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Current Topics in Medicinal Chemistry


ISSN (Print): 1568-0266
ISSN (Online): 1873-4294

Review Article

Rexinoids for Prevention and Treatment of Cancer: Opportunities and Challenges

Author(s): Karen T. Liby and Michael B. Sporn

Volume 17, Issue 6, 2017

Page: [721 - 730] Pages: 10

DOI: 10.2174/1568026616666160617090702

Price: $65


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.

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