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

被引：62

作者：

Komoda, M

Kakuta, H

Takahashi, H

Fujimoto, Y

Kadoya, S

Kato, F

Hashimoto, Y

机构：

[1] Univ Tokyo, Inst Mol & Cellular Biosci, Bunkyo Ku, Tokyo 1130032, Japan

[2] Ishihara Sangyo Kaisha Ltd, Cent Res Inst, R&D Grp Pharmaceut, Shiga 5250025, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2001年 / 9卷 / 01期

关键词：

D O I：

10.1016/S0968-0896(00)00231-5

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

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. (C) 2000 Elsevier Science Ltd. All rights reserved.

引用

页码：121 / 131

页数：11

共 32 条

[31] The main neutral aminopeptidase activity of human lymphoid tumour cell lines does not originate from the aminopeptidase N-(APN; CD13) gene [J].