Quasi-irreversible inhibitor

For acetylcholine esterase (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, drugs that irreversibly inhibit acetylcholine esterase have been used as insecticides and chemical weapons [2]

See also

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. pp. 50. ISBN 9781429206792.