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Structure-activity relationship study on a novel series of cyclopentane-containing macrocyclic inhibitors of the hepatitis C virus NS3/4A protease leading to the discovery of TMC435350.
Raboisson P, de Kock H, Rosenquist A, Nilsson M, Salvador-Oden L, Lin TI, Roue N, Ivanov V, Wähling H, Wickström K, Hamelink E, Edlund M, Vrang L, Vendeville S, Van de Vreken W, McGowan D, Tahri A, Hu L, Boutton C, Lenz O, Delouvroy F, Pille G, Surleraux D, Wigerinck P, Samuelsson B, Simmen K. Raboisson P, et al. Among authors: lenz o. Bioorg Med Chem Lett. 2008 Sep 1;18(17):4853-8. doi: 10.1016/j.bmcl.2008.07.088. Epub 2008 Jul 24. Bioorg Med Chem Lett. 2008. PMID: 18678486
Discovery of novel potent and selective dipeptide hepatitis C virus NS3/4A serine protease inhibitors.
Raboisson P, Lin TI, Kock Hd, Vendeville S, Vreken WV, McGowan D, Tahri A, Hu L, Lenz O, Delouvroy F, Surleraux D, Wigerinck P, Nilsson M, Rosenquist S, Samuelsson B, Simmen K. Raboisson P, et al. Among authors: lenz o. Bioorg Med Chem Lett. 2008 Sep 15;18(18):5095-100. doi: 10.1016/j.bmcl.2008.07.124. Epub 2008 Aug 3. Bioorg Med Chem Lett. 2008. PMID: 18722116
Discovery of novel, potent and bioavailable proline-urea based macrocyclic HCV NS3/4A protease inhibitors.
Vendeville S, Nilsson M, de Kock H, Lin TI, Antonov D, Classon B, Ayesa S, Ivanov V, Johansson PO, Kahnberg P, Eneroth A, Wikstrom K, Vrang L, Edlund M, Lindström S, Van de Vreken W, McGowan D, Tahri A, Hu L, Lenz O, Delouvroy F, Van Dooren M, Kindermans N, Surleraux D, Wigerinck P, Rosenquist A, Samuelsson B, Simmen K, Raboisson P. Vendeville S, et al. Among authors: lenz o. Bioorg Med Chem Lett. 2008 Dec 1;18(23):6189-93. doi: 10.1016/j.bmcl.2008.10.004. Epub 2008 Oct 5. Bioorg Med Chem Lett. 2008. PMID: 18954982
In vitro activity and preclinical profile of TMC435350, a potent hepatitis C virus protease inhibitor.
Lin TI, Lenz O, Fanning G, Verbinnen T, Delouvroy F, Scholliers A, Vermeiren K, Rosenquist A, Edlund M, Samuelsson B, Vrang L, de Kock H, Wigerinck P, Raboisson P, Simmen K. Lin TI, et al. Among authors: lenz o. Antimicrob Agents Chemother. 2009 Apr;53(4):1377-85. doi: 10.1128/AAC.01058-08. Epub 2009 Jan 26. Antimicrob Agents Chemother. 2009. PMID: 19171797 Free PMC article.
Induced-fit binding of the macrocyclic noncovalent inhibitor TMC435 to its HCV NS3/NS4A protease target.
Cummings MD, Lindberg J, Lin TI, de Kock H, Lenz O, Lilja E, Felländer S, Baraznenok V, Nyström S, Nilsson M, Vrang L, Edlund M, Rosenquist A, Samuelsson B, Raboisson P, Simmen K. Cummings MD, et al. Among authors: lenz o. Angew Chem Int Ed Engl. 2010 Feb 22;49(9):1652-5. doi: 10.1002/anie.200906696. Angew Chem Int Ed Engl. 2010. PMID: 20166108 No abstract available.
In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435.
Lenz O, Verbinnen T, Lin TI, Vijgen L, Cummings MD, Lindberg J, Berke JM, Dehertogh P, Fransen E, Scholliers A, Vermeiren K, Ivens T, Raboisson P, Edlund M, Storm S, Vrang L, de Kock H, Fanning GC, Simmen KA. Lenz O, et al. Antimicrob Agents Chemother. 2010 May;54(5):1878-87. doi: 10.1128/AAC.01452-09. Epub 2010 Feb 22. Antimicrob Agents Chemother. 2010. PMID: 20176898 Free PMC article.
Discovery and development of simeprevir (TMC435), a HCV NS3/4A protease inhibitor.
Rosenquist Å, Samuelsson B, Johansson PO, Cummings MD, Lenz O, Raboisson P, Simmen K, Vendeville S, de Kock H, Nilsson M, Horvath A, Kalmeijer R, de la Rosa G, Beumont-Mauviel M. Rosenquist Å, et al. Among authors: lenz o. J Med Chem. 2014 Mar 13;57(5):1673-93. doi: 10.1021/jm401507s. Epub 2014 Feb 14. J Med Chem. 2014. PMID: 24446688
TMC647055, a potent nonnucleoside hepatitis C virus NS5B polymerase inhibitor with cross-genotypic coverage.
Devogelaere B, Berke JM, Vijgen L, Dehertogh P, Fransen E, Cleiren E, van der Helm L, Nyanguile O, Tahri A, Amssoms K, Lenz O, Cummings MD, Clayton RF, Vendeville S, Raboisson P, Simmen KA, Fanning GC, Lin TI. Devogelaere B, et al. Among authors: lenz o. Antimicrob Agents Chemother. 2012 Sep;56(9):4676-84. doi: 10.1128/AAC.00245-12. Epub 2012 Jun 18. Antimicrob Agents Chemother. 2012. PMID: 22710121 Free PMC article.
316 results