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Page 1
A pan-serotype dengue virus inhibitor targeting the NS3-NS4B interaction.
Kaptein SJF, Goethals O, Kiemel D, Marchand A, Kesteleyn B, Bonfanti JF, Bardiot D, Stoops B, Jonckers THM, Dallmeier K, Geluykens P, Thys K, Crabbe M, Chatel-Chaix L, Münster M, Querat G, Touret F, de Lamballerie X, Raboisson P, Simmen K, Chaltin P, Bartenschlager R, Van Loock M, Neyts J. Kaptein SJF, et al. Among authors: simmen k. Nature. 2021 Oct;598(7881):504-509. doi: 10.1038/s41586-021-03990-6. Epub 2021 Oct 6. Nature. 2021. PMID: 34616043
1,5-benzodiazepines, a novel class of hepatitis C virus polymerase nonnucleoside inhibitors.
Nyanguile O, Pauwels F, Van den Broeck W, Boutton CW, Quirynen L, Ivens T, van der Helm L, Vandercruyssen G, Mostmans W, Delouvroy F, Dehertogh P, Cummings MD, Bonfanti JF, Simmen KA, Raboisson P. Nyanguile O, et al. Antimicrob Agents Chemother. 2008 Dec;52(12):4420-31. doi: 10.1128/AAC.00669-08. Epub 2008 Oct 13. Antimicrob Agents Chemother. 2008. PMID: 18852280 Free PMC article.
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: simmen k. 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.
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. Among authors: simmen ka. 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.
2'-Deoxy-2'-spirocyclopropylcytidine revisited: a new and selective inhibitor of the hepatitis C virus NS5B polymerase.
Jonckers TH, Lin TI, Buyck C, Lachau-Durand S, Vandyck K, Van Hoof S, Vandekerckhove LA, Hu L, Berke JM, Vijgen L, Dillen LL, Cummings MD, de Kock H, Nilsson M, Sund C, Rydegård C, Samuelsson B, Rosenquist A, Fanning G, Van Emelen K, Simmen K, Raboisson P. Jonckers TH, et al. Among authors: simmen k. J Med Chem. 2010 Nov 25;53(22):8150-60. doi: 10.1021/jm101050a. Epub 2010 Oct 29. J Med Chem. 2010. PMID: 21033671
Discovery of 4'-azido-2'-deoxy-2'-C-methyl cytidine and prodrugs thereof: a potent inhibitor of Hepatitis C virus replication.
Nilsson M, Kalayanov G, Winqvist A, Pinho P, Sund C, Zhou XX, Wähling H, Belfrage AK, Pelcman M, Agback T, Benckestock K, Wikström K, Boothee M, Lindqvist A, Rydegård C, Jonckers TH, Vandyck K, Raboisson P, Lin TI, Lachau-Durand S, de Kock H, Smith DB, Martin JA, Klumpp K, Simmen K, Vrang L, Terelius Y, Samuelsson B, Rosenquist S, Johansson NG. Nilsson M, et al. Among authors: simmen k. Bioorg Med Chem Lett. 2012 May 1;22(9):3265-8. doi: 10.1016/j.bmcl.2012.03.021. Epub 2012 Mar 16. Bioorg Med Chem Lett. 2012. PMID: 22472694
Structure-based macrocyclization yields hepatitis C virus NS5B inhibitors with improved binding affinities and pharmacokinetic properties.
Cummings MD, Lin TI, Hu L, Tahri A, McGowan D, Amssoms K, Last S, Devogelaere B, Rouan MC, Vijgen L, Berke JM, Dehertogh P, Fransen E, Cleiren E, van der Helm L, Fanning G, Van Emelen K, Nyanguile O, Simmen K, Raboisson P, Vendeville S. Cummings MD, et al. Among authors: simmen k. Angew Chem Int Ed Engl. 2012 May 7;51(19):4637-40. doi: 10.1002/anie.201200110. Epub 2012 Mar 30. Angew Chem Int Ed Engl. 2012. PMID: 22473861 No abstract available.
Finger-loop inhibitors of the HCV NS5b polymerase. Part 1: Discovery and optimization of novel 1,6- and 2,6-macrocyclic indole series.
McGowan D, Vendeville S, Lin TI, Tahri A, Hu L, Cummings MD, Amssoms K, Berke JM, Canard M, Cleiren E, Dehertogh P, Last S, Fransen E, Van Der Helm E, Van den Steen I, Vijgen L, Rouan MC, Fanning G, Nyanguile O, Van Emelen K, Simmen K, Raboisson P. McGowan D, et al. Among authors: simmen k. Bioorg Med Chem Lett. 2012 Jul 1;22(13):4431-6. doi: 10.1016/j.bmcl.2012.03.097. Epub 2012 Apr 3. Bioorg Med Chem Lett. 2012. PMID: 22542193
Finger loop inhibitors of the HCV NS5b polymerase. Part II. Optimization of tetracyclic indole-based macrocycle leading to the discovery of TMC647055.
Vendeville S, Lin TI, Hu L, Tahri A, McGowan D, Cummings MD, Amssoms K, Canard M, Last S, Van den Steen I, Devogelaere B, Rouan MC, Vijgen L, Berke JM, Dehertogh P, Fransen E, Cleiren E, van der Helm L, Fanning G, Van Emelen K, Nyanguile O, Simmen K, Raboisson P. Vendeville S, et al. Among authors: simmen k. Bioorg Med Chem Lett. 2012 Jul 1;22(13):4437-43. doi: 10.1016/j.bmcl.2012.04.113. Epub 2012 Apr 30. Bioorg Med Chem Lett. 2012. PMID: 22633687
61 results