Abstract
This review describes the role of nuclear receptors in the regulation of genes involved in cholesterol transport and synthetic modulators of these receptors. Increasing the efflux of cholesterol from peripheral cells, such as lipid-laden macrophages, through a process called reverse cholesterol transport (RCT) requires HDL. Increasing the circulating levels of HDL, as well as the efficiency of the RCT process, could result in a reduction in the development of coronary artery disease and atherosclerosis. Nuclear receptors of the RXR heterodimer family have recently been shown to regulate key genes involved in HDL metabolism and reverse cholesterol transport. These include the PPARs (peroxisome proliferator activated receptors), the LXR (liver X receptor) and the farnesoid X receptor (FXR). The synthesis of specific and potent ligands for these receptors has aided in ascertaining the physiological role of these receptors as lipid sensors and the potential therapeutic utility of modulators of these receptors in dyslipidemias and cardiovascular disease.
Keywords: atherosclerotic disease, low density lipoproteins (ldl), reverse cholesterol transport (rct), coronary artery disease, peroxisome proliferator activated receptor alpha, rexinoid x receptor (rxr), phospholipid, expression
Current Topics in Medicinal Chemistry
Title: Nuclear Receptors as Potential Targets for Modulating Reverse Cholesterol Transport
Volume: 5 Issue: 3
Author(s): Patricia D. Pelton, Mona Patel and Keith T. Demarest
Affiliation:
Keywords: atherosclerotic disease, low density lipoproteins (ldl), reverse cholesterol transport (rct), coronary artery disease, peroxisome proliferator activated receptor alpha, rexinoid x receptor (rxr), phospholipid, expression
Abstract: This review describes the role of nuclear receptors in the regulation of genes involved in cholesterol transport and synthetic modulators of these receptors. Increasing the efflux of cholesterol from peripheral cells, such as lipid-laden macrophages, through a process called reverse cholesterol transport (RCT) requires HDL. Increasing the circulating levels of HDL, as well as the efficiency of the RCT process, could result in a reduction in the development of coronary artery disease and atherosclerosis. Nuclear receptors of the RXR heterodimer family have recently been shown to regulate key genes involved in HDL metabolism and reverse cholesterol transport. These include the PPARs (peroxisome proliferator activated receptors), the LXR (liver X receptor) and the farnesoid X receptor (FXR). The synthesis of specific and potent ligands for these receptors has aided in ascertaining the physiological role of these receptors as lipid sensors and the potential therapeutic utility of modulators of these receptors in dyslipidemias and cardiovascular disease.
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Cite this article as:
Pelton D. Patricia, Patel Mona and Demarest T. Keith, Nuclear Receptors as Potential Targets for Modulating Reverse Cholesterol Transport, Current Topics in Medicinal Chemistry 2005; 5 (3) . https://dx.doi.org/10.2174/1568026053544588
DOI https://dx.doi.org/10.2174/1568026053544588 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
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