Specific inhibitor of puromycin-sensitive aminopeptidase with a homophthalimide skeleton: Identification of the target molecule and a structure-activity relationship study

Citation
M. Komoda et al., Specific inhibitor of puromycin-sensitive aminopeptidase with a homophthalimide skeleton: Identification of the target molecule and a structure-activity relationship study, BIO MED CH, 9(1), 2001, pp. 121-131
Citations number
32
Language
INGLESE
art.tipo
Article
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY
ISSN journal
0968-0896 → ACNP
Volume
9
Issue
1
Year of publication
2001
Pages
121 - 131
Database
ISI
SICI code
0968-0896(200101)9:1<121:SIOPAW>2.0.ZU;2-1
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 amin opeptidase (PSA). Lineweaver-Burk plot analysis showed that PSA is inhibite d by PIQ-22 in a non-competitive manner. Structure-activity relationship st udies indicated that tautomerism of the imidobenzoylketone group in the cyc lic imide moiety of the PIQ-22 skeleton is important for the inhibitory act ivity. (C) 2000 Elsevier Science Ltd. All rights reserved.