新型强效载脂蛋白 A-I 肽模拟物，可刺激胆固醇外排和前-β 颗粒形成体外。

Novel potent apoA-I peptide mimetics that stimulate cholesterol efflux and pre-beta particle formation in vitro.

机构信息

IRBM P. Angeletti, Merck Research Laboratories Peptide Centre of Excellence, via Pontina km 30,600, 00040 Pomezia, Italy.

出版信息

Bioorg Med Chem Lett. 2010 Jan 1;20(1):236-9. doi: 10.1016/j.bmcl.2009.10.128. Epub 2009 Oct 30.

DOI:10.1016/j.bmcl.2009.10.128

PMID:19932961

Abstract

Reverse cholesterol transport (RCT) is believed to be the primary mechanism by which HDL and its major protein apoA-I protect against atherosclerosis. Starting from the inactive 22-amino acid peptide representing the consensus sequence of the class A amphipathic helical repeats of apoA-I, we designed novel peptides able to mobilize cholesterol from macrophages in vitro, and to stimulate the formation of 'nascent HDL' particles, with potency comparable to the entire apoA-I protein.

摘要

胆固醇逆向转运（RCT）被认为是 HDL 和其主要蛋白载脂蛋白 A-I 预防动脉粥样硬化的主要机制。从无活性的 22 个氨基酸肽开始，该肽代表载脂蛋白 A-I 的 A 类两亲性螺旋重复序列的共识序列，我们设计了新型肽，能够从体外的巨噬细胞中动员胆固醇，并刺激“新生 HDL”颗粒的形成，其效力与整个载脂蛋白 A-I 蛋白相当。