Butyrylcholinesterase

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Butyrylcholinesterase (BChE) is an enzyme widely distributed throughout the body in humans, but particularly prevalent in serum, where it occurs as a tetramer of catalytic subunits. It is distinguished from the homologous enzyme, acetylcholinesterase, by its ability to hydrolyze the non-natural substrate butyrylcholine as well as the neurotransmitter, acetylcholine. Its biological role remains obscure, but mutations in the human BCHE gene result in prolonged post-surgical apnea due to the inability of the mutant BChEs to hydrolyse the local anaesthetic, succinylcholine. BChE finds medical use as a bioscavenger for overcoming organophosphate (OP) nerve agent and insecticide intoxication by interacting rapidly with the toxic agents. Crystal structures of both the native enzyme and of its conjugates with nerve agents are available.

Contents

hBChE - Apo human

2pm8
1p0i

BChE+OP irreversible inhibitors, including nerve agents and insecticides

3djy, 3dkk - hBChE+tabun
2wid, 2wif - hBChE+Tabun analogue TA1
2wsl, 2wig – hBChE+Tabun analogue TA4
2wil, 2wij - hBChE+Tabun analogue TA5
2wik - hBChE+Tabun analogue TA6
1xlw - hBChE+echothiophate
1p0q - hBChE+soman
1xlu - hBChE+Di-Isopropyl-Phosphoro-Fluoridate (DFP)

BChE+inhibitor binding at surface of the protein (far from the active site)

2j4c – hBChE+ HgCl2

BChE+substrate analogues mimicking BCh (so as to study the enzyme/substrate complex)

1p0m - hBChE+choline
1p0p - hBChE+butyrylthiocholine

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