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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| Format: | Article |
| Language: | English |
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Wiley
2007-01-01
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| 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. |
| format | Article |
| id | doaj-art-22e3dc46a3844ce582b2016d019d6f6f |
| institution | Kabale University |
| issn | 1687-4757 1687-4765 |
| language | English |
| publishDate | 2007-01-01 |
| publisher | Wiley |
| record_format | Article |
| series | PPAR Research |
| 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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