Label-Free Cell Phenotypic Identification of D-Luciferin as an Agonist for GPR35

Methods Mol Biol. 2016:1461:3-17. doi: 10.1007/978-1-4939-3813-1_1.

Abstract

D-Luciferin (also known as beetle or firefly luciferin) is one of the most widely used bioluminescent reporters for monitoring in vitro or in vivo luciferase activity. The identification of several natural phenols and thieno[3,2-b]thiophene-2-carboxylic acid derivatives as agonists for GPR35, an orphan G protein-coupled receptor, had motivated us to examine the pharmacological activity of D-Luciferin, given that it also contains phenol and carboxylic acid moieties. Here, we describe label-free cell phenotypic assays that ascertain D-Luciferin as a partial agonist for GPR35. The agonistic activity of D-Luciferin at the GPR35 shall evoke careful interpretation of biological data when D-Luciferin or its analogues are used as probes.

Keywords: Bioluminescence; D-Luciferin; Dynamic mass redistribution; G protein-coupled receptor; GPR35; Resonant waveguide grating biosensor.

MeSH terms

  • Benzothiazoles / chemistry
  • Benzothiazoles / pharmacology*
  • Biosensing Techniques
  • Cell Culture Techniques
  • Cell Line, Tumor
  • Dose-Response Relationship, Drug
  • Humans
  • Luminescent Measurements / methods
  • Protein Transport
  • Receