The retinoid X receptor (RXR) is a member of the steroid/thyroid hormone superfamily of nuclear receptors (NRs) which are transcription factors that are essential in embryonic development, maintenance of differentiated phenotypes, metabolism and cell death. This review is to provide an overview of the mechanism of RXRα and RXRα signaling pathways involving RXR/TR3, RAR/RXR, PPAR/RXR, VDR/RXR, LXR/RXR, FXR/RXR in cancer cells and other diseases, which will enhance our ability to design rational therapeutic drugs for cancer. Recent studies have shown that an N-terminally truncated RXRα (tRXRα) exists in several cancer cell lines and primary tumors, which is considered as a kind of oncoprotein, demonstrating the new suitability of targeting tRXRα for cancer therapy.

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