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Page 1
Discovery of GS-9669, a thumb site II non-nucleoside inhibitor of NS5B for the treatment of genotype 1 chronic hepatitis C infection.
Lazerwith SE, Lew W, Zhang J, Morganelli P, Liu Q, Canales E, Clarke MO, Doerffler E, Byun D, Mertzman M, Ye H, Chong L, Xu L, Appleby T, Chen X, Fenaux M, Hashash A, Leavitt SA, Mabery E, Matles M, Mwangi JW, Tian Y, Lee YJ, Zhang J, Zhu C, Murray BP, Watkins WJ. Lazerwith SE, et al. Among authors: mertzman m. J Med Chem. 2014 Mar 13;57(5):1893-901. doi: 10.1021/jm401420j. Epub 2013 Nov 6. J Med Chem. 2014. PMID: 24144213
Discovery of GS-9256: a novel phosphinic acid derived inhibitor of the hepatitis C virus NS3/4A protease with potent clinical activity.
Sheng XC, Casarez A, Cai R, Clarke MO, Chen X, Cho A, Delaney WE 4th, Doerffler E, Ji M, Mertzman M, Pakdaman R, Pyun HJ, Rowe T, Wu Q, Xu J, Kim CU. Sheng XC, et al. Among authors: mertzman m. Bioorg Med Chem Lett. 2012 Feb 1;22(3):1394-6. doi: 10.1016/j.bmcl.2011.12.038. Epub 2011 Dec 13. Bioorg Med Chem Lett. 2012. PMID: 22244938
Preclinical characterization of GS-9669, a thumb site II inhibitor of the hepatitis C virus NS5B polymerase.
Fenaux M, Eng S, Leavitt SA, Lee YJ, Mabery EM, Tian Y, Byun D, Canales E, Clarke MO, Doerffler E, Lazerwith SE, Lew W, Liu Q, Mertzman M, Morganelli P, Xu L, Ye H, Zhang J, Matles M, Murray BP, Mwangi J, Zhang J, Hashash A, Krawczyk SH, Bidgood AM, Appleby TC, Watkins WJ. Fenaux M, et al. Among authors: mertzman m. Antimicrob Agents Chemother. 2013 Feb;57(2):804-10. doi: 10.1128/AAC.02052-12. Epub 2012 Nov 26. Antimicrob Agents Chemother. 2013. PMID: 23183437 Free PMC article. Clinical Trial.
Optimization of Pharmacokinetics through Manipulation of Physicochemical Properties in a Series of HCV Inhibitors.
Lazerwith SE, Bahador G, Canales E, Cheng G, Chong L, Clarke MO, Doerffler E, Eisenberg EJ, Hayes J, Lu B, Liu Q, Matles M, Mertzman M, Mitchell ML, Morganelli P, Murray BP, Robinson M, Strickley RG, Tessler M, Tirunagari N, Wang J, Wang Y, Zhang JR, Zheng X, Zhong W, Watkins WJ. Lazerwith SE, et al. Among authors: mertzman m. ACS Med Chem Lett. 2011 Aug 8;2(10):715-9. doi: 10.1021/ml200163b. eCollection 2011 Oct 13. ACS Med Chem Lett. 2011. PMID: 24900257 Free PMC article.
Discovery of a JAK1/3 Inhibitor and Use of a Prodrug To Demonstrate Efficacy in a Model of Rheumatoid Arthritis.
Spergel SH, Mertzman ME, Kempson J, Guo J, Stachura S, Haque L, Lippy JS, Zhang RF, Galella M, Pitt S, Shen G, Fura A, Gillooly K, McIntyre KW, Tang V, Tokarski J, Sack JS, Khan J, Carter PH, Barrish JC, Nadler SG, Salter-Cid LM, Schieven GL, Wrobleski ST, Pitts WJ. Spergel SH, et al. Among authors: mertzman me. ACS Med Chem Lett. 2019 Feb 13;10(3):306-311. doi: 10.1021/acsmedchemlett.8b00508. eCollection 2019 Mar 14. ACS Med Chem Lett. 2019. PMID: 30891131 Free PMC article.
Identification of RIPK3 Type II Inhibitors Using High-Throughput Mechanistic Studies in Hit Triage.
Hart AC, Abell L, Guo J, Mertzman ME, Padmanabha R, Macor JE, Chaudhry C, Lu H, O'Malley K, Shaw PJ, Weigelt C, Pokross M, Kish K, Kim KS, Cornelius L, Douglas AE, Calambur D, Zhang P, Carpenter B, Pitts WJ. Hart AC, et al. Among authors: mertzman me. ACS Med Chem Lett. 2019 May 6;11(3):266-271. doi: 10.1021/acsmedchemlett.9b00065. eCollection 2020 Mar 12. ACS Med Chem Lett. 2019. PMID: 32184955 Free PMC article.
Identification of N-Methyl Nicotinamide and N-Methyl Pyridazine-3-Carboxamide Pseudokinase Domain Ligands as Highly Selective Allosteric Inhibitors of Tyrosine Kinase 2 (TYK2).
Moslin R, Zhang Y, Wrobleski ST, Lin S, Mertzman M, Spergel S, Tokarski JS, Strnad J, Gillooly K, McIntyre KW, Zupa-Fernandez A, Cheng L, Sun H, Chaudhry C, Huang C, D'Arienzo C, Heimrich E, Yang X, Muckelbauer JK, Chang C, Tredup J, Mulligan D, Xie D, Aranibar N, Chiney M, Burke JR, Lombardo L, Carter PH, Weinstein DS. Moslin R, et al. Among authors: mertzman m. J Med Chem. 2019 Oct 24;62(20):8953-8972. doi: 10.1021/acs.jmedchem.9b00443. Epub 2019 Jul 17. J Med Chem. 2019. PMID: 31314518
Organic chemistry. Practical olefin hydroamination with nitroarenes.
Gui J, Pan CM, Jin Y, Qin T, Lo JC, Lee BJ, Spergel SH, Mertzman ME, Pitts WJ, La Cruz TE, Schmidt MA, Darvatkar N, Natarajan SR, Baran PS. Gui J, et al. Among authors: mertzman me. Science. 2015 May 22;348(6237):886-91. doi: 10.1126/science.aab0245. Epub 2015 May 21. Science. 2015. PMID: 25999503
16 results