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Page 1
Fragment Binding to β-Secretase 1 without Catalytic Aspartate Interactions Identified via Orthogonal Screening Approaches.
Rombouts FJR, Alexander R, Cleiren E, De Groot A, Carpentier M, Dijkmans J, Fierens K, Masure S, Moechars D, Palomino-Schätzlein M, Pineda-Lucena A, Trabanco AA, Van Glabbeek D, Vos A, Tresadern G. Rombouts FJR, et al. Among authors: cleiren e. ACS Omega. 2017 Feb 28;2(2):685-697. doi: 10.1021/acsomega.6b00482. Epub 2017 Feb 24. ACS Omega. 2017. PMID: 28626832 Free PMC article.
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
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, Nyanguile O, Simmen K, Van Remoortere P, Raboisson P, Vendeville S. Cummings MD, et al. Among authors: cleiren e. J Med Chem. 2014 Mar 13;57(5):1880-92. doi: 10.1021/jm401396p. Epub 2013 Nov 8. J Med Chem. 2014. PMID: 24144360
1a/1b subtype profiling of nonnucleoside polymerase inhibitors of hepatitis C virus.
Nyanguile O, Devogelaere B, Vijgen L, Van den Broeck W, Pauwels F, Cummings MD, De Bondt HL, Vos AM, Berke JM, Lenz O, Vandercruyssen G, Vermeiren K, Mostmans W, Dehertogh P, Delouvroy F, Vendeville S, VanDyck K, Dockx K, Cleiren E, Raboisson P, Simmen KA, Fanning GC. Nyanguile O, et al. Among authors: cleiren e. J Virol. 2010 Mar;84(6):2923-34. doi: 10.1128/JVI.01980-09. Epub 2010 Jan 13. J Virol. 2010. PMID: 20071590 Free PMC article.
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: cleiren e. 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 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: cleiren e. 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
Discovery of N-(Pyridin-4-yl)-1,5-naphthyridin-2-amines as Potential Tau Pathology PET Tracers for Alzheimer's Disease.
Rombouts FJ, Andrés JI, Ariza M, Alonso JM, Austin N, Bottelbergs A, Chen L, Chupakhin V, Cleiren E, Fierens K, Fontana A, Langlois X, Leenaerts JE, Mariën J, Martínez Lamenca C, Salter R, Schmidt ME, Te Riele P, Wintmolders C, Trabanco AA, Zhang W, Macdonald G, Moechars D. Rombouts FJ, et al. Among authors: cleiren e. J Med Chem. 2017 Feb 23;60(4):1272-1291. doi: 10.1021/acs.jmedchem.6b01173. Epub 2017 Feb 10. J Med Chem. 2017. PMID: 28106992
1,5-Benzodiazepine inhibitors of HCV NS5B polymerase.
McGowan D, Nyanguile O, Cummings MD, Vendeville S, Vandyck K, Van den Broeck W, Boutton CW, De Bondt H, Quirynen L, Amssoms K, Bonfanti JF, Last S, Rombauts K, Tahri A, Hu L, Delouvroy F, Vermeiren K, Vandercruyssen G, Van der Helm L, Cleiren E, Mostmans W, Lory P, Pille G, Van Emelen K, Fanning G, Pauwels F, Lin TI, Simmen K, Raboisson P. McGowan D, et al. Among authors: cleiren e. Bioorg Med Chem Lett. 2009 May 1;19(9):2492-6. doi: 10.1016/j.bmcl.2009.03.035. Epub 2009 Mar 14. Bioorg Med Chem Lett. 2009. PMID: 19342234
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: cleiren e. 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
23 results