Abstract
Epidemiological studies have demonstrated an inverse correlation between plasma concentrations of highdensity lipoprotein cholesterol (HDL-C) and incidence of coronary heart disease (CHD); thus new therapies for raising HDL-C levels have been the focus of significant efforts by the cardiovascular medicine community. Inhibition of cholesteryl ester transfer protein (CETP) is one approach to increasing HDL-C concentrations. CETP is a plasma glycoprotein that mediates the transfer of cholesteryl esters from HDL to the apoB-containing lipoproteins, with a balanced transfer of triglycerides. Inhibition of CETP results in an accumulation of cholesteryl esters in HDL, thus resulting in increased HDL-C. Pharmacological inhibition of CETP in humans has been shown to result in increased levels of HDL-C, although any beneficial effect of this inhibition on CHD has yet to be established. This review article will discuss the complex role of CETP in lipid metabolism, recent developments for small-molecule inhibitors of CETP, and future prospects for CETP inhibitors in the treatment of CHD.
Keywords: Atherosclerosis, CETP inhibitor, cholesteryl ester transfer protein, coronary heart disease, high-density lipoprotein cholesterol, low-density lipoprotein cholesterol
Current Topics in Medicinal Chemistry
Title: Cholesteryl Ester Transfer Protein (CETP) Inhibitors
Volume: 9 Issue: 5
Author(s): Julianne A. Hunt and Zhijian Lu
Affiliation:
Keywords: Atherosclerosis, CETP inhibitor, cholesteryl ester transfer protein, coronary heart disease, high-density lipoprotein cholesterol, low-density lipoprotein cholesterol
Abstract: Epidemiological studies have demonstrated an inverse correlation between plasma concentrations of highdensity lipoprotein cholesterol (HDL-C) and incidence of coronary heart disease (CHD); thus new therapies for raising HDL-C levels have been the focus of significant efforts by the cardiovascular medicine community. Inhibition of cholesteryl ester transfer protein (CETP) is one approach to increasing HDL-C concentrations. CETP is a plasma glycoprotein that mediates the transfer of cholesteryl esters from HDL to the apoB-containing lipoproteins, with a balanced transfer of triglycerides. Inhibition of CETP results in an accumulation of cholesteryl esters in HDL, thus resulting in increased HDL-C. Pharmacological inhibition of CETP in humans has been shown to result in increased levels of HDL-C, although any beneficial effect of this inhibition on CHD has yet to be established. This review article will discuss the complex role of CETP in lipid metabolism, recent developments for small-molecule inhibitors of CETP, and future prospects for CETP inhibitors in the treatment of CHD.
Export Options
About this article
Cite this article as:
Hunt A. Julianne and Lu Zhijian, Cholesteryl Ester Transfer Protein (CETP) Inhibitors, Current Topics in Medicinal Chemistry 2009; 9 (5) . https://dx.doi.org/10.2174/156802609788340823
DOI https://dx.doi.org/10.2174/156802609788340823 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
Call for Papers in Thematic Issues
Medicinal Chemistry Advancement in Life-Threatening Diseases
The current issue will highlight concise reports that specify ground-breaking insights, including the novel discovery of drug targets and their action mechanism or drugs of novel classes. These are projected to encourage medicinal chemistry future efforts to address the most challenging medical needs. The current issue highlights further efforts to ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
Pharmacovigilance and the Cardiovascular System: Two Sides to Every Story
Current Drug Safety The Prevalence of Frailty in Patients Admitted to Hospital with Vertebral Fragility Fractures
Current Rheumatology Reviews Casein Phosphopeptides in Oral Health - Chemistry and Clinical Applications
Current Pharmaceutical Design New Pharmacologic Approaches to Prevent Thromboembolism in Patients with Atrial Fibrillation
Current Vascular Pharmacology Development of New Fibrinolytic Agents
Current Pharmaceutical Design Role of Polyunsaturated Fatty Acids and Fatty Acid Binding Protein in the Pathogenesis of Schizophrenia
Current Pharmaceutical Design Pathogenesis of Neointima Formation Following Vascular Injury
Cardiovascular & Hematological Disorders-Drug Targets Application of NMR Metabolomics to Search for Human Disease Biomarkers
Combinatorial Chemistry & High Throughput Screening Antiarrhythmic Potential of Drugs Targeting the Cardiac Ryanodine Receptor Ca<sup>2+</sup> Release Channel: Case Study of Dantrolene
Current Pharmaceutical Design Ascorbic Acid: An Old Player with a Broad Impact on Body Physiology Including Oxidative Stress Suppression and Immunomodulation: A Review
Mini-Reviews in Medicinal Chemistry Editorial [Hot Topic: Pharmacogenomics: Achievements, Challenges and Prospects, for Patients, Pharmaceutical Industries and Healthcare Systems (Guest Editor: Despina Sanoudou)]
Current Pharmaceutical Design Neuroprotective Actions of Flavones and Flavonols: Mechanisms and Relationship to Flavonoid Structural Features
Central Nervous System Agents in Medicinal Chemistry Circadian Variation of Cardiovascular Events and Morning Blood Pressure Surge
Vascular Disease Prevention (Discontinued) Copper as a Biocidal Tool
Current Medicinal Chemistry Abdominal Aortic Calcification: Clinical Significance, Mechanisms and Therapies
Current Pharmaceutical Design Availability of Some Elements from Different Types of Teas
The Natural Products Journal IL-1 Cytokines in Cardiovascular Disease: Diagnostic, Prognostic and Therapeutic Implications
Cardiovascular & Hematological Agents in Medicinal Chemistry Present Drug Therapy of Demyelinating Disorders
Current Drug Therapy Can We Move Forward After ADVANCE?
Vascular Disease Prevention (Discontinued) Risk of Bleeding Related to Antithrombotic Treatment in Cardiovascular Disease
Current Pharmaceutical Design