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]

References

^ Millary, CB; Kryger, G (199). "Crystal structures of aged phosphorylated acetylcholinesterase: nerve agent reaction products at the atomic level". Biochemistry. 38 (22). Weizmann Institute of Science: 7032–7039. doi:10.1021/bi982678l. PMID 10353814.
^ Julien, Robert (2008). A Primer of Drug Action (Eleventh ed.). Worth Publishers. p. 50. ISBN 978-1-4292-0679-2.

[1] Millary, CB; Kryger, G (199). "Crystal structures of aged phosphorylated acetylcholinesterase: nerve agent reaction products at the atomic level". Biochemistry. 38 (22). Weizmann Institute of Science: 7032–7039. doi:10.1021/bi982678l. PMID 10353814.

[2] Julien, Robert (2008). A Primer of Drug Action (Eleventh ed.). Worth Publishers. p. 50. ISBN 978-1-4292-0679-2.

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See also

References