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Discovery of the Irreversible Covalent FGFR Inhibitor 8-(3-(4-Acryloylpiperazin-1-yl)propyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (PRN1371) for the Treatment of Solid Tumors.
Brameld KA, Owens TD, Verner E, Venetsanakos E, Bradshaw JM, Phan VT, Tam D, Leung K, Shu J, LaStant J, Loughhead DG, Ton T, Karr DE, Gerritsen ME, Goldstein DM, Funk JO. Brameld KA, et al. Among authors: leung k. J Med Chem. 2017 Aug 10;60(15):6516-6527. doi: 10.1021/acs.jmedchem.7b00360. Epub 2017 Jul 25. J Med Chem. 2017. PMID: 28665128
The Irreversible Covalent Fibroblast Growth Factor Receptor Inhibitor PRN1371 Exhibits Sustained Inhibition of FGFR after Drug Clearance.
Venetsanakos E, Brameld KA, Phan VT, Verner E, Owens TD, Xing Y, Tam D, LaStant J, Leung K, Karr DE, Hill RJ, Gerritsen ME, Goldstein DM, Funk JO, Bradshaw JM. Venetsanakos E, et al. Among authors: leung k. Mol Cancer Ther. 2017 Dec;16(12):2668-2676. doi: 10.1158/1535-7163.MCT-17-0309. Epub 2017 Oct 4. Mol Cancer Ther. 2017. PMID: 28978721
Potent nonimmunosuppressive cyclophilin inhibitors with improved pharmaceutical properties and decreased transporter inhibition.
Fu J, Tjandra M, Becker C, Bednarczyk D, Capparelli M, Elling R, Hanna I, Fujimoto R, Furegati M, Karur S, Kasprzyk T, Knapp M, Leung K, Li X, Lu P, Mergo W, Miault C, Ng S, Parker D, Peng Y, Roggo S, Rivkin A, Simmons RL, Wang M, Wiedmann B, Weiss AH, Xiao L, Xie L, Xu W, Yifru A, Yang S, Zhou B, Sweeney ZK. Fu J, et al. Among authors: leung k. J Med Chem. 2014 Oct 23;57(20):8503-16. doi: 10.1021/jm500862r. Epub 2014 Oct 13. J Med Chem. 2014. PMID: 25310383
Discovery of Tirasemtiv, the First Direct Fast Skeletal Muscle Troponin Activator.
Collibee SE, Bergnes G, Muci A, Browne WF 4th, Garard M, Hinken AC, Russell AJ, Suehiro I, Hartman J, Kawas R, Lu PP, Lee KH, Marquez D, Tomlinson M, Xu D, Kennedy A, Hwee D, Schaletzky J, Leung K, Malik FI, Morgans DJ Jr, Morgan BP. Collibee SE, et al. Among authors: leung k. ACS Med Chem Lett. 2018 Feb 13;9(4):354-358. doi: 10.1021/acsmedchemlett.7b00546. eCollection 2018 Apr 12. ACS Med Chem Lett. 2018. PMID: 29670700 Free PMC article.
Single-shot 20-fold expansion microscopy.
Wang S, Shin TW, Yoder HB 2nd, McMillan RB, Su H, Liu Y, Zhang C, Leung KS, Yin P, Kiessling LL, Boyden ES. Wang S, et al. Among authors: leung ks. Nat Methods. 2024 Oct 11. doi: 10.1038/s41592-024-02454-9. Online ahead of print. Nat Methods. 2024. PMID: 39394503
4,286 results