Therapeutic Potential of Retinoid X Receptor Modulators for the Treatment of the Metabolic Syndrome

The increasing prevalence of obesity is a fundamental contributor to the growing prevalence of the metabolic syndrome. Rexinoids, a class of compounds that selectively bind and activate RXR, are being studied as a potential option for the treatment of metabolic syndrome. These compounds have glucose...

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Main Authors: Jane A. Pinaire, Anne Reifel-Miller
Format: Article
Language:English
Published: Wiley 2007-01-01
Series:PPAR Research
Online Access:http://dx.doi.org/10.1155/2007/94156
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author Jane A. Pinaire
Anne Reifel-Miller
author_facet Jane A. Pinaire
Anne Reifel-Miller
author_sort Jane A. Pinaire
collection DOAJ
description The increasing prevalence of obesity is a fundamental contributor to the growing prevalence of the metabolic syndrome. Rexinoids, a class of compounds that selectively bind and activate RXR, are being studied as a potential option for the treatment of metabolic syndrome. These compounds have glucose-lowering, insulin-sensitizing, and antiobesity effects in animal models of insulin resistance and type 2 diabetes. However, undesirable side effects such as hypertriglyceridemia and suppression of the thyroid hormone axis also occur. This review examines and compares the effects of four RXR-selective ligands: LGD1069, LG100268, AGN194204, and LG101506, a selective RXR modulator. Similar to selective modulators of other nuclear receptors such as the estrogen receptor (SERMs), LG101506 binding to RXR selectively maintains the desirable characteristic effects of rexinoids while minimizing the undesirable effects. These recent findings suggest that, with continued research efforts, RXR-specific ligands with improved pharmacological profiles may eventually be available as additional treatment options for the current epidemic of obesity, insulin resistance, type 2 diabetes, and all of the associated metabolic sequelae.
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spelling doaj-art-22e3dc46a3844ce582b2016d019d6f6f2025-02-03T05:59:12ZengWileyPPAR Research1687-47571687-47652007-01-01200710.1155/2007/9415694156Therapeutic Potential of Retinoid X Receptor Modulators for the Treatment of the Metabolic SyndromeJane A. Pinaire0Anne Reifel-Miller1Lilly Research Laboratories, Lilly Corporate Center, Indianapolis 46285, IN, USALilly Research Laboratories, Lilly Corporate Center, Indianapolis 46285, IN, USAThe increasing prevalence of obesity is a fundamental contributor to the growing prevalence of the metabolic syndrome. Rexinoids, a class of compounds that selectively bind and activate RXR, are being studied as a potential option for the treatment of metabolic syndrome. These compounds have glucose-lowering, insulin-sensitizing, and antiobesity effects in animal models of insulin resistance and type 2 diabetes. However, undesirable side effects such as hypertriglyceridemia and suppression of the thyroid hormone axis also occur. This review examines and compares the effects of four RXR-selective ligands: LGD1069, LG100268, AGN194204, and LG101506, a selective RXR modulator. Similar to selective modulators of other nuclear receptors such as the estrogen receptor (SERMs), LG101506 binding to RXR selectively maintains the desirable characteristic effects of rexinoids while minimizing the undesirable effects. These recent findings suggest that, with continued research efforts, RXR-specific ligands with improved pharmacological profiles may eventually be available as additional treatment options for the current epidemic of obesity, insulin resistance, type 2 diabetes, and all of the associated metabolic sequelae.http://dx.doi.org/10.1155/2007/94156
spellingShingle Jane A. Pinaire
Anne Reifel-Miller
Therapeutic Potential of Retinoid X Receptor Modulators for the Treatment of the Metabolic Syndrome
PPAR Research
title Therapeutic Potential of Retinoid X Receptor Modulators for the Treatment of the Metabolic Syndrome
title_full Therapeutic Potential of Retinoid X Receptor Modulators for the Treatment of the Metabolic Syndrome
title_fullStr Therapeutic Potential of Retinoid X Receptor Modulators for the Treatment of the Metabolic Syndrome
title_full_unstemmed Therapeutic Potential of Retinoid X Receptor Modulators for the Treatment of the Metabolic Syndrome
title_short Therapeutic Potential of Retinoid X Receptor Modulators for the Treatment of the Metabolic Syndrome
title_sort therapeutic potential of retinoid x receptor modulators for the treatment of the metabolic syndrome
url http://dx.doi.org/10.1155/2007/94156
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