, J., Weirauch, M., Heinz, S., Benner, C., van Bake, H., Basler, C., García-Sastre, A., Bukreyev, A., Marazzi, I.* “Topoisomerase 1 inhibition suppresses inflammatory genes and protects from death by inflammation” Science 2016, 352, aad7993. PMID: 27127234  PMCID: PMC5193222

Butler, K. V.;  Bohn, K.;  Hrycyna, C. A.*; Jin, J.* “Non-substrate based, small molecule inhibitors of the human isoprenylcysteine carboxyl methyltransferase” MedChemComm 2016, 7, 1016-1021. PMCID: PMC4990076

Wagner, T.; Greschik, H.; Burgahn, T.; Schmidtkunz, K.; Schott, A.-K.; McMillan, J.; Baranauskienė, L.; Xiong, Y.; Fedorov, O.; Jin, J.; Oppermann, U.; Matulis, D.; Schüle, R.; Jung, M*. “Identification of a small-molecule ligand of the epigenetic reader protein Spindlin1 via a versatile screening platform” Nucleic Acids Research 2016, 44, e88. PMID: 26893353  PMCID: PMC4872087

Agarwal, P.; Alzrigat, M.; Párraga, A. A.; Enroth, S.; Singh, U.; Ungerstedt, J.; Österborg, A.; Brown, P. J.; Ma, A.; Jin, J.; Nilsson, K.; Öberg, F.; Kalushkova, A.*; Jernberg-Wiklund, H*. “Genome-wide profiling of histone H3 lysine 27 and lysine 4 trimethylation in multiple myeloma reveals the importance of Polycomb gene targeting and highlights EZH2 as a potential therapeutic target” Oncotarget 2016, 7, 6809-6823. PMID: 26755663  PMCID: PMC4872750

Eram, M. S.; Shen, Y.; Szewczyk, M.; Wu, H.; Senisterra, G.; Li, F.; Butler, K. V.; Kaniskan, H. Ü.; Speed, B. A.; dela Seña, C.; Dong, A.; Zeng, H.; Schapira, M.; Brown, P. J.; Arrowsmith, C. H.; Barsyte-Lovejoy, D.; Liu, J.*; Vedadi, M.*; Jin, J.* “A Potent, Selective and Cell-active Inhibitor of Human Type I Protein Arginine Methyltransferases” ACS Chemical Biology 2016, 11, 772-781. PMID: 26598975  PMCID: PMC4798913

Park, S. M.; Chen, M.; Schmerberg, C. M.; Dulman, R. S.; Rodriguiz, R. M.; Caron, M. G.; Jin, J.; Wetsel, W. C.* “Effects of [beta]-Arrestin-Biased Dopamine D2 Receptor Ligands on Schizophrenia-like Behavior in Hypoglutamatergic Mice” Neuropsychopharmacology 2016, 41, 704-715. PMID: 26129680  PMCID: PMC4707817

2015

Huang, X.-P.; Karpiak, J.; Kroeze, W. K.; Zhu, H.; Chen, X.; Moy, S. S.; Saddoris, K. A.; Nikolova, V. D.; Farrell, M. S.; Wang, S.; Mangano, T. J.; Deshpande, D. A.; Jiang, A.; Penn, R. B.; Jin, J.; Koller, B. H.; Kenakin, T.; Shoichet, B. K.*; Roth, B. L.* “Allosteric ligands for the pharmacologically dark receptors GPR68 and GPR65” Nature 2015, 527, 477-483. PMID: 26550826  PMCID: PMC4796946

Simon, J. M.; Parker, J. S.; Liu, F.; Rothbart, S. B.; Ait-Si-Ali, S.; Strahl, B. D.; Jin, J.; Davis, I. J.; Mosley, A. L.; Pattenden, S. G.* “A Role for Widely Interspaced Zinc Finger (WIZ) in Retention of the G9a Methyltransferase on Chromatin” Journal of Biological Chemistry, 2015, 290, 26088-26102. PMID: 26338712 PMCID: PMC4646261

Wallace, B. D.; Roberts, A. B.; Pollet, R. M.; Ingle, J. D.; Biernat, K.; Venkatesh, M.K.; Guthrie, L.; O’Neal, S. K.; Robinson, S. J.; Dollinger, M.; Figueroa, E.; McShane, S. R.; Jin, J.; Frye, S. V.; Zamboni, W. C.; Pepe-Ranney, C.; Mani, S.; Kelly, L.; Redinbo, M. R.* “Structure and Inhibition of Microbiome β-Glucuronidases Essential to the Alleviation of Cancer Drug Toxicity” Chemistry & Biology, 2015, 22, 1238-1249. PMID: 26364932 PMCID: PMC4575908

Arrowsmith, C. H.; Audia, J. E.; Austin, C.; Baell, J.; Bennett, J.; Blagg, J.; Bountra, C.; Brennan, P. E.; Brown, P. J.; Bunnage, M. E.; Buser-Doepner, C.; Campbell, R. M.; Carter, A. J.; Cohen, P.; Copeland, R. A.; Cravatt, B.; Dahlin, J. L.; Dhanak, D.; Edwards, A. M.; Frye, S. V.; Gray, N.; Grimshaw, C. E.; Hepworth, D.; Howe, T.; Huber, K. V. M.; Jin, J.; Knapp, S.; Kotz, J. D.; Kruger, R. G.; Lowe, D.; Mader, M. M.; Marsden, B.; Mueller-Fahrnow, A.; Muller, S.; O’Hagan, R. C.; Overington, J. P.; Owen, D. R.; Rosenberg, S. H.; Roth, B.; Ross, R.; Schapira, M.; Schreiber, S. L.; Shoichet, B.; Sundstrom, M.; Superti-Furga, G.; Taunton, J.; Toledo-Sherman, L.; Walpole, C.; Walters, M. A.; Willson, T. M.; Workman, P.; Young, R. N.; Zuercher, W. J. “The promise and peril of chemical probes” Nature Chemical Biology 2015, 11, 536-541. PMID: 26196764  PMCID: PMC4706458

