Title : Binding sites on acetylcholinesterase for reversible ligands and phosphorylating agents. A theoretical model tested on haloxon and phosphostigmine.

Pub. Date : 1984 Feb 15

PMID : 6704184






2 Functional Relationships(s)
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1 The reaction of acetylcholinesterase (EC 3.1.1.7; human erythrocytes) with phosphostigmine, haloxon and VX was studied, and the effect of three reversible ligands (TMA, edrophonium, coumarin) and of acetylthiocholine upon the time-dependent and time-independent (reversible) inhibition by the organophosphates was evaluated. Parathion acetylcholinesterase (Cartwright blood group) Homo sapiens
2 We conclude that phosphostigmine and haloxon bind reversibly to different sites on the enzyme and the experiments agree with a theoretical model that haloxon binds reversibly to a peripheral site on acetylcholinesterase, and phosphostigmine to the catalytic site. Parathion acetylcholinesterase (Cartwright blood group) Homo sapiens