基于天然和非天然氨基酸的人磷脂酶A(2)酶酰胺及2-氧代酰胺抑制剂的构效关系
Structure-activity relationships of natural and non-natural amino acid-based amide and 2-oxoamide inhibitors of human phospholipase A(2) enzymes.
作者信息
Antonopoulou Georgia, Barbayianni Efrosini, Magrioti Victoria, Cotton Naomi, Stephens Daren, Constantinou-Kokotou Violetta, Dennis Edward A, Kokotos George
机构信息
Laboratory of Organic Chemistry, Department of Chemistry, University of Athens, Panepistimiopolis, Athens 15771, Greece.
出版信息
Bioorg Med Chem. 2008 Dec 15;16(24):10257-69. doi: 10.1016/j.bmc.2008.10.046. Epub 2008 Nov 1.
Abstract
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 sPLA(2).
摘要
合成了多种基于天然和非天然氨基酸的2-氧代酰胺及相关酰胺。评估了它们对两种人细胞内磷脂酶（GIVA cPLA(2)和GVIA iPLA(2)）以及一种人分泌型磷脂酶（GV sPLA(2)）的活性。我们发现，一种基于（R）-γ-正亮氨酸的酰胺是GV sPLA(2)的高选择性抑制剂。
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