RXR signaling targeted cancer therapy

Abstract

<sec><p>Retinoic X receptor (RXR) acts as a critical player in regulating a series of genetic transcriptions in cancer cells since it heterodimerizes with a third of nuclear receptors (NRs). However, RXR-targeted cancer therapy was greatly undervalued. Bexarotene (Targretin®) was the first synthetic rexinoid that was approved by Food and Drug Administration for refractory cutaneous T-cell lymphoma treatment in 2000. Afterward, researchers started to focus more on the function of RXR and modifications of RXR, such as phosphorylated-RXRα (p-RXRα) and truncated RXRα (tRXRα). Meanwhile, RXR-modulating drugs began to attract more interest from oncologists because of their potential in interfering with cancer cell proliferation, differentiation, and apoptosis according to the important and comprehensive regulation effects of RXR in tumorigenesis.</p></sec><sec><p>Herein, we will review the comprehensive role of RXR between RXR signaling and oncogenesis, with a highlighted focus on the undervalued rexinoid-related cancer therapy, and discuss and propose its great potential in future clinics.</p></sec>