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Published on: November 10, 2017
High-density lipoprotein-based drug discovery for treatment of atherosclerosis
1Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College , No.1 Tiantan Xili, Beijing 100050 , China.
Insights
High-density lipoprotein (HDL) functionality, not just cholesterol levels, is key for treating atherosclerotic cardiovascular disease (CVD). Enhancing HDL
Area of Science:
- Cardiovascular Research
- Lipid Metabolism
- Pharmacology
Background:
- Despite statin therapy, atherosclerotic cardiovascular disease (CVD) remains a significant health burden.
- Novel high-density lipoprotein (HDL)-based therapeutics are being explored to address this challenge.
- Focus has shifted from raising HDL cholesterol (HDL-C) to improving HDL functionality, particularly reverse cholesterol transport (RCT).
Purpose of the Study:
- To review key factors in the reverse cholesterol transport (RCT) process for potential drug targets.
- To summarize screening methods for targeting RCT and their applications.
- To introduce emerging clinical strategies for enhancing HDL function in RCT.
Main Methods:
- Literature review of RCT factors and drug targets.
- Summary of screening methodologies for RCT.
- Overview of current clinical development strategies for HDL function.
Main Results:
- Identified key factors within the RCT process as potential therapeutic targets.
- Cataloged effective screening methods for evaluating RCT.
- Highlighted novel strategies in clinical development to improve HDL function.
Conclusions:
- HDL functionality is a more critical metric than HDL-C levels for evaluating pharmacological treatments for atherosclerosis.
- HDL-based strategies promoting macrophage RCT are central to current drug discovery for atherosclerotic diseases.
- Further understanding of HDL functionality in atherosclerosis promises future therapeutic advancements.
Introduction:
Although there has been great progress achieved by the use of intensive statin therapy, the burden of atherosclerotic cardiovascular disease (CVD) remains high. This has initiated the search for novel high-density lipoprotein (HDL)-based therapeutics. Recent years have witnessed a shift from traditional raising HDL-C levels to enhancing HDL functionality, in which the process of reverse cholesterol transport (RCT) has acquired much attention.
Areas Covered:
In this review, the authors describe the key factors involved in RCT process for potential drug targets to reduce the CVD risk. Furthermore, the review provides a summary of the effective screening methods that have been developed to target RCT and their applications. This review also introduces some new strategies currently being clinically developed, which have the potential to improve HDL function in the RCT process.
Expert Opinion:
It is rational that the functionality of HDL is more important than the plasma HDL-C level in the evaluation of pharmacological treatment in atherosclerosis. HDL-based strategies designed to promote macrophage RCT are a major area of current drug discovery and development for atherosclerotic diseases. A better understanding of the functionality of HDL and its relationship with atherosclerosis will expand our knowledge of the role of HDL in lipid metabolism, holding promise for a future successful HDL-based therapy.
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