Retinoid X受体（RXR）是一种核受体（NR），以配体结合依赖的方式调节靶基因的转录，具有药物靶点的兴趣。RXR激动剂已经开发为治疗皮肤浸润性T细胞淋巴瘤（如bexarotene（1）），并作为潜在的抗炎药物进行研究。已经报道了用于RXR单独结合的筛选系统。然而，尽管RXR作为RXR异二聚体发挥作用，但关于评估RXR激动剂作为RXR异二聚体的差异结合的系统信息一直不可用，直到最近。在这里，我们展示了我们设计的荧光RXR激动剂CU-6PMN（3）可用于评估RXR与PPARγ / RXRα的结合，且结合数据与仅RXRα的不同。这种筛选方法为RXR异二聚体的结合测试开辟了一条新途径。 ©2023美国化学学会。

Retinoid X receptor (RXR), a nuclear receptor (NR) that regulates transcription of target genes in a ligand binding-dependent manner, is of interest as a drug target. RXR agonists have been developed as therapeutic agents for cutaneous invasive T-cell lymphoma (e.g., bexarotene (1)) and investigated as potential anti-inflammatory agents. Screening systems for the binding of RXR alone have been reported. However, although RXRs function as RXR heterodimers, information on systems to evaluate the differential binding of RXR agonists as RXR heterodimers has not been available until recently. Here we show that the fluorescent RXR agonist CU-6PMN (3), designed by our group, can be useful for assessing RXR binding to PPARγ/RXRα, and that the binding data differ from those of RXRα alone. This screening method opens a new avenue for binding assays for RXR heterodimers.© 2023 American Chemical Society.