Ligand Screening System for the RXRα Heterodimer Using the Fluorescence RXR Agonist CU-6PMN

Mayu Kawasaki, Tomoharu Motoyama, Shoya Yamada, Masaki Watanabe, Michiko Fujihara, Akira Kambe, Shogo Nakano, Hiroki Kakuta, Sohei Ito

Research output: Contribution to journalArticlepeer-review


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.

Original languageEnglish
JournalACS Medicinal Chemistry Letters
Publication statusAccepted/In press - 2022


  • Fluorescent agonist
  • PPAR/RXR heterodimer
  • Retinoid X receptor
  • Screening assay

ASJC Scopus subject areas

  • Biochemistry
  • Drug Discovery
  • Organic Chemistry


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