A light-up fluorescence probe for wash-free analysis of Mu-opioid receptor and ligand-binding events.
Anal Chim Acta
; 1261: 341220, 2023 Jun 22.
Article
en En
| MEDLINE
| ID: mdl-37147056
ABSTRACT
With the aggravated burden of opioid use disorder spreading worldwide, demands for new forms of opioid receptor agonist/antagonist constitute immense research interest. The Mu-opioid receptor (MOR) is currently in the spotlight on account of its general involvement in opioid-induced antinociception, tolerance and dependence. MOR binding assay, however, is often complicated by difficulty in MOR separation and purification, as well as the tedious procedure in standard biolayer interferometry and surface plasmon resonance measurements. To this end, we present TPE2N as a light-up fluorescent probe for MOR, which exhibits satisfactory performance in both live cells and lysates. TPE2N was elaborately designed based on the synergistic effect of twisted intramolecular charge-transfer and aggregation-induced emission by incorporating a tetraphenylethene unit to emit strong fluorescence in a restrained environment upon binding with MOR through the naloxone pharmacore. The developed assay enabled high-throughput screening of a compound library, and successfully identified three ligands as lead compounds for further development.
Palabras clave
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Colorantes Fluorescentes
/
Naloxona
Idioma:
En
Revista:
Anal Chim Acta
Año:
2023
Tipo del documento:
Article
País de afiliación:
China