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Biotransformation of Daclatasvir In Vitro and in Nonclinical Species: Formation of the Main Metabolite by Pyrrolidine δ-Oxidation and Rearrangement.
Li W, Zhao W, Liu X, Huang X, Lopez OD, Leet JE, Fancher RM, Nguyen V, Goodrich J, Easter J, Hong Y, Caceres-Cortes J, Chang SY, Ma L, Belema M, Hamann LG, Gao M, Zhu M, Shu YZ, Humphreys WG, Johnson BM. Li W, et al. Among authors: gao m. Drug Metab Dispos. 2016 Jun;44(6):809-20. doi: 10.1124/dmd.115.068866. Epub 2016 Mar 30. Drug Metab Dispos. 2016. PMID: 27029743
Hepatitis C virus NS5A replication complex inhibitors: the discovery of daclatasvir.
Belema M, Nguyen VN, Bachand C, Deon DH, Goodrich JT, James CA, Lavoie R, Lopez OD, Martel A, Romine JL, Ruediger EH, Snyder LB, St Laurent DR, Yang F, Zhu J, Wong HS, Langley DR, Adams SP, Cantor GH, Chimalakonda A, Fura A, Johnson BM, Knipe JO, Parker DD, Santone KS, Fridell RA, Lemm JA, O'Boyle DR 2nd, Colonno RJ, Gao M, Meanwell NA, Hamann LG. Belema M, et al. Among authors: gao m. J Med Chem. 2014 Mar 13;57(5):2013-32. doi: 10.1021/jm401836p. Epub 2014 Feb 12. J Med Chem. 2014. PMID: 24521299
Discovery of potent hepatitis C virus NS5A inhibitors with dimeric structures.
Lemm JA, Leet JE, O'Boyle DR 2nd, Romine JL, Huang XS, Schroeder DR, Alberts J, Cantone JL, Sun JH, Nower PT, Martin SW, Serrano-Wu MH, Meanwell NA, Snyder LB, Gao M. Lemm JA, et al. Among authors: gao m. Antimicrob Agents Chemother. 2011 Aug;55(8):3795-802. doi: 10.1128/AAC.00146-11. Epub 2011 May 16. Antimicrob Agents Chemother. 2011. PMID: 21576451 Free PMC article.
HCV NS5A replication complex inhibitors. Part 2: investigation of stilbene prolinamides.
St Laurent DR, Belema M, Gao M, Goodrich J, Kakarla R, Knipe JO, Lemm JA, Liu M, Lopez OD, Nguyen VN, Nower PT, O'Boyle D 2nd, Qiu Y, Romine JL, Serrano-Wu MH, Sun JH, Valera L, Yang F, Yang X, Meanwell NA, Snyder LB. St Laurent DR, et al. Among authors: gao m. Bioorg Med Chem Lett. 2012 Oct 1;22(19):6063-6. doi: 10.1016/j.bmcl.2012.08.049. Epub 2012 Aug 21. Bioorg Med Chem Lett. 2012. PMID: 22959243
Hepatitis C virus NS5A replication complex inhibitors. Part 6: Discovery of a novel and highly potent biarylimidazole chemotype with inhibitory activity toward genotypes 1a and 1b replicons.
Belema M, Nguyen VN, Romine JL, St Laurent DR, Lopez OD, Goodrich JT, Nower PT, O'Boyle DR 2nd, Lemm JA, Fridell RA, Gao M, Fang H, Krause RG, Wang YK, Oliver AJ, Good AC, Knipe JO, Meanwell NA, Snyder LB. Belema M, et al. Among authors: gao m. J Med Chem. 2014 Mar 13;57(5):1995-2012. doi: 10.1021/jm4016203. Epub 2014 Jan 17. J Med Chem. 2014. PMID: 24437689
Resensitizing daclatasvir-resistant hepatitis C variants by allosteric modulation of NS5A.
Sun JH, O'Boyle DR 2nd, Fridell RA, Langley DR, Wang C, Roberts SB, Nower P, Johnson BM, Moulin F, Nophsker MJ, Wang YK, Liu M, Rigat K, Tu Y, Hewawasam P, Kadow J, Meanwell NA, Cockett M, Lemm JA, Kramer M, Belema M, Gao M. Sun JH, et al. Among authors: gao m. Nature. 2015 Nov 12;527(7577):245-8. doi: 10.1038/nature15711. Epub 2015 Nov 4. Nature. 2015. PMID: 26536115
Chemical genetics strategy identifies an HCV NS5A inhibitor with a potent clinical effect.
Gao M, Nettles RE, Belema M, Snyder LB, Nguyen VN, Fridell RA, Serrano-Wu MH, Langley DR, Sun JH, O'Boyle DR 2nd, Lemm JA, Wang C, Knipe JO, Chien C, Colonno RJ, Grasela DM, Meanwell NA, Hamann LG. Gao M, et al. Nature. 2010 May 6;465(7294):96-100. doi: 10.1038/nature08960. Epub 2010 Apr 21. Nature. 2010. PMID: 20410884 Free PMC article. Clinical Trial.
HCV NS5A replication complex inhibitors. Part 4. Optimization for genotype 1a replicon inhibitory activity.
St Laurent DR, Serrano-Wu MH, Belema M, Ding M, Fang H, Gao M, Goodrich JT, Krause RG, Lemm JA, Liu M, Lopez OD, Nguyen VN, Nower PT, O'Boyle DR 2nd, Pearce BC, Romine JL, Valera L, Sun JH, Wang YK, Yang F, Yang X, Meanwell NA, Snyder LB. St Laurent DR, et al. Among authors: gao m. J Med Chem. 2014 Mar 13;57(5):1976-94. doi: 10.1021/jm301796k. Epub 2013 Apr 10. J Med Chem. 2014. PMID: 23573957
Synergistic Activity of Combined NS5A Inhibitors.
O'Boyle DR 2nd, Nower PT, Gao M, Fridell R, Wang C, Hewawasam P, Lopez O, Tu Y, Meanwell NA, Belema M, Roberts SB, Cockett M, Sun JH. O'Boyle DR 2nd, et al. Among authors: gao m. Antimicrob Agents Chemother. 2015 Dec 28;60(3):1573-83. doi: 10.1128/AAC.02639-15. Antimicrob Agents Chemother. 2015. PMID: 26711745 Free PMC article.
O'Boyle II, R. A. Fridell, D. R. Langley, C. Wang, S. Roberts, P. Nower, B. M. Johnson F. Moulin, M. J. Nophsker, Y. Wang, M. Liu, K. Rigat, Y. Tu, P. Hewawasam, J. Kadow, N. A. Meanwell, M. Cockett, J. A. Lemm, M. Kramer, M. Belema, and …
O'Boyle II, R. A. Fridell, D. R. Langley, C. Wang, S. Roberts, P. Nower, B. M. Johnson F. Moulin, M. J. Nophsker, Y. Wang, …
9,038 results