Wang, L.; Xie, L.; Ramachandran, S.; Lee, Y.; Yan, Z.; Zhou, L.; Krajewski, K.; Liu, F.; Zhu, C.; Chen, David J.; Strahl, Brian D.; Jin, J.; Dokholyan, Nikolay V.*; Chen, X.* “Non-canonical Bromodomain within DNA-PKcs Promotes DNA Damage Response and Radioresistance through Recognizing an IR-Induced Acetyl-Lysine on H2AX” Chemistry & Biology 2015, 22, 849-861. PMID: 26119999  PMCID: PMC4695401

Xu, B.; Konze, K. D.; Jin, J.; Wang, G. G.* “Targeting EZH2 and PRC2 dependence as novel anti-cancer therapy” Experimental Hematology 2015, 43, 698-712. PMID: 26027790  PMCID: PMC4706459

Abou El Hassan, M.; Huang, K.; Eswara, M. B. K.; Zhao, M.; Song, L.; Yu, T.; Liu, Y.; Liu, J. C.; McCurdy, S.; Ma, A.; Wither, J.; Jin, J.; Zacksenhaus, E.; Wrana, J. L.; Bremner, R.* “Cancer Cells Hijack PRC2 to Modify Multiple Cytokine Pathways” PLoS ONE 2015, 10, e0126466. PMID: 26030458  PMCID: PMC4450877

Stuhlmiller, Timothy J.; Miller, Samantha M.; Zawistowski, Jon S.; Nakamura, K.; Beltran, Adriana S.; Duncan, James S.; Angus, Steven P.; Collins, Kyla A. L.; Granger, Deborah A.; Reuther, Rachel A.; Graves, Lee M.; Gomez, Shawn M.; Kuan, P.-F.; Parker, Joel S.; Chen, X.; Sciaky, N.; Carey, Lisa A.; Earp, H. S.; Jin, J.; Johnson, Gary L.* Inhibition of Lapatinib-Induced Kinome Reprogramming in ERBB2-Positive Breast Cancer by Targeting BET Family Bromodomains. Cell Reports 2015, 11, 390-404. PMID: 25865888  PMCID: PMC4408261

Kaniskan, H. Ü.; Szewczyk, M. M.; Yu, Z.; Eram, M. S.; Yang, X.; Schmidt, K.; Luo, X.; Dai, M.; He, F.; Zang, I.; Lin, Y.; Kennedy, S.; Li, F.; Dobrovetsky, E.; Dong, A.; Smil, D.; Min, S.-J.; Landon, M.; Lin-Jones, J.; Huang, X.-P.; Roth, B. L.; Schapira, M.; Atadja, P.; Barsyte-Lovejoy, D.; Arrowsmith, C. H.; Brown, P. J.; Zhao, K.*; Jin, J.*; Vedadi, M.* “A Potent, Selective and Cell-Active Allosteric Inhibitor of Protein Arginine Methyltransferase 3 (PRMT3)” Angewandte Chemie International Edition 2015, 54, 5166-5170. PMID: 25728001  PMCID: PMC4400258

Chen, X.; Choo, H.; Huang, X.-P.; Yang, X.; Stone, O.; Roth, B. L.*; Jin, J.* “The First Structure-activity Relationship Studies for Designer Receptors Exclusively Activated by Designer Drugs (DREADDs)” ACS Chemical Neuroscience 2015, 6, 476-484. PMID: 25587888  PMCID: PMC4368042

Kaniskan, H. Ü.; Konze, K.D.; Jin, J.* “Selective Inhibitors of Protein Methyltransferases” J. Med. Chem. 2015, 58, 1596-1629. PMID: 25406853  PMCID: PMC4345896

Kaniskan, H. Ü.; Jin, J.* “Chemical Probes of Histone Lysine Methyltransferases” ACS Chem. Biol. 2015, 10, 40-50. PMID: 25423077  PMCID: PMC4301070

Xu, B.; On, D. M.; Ma, A.; Parton, T.; Konze, K.D.; Pattenden, S. G.; Allison, D.F.; Cai, L.; Rockowitz, S.; Liu, S.; Liu, Y.; Li, F.; Vedadi, M.; Frye, S. V.; Garcia, B. A.; Zheng, D.; Jin, J.; Wang, G. G.* “Selective Inhibition of EZH2 and EZH1 Enzymatic Activity by a Small Molecule Suppresses MLL–rearranged Leukemia” Blood, 2015, 125, 346-357. PMID: 25395428  PMCID: PMC4287641

2014

Katona, B., Liu, Y., Ma, A., Jin, J., Hua, X.* “EZH2 inhibition enhances the efficacy of an EGFR inhibitor in suppressing colon cancer cells” Cancer Biology & Therapy, 2014, 15, 1677-1687. PMID: 25535899  PMCID: PMC4622469

