Fluorescence properties of retinoid X receptor antagonist NEt-SB.
Binding assay
Fluorescence
RXR
Solvatochromism
Stilbene
Journal
Bioorganic & medicinal chemistry letters
ISSN: 1464-3405
Titre abrégé: Bioorg Med Chem Lett
Pays: England
ID NLM: 9107377
Informations de publication
Date de publication:
01 01 2021
01 01 2021
Historique:
received:
07
09
2020
revised:
24
10
2020
accepted:
28
10
2020
pubmed:
6
11
2020
medline:
23
7
2021
entrez:
5
11
2020
Statut:
ppublish
Résumé
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.
Identifiants
pubmed: 33152377
pii: S0960-894X(20)30777-0
doi: 10.1016/j.bmcl.2020.127666
pii:
doi:
Substances chimiques
Ligands
0
Retinoid X Receptors
0
Stilbenes
0
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
127666Informations de copyright
Copyright © 2020 Elsevier Ltd. All rights reserved.