ArticleThe Journal of pharmacology and experimental therapeutics2010
5A apolipoprotein mimetic peptide promotes cholesterol efflux and reduces atherosclerosis in mice.
Article in The Journal of pharmacology and experimental therapeutics, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 70 papers, 1 of them a synthesis that pooled it.
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Who cites it
70 citing papers in PubMed, 1 synthesis or guideline pooled it, 110 citations in OpenAlex.
- Efficacy and Safety of High-Density Lipoprotein/Apolipoprotein A1 Replacement Therapy in Humans and Mice With Atherosclerosis: A Systematic Review and Meta-Analysis.Frontiers in cardiovascular medicine · 2021Pooled it
- Macrophage source influences peritoneal persistence and immune cell dynamics in assays of reverse cholesterol transport.Journal of lipid research · 2026Article
- Bioactive peptides targeting dyslipidemia and atherosclerosis: from computational discovery and data bottlenecks to precision medicine translation.Frontiers in molecular biosciences · 2026Review
- Inventive HDL Mimicking Nanoparticles: A Promising Frontier in Cardiovascular Disease Management.Cardiovascular toxicology · 2025Review
- Proteomic Determinants of Variation in Cholesterol Efflux: Observations from the Dallas Heart Study.International journal of molecular sciences · 2023Article
- Apolipoprotein-mimetic nanodiscs reduce lipid accumulation and improve liver function in acid sphingomyelinase deficiency.Nanomedicine : nanotechnology, biology, and medicine · 2023Article
- A Current Update on the Role of HDL-Based Nanomedicine in Targeting Macrophages in Cardiovascular Disease.Pharmaceutics · 2023Review
- Apolipoproteins as potential communicators play an essential role in the pathogenesis and treatment of early atherosclerosis.International journal of biological sciences · 2023Review
- Novel peptide inhibitors targeting CD40 and CD40L interaction: A potential for atherosclerosis therapy.Current research in structural biology · 2023Article
- The HDL particle composition determines its antitumor activity in pancreatic cancer.Life science alliance · 2022Article
- A Systematic Review of Apolipoprotein A-I Mimetic Peptides for Atherosclerosis Therapy via Activation of the Reverse Cholesterol Transport Pathway.ARYA atherosclerosis · 2022Review
- High-density lipoproteins, reverse cholesterol transport and atherogenesis.Nature reviews. Cardiology · 2021Review
- Apolipoprotein and LRP1-Based Peptides as New Therapeutic Tools in Atherosclerosis.Journal of clinical medicine · 2021Review
- Review
- A novel apoA-I mimetic peptide suppresses atherosclerosis by promoting physiological HDL function in apoEBritish journal of pharmacology · 2020Article
- High-density lipoproteins are a potential therapeutic target for age-related macular degeneration.The Journal of biological chemistry · 2020Article
- Stearoyl-CoA desaturase-1 impairs the reparative properties of macrophages and microglia in the brain.The Journal of experimental medicine · 2020Article
- Probing the Assembly of HDL Mimetic, Drug Carrying Nanoparticles Using Intrinsic Fluorescence.The Journal of pharmacology and experimental therapeutics · 2020Article
- Phospholipid Component Defines Pharmacokinetic and Pharmacodynamic Properties of Synthetic High-Density Lipoproteins.The Journal of pharmacology and experimental therapeutics · 2020Article
- A dual apolipoprotein C-II mimetic-apolipoprotein C-III antagonist peptide lowers plasma triglycerides.Science translational medicine · 2020Article
10 more citing papers are in PubMed but not listed here.
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
11 authors at 5 institutions in 2 countries.
Funding
Abstract
Intravenous administration of apolipoprotein (apo) A-I complexed with phospholipid has been shown to rapidly reduce plaque size in both animal models and humans. Short synthetic amphipathic peptides can mimic the antiatherogenic properties of apoA-I and have been proposed as alternative therapeutic agents. In this study, we investigated the atheroprotective effect of the 5A peptide, a bihelical amphipathic peptide that specifically effluxes cholesterol from cells by ATP-binding cassette transporter 1 (ABCA1). 5A stimulated a 3.5-fold increase in ABCA1-mediated efflux from cells and an additional 2.5-fold increase after complexing it with phospholipid (1:7 mol/mol). 5A-palmitoyl oleoyl phosphatidyl choline (POPC), but not free 5A, was also found to promote cholesterol efflux by ABCG1. When incubated with human serum, 5A-POPC bound primarily to high-density lipoprotein (HDL) but also to low-density lipoprotein (LDL) and promoted the transfer of cholesterol from LDL to HDL. Twenty-four hours after intravenous injection of 5A-POPC (30 mg/kg) into apoE-knockout (KO) mice, both the cholesterol (181%) and phospholipid (219%) content of HDL significantly increased. By an in vivo cholesterol isotope dilution study and monitoring of the flux of cholesterol from radiolabeled macrophages to stool, 5A-POPC treatment was observed to increase reverse cholesterol transport. In three separate studies, 5A when complexed with various phospholipids reduced aortic plaque surface area by 29 to 53% (n = 8 per group; p < 0.02) in apoE-KO mice. No signs of toxicity from the treatment were observed during these studies. In summary, 5A promotes cholesterol efflux both in vitro and in vivo and reduces atherosclerosis in apoE-KO mice, indicating that it may be a useful alternative to apoA-I for HDL therapy.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.