Liu, C.; Yu, Y.; Liu, F.; Wei, X.; Wrobel, J. A.; Gunawardena, H. P.; Zhou, L.; Jin, J.; Chen, X.* “A chromatin activity-based chemoproteomic approach reveals a transcriptional repressome for gene-specific silencing” Nature Communications, 2014, 5, 5733. PMID: 25502336  PMCID: PMC4360912

Ma, A.; Yu, W.; Xiong, Y.; Butler, K. V.; Brown, P. J.; Jin, J.* “Structure-activity Relationship Studies of SETD8 Inhibitors”  MedChemComm,  2014, 5, 1892-1898. PMID: 25554733  PMCID: PMC4278651

Ma, A.; Yu, W.; Li, F.; Bleich, R. M.; Herold, J. M.; Butler, K. V.; Norris, J. L.; Korboukh, V.; Tripathy, A.; Janzen, W. P.; Arrowsmith, C. H.; Frye, S. V.; Vedadi, M.; Brown, P. J.; Jin, J.* “Discovery of a Selective, Substrate-Competitive Inhibitor of the Lysine Methyltransferase SETD8” J. Med. Chem. 2014, 57, 6822-6833. PMID: 25032507  PMCID: PMC4136711

Sundriyal, S.; Malmquist, N. A.; Caron, J.;Blundell, S.; Liu, F.; Chen, X.; Srimongkolpithak, N.; Jin, J.; Charman, S. A.; Scherf, A.; Fuchter, M. J.* “Development of Diaminoquinazoline Histone Lysine Methyltransferase Inhibitors as Potent Blood-stage Anti-Malarial Compounds” ChemMedChem, 2014, 9, 2360-2373. PMID: 25044750  PMCID: PMC4177335

Wright, B. D.; Loo, L.; Street, S. E.; Ma, A.; Taylor-Blake, B.; Stashko, M.A.; Jin, J.; Janzen, W. P.; Frye, S. V.; Zylka, M. J.* “The Lipid Kinase PIP5K1C Regulates Pain Signaling and Sensitization” Neuron, 2014, 82, 836-847. PMID: 24853942  PMCID: PMC4074510

Konze, K. D.; Pattenden, S. G.; Liu, F.; Barsyte-Lovejoy, D.; Li, F.; Simon, J. M.; Davis, I. J.; Vedadi, M.; Jin, J.* “A Chemical Tool for in vitro and in vivo Precipitation of the Lysine Methyltransferase G9a” ChemMedChem, 2014, 9, 549-553. (Cover story) PMID: 24443078  PMCID: PMC4005005

Lehnertz, B.; Pabst, C.; Su, L.; Miller, M.; Liu, F.; Yi, L.; Zhang, R.; Krosl, J.; Yung, E.; Kirschner, J.; Rosten, P.; Underhill, T. M.; Jin, J.; Hébert, J.; Sauvageau, G.; Humphries, R. K.; Rossi, F. M.* “The Methyltransferase G9a Regulates HoxA9-Dependent Transcription in AML” Genes & Development, 2014, 28, 317-327. PMID: 24532712  PMCID: PMC3937511

Zhou, B.; Damrauer, J. S.; Hadzic, T.; Jeong, Y.; Clark, K.; Fan, C.; Murphy, L.; Lee, C. Y.; Troester, M. A.; Miller, C. R.; Jin, J.; Darr, D.; Perou, C. M.; Levine, R.; Diehn, M.; Kim, W. Y. “Erythropoietin Promotes Breast Tumorigenesis Through Tumor Initiating Cell Self-renewal”, Journal of Clinical Investigation, 2014, 124, 553-563. PMID: 24435044  PMCID: PMC3904607

2013

Liu, F.; Barsyte-Lovejoy, D.; Li, F.; Xiong, Y.; Korboukh, V.; Huang, X. P.; Allali-Hassani, A.; Janzen, W. P.; Roth, B. L.; Frye, S. V.; Arrowsmith, C. H.; Brown, P. J.; Vedadi, M.; Jin, J.* “Discovery of an in vivo Chemical Probe of the Lysine Methyltransferases G9a and GLP” J. Med. Chem. 2013, 56, 8931-8942. PMID: 24102134  PMCID: PMC3880643

Konze, K. D.; Ma, A.; Li, F.; Barsyte-Lovejoy, D.; Parton, T.; MacNevin, C. J.; Liu, F.; Gao, C.; Huang, X. P.; Kuznetsova, E.; Rougie, M.; Jiang, A.; Pattenden, S. G.; Norris, J. L.; James, L. I.; Roth, B. L.; Brown, P. J.; Frye, S. V.; Arrowsmith, C. H.; Hahn, K. M.; Wang, G. G.; Vedadi, M.; Jin, J.* “An Orally Bioavailable Chemical Probe of the Lysine Methyltransferases EZH2 and EZH1”, ACS Chemical Biology, 2013, 8, 1324-1334. (the most read article since online publication on 4/8/2013) PMID: 23614352  PMCID: PMC3773059

Liu, F.; Li, F.; Ma, A.; Dobrovetsky, E.; Dong, A.; Gao, C.; Korboukh, I.; Liu, J.; Smil, D.; Brown, P. J.; Frye, S. V.; Arrowsmith, C. H.; Schapira, M.; Vedadi, M.*; Jin, J.* “Exploiting an Allosteric Binding Site of PRMT3 Yields Potent and Selective Inhibitors” J. Med. Chem. 2013, 56, 2110-2124. PMID: 23445220  PMCID: PMC4319713

