Discovery of Small-Molecule Sulfonamide Fluorescent Probes for GPR120

Anal Chem. 2019 Dec 3;91(23):15235-15239. doi: 10.1021/acs.analchem.9b04157. Epub 2019 Nov 15.

Abstract

GPR120 is a novel target for the treatment of metabolic disease and type 2 diabetes. The small-molecule fluorescent probe could help us locate GPR120 visually and guide in-depth study of GPR120. In this study, we synthesized six nonacidic sulfonamide fluorescent probes and tested their optical and biological properties. Compared to previous probes for GPR120, these probes, with sulfonamide structure, have high selectivity on GPR120. We used these probes to establish a BRET binding assay system to screen agonists and antagonists of GPR120. It is expected that these novel fluorescent probes may become useful tools in studying pharmacology and physiology of GPR120.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Bioluminescence Resonance Energy Transfer Techniques
  • Drug Discovery*
  • Fluorescent Dyes / chemical synthesis
  • Fluorescent Dyes / chemistry*
  • HEK293 Cells
  • Humans
  • Molecular Structure
  • Receptors, G-Protein-Coupled / analysis*
  • Small Molecule Libraries / chemical synthesis
  • Small Molecule Libraries / chemistry*
  • Sulfonamides / chemical synthesis
  • Sulfonamides / chemistry*

Substances

  • FFAR4 protein, human
  • Fluorescent Dyes
  • Receptors, G-Protein-Coupled
  • Small Molecule Libraries
  • Sulfonamides