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

By Ingenito, Raffaele; Burton, Charlotte; Langella, Annunziata; Chen, Xun; Zytko, Karolina; Pessi, Antonello; Wang, Jun; Bianchi, Elisabetta
From Bioorganic & Medicinal Chemistry Letters (2010), 20(1), 236-239. Language: English, Database: CAPLUS, DOI:10.1016/j.bmcl.2009.10.128

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.