James, L. I.; Barsyte-Lovejoy, D.; Zhong, N.; Krichevsky, L.; Korboukh, V. K.; Herold, J. M.; MacNevin, C. J.; Norris, J. L.; Sagum, C. A.; Tempel, W.; Marcon, E.; Guo, H.; Gao, C.; Huang, X.-P.; Duan, S.; Emili, A.; Greenblatt, J. F.; Kireev, D. B.; Jin, J.; Janzen, W. P.; Brown, P. J.; Bedford, M. T.; Arrowsmith, C. H.*; Frye, S. V.* “Discovery of a Chemical Probe for the L3MBTL3 Methyllysine Reader Domain” Nat. Chem. Biol. 2013, 9, 184-191. PMID: 23292653  PMCID: PMC3577944

James, L. I.; Korboukh, V. K.; Krichevsky, L.; Baughman, B.; Herold, J. M.; Norris, J. L.; Jin, J.; Kireev, D. B.; Janzen, W. P.; Arrowsmith, C. H.; Frye, S. V.* “Small-Molecule Ligands of Methyl-Lysine Binding Proteins: Optimization of Selectivity for L3MBTL3” J. Med. Chem. 2013, 56, 7358-7371. PMID: 24040942  PMCID: PMC3846386

Cooper, M. J.; Cox, N. J.; Zimmerman, E. I.; Dewar, B. J.; Duncan, J. S.; Whittle, M. C.; Nguyen, T. A.; Jones, L. S.; Roy, S. G.; Smalley, D. M.; Kuan, P. F.; Richards, K. L.; Christopherson, R. I.; Jin, J.; Frye, S. V.; Johnson, G. L.; Baldwin, A. S.; Graves; L. M.* “Application of Multiplexed Kinase Inhibitor Beads to Study Kinome Adaptations in Drug Resistant Leukemia” PLoS ONE, 2013, 8, e66755. PMID: 23826126  PMCID: PMC3691232

Alam, M. R.; Ming, X.; Nakagawa, O.; Jin, J.; Juliano, R. L. “Covalent Conjugation of Oligonucleotides with Cell-Targeting Ligands” Bioorg. Med. Chem. 2013, 21, 6217-6223. PMID: 23777829  PMCID: PMC3789861

Blancafort, P.*; Jin, J.; Frye, S. V. “Writing and Re-Writing the Epigenetic Code of Cancer Cells: From Engineered Proteins to Small Molecules” Mol Pharmacol 2013, 83, 563-576. PMID: 23150486  PMCID: PMC3920093

2012

Chen, X.; Sassano, M. F.; Zheng, L.; Setola, V.; Chen, M.; Bai, X.; Frye, S. V.; Wetsel, W. C.; Roth, B. L.*; Jin, J.* “Structure-Functional Selectivity Relationship Studies of Beta-arrestin-biased Dopamine D₂ Receptor Agonists” J. Med. Chem. 2012, 55, 7141-7153. PMID: 22845053  PMCID: PMC3443605

Korboukh, I.; Hull-Ryde, E. A.; Rittiner, J. E.; Randhawa, A. S.; Coleman, J.; Fitzpatrick, B. J.; Setola, V.; Janzen, W. P.; Frye, S. V.; Zylka, M. J.*; Jin, J.* “Orally Active Adenosine A1 Receptor Agonists with Antinociceptive Effects in Mice” Journal of Medicinal Chemistry 2012, 55, 6467-6477. (Highlighted by Pain Research Forum) PMID: 22738238  PMCID: PMC3501123

Siarheyeva, A.; Senisterra, G.; Allali-Hassani, A.; Dong, A.; Dobrovetsky, E.; Wasney, Gregory A.; Chau, I.; Marcellus, R.; Hajian, T.; Liu, F.; Korboukh, I.; Smil, D.; Bolshan, Y.; Min, J.; Wu, H.; Zeng, H.; Loppnau, P.; Poda, G.; Griffin, C.; Aman, A.; Brown, Peter J.; Jin, J.; Al-awar, R.; Arrowsmith, Cheryl H.; Schapira, M.*; Vedadi, M.* “An Allosteric Inhibitor of Protein Arginine Methyltransferase 3” Structure 2012, 20, 1425-1435. PMID: 22795084

Roberts, P. J.; Usary, J. E.; Darr, D. B.; Dillon, P. M.; Pfefferle, A. D.; Whittle, M. C.; Duncan, J. S.; Johnson, S. M.; Combest, A. J.; Jin, J.; Zamboni, W. C.; Johnson, G. L.; Perou, C. M.*; Sharpless, N. E.* “Combined PI3K/mTOR and MEK Inhibition Provides Broad Anti-Tumor Activity in Faithful Murine Cancer Models” Clinical Cancer Research, 2012, 18, 5290-5303. PMID: 22872574  PMCID: PMC3715399

Duncan, J. S.; Whittle, M. C.; Nakamura, K.; Abell, A. N.; Midland, A. A.; Zawistowski, J. S.; Johnson, N. L.; Granger, D. A.; Jordan, N. V.; Darr, D. B.; Usary, J.; Kuan, P.-F.; Smalley, D. M.; Major, B.; He, X.; Hoadley, K.; Sharpless, N. E.; Perou, C. M.; Gomez, S. M.; Chen, X.; Jin, J.; Frye, S. V.; Earp, H. S.; Graves, L. M.; Johnson, G. L.* “Dynamic Reprogramming of the Kinome In Response to Targeted MEK Inhibition In Triple Negative Breast Cancer” Cell, 2012, 149, 307-321. (Highlighted by Faculty of 1000) PMID: 22500798  PMCID: PMC3328787

