Molecules That Mimic Apolipoprotein A‑I: Potential Agents for Treating Atherosclerosis

• Published in: Journal of medicinal chemistry Vol. 57; no. 6; pp. 2169 - 2196
• Main Authors: Leman, Luke J, Maryanoff, Bruce E, Ghadiri, M. Reza
• Format: Journal Article
• Language: English
• Published: United States American Chemical Society 27.03.2014
• Subjects: Amino Acid Sequence; Animals; Anticholesteremic Agents - chemical synthesis; Anticholesteremic Agents - chemistry; Anticholesteremic Agents - pharmacology; Apolipoprotein A-I - chemistry; Atherosclerosis - drug therapy; Atherosclerosis - prevention & control; Biomimetics; Cardiotonic Agents - chemical synthesis; Cardiotonic Agents - pharmacology; Cholesterol, HDL - drug effects; Humans; Models, Molecular; Molecular Mimicry; Molecular Sequence Data; Peptide Fragments - chemistry; Protein Conformation; Protein Structure, Secondary; Protein Structure, Tertiary
• ISSN: 0022-2623; 1520-4804
• DOI: 10.1021/jm4005847

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.