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Page 1
Structure-based drug design of RN486, a potent and selective Bruton's tyrosine kinase (BTK) inhibitor, for the treatment of rheumatoid arthritis.
Lou Y, Han X, Kuglstatter A, Kondru RK, Sweeney ZK, Soth M, McIntosh J, Litman R, Suh J, Kocer B, Davis D, Park J, Frauchiger S, Dewdney N, Zecic H, Taygerly JP, Sarma K, Hong J, Hill RJ, Gabriel T, Goldstein DM, Owens TD. Lou Y, et al. Among authors: taygerly jp. J Med Chem. 2015 Jan 8;58(1):512-6. doi: 10.1021/jm500305p. Epub 2014 Apr 16. J Med Chem. 2015. PMID: 24712864
Finding the perfect spot for fluorine: improving potency up to 40-fold during a rational fluorine scan of a Bruton's Tyrosine Kinase (BTK) inhibitor scaffold.
Lou Y, Sweeney ZK, Kuglstatter A, Davis D, Goldstein DM, Han X, Hong J, Kocer B, Kondru RK, Litman R, McIntosh J, Sarma K, Suh J, Taygerly J, Owens TD. Lou Y, et al. Bioorg Med Chem Lett. 2015 Jan 15;25(2):367-71. doi: 10.1016/j.bmcl.2014.11.030. Epub 2014 Nov 20. Bioorg Med Chem Lett. 2015. PMID: 25466710
Discovery of N-[4-[6-tert-butyl-5-methoxy-8-(6-methoxy-2-oxo-1H-pyridin-3-yl)-3-quinolyl]phenyl]methanesulfonamide (RG7109), a potent inhibitor of the hepatitis C virus NS5B polymerase.
Talamas FX, Abbot SC, Anand S, Brameld KA, Carter DS, Chen J, Davis D, de Vicente J, Fung AD, Gong L, Harris SF, Inbar P, Labadie SS, Lee EK, Lemoine R, Le Pogam S, Leveque V, Li J, McIntosh J, Nájera I, Park J, Railkar A, Rajyaguru S, Sangi M, Schoenfeld RC, Staben LR, Tan Y, Taygerly JP, Villaseñor AG, Weller PE. Talamas FX, et al. Among authors: taygerly jp. J Med Chem. 2014 Mar 13;57(5):1914-31. doi: 10.1021/jm401329s. Epub 2013 Nov 6. J Med Chem. 2014. PMID: 24195700 Free PMC article.
Discovery of a novel series of potent non-nucleoside inhibitors of hepatitis C virus NS5B.
Schoenfeld RC, Bourdet DL, Brameld KA, Chin E, de Vicente J, Fung A, Harris SF, Lee EK, Le Pogam S, Leveque V, Li J, Lui AS, Najera I, Rajyaguru S, Sangi M, Steiner S, Talamas FX, Taygerly JP, Zhao J. Schoenfeld RC, et al. Among authors: taygerly jp. J Med Chem. 2013 Oct 24;56(20):8163-82. doi: 10.1021/jm401266k. Epub 2013 Oct 10. J Med Chem. 2013. PMID: 24069953 Free PMC article.
Discovery of INT131: a selective PPARγ modulator that enhances insulin sensitivity.
Taygerly JP, McGee LR, Rubenstein SM, Houze JB, Cushing TD, Li Y, Motani A, Chen JL, Frankmoelle W, Ye G, Learned MR, Jaen J, Miao S, Timmermans PB, Thoolen M, Kearney P, Flygare J, Beckmann H, Weiszmann J, Lindstrom M, Walker N, Liu J, Biermann D, Wang Z, Hagiwara A, Iida T, Aramaki H, Kitao Y, Shinkai H, Furukawa N, Nishiu J, Nakamura M. Taygerly JP, et al. Bioorg Med Chem. 2013 Feb 15;21(4):979-92. doi: 10.1016/j.bmc.2012.11.058. Epub 2012 Dec 10. Bioorg Med Chem. 2013. PMID: 23294830
AMG 176, a Selective MCL1 Inhibitor, Is Effective in Hematologic Cancer Models Alone and in Combination with Established Therapies.
Caenepeel S, Brown SP, Belmontes B, Moody G, Keegan KS, Chui D, Whittington DA, Huang X, Poppe L, Cheng AC, Cardozo M, Houze J, Li Y, Lucas B, Paras NA, Wang X, Taygerly JP, Vimolratana M, Zancanella M, Zhu L, Cajulis E, Osgood T, Sun J, Damon L, Egan RK, Greninger P, McClanaghan JD, Gong J, Moujalled D, Pomilio G, Beltran P, Benes CH, Roberts AW, Huang DC, Wei A, Canon J, Coxon A, Hughes PE. Caenepeel S, et al. Among authors: taygerly jp. Cancer Discov. 2018 Dec;8(12):1582-1597. doi: 10.1158/2159-8290.CD-18-0387. Epub 2018 Sep 25. Cancer Discov. 2018. PMID: 30254093
Prospective discovery of small molecule enhancers of an E3 ligase-substrate interaction.
Simonetta KR, Taygerly J, Boyle K, Basham SE, Padovani C, Lou Y, Cummins TJ, Yung SL, von Soly SK, Kayser F, Kuriyan J, Rape M, Cardozo M, Gallop MA, Bence NF, Barsanti PA, Saha A. Simonetta KR, et al. Nat Commun. 2019 Mar 29;10(1):1402. doi: 10.1038/s41467-019-09358-9. Nat Commun. 2019. PMID: 30926793 Free PMC article.
Novel WRN Helicase Inhibitors Selectively Target Microsatellite-Unstable Cancer Cells.
Picco G, Rao Y, Al Saedi A, Lee Y, Vieira SF, Bhosle S, May K, Herranz-Ors C, Walker SJ, Shenje R, Dincer C, Gibson F, Banerjee R, Hewitson Z, Werner T, Cottom JE, Peng Y, Deng N, Zhang Y, Nartey EN, Nickels L, Landis P, Conticelli D, McCarten K, Bush J, Sharma M, Lightfoot H, House D, Milford E, Grant EK, Glogowski MP, Wagner CD, Bantscheff M, Rutkowska-Klute A; Cell Model Network UK Group; Zappacosta F, Pettinger J, Barthorpe S, Eberl HC, Jones BT, Schneck JL, Murphy DJ, Voest EE, Taygerly JP, DeMartino MP, Coelho MA, Houseley J, Sharma G, Schwartz B, Garnett MJ. Picco G, et al. Among authors: taygerly jp. Cancer Discov. 2024 Aug 2;14(8):1457-1475. doi: 10.1158/2159-8290.CD-24-0052. Cancer Discov. 2024. PMID: 38587317 Free PMC article.