Huang, H.-S.; Allen, J. A.; Mabb, A. M.; King, I. F.; Miriyala, J.; Taylor-Blake, B.; Sciaky, N.; Dutton Jr, J. W.; Lee, H.-M.; Chen, X.; Jin, J.; Bridges, A. S.; Zylka, M. J.*; Roth, B. L.*; Philpot, B. D.* “Topoisomerase Inhibitors Unsilence the Dormant Allele of Ube3a in Neurons” Nature, 2012, 481, 185-189. (Highlighted in Science, Nature, the Scientist, and many others and listed as one of top 10 Scientific Achievements of 2011 by NIMH) PMID: 22190039  PMCID: PMC3257422

Rittiner, J. E.; Korboukh, I.; Hull-Ryde, E.; Jin, J.; Janzen, W. P.; Frye, S. V.; Zylka, M. J.* “AMP Is an Adenosine A₁ Receptor Agonist” J. Bio. Chem. 2012, 287, 5301-5309. PMID: 22215671  PMCID: PMC3285310

Jin, Q.; Davis, R. S.; Bullion, A. M.; Jin, J.; Wang, Y.; Widdowson, K. L.; Palovich, M. R.; Foley, J. J.; Schmidt, D. B.; Buckley, P. T.; Webb, E. F.; Salmon, M.; Belmonte, K. E.; Sarau, H. M.; Busch-Petersen, J.* “Tyrosine Urea Muscarinic Acetylcholine Receptor Antagonists: Achiral Quaternary Ammonium Groups” Bioorg. Med. Chem. Lett. 2012, 22, 7087-7091. PMID: 23099092

Wang, X. F.; Tian, X. T.; Ohkoshi, E.; Qin, B.; Liu, Y. N.; Wu, P. C.; Hour, M. J.; Hung, H. Y.; Qian, K.; Huang, R.; Bastow, K. F.; Janzen, W. P.; Jin, J.; Morris-Natschke, S. L.; Lee, K. H.; Xie, L.* “Design and Synthesis of Diarylamines and Diarylethers as Cytotoxic Antitumor Agents”. Bioorg. Med. Chem. Lett. 2012, 22, 6224-6228. PMID: 22932313

Herold, J. M.; James, L. I.; Korboukh, V. K.; Gao, C.; Coil, K. E.; Bua, D. J.; Norris, J. L.; Kireev, D. B.; Brown, P. J.; Jin, J., Janzen, W. P.; Gozani, O.; Frye, S. V.*  “Structure-Activity Relationships of Methyl-Lysine Reader Antagonists” MedChemComm, 2012, 3, 45-51. PMID: N/A

He, Y.; Korboukh, I.; Jin, J.*; Huang, J.* “Targeting protein lysine methylation and demethylation in cancers” Acta Biochim Biophys Sin, 2012, 44, 70-79. PMID: 22194015  PMCID: PMC3244655

2011

Allen, J. A.; Yost, J. M.; Setola, V.; Chen, X.; Sassano, M. F.; Chen, M.; Peterson, S.; Yadav, P. N.; Huang, X.-P.; Feng, B.; Jensen, N. H.; Che, X.; Bai, X.; Frye, S. V.; Wetsel, W. C.; Caron, M. G.; Javitch, J. A.; Roth, B. L.*; Jin, J.* “Discovery of Beta-Arrestin-Biased Dopamine D₂ Ligands for Probing Signal Transduction Pathways Essential for Antipsychotic Efficacy” PNAS, 2011, 108, 18488-18493.  (highlighted by SciBX as a cover story (2011, 4(44), doi:10.1038/scibx.2011.1224), Schizophrenia Research Forum, and Faculty of 1000). PMID: 22025698  PMCID: PMC3215024

Vedadi, M.; Barsyte-Lovejoy, D.; Liu, F.; Rival-Gervier, S.; Allali-Hassani, A.; Labrie, V.; Wigle, T. J.; DiMaggio, P. A.; Wasney, G. A.; Siarheyeva, A.; Dong, A.; Tempel, W.; Wang, S.-C.; Chen, X.; Chau, I.; Mangano, T.; Huang, X.-P.; Simpson, C. D.; Pattenden, S. G.; Norris, J. L.; Kireev, D. B.; Tripathy, A.; Edwards, A.; Roth, B. L.; Janzen, W. P.; Garcia, B. A.; Petronis, A.; Ellis, J.; Brown, P. J.; Frye, S. V.; Arrowsmith, C. H.*; Jin, J.* “A Chemical Probe Selectively Inhibits G9a and GLP Methyltransferase Activity in Cells” Nature Chemical Biology, 2011, 7, 566-574. (Highlighted by News and Views in Nature Chemical Biology (2011, 7, 499-500), SciBX (2011, 4(31), doi:10.1038/scibx.2011.890). PMID: 21743462  PMCID: PMC3184254

Liu, F.; Barsyte-Lovejoy, D.; Allali-Hassani, A.; He, Y.; Herold, J. M.; Chen, X.; Yates, C. M.; Frye, S. V.; Brown, P. J.; Huang, J.; Vedadi, M.; Arrowsmith, C. H.; Jin, J.*  “Optimization of Cellular Activity of G9a Inhibitors 7-Aminoalkoxy-quinazolines” J. Med. Chem. 2011, 54, 6139-6150. PMID: 21780790  PMCID: PMC3171737

