Document Detail


Apolipoprotein A-I mimetic peptides: a potential new therapy for the prevention of atherosclerosis.
MedLine Citation:
PMID:  20395699     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
The beneficial effects of high-density lipoprotein (HDL) on atherosclerosis have largely been attributed to its major protein, apolipoprotein A-I (apoA-I). Used as a therapeutic intervention, apoA-I is a large protein that requires venous administration, and is both difficult and expensive to manufacture. Because of these problems with apoA-I, the generation of smaller, easier to manufacture apoA-I mimetic peptides has become a target for pharmacologic development in the therapeutic management of human atherosclerosis. A potent apoA-I mimetic peptide, 4F, was found to have significant activity in various inflammatory states in both mice and monkeys. The anti-inflammatory and antiatherogenic effects of 4F include increased pre-beta HDL formation, increased cholesterol efflux, the conversion of pro-inflammatory HDL to anti-inflammatory HDL, and reduced lipoprotein oxidation. In addition, improved arterial vasoreactivity is another important function of 4F. In a rat model of diabetes, D-4F increased arterial concentrations of heme oxygenase-1 (HO-1) and superoxide dismutase, decreased superoxide levels, reduced levels of circulating endothelial cells, decreased endothelial cell fragmentation, and restored arterial vasoreactivity to normal. In a mouse model of systemic sclerosis, D-4F functioned to improve vasodilation and angiogenic potential, while reducing myocardial inflammation and oxidative stress. With respect to mouse models of heart transplant-associated atherosclerosis, D-4F induced HO-1. In addition, D-4F was shown to improve cognitive performance in low-density lipoprotein-receptor null mice with Western diet-induced cognitive decline. D-4F also reduced the kidney content of oxidized phospholipids in a mouse model of hyperlipidemia-induced renal inflammation. In early human studies in patients with significant cardiovascular risk, a single dose of oral D-4F was found to safely improve the anti-inflammatory index of HDL. L-4F is also being studied in clinical trials as a potential treatment modality for obesity and the metabolic syndrome.
Authors:
Courtney B Sherman; Stephen J Peterson; William H Frishman
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Publication Detail:
Type:  Journal Article; Review    
Journal Detail:
Title:  Cardiology in review     Volume:  18     ISSN:  1538-4683     ISO Abbreviation:  Cardiol Rev     Publication Date:    2010 May-Jun
Date Detail:
Created Date:  2010-04-16     Completed Date:  2010-07-13     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9304686     Medline TA:  Cardiol Rev     Country:  United States    
Other Details:
Languages:  eng     Pagination:  141-7     Citation Subset:  IM    
Affiliation:
Department of Medicine, University of California, San Francisco, CA, USA.
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MeSH Terms
Descriptor/Qualifier:
Animals
Apolipoprotein A-I / therapeutic use*
Atherosclerosis / metabolism,  prevention & control*
Biomimetic Materials / therapeutic use*
Disease Models, Animal
Humans
Lipoproteins, HDL / metabolism
Mice
Peptides / therapeutic use
Rats
Chemical
Reg. No./Substance:
0/Apolipoprotein A-I; 0/D-4F peptide; 0/L-4F peptide; 0/Lipoproteins, HDL; 0/Peptides

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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