title: Proctolin: a potent inhibitor of aminoenkephalinase.
abstract: Proctolin is a potent selective inhibitor of aminoenkephalinase. The specificity of its inhibition of various aminopeptidases is similar to that of puromycin; it inhibits aminoenkephalinase, but not leucine aminopeptidase or aminopeptidase M. Enkephalin breakdown by synaptic plasma membrane, but not by brain slices, is sensitive to proctolin. The inhibition by proctolin is partially caused by its resistance to enzymatic breakdown. The inhibition is of mixed type and is concentration dependent, and the two amino acids at the N-terminal are important for its action. The minimal structure for inhibition is a dipeptide with a basic amino acid at the N-terminal and a basic or an aromatic amino acid at the C-terminal.
authors.forename: K S
authors.initials: KS
authors.lastname: Hui
authors.forename: M P
authors.initials: MP
authors.lastname: Hui
authors.forename: N
authors.initials: N
authors.lastname: Ling
authors.forename: A
authors.initials: A
authors.lastname: Lajtha
mesh_terms: D000626:Aminopeptidases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D000818:Animals; D002462:Cell Membrane / Q000201:enzymology; D003600:Cytosol / Q000201:enzymology; D004744:Enkephalin, Methionine / Q000378:metabolism; D066298:In Vitro Techniques; D009419:Nerve Tissue Proteins / Q000494:pharmacology; D009479:Neuropeptides; D018377:Neurotransmitter Agents / Q000378:metabolism / Q000494:pharmacology*; D009842:Oligopeptides / Q000378:metabolism / Q000494:pharmacology*; D051381:Rats; D013329:Structure-Activity Relationship
chemical_list: D009419:Nerve Tissue Proteins; D009479:Neuropeptides; D018377:Neurotransmitter Agents; D009842:Oligopeptides; C011536:proctolin; D004744:Enkephalin, Methionine; D000626:Aminopeptidases; C025579:enkephalin degrading enzyme