Abstract
Rexinoids are selective ligands for the nuclear receptors known as RXRs. They do not bind to the receptors for all-trans-retinoic acid (RARs). Many new rexinoids have been synthesized and then assayed for their ability to suppress proliferation of cancer cells, to inhibit activation of inflammatory cells of the tumor microenvironment, and to prevent carcinogenesis in animal models relevant to human disease. Here we review the literature on the effects of 4 such rexinoids: bexarotene, LG100268, LG101506, and NRX194204. These rexinoids also have potent synergistic effects when used in combination with other active pharmacological agents, and practical clinical applications would benefit from these actions.
Keywords: RXR, Bexarotene, LG100268, Inflammation, Carcinogenesis, Combination therapy.
Graphical Abstract
Current Topics in Medicinal Chemistry
Title:Rexinoids for Prevention and Treatment of Cancer: Opportunities and Challenges
Volume: 17 Issue: 6
Author(s): Karen T. Liby and Michael B. Sporn
Affiliation:
Keywords: RXR, Bexarotene, LG100268, Inflammation, Carcinogenesis, Combination therapy.
Abstract: Rexinoids are selective ligands for the nuclear receptors known as RXRs. They do not bind to the receptors for all-trans-retinoic acid (RARs). Many new rexinoids have been synthesized and then assayed for their ability to suppress proliferation of cancer cells, to inhibit activation of inflammatory cells of the tumor microenvironment, and to prevent carcinogenesis in animal models relevant to human disease. Here we review the literature on the effects of 4 such rexinoids: bexarotene, LG100268, LG101506, and NRX194204. These rexinoids also have potent synergistic effects when used in combination with other active pharmacological agents, and practical clinical applications would benefit from these actions.
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Cite this article as:
Liby T. Karen and Sporn B. Michael, Rexinoids for Prevention and Treatment of Cancer: Opportunities and Challenges, Current Topics in Medicinal Chemistry 2017; 17 (6) . https://dx.doi.org/10.2174/1568026616666160617090702
DOI https://dx.doi.org/10.2174/1568026616666160617090702 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
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