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Discovery of SAR184841, a potent and long-lasting inhibitor of 11β-hydroxysteroid dehydrogenase type 1, active in a physiopathological animal model of T2D.
Venier O, Pascal C, Braun A, Namane C, Mougenot P, Crespin O, Pacquet F, Mougenot C, Monseau C, Onofri B, Dadji-Faïhun R, Leger C, Ben-Hassine M, Van-Pham T, Ragot JL, Philippo C, Farjot G, Noah L, Maniani K, Boutarfa A, Nicolaï E, Guillot E, Pruniaux MP, Güssregen S, Engel C, Coutant AL, de Miguel B, Castro A. Venier O, et al. Among authors: engel c. Bioorg Med Chem Lett. 2013 Apr 15;23(8):2414-21. doi: 10.1016/j.bmcl.2013.02.018. Epub 2013 Feb 22. Bioorg Med Chem Lett. 2013. PMID: 23478147
Pyrrolidine-pyrazole ureas as potent and selective inhibitors of 11β-hydroxysteroid-dehydrogenase type 1.
Venier O, Pascal C, Braun A, Namane C, Mougenot P, Crespin O, Pacquet F, Mougenot C, Monseau C, Onofri B, Dadji-Faïhun R, Leger C, Ben-Hassine M, Van-Pham T, Ragot JL, Philippo C, Güssregen S, Engel C, Farjot G, Noah L, Maniani K, Nicolaï E. Venier O, et al. Among authors: engel c. Bioorg Med Chem Lett. 2011 Apr 15;21(8):2244-51. doi: 10.1016/j.bmcl.2011.02.111. Epub 2011 Mar 23. Bioorg Med Chem Lett. 2011. PMID: 21439819
Characterization of RA839, a Noncovalent Small Molecule Binder to Keap1 and Selective Activator of Nrf2 Signaling.
Winkel AF, Engel CK, Margerie D, Kannt A, Szillat H, Glombik H, Kallus C, Ruf S, Güssregen S, Riedel J, Herling AW, von Knethen A, Weigert A, Brüne B, Schmoll D. Winkel AF, et al. Among authors: engel ck. J Biol Chem. 2015 Nov 20;290(47):28446-28455. doi: 10.1074/jbc.M115.678136. Epub 2015 Oct 12. J Biol Chem. 2015. PMID: 26459563 Free PMC article.
Structural basis for the highly selective inhibition of MMP-13.
Engel CK, Pirard B, Schimanski S, Kirsch R, Habermann J, Klingler O, Schlotte V, Weithmann KU, Wendt KU. Engel CK, et al. Chem Biol. 2005 Feb;12(2):181-9. doi: 10.1016/j.chembiol.2004.11.014. Chem Biol. 2005. PMID: 15734645
954 results