Morales-Ramos, A. I.*; Li, Y.; Hilfiker, M.; Mecom, J. S.; Eidam, P.; Shi, D.; Tseng, P.-S.; Brooks, C.; Zhang, D.; Wang, N.; Jaworski, J.; Morrow, D.; Fries, H.; Edwards, R. Jin, J.* “Structure-Activity Relationship Studies of Novel 3-Oxazolidinedione-6-Naphthyl-2-Pyridinones as Potent and Orally Bioavailable EP₃ Receptor Antagonists” Bioorg. Med. Chem. Lett. 2011, 21, 2806-2811. PMID: 21514150

Yost, J. M.; Korboukh, I.; Liu, F.; Gao, C.; Jin, J.* “Targets in Epigenetics: Inhibiting the Methyl Writers of the Histone Code” Current Chemical Genomics, 2011, 5, 72-84. PMID: 21966347  PMCID: PMC3178896

Chen, X.; Jin, J.* book chapter “Small Molecule Inhibitors as Targeted Cancer Therapeutics” in The Molecular Basis of Human Cancer, Second Edition (Springer Press), 2011, in press. PMID: N/A

Herold, J. M.; Wigle, T. J.; Norris, J. L.; Lam, R.; Korboukh, V. K.; Gao, C.; Ingerman, L. A.; Kireev, D. B.; Senisterra, G.; Vedadi, M.;Tripathy, A.; Brown, P. J.; Arrowsmith, C. H.; Jin, J.; Janzen, W. P.; Frye, S. V.* “Small Molecule Ligands of Methyl-Lysine Binding Proteins” J. Med. Chem. 2011, 54, 2504-2511. PMID: 21417280  PMCID: PMC3109722

Evans, K, A.*; Shearer, B. G.; Wisnoski, D. D.; Shi, D.; Sparks, S. M.; Sternbach, D. D.; Winegar, D. A,; Billin, A. N.; Britt, C.; Way,J. M.; Epperly, A. H.; Leesnitzer, L. M.; Merrihew, R. V.; Xu, R. X.; Lambert, M. H.; Jin, J. “Phenoxyacetic Acids as PPARd Partial Agonists: Synthesis, Optimization, and In Vivo Efficacy” Bioorg. Med. Chem. Lett. 2011, 21, 2345-2350. PMID: 21414782

2010

Liu, F.; Chen, X.; Allali-Hassani, A.; Quinn, A. M.; Wigle, T. J.; Wasney, G. A.; Dong, A.; Senisterra, G.; Chau, I.; Siarheyeva, A.; Norris, J. L.; Kireev, D. B.; Jadhav, A.; Herold, J. M.; Janzen, W. P.; Arrowsmith, C. H.; Frye, S. V.; Brown, P. J.; Simeonov, A.; Vedadi, M.; Jin, J.*  “Protein Lysine Methyltransferase G9a Inhibitors: Design, Synthesis, and Structure Activity Relationships of 2,4-Diamino-7-aminoalkoxy-quinazolines” J. Med. Chem. 2010, 53, 5844-5857. PMID: 20614940  PMCID: PMC2920043

Jin, J.*; Morales-Ramos, A.; Eidam, P.; Mecom, J.; Li, Y.; Brooks, C.; Hilfiker, M.; Zhang, D.; Wang, N.; Shi, D.; Tseng, P.-S.; Wheless, K.; Budzik, B.; Evans, K.; Jaworski, J.; Jugus, J.; Leon, L.; Wu, C.; Pullen, M.; Karamshi, B.; Rao, P.; Ward, E.; Laping, N.; Evans, C.; Leach, C.; Holt, D.; Su, X.; Morrow, D.; Fries, H.; Thorneloe, K.; Edwards, R. “Novel 3-Oxazolidinedione-6-aryl-pyridinones as Potent, Selective, and Orally Active EP3 Receptor Antagonists” ACS Med. Chem. Lett. 2010, 1, 316-320. (Highlighted as a feature article in the October issue) PMID: 24900213  PMCID: PMC4007852

Budzik, B.; Garzya, V.; Shi, D.; Walker, G.; Woolley-Roberts, M.; Pardoe, J.; Lucas, A. J.; Tehan, B.; Rivero, R. A.; Langmead, C. L.; Watson, J.; Wu, Z.; Forbes, I. T.; Jin, J.* “Novel N-Substituted Benzimidazolones as Potent, Selective, CNS-penetrant, and Orally Active M1 mAChR Agonists” ACS Med. Chem. Lett. 2010, 1, 244-248. (Highlighted as a feature article in the September issue) PMID: 24900202  PMCID: PMC4007837

Wigle, T. J.; Provencher, L. M.; Norris, J. L.; Jin, J.; Brown, P. J.; Frye, S. V.; Janzen, W. P.* “Accessing Protein Methyltransferase and Demethylase Enzymology Using Microfluidic Capillary Electrophoresis” Chemistry & Biology 2010, 17, 695-704. (Cover story) PMID: 20659682  PMCID: PMC2914686

Johnson, S.; Torrice, C.; Bell, J.; Monahan, K.; Jiang, Q.; Wang, Y.; Ramsey, M.; Jin, J.; Wong, K.; Su, L.; Zhou, D.; Sharpless, N.* “Mitigation of hematologic radiation toxicity in mice through pharmacological quiescence induced by CDK4/6” Journal of Clinical Investigation 2010, 120, 2528–2536. PMID: 20577054  PMCID: PMC2898594

