Article
Inhibitors tethered near the acetylcholinesterase active site serve as molecular rulers of the peripheral and acylation sites.
The Journal of biological chemistry - 3 Oct 2003
Johnson Joseph L, Cusack Bernadette, Hughes Thomas F, McCullough Elizabeth H, Fauq Abdul, Romanovskis Peteris, Spatola Arno F, Rosenberry Terrone L
Abstract excerpt
The acetylcholinesterase (AChE) active site consists of a narrow gorge with two separate ligand binding sites: an acylation site (or A-site) at the bottom of the gorge where substrate hydrolysis occurs and a peripheral site (or P-site) at the gorge mouth. AChE is inactivated by organophosphates as they pass through the P-site and phosphorylate the catalytic serine in the A-site. One strategy to protect against...
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