Quasi-irreversible inhibitor

For acetylcholinesterase (AChE), quasi-irreversible inhibitors are those that rapidly phosphorylate AChE. A subsequent internal dealkylation reaction may then occur, which, according to X-ray crystallography data, is suggestive of covalent bond formation. The newly formed OP-enzyme conjugate is as a result permanently deactivated.^[1]

Historically, irreversible acetylcholinesterase inhibitors have been used as insecticides and chemical weapons.^[2]

See also

• Reversible inhibitors
• Monoamine oxidase inhibitors
• Enzyme inhibitor

References

1. Millary, CB; Kryger, G (199). "Crystal structures of aged phosphorylated acetylcholinesterase: nerve agent reaction products at the atomic level". Biochemistry (Weizmann Institute of Science) 38 (22): 7032–7039. doi:10.1021/bi982678l. PMID 10353814.
2. Julien, Robert. A Primer of Drug Action (Eleventh ed.). Worth Publishers. p. 50. ISBN 978-1-4292-0679-2.