Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute , 10550 North Torrey Pines Road, La Jolla, California 92037, United States.
J Med Chem. 2014 Mar 27;57(6):2169-96. doi: 10.1021/jm4005847. Epub 2013 Oct 29.
Certain amphipathic α-helical peptides can functionally mimic many of the properties of full-length apolipoproteins, thereby offering an approach to modulate high-density lipoprotein (HDL) for combating atherosclerosis. In this Perspective, we summarize the key findings and advances over the past 25 years in the development of peptides that mimic apolipoproteins, especially apolipoprotein A-I (apoA-I). This assemblage of information provides a reasonably clear picture of the state of the art in the apolipoprotein mimetic field, an appreciation of the potential for such agents in pharmacotherapy, and a sense of the opportunities for optimizing the functional properties of HDL.
某些两亲性 α-螺旋肽可以在功能上模拟全长载脂蛋白的许多特性,从而提供了一种调节高密度脂蛋白 (HDL) 以对抗动脉粥样硬化的方法。在本观点中,我们总结了过去 25 年来在开发模拟载脂蛋白的肽方面的关键发现和进展,特别是载脂蛋白 A-I (apoA-I)。这些信息的集合提供了一个相当清晰的载脂蛋白模拟领域的最新技术状况的画面,对这些药物在药物治疗中的潜力的欣赏,以及优化 HDL 功能特性的机会的感觉。