Frye, S. V.*; Heightman, T.; Jin, J. “Targeting Methyl Lysine” Annual Reports in Medicinal Chemistry 2010, 45, 329-343. PMID: N/A

Janzen, W. P.*; Wigle, T. J.; Jin, J.; Frye, S. V. “Epigenetics: Tools and Technologies” Drug Discovery Today: Technologies 2010, 7, e59-e65. PMID: 21243036  PMCID: PMC3018755

Li, Y. H.*; Tseng, P.-S.; Evans, K. A.; Jaworski, J.-P.; Morrow, D. M.; Fries, H. E.; Wu, C. W.; Edwards, R. M.; Jin, J.* “3-Urea-1-(phenylmethyl)-pyridones as novel, potent, and selective EP3 receptor antagonists” Bioorg. Med. Chem. Lett. 2010, 20, 6744-6747. PMID: 20926294

Budzik, B.; Garzya, V.; Shi, D.; Walker, G.; Lauchart, Y.; Lucas, A. J.; Rivero, R. A.; Langmead, C. L.; Watson, J.; Wu, Z.; Forbes, I. T.; Jin, J.* “2’ Biaryl amides as novel and subtype selective M1 agonists. Part II: Further optimization and profiling” Bioorg. Med. Chem. Lett. 2010, 20, 3545-3549. PMID: 20483599

Budzik, B.; Garzya, V.; Shi, D.; Foley, J. J.; Rivero, R. A.; Langmead, C. L.; Watson, J.; Wu, Z.; Forbes, I. T.; Jin, J.* “2’ Biaryl amides as novel and subtype selective M1 agonists. Part I: Identification, synthesis, and initial SAR” Bioorg. Med. Chem. Lett. 2010, 20, 3540-3544. PMID: 20483611

Budzik, B. W.; Evans, K, A.*; Wisnoski, D. D.; Jin, J.; Rivero, R. A.; Szewczyk, G. R.; Jayawickreme, C.; Moncol, D. L.; Yu, H. “Synthesis and Structure-activity Relationships of a Series of 3-Aryl-4-isoxazolecarboxamides as a New Class of TGR5 Agonists” Bioorg. Med. Chem. Lett. 2010, 20, 1363-1367. PMID: 20097073

2009

Liu, F.; Chen, X.; Allali-Hassani, A.; Quinn, A. M.; Wasney, G. A.; Dong, A.; Barsyte, D.; Kozieradzki, I.; Senisterra, G.; Chau, I.; Siarheyeva, A.; Kireev, D. B.; Jadhav, A.; Herold, J. M.; Frye, S. V.; Arrowsmith, C. H.; Brown, P. J.; Simeonov, A.; Vedadi, M.; Jin, J.* “Discovery of a 2,4-Diamino-7-aminoalkoxyquinazoline as a Potent and Selective Inhibitor of Histone Lysine Methyltransferase G9a” J. Med. Chem. 2009, 52, 7950-7953. PMID: 19891491  PMCID: PMC2825141

Evans, K, A.*; Budzik, B. W.; Ross, S. A.; Wisnoski, D. D.; Jin, J.; Rivero, R. A.; Vimal, M.; Szewczyk, G. R.; Jayawickreme, C.; Moncol, D. L.; Rimele, T. J.; Armour, S. L.; Weaver, S. P.; Griffin, R. J.; Tadepalli, S. M.; Jeune, M. R.; Shearer, T. W.; Chen, Z. B.; Chen, L.; Hertzog, D. L.; Anderson, D. L.; Becherer, D.; De Los Frailes, M.; Colilla, F. J. “Discovery of 3-Aryl-4-isoxazolecarboxamides as TGR5 Receptor Agonists” J. Med. Chem. 2009, 52, 7962-7965. PMID: 19902954

Jugus, M. J.; Jaworski, J. P.; Patra, P. B.; Jin, J.; Morrow, D. M.; Laping, N. J.; Edwards, R. M.; Thorneloe, K. S.* “Dual Modulation of Uninary Bladder Activity and Urine Flow by Prostanoid EP₃ Receptors in the Conscious Rat” Br. J. Pharmacol. 2009, 158, 372-381. PMID: 19486006  PMCID: PMC2795235

Hilfiker, M. A.*; Wang, N.; Hou, X.; Du, Z.; Pullen, M. A.; Nord, M.; Nagilla, R.; Fries, H. E.; Wu, C. W.; Sulpizio, A. C.; Jaworski, J. P.; Morrow, D.; Edwards, R. M.; Jin, J. “Discovery of Novel Aminothiadiazole Amides as Selective EP₃ Receptor Antagonists” Bioorg. Med. Chem. Lett. 2009, 19, 4292-4295. PMID: 19487124

Budzik, B. W.*; Wang, Y.*; Shi, D.; Wang, F.; Xie, H.; Wan, Z.; Zhu, C.; Foley, J. J.; Rao, P.; Kallal, L. A.; Sarau, H. M.; Morrow, D. M.; Moore, M. L; Rivero, R. A.; Palovich, M.; Salmon, M.; Belmonte, K. E.; Laine, D. I.; Jin, J.* “M3 Muscarinic Acetylcholine Receptor Antagonists: SAR and Optimization of Bi-aryl Amines” Bioorg. Med. Chem. Lett. 2009, 19, 1686-1690. PMID: 19243945

Li, Y. H.*; Zhang, L.; Tseng, P. S.; Zhang, Y.; Jin, Y.; Shen, J. K.; Jin, J. “A Facile One-pot  Synthesis of 3-Unsubstituted-2,4-oxazolidinediones via in situ Generation of Carbamate From α-Hydroxyesters Using Trichloroacetyl Isocyanate” Tetrahedron Letters 2009, 50, 790-792. PMID: N/A

Wang, Y.*; Busch-Petersen, J.; Wang, F.; Kiesow T. J.; Graybill, T. L.; Jin, J.; Palovich, M.; Foley, J. J.; Hunsberger, G. E.; Schmidt, D. B.; Sarau, H. M.; Spudich, E. A.; Wu, Z.; Fisher, L. S.; McQueney, M. S.; Rivero, R. A.; Widdowson, K. L. “Camphor Sulfonamides and Derivatives as Novel, Potent and Selective CXCR3 Antagonists” Bioorg. Med. Chem. Lett. 2009, 19, 114-118. PMID: 19014886

2008

Jin, J.*; Budzik, B. W.; Wang, Y.; Shi, D.; Wang, F.; Xie, H.; Wan, Z.; Zhu, C.; Foley, J. J.; Webb, E. F.; Berlanga, M.; Burman, M.; Sarau, H. M.; Morrow, D. M.; Moore, M. L; Rivero, R. A.; Palovich, M.; Salmon, M.; Belmonte, K. E.; Laine, D. I.* “Discovery of Bi-phenyl Piperazines as Novel and Long Acting Muscarinic Acetylcholine Receptor Antagonists” J. Med. Chem. 2008, 51, 5915-5918. PMID: 18798607

Jin, J.*; Wang, Y.; Shi, D.; Wang, F.; Davis, R. S.; Jin, Q.; Fu, W.; Foley, J. J.; Webb, E. F.; Dehaas, C. J.; Berlanga, M.; Burman, M.; Sarau, H. M.; Morrow, D. M.; Rao, P.; Kallal, L. A.; Moore, M. L; Rivero, R. A.; Palovich, M.; Salmon, M.; Belmonte, K. E.; Busch-Petersen, J.* “Discovery of Novel and Long Acting Muscarinic Acetylcholine Receptor Antagonists” J. Med. Chem. 2008, 51, 4866-4869. PMID: 18680280

Su, X.*; Leon, L. A.; Wu, C. W.; Morrow, D. M.; Jaworski, J. P.; Heibler, J. P.; Lashinger, E. S. R.; Jin, J.; Edwards, R. M.; Laping, N. J. “Modulation of Bladder Function by Prostaglandin EP3 Receptors In the Central Nervous System” Am. J. Physiology – Renal Physiology 2008, 295, F984-F994. PMID: 18632791

Jin, J.*; Wang, Y.*; Shi, D.; Wang, F.; Fu, W.; Davis, R. S.; Jin, Q.; Foley, J. J.; Sarau, H. M.; Morrow, D. M.; Moore, M. L; Rivero, R. A.; Palovich, M.; Salmon, M.; Belmonte, K. E.; Busch-Petersen, J. “Muscarinic Acetylcholine Receptor Antagonists: SAR and Optimization of Tyrosine Ureas” Bioorg. Med. Chem. Lett. 2008, 18, 5481-5486. PMID: 18818072

Wang, Y.*; Wu, Z.; Guida, B. F.; Lawrence, S. K.; Neeb, M. J.; Rivero, R. A.; Douglas, S. A.; Jin, J.*  “N-Alkyl-5H-pyrido[4,3-b]indol-1-amines and Derivatives as Novel Urotensin-II Receptor Antagonists” Bioorg. Med. Chem. Lett. 2008, 18, 4936-4939. PMID: 18768319

Jin, J.*; An, M.; Sapienza, A.; Aiyar, N. V.; Naselsky, D.; Sarau, H. M.; Foley, J. J.; Salyers, K. L.; Knight, S. D.; Keenan, R. M.; Rivero, R. A.; Dhanak, D.; Douglas, S. A. “Urotensin-II Receptor Antagonists: Synthesis and SAR of N-cyclic Azaalkyl Benzamides” Bioorg. Med. Chem. Lett. 2008, 18, 3950-3954. PMID: 18573659

McAtee, J. J.*; Dodson, J. W.; Dowdell, S. E.; Erhard, K. F.; Girard, G. R.; Goodman, K. B.; Hilfiker, M. A.; Jin, J.; Sehon, C. A.; Sha, D.; Shi, D.; Wang, F.; Wang, G. Z.; Wang, N.; Wang, Y.; Viet, A. Q.; Yuan, C. K.; Zhang, D.; Aiyar, N. V.; Behm, D. J.; Carballo, L. H.; Evans, C.; Fries, H. E.; Nagilla, R.; Roethke, T. J.; Xu, X.; Douglas, S. A.; Neeb, M. J. “Potent and Selective Small-Molecule Human Urotensin-II Antagonists with Improved Pharmacokinetic Profiles” Bioorg. Med. Chem. Lett. 2008, 18, 3716-3719. PMID: 18524591

Jin, J.*; Wang, Y.; Wang, F.; Shi, D.; Erhard, K. F.; Wu, Z.; Guida, B. F.; Lawrence, S. K.; Behm, D. J.; Disa, J.; Vaidya, K. S.; Evans, C.; McMillan, L. J.; Rivero, R. A.; Neeb, M. J.; Douglas, S. A. “2-Aminomethyl Piperidines as Novel Urotensin-II Receptor Antagonists” Bioorg. Med. Chem. Lett. 2008, 18, 2860-2864. PMID: 18420409