Abstract
Large-scale epidemiological studies firmly established the association between low plasma levels of high-density lipoprotein-cholesterol (HDL-C) and elevated risk of cardiovascular disease. This relationship is thought to reflect the key biological function of HDL, which involves reverse cholesterol transport from the arterial wall to the liver for further excretion from the body. Other aspects of the cardioprotective HDL functionality include antioxidative, anti-inflammatory, anti-apoptotic, anti-thrombotic, vasodilatory, anti-infectious and antidiabetic activities. Over the last decades, wide interest in HDL as an athero- and cardioprotective particle has resulted in the development of HDL-C raising as a therapeutic approach to reduce cardiovascular risk. Several strategies to increase circulating HDL-C concentrations were developed that primarily included use of niacin and fibrates as potent HDL-C raising agents. In the statin era, inhibition of cholesteryl ester transfer protein, infusion of artificially reconstituted HDL and administration of apolipoprotein A-I mimetics were established as novel approaches to raise HDL-C. More recently, other strategies targeting HDL metabolism, such as upregulation of apolipoprotein A-I production by the liver, were added to the list of HDL therapeutics. This review summarises current knowledge of novel HDL-targeting therapies and discusses perspectives of their use.
Keywords: Atherosclerosis, apoA-I, cardiovascular disease, CETP, HDL, lipoprotein, miRNA, rHDL.
Current Pharmaceutical Design
Title:HDL-Targeting Therapeutics: Past, Present and Future
Volume: 23 Issue: 8
Author(s): Emile Zakiev, Ma Feng, Vasily Sukhorukov and Anatol Kontush*
Affiliation:
- INSERM UMR_S 1166, Faculte de Medecine Pitie-Salpetriere, Bld de L'Hopital 91, 75013 Paris,France
Keywords: Atherosclerosis, apoA-I, cardiovascular disease, CETP, HDL, lipoprotein, miRNA, rHDL.
Abstract: Large-scale epidemiological studies firmly established the association between low plasma levels of high-density lipoprotein-cholesterol (HDL-C) and elevated risk of cardiovascular disease. This relationship is thought to reflect the key biological function of HDL, which involves reverse cholesterol transport from the arterial wall to the liver for further excretion from the body. Other aspects of the cardioprotective HDL functionality include antioxidative, anti-inflammatory, anti-apoptotic, anti-thrombotic, vasodilatory, anti-infectious and antidiabetic activities. Over the last decades, wide interest in HDL as an athero- and cardioprotective particle has resulted in the development of HDL-C raising as a therapeutic approach to reduce cardiovascular risk. Several strategies to increase circulating HDL-C concentrations were developed that primarily included use of niacin and fibrates as potent HDL-C raising agents. In the statin era, inhibition of cholesteryl ester transfer protein, infusion of artificially reconstituted HDL and administration of apolipoprotein A-I mimetics were established as novel approaches to raise HDL-C. More recently, other strategies targeting HDL metabolism, such as upregulation of apolipoprotein A-I production by the liver, were added to the list of HDL therapeutics. This review summarises current knowledge of novel HDL-targeting therapies and discusses perspectives of their use.
Export Options
About this article
Cite this article as:
Zakiev Emile, Feng Ma, Sukhorukov Vasily and Kontush Anatol*, HDL-Targeting Therapeutics: Past, Present and Future, Current Pharmaceutical Design 2017; 23(8) . https://dx.doi.org/10.2174/1381612822666161027153140
DOI https://dx.doi.org/10.2174/1381612822666161027153140 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |

- Author Guidelines
- Editorial Policies
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Allegations from Whistleblowers
- Publishing Ethics and Rectitude
- Increase Visibility Of Your Article
- Archiving Policies
- Reviewer Guidelines
- Guest Editor Guidelines
- Board Recruitment Workflow
- Short Guide for New Editors
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Announcements
- Forthcoming Thematic Issues
Related Articles
-
Microparticles: From Biogenesis to Biomarkers and Diagnostic Tools in Cardiovascular Disease
Current Stem Cell Research & Therapy Patients with Rheumatic Diseases Overlooked during COVID-19 Pandemic: How are They Doing and Behaving?
Current Rheumatology Reviews A Novel Potential Reproductive Effects of Pterocarpus marsupium Methanolic Extract on Testosterone Propionate Induced Polycystic Ovary Syndrome in Female Albino Rats
Endocrine, Metabolic & Immune Disorders - Drug Targets Pro-Angiogenic Effect of Endomyocardial Biopsy-Derived Cells for Cardiac Regeneration
Current Tissue Engineering (Discontinued) Preoperative and Follow up Multi-Detector Row CT Angiography (MDCTA) in the Evaluation of Interrupted Aortic Arch (IAA)
Current Medical Imaging Mitral Balloon Valvuloplasty: State-of-the-Art Paper
Current Cardiology Reviews The Lung Disease of Rheumatoid Arthritis
Current Respiratory Medicine Reviews Arterial Hypertension and Kidney Circulation
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) Obesity-Induced Cerebral Hypoperfusion Derived from Endothelial Dysfunction: One of the Risk Factors for Alzheimer's Disease
Current Alzheimer Research Editorial (Thematic Issue: Protection, Repair and Regeneration of Achybreaky Heart)
Current Drug Targets Why are People with “Poor Lung Function” At Increased Atherothrombotic Risk?A Critical Review with Potential Therapeutic Indications
Current Vascular Pharmacology Reactive Oxygen Species in the Initiation of IL-4 Driven Autoimmunity as a Potential Therapeutic Target
Current Pharmaceutical Design Prognostic Significance of Asymptomatic Myocardial Ischemia in Women vs. Men
Current Pharmaceutical Design Tumor Angiogenesis: A Potential Target In Cancer Control by Phytochemicals
Current Cancer Drug Targets Homocysteine and Heart Failure: An Overview
Recent Patents on Cardiovascular Drug Discovery Functional and Structural Alterations of Large Arteries: Methodological Issues
Current Pharmaceutical Design Mechanisms of Fetal and Neonatal Renal Impairment by Pharmacologic Inhibition of Angiotensin
Current Medicinal Chemistry Inflammation in Ischemic Stroke Subtypes
Current Pharmaceutical Design Editorial [Hot topic: The Inflammation Paradigm in Cardiovascular Disease (Guest Editor: Guha Krishnaswamy)]
Cardiovascular & Hematological Disorders-Drug Targets Using Properties of Tumor Microenvironments for Controlling Local, On-Demand Delivery from Biopolymer-Based Nanocarriers
Current Pharmaceutical Design