Novel potent apoA-I peptide mimetics that stimulate cholesterol efflux and pre-beta particle formation in vitro.
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.
Ingenito
Raffaele
R
IRBM P. Angeletti, Merck Research Laboratories Peptide Centre of Excellence, via Pontina km 30,600, 00040 Pomezia, Italy. raffaele_ingenito@merck.com
Burton
Charlotte
C
Langella
Annunziata
A
Chen
Xun
X
Zytko
Karolina
K
Pessi
Antonello
A
Wang
Jun
J
Bianchi
Elisabetta
E
D000595:Amino Acid Sequence; D000818:Animals; D016632:Apolipoprotein A-I / Q000737:chemistry* / Q000378:metabolism; D002460:Cell Line; D002784:Cholesterol / Q000378:metabolism*; D002942:Circular Dichroism; D053442:High-Density Lipoproteins, Pre-beta / Q000378:metabolism*; D008264:Macrophages / Q000378:metabolism; D051379:Mice; D008969:Molecular Sequence Data; D010455:Peptides / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity; D017510:Protein Folding; D017433:Protein Structure, Secondary
D016632:Apolipoprotein A-I; D053442:High-Density Lipoproteins, Pre-beta; D010455:Peptides; D002784:Cholesterol