title: Specific inhibitor of puromycin-sensitive aminopeptidase with a homophthalimide skeleton: identification of the target molecule and a structure-activity relationship study.
abstract: 2-(2,6-Diethylphenyl)-1,2,3,4-tetrahydroisoquinoline-1,3-dione (2: PIQ-22) was found to be a potent and specific inhibitor of puromycin-sensitive aminopeptidase (PSA). Lineweaver-Burk plot analysis showed that PSA is inhibited by PIQ-22 in a non-competitive manner. Structure -activity relationship studies indicated that tautomerism of the imidobenzoylketone group in the cyclic imide moiety of the PIQ-22 skeleton is important for the inhibitory activity.
authors.affiliation: Institute of Molecular and Cellular Biosciences, University of Tokyo, Japan.
authors.forename: M
authors.initials: M
authors.lastname: Komoda
authors.forename: H
authors.initials: H
authors.lastname: Kakuta
authors.forename: H
authors.initials: H
authors.lastname: Takahashi
authors.forename: Y
authors.initials: Y
authors.lastname: Fujimoto
authors.forename: S
authors.initials: S
authors.lastname: Kadoya
authors.forename: F
authors.initials: F
authors.lastname: Kato
authors.forename: Y
authors.initials: Y
authors.lastname: Hashimoto
mesh_terms: D000626:Aminopeptidases / Q000037:antagonists & inhibitors*; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D007546:Isoquinolines / Q000737:chemistry / Q000494:pharmacology*; D011691:Puromycin / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D004791:Enzyme Inhibitors; D007546:Isoquinolines; C400282:N-(2,6-diethylphenyl)homophthalimide; D011691:Puromycin; D000626:Aminopeptidases