Structure-activity relationships of natural and non-natural amino acid-based amide and 2-oxoamide inhibitors of human phospholipase A2 enzymes

被引：26

作者：

Antonopoulou, Georgia ^{[2
]}

Barbayianni, Efrosini ^{[2
]}

Magrioti, Victoria ^{[2
]}

Cotton, Naomi ^{[1
]}

Stephens, Daren ^{[1
]}

Constantinou-Kokotou, Violetta ^{[3
]}

Dennis, Edward A. ^{[1
]}

Kokotos, George ^{[2
]}

机构：

[1] Univ Calif San Diego, Dept Chem & Biochem, La Jolla, CA 92093 USA

[2] Univ Athens, Dept Chem, Organ Chem Lab, Athens 15771, Greece

[3] Agr Univ Athens, Chem Labs, Athens 11855, Greece

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2008年 / 16卷 / 24期

关键词：

Amides; Amino acids; Inhibitors; 2-Oxoamides; Phospholipase A(2);

D O I：

10.1016/j.bmc.2008.10.046

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 [生物化学与分子生物学]; 081704 [应用化学];

摘要：

A variety of 2-oxoamides and related amides based on natural and non-natural amino acids were synthesized. Their activity on two human intracellular phospholipases (GIVA cPLA(2) and GVIA iPLA(2)) and one human secretory phospholipase (GV sPLA(2)) was evaluated. We show that an amide based on (R)-gamma-norleucine is a highly selective inhibitor of GV sPLA2. (C) 2008 Elsevier Ltd. All rights reserved.

引用

页码：10257 / 10269

页数：13

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