Structure-activity analysis of aging and reactivation of human butyrylcholinesterase inhibited by analogues of tabun.

@article{Carletti2009StructureactivityAO,
  title={Structure-activity analysis of aging and reactivation of human butyrylcholinesterase inhibited by analogues of tabun.},
  author={Eug{\'e}nie Carletti and Nadine Aurbek and {\'E}milie Gillon and M{\'e}lanie Loiodice and Yvain Nicolet and Juan-Carlos Fontecilla-Camps and Patrick Masson and Horst Thiermann and Florian Nachon and Franz Worek},
  journal={The Biochemical journal},
  year={2009},
  volume={421 1},
  pages={97-106}
}
hBChE [human BChE (butyrylcholinesterase)] naturally scavenges OPs (organophosphates). This bioscavenger is currently in Clinical Phase I for pretreatment of OP intoxication. Phosphylated ChEs (cholinesterases) can undergo a spontaneous time-dependent process called 'aging' during which the conjugate is dealkylated, leading to creation of an enzyme that cannot be reactivated. hBChE inhibited by phosphoramidates such as tabun displays a peculiar resistance to oxime-mediated reactivation. We… CONTINUE READING

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