Concepedia

First efficient uncharged reactivators for the dephosphylation of poisoned human acetylcholinesterase

Guillaume Mercey, Tristan Verdelet, Géraldine Saint-André, Émilie Gillon, Alain Wagner, Rachid Baati, Ludovic Jean, Florian Nachon, Pierre‐Yves Renard

Chemical Communications · 2011 · 103 citations · 13 references

DOI

Concepts

Abstract

Nerve agents are highly toxic organophosphorus compounds with strong inhibition potency against acetylcholinesterase (AChE). Herein, we describe two first extremely promising uncharged reactivators for poisoned human AChE with a superior or similar in vitro ability to reactivate the enzyme as compared to that of HI-6, obidoxime, TMB-4 and HLö-7.

References

13

Kinetic analysis of interactions between human acetylcholinesterase, structurally different organophosphorus compounds and oximes

Franz Worek, Horst Thiermann, L. Szinicz et al. · Biochemical Pharmacology · 2004 · 495 citations

, , +11

In Situ Selection of Lead Compounds by Click Chemistry:  Target-Guided Optimization of Acetylcholinesterase Inhibitors

Antoni Krasiński, Zoran Radić, Roman Manetsch et al. · Journal of the American Chemical Society · 2005 · 339 citations

, , +17

Pralidoxime Iodide (2-PAM) Penetrates Across the Blood-Brain Barrier

Koichi Sakurada, Kazuo Matsubara, Keiko Shimizu et al. · Neurochemical Research · 2003 · 193 citations

, , +12

Hydroxy Oximes as Organophosphorus Nerve Agent Sensors

Trevor J. Dale, Julius Rebek · Angewandte Chemie International Edition · 2009 · 170 citations

, , +7

Structure of HI-6•Sarin-Acetylcholinesterase Determined by X-Ray Crystallography and Molecular Dynamics Simulation: Reactivator Mechanism and Design

Fredrik Ekström, Andreas Hörnberg, Elisabet Artursson et al. · PLoS ONE · 2009 · 83 citations · Full text

, , +17