Fluorescence properties of retinoid X receptor antagonist NEt-SB

Shoya Yamada, Yuta Takamura, Michiko Fujihara, Mayu Kawasaki, Sohei Ito, Shogo Nakano, Hiroki Kakuta

Research output: Contribution to journalArticlepeer-review

1 Citation (Scopus)

Abstract

Ligands of retinoid X receptors (RXRs) are effective against various diseases, so there is a need for efficient screening methods to discover new ligands. Existing screening methods are complex and time-consuming, and a simple fluorescence assay would be highly desirable. Here, we focused on NEt-SB (4), which has a stilbene structure, as a candidate for this purpose, and examined its fluorescence properties in detail. The fluorescence intensity of 4 was remarkably increased in highly viscous solvents and upon binding to hRXRα-LBD, due to suppression of free rotation of the stilbene moiety. Although the relatively low fluorescence intensity and the short fluorescence wavelength of 4 make this compound itself unsuitable for use in RXR binding assay, our findings provide a basis for further structural evolution, which may lead to a derivative that would be suitable for fluorescence assay of RXR binders.

Original languageEnglish
Article number127666
JournalBioorganic and Medicinal Chemistry Letters
Volume31
DOIs
Publication statusPublished - Jan 1 2021
Externally publishedYes

Keywords

  • Binding assay
  • Fluorescence
  • RXR
  • Solvatochromism
  • Stilbene

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

Fingerprint Dive into the research topics of 'Fluorescence properties of retinoid X receptor antagonist NEt-SB'. Together they form a unique fingerprint.

Cite this