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The Magic of Crystal Structure-Based Inhibitor Optimization: Development of a Butyrylcholinesterase Inhibitor with Picomolar Affinity and in Vivo Activity.
Košak U, Brus B, Knez D, Žakelj S, Trontelj J, Pišlar A, Šink R, Jukič M, Živin M, Podkowa A, Nachon F, Brazzolotto X, Stojan J, Kos J, Coquelle N, Sałat K, Colletier JP, Gobec S. Košak U, et al. Among authors: coquelle n. J Med Chem. 2018 Jan 11;61(1):119-139. doi: 10.1021/acs.jmedchem.7b01086. Epub 2017 Dec 22. J Med Chem. 2018. PMID: 29227101
Development of an in-vivo active reversible butyrylcholinesterase inhibitor.
Košak U, Brus B, Knez D, Šink R, Žakelj S, Trontelj J, Pišlar A, Šlenc J, Gobec M, Živin M, Tratnjek L, Perše M, Sałat K, Podkowa A, Filipek B, Nachon F, Brazzolotto X, Więckowska A, Malawska B, Stojan J, Raščan IM, Kos J, Coquelle N, Colletier JP, Gobec S. Košak U, et al. Among authors: coquelle n. Sci Rep. 2016 Dec 21;6:39495. doi: 10.1038/srep39495. Sci Rep. 2016. PMID: 28000737 Free PMC article.
Discovery of a Potent Dual Inhibitor of Acetylcholinesterase and Butyrylcholinesterase with Antioxidant Activity that Alleviates Alzheimer-like Pathology in Old APP/PS1 Mice.
Viayna E, Coquelle N, Cieslikiewicz-Bouet M, Cisternas P, Oliva CA, Sánchez-López E, Ettcheto M, Bartolini M, De Simone A, Ricchini M, Rendina M, Pons M, Firuzi O, Pérez B, Saso L, Andrisano V, Nachon F, Brazzolotto X, García ML, Camins A, Silman I, Jean L, Inestrosa NC, Colletier JP, Renard PY, Muñoz-Torrero D. Viayna E, et al. Among authors: coquelle n. J Med Chem. 2021 Jan 14;64(1):812-839. doi: 10.1021/acs.jmedchem.0c01775. Epub 2020 Dec 28. J Med Chem. 2021. PMID: 33356266
Design, biological evaluation and X-ray crystallography of nanomolar multifunctional ligands targeting simultaneously acetylcholinesterase and glycogen synthase kinase-3.
Oukoloff K, Coquelle N, Bartolini M, Naldi M, Le Guevel R, Bach S, Josselin B, Ruchaud S, Catto M, Pisani L, Denora N, Iacobazzi RM, Silman I, Sussman JL, Buron F, Colletier JP, Jean L, Routier S, Renard PY. Oukoloff K, et al. Among authors: coquelle n. Eur J Med Chem. 2019 Apr 15;168:58-77. doi: 10.1016/j.ejmech.2018.12.063. Epub 2019 Feb 13. Eur J Med Chem. 2019. PMID: 30798053 Free article.
44 results