Quasi-irreversible inhibitor explained

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

Notes and References

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