Liby Karen T, Sporn Michael B
Michigan State University, Department of Pharmacology & Toxicology, B430 Life Science Building, 1355 Bogue Street, East Lansing, MI 48824.
Curr Top Med Chem. 2016 Jun 16.
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.
类视黄醛X受体激动剂是被称为RXRs的核受体的选择性配体。它们不与全反式维甲酸（RARs）的受体结合。许多新的类视黄醛X受体激动剂已被合成，然后检测它们抑制癌细胞增殖、抑制肿瘤微环境中炎症细胞活化以及在与人类疾病相关的动物模型中预防癌症发生的能力。在此，我们综述了关于4种类视黄醛X受体激动剂（贝沙罗汀、LG100268、LG101506和NRX194204）作用的文献。这些类视黄醛X受体激动剂与其他活性药物联合使用时也具有强大的协同作用，实际临床应用将受益于这些作用。
