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