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

Overview

Journal ACS Med Chem Lett

Publisher American Chemical Society

Specialty Chemistry

Date 2023 Mar 16

PMID 36923911

Authors

Mayu Kawasaki

Tomoharu Motoyama

Shoya Yamada

Masaki Watanabe

Michiko Fujihara

Akira Kambe

Shogo Nakano

Hiroki Kakuta

Sohei Ito

Affiliations

Soon will be listed here.

Abstract

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 ()) 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 (), 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.

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