Potent complement C3a receptor agonists derived from oxazole amino acids: Structure-activity relationships

被引：7

作者：

Singh, Ranee ^{[1
]}

Reed, Anthony N. ^{[1
]}

Chu, Peifei ^{[1
]}

Scully, Conor C. G. ^{[1
]}

Yau, Mei-Kwan ^{[1
]}

Suen, Jacky Y. ^{[1
]}

Durek, Thomas ^{[1
]}

Reid, Robert C. ^{[1
]}

Fairlie, David P. ^{[1
]}

机构：

[1] Univ Queensland, Inst Mol Biosci, Div Chem & Struct Biol, Brisbane, Qld 4072, Australia

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2015年 / 25卷 / 23期

基金：

澳大利亚研究理事会; 英国医学研究理事会;

关键词：

C3aR agonist; C3a; Oxazole; Complement; Inflammation; ANAPHYLATOXIN C3A; ANTAGONISTS; LIGANDS; IDENTIFICATION; DERIVATIVES; INHIBITION; DISCOVERY; PROTEIN; ASTHMA;

D O I：

10.1016/j.bmcl.2015.10.038

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Potent ligands for the human complement C3a receptor (C3aR) were developed from the almost inactive tripeptide Leu-Ala-Arg corresponding to the three C-terminal residues of the endogenous peptide agonist C3a. The analogous Leu-Ser-Arg was modified by condensing the serine side chain with the leucine carbonyl with elimination of water to form leucine-oxazole-arginine. Subsequent elaboration with a variety of N-terminal amide capping groups produced agonists as potent as human C3a itself in stimulating Ca2+ release from human macrophages. Structure-activity relationships are discussed. (C) 2015 Elsevier Ltd. All rights reserved.

引用

页码：5604 / 5608

页数：5

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