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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: watkins wj. 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.
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: watkins wj. J Med Chem. 2014 Mar 13;57(5):1893-901. doi: 10.1021/jm401420j. Epub 2013 Nov 6. J Med Chem. 2014. PMID: 24144213
Structural and regulatory elements of HCV NS5B polymerase--β-loop and C-terminal tail--are required for activity of allosteric thumb site II inhibitors.
Boyce SE, Tirunagari N, Niedziela-Majka A, Perry J, Wong M, Kan E, Lagpacan L, Barauskas O, Hung M, Fenaux M, Appleby T, Watkins WJ, Schmitz U, Sakowicz R. Boyce SE, et al. Among authors: watkins wj. PLoS One. 2014 Jan 9;9(1):e84808. doi: 10.1371/journal.pone.0084808. eCollection 2014. PLoS One. 2014. PMID: 24416288 Free PMC article.
Structural and binding analysis of pyrimidinol carboxylic acid and N-hydroxy quinazolinedione HIV-1 RNase H inhibitors.
Lansdon EB, Liu Q, Leavitt SA, Balakrishnan M, Perry JK, Lancaster-Moyer C, Kutty N, Liu X, Squires NH, Watkins WJ, Kirschberg TA. Lansdon EB, et al. Among authors: watkins wj. Antimicrob Agents Chemother. 2011 Jun;55(6):2905-15. doi: 10.1128/AAC.01594-10. Epub 2011 Apr 4. Antimicrob Agents Chemother. 2011. PMID: 21464257 Free PMC article.
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: watkins wj. 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.
RNase H active site inhibitors of human immunodeficiency virus type 1 reverse transcriptase: design, biochemical activity, and structural information.
Kirschberg TA, Balakrishnan M, Squires NH, Barnes T, Brendza KM, Chen X, Eisenberg EJ, Jin W, Kutty N, Leavitt S, Liclican A, Liu Q, Liu X, Mak J, Perry JK, Wang M, Watkins WJ, Lansdon EB. Kirschberg TA, et al. Among authors: watkins wj. J Med Chem. 2009 Oct 8;52(19):5781-4. doi: 10.1021/jm900597q. J Med Chem. 2009. PMID: 19791799
HCV NS5B polymerase inhibitors.
Watkins WJ, Ray AS, Chong LS. Watkins WJ, et al. Curr Opin Drug Discov Devel. 2010 Jul;13(4):441-65. Curr Opin Drug Discov Devel. 2010. PMID: 20597029 Review.
Phosphonic acid-containing analogues of mycophenolic acid as inhibitors of IMPDH.
Watkins WJ, Chen JM, Cho A, Chong L, Collins N, Fardis M, Huang W, Hung M, Kirschberg T, Lee WA, Liu X, Thomas W, Xu J, Zeynalzadegan A, Zhang J. Watkins WJ, et al. Bioorg Med Chem Lett. 2006 Jul 1;16(13):3479-83. doi: 10.1016/j.bmcl.2006.03.097. Epub 2006 Apr 18. Bioorg Med Chem Lett. 2006. PMID: 16621550
133 results