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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: nachon f. 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
Use of a 'caged' analogue to study the traffic of choline within acetylcholinesterase by kinetic crystallography.
Colletier JP, Royant A, Specht A, Sanson B, Nachon F, Masson P, Zaccai G, Sussman JL, Goeldner M, Silman I, Bourgeois D, Weik M. Colletier JP, et al. Among authors: nachon f. Acta Crystallogr D Biol Crystallogr. 2007 Nov;63(Pt 11):1115-28. doi: 10.1107/S0907444907044472. Epub 2007 Oct 17. Acta Crystallogr D Biol Crystallogr. 2007. PMID: 18007027
Reaction of cresyl saligenin phosphate, the organophosphorus agent implicated in aerotoxic syndrome, with human cholinesterases: mechanistic studies employing kinetics, mass spectrometry, and X-ray structure analysis.
Carletti E, Schopfer LM, Colletier JP, Froment MT, Nachon F, Weik M, Lockridge O, Masson P. Carletti E, et al. Among authors: nachon f. Chem Res Toxicol. 2011 Jun 20;24(6):797-808. doi: 10.1021/tx100447k. Epub 2011 Apr 18. Chem Res Toxicol. 2011. PMID: 21438623 Free PMC article.
Organophosphate hydrolases as catalytic bioscavengers of organophosphorus nerve agents.
Trovaslet-Leroy M, Musilova L, Renault F, Brazzolotto X, Misik J, Novotny L, Froment MT, Gillon E, Loiodice M, Verdier L, Masson P, Rochu D, Jun D, Nachon F. Trovaslet-Leroy M, et al. Among authors: nachon f. Toxicol Lett. 2011 Sep 25;206(1):14-23. doi: 10.1016/j.toxlet.2011.05.1041. Epub 2011 Jun 12. Toxicol Lett. 2011. PMID: 21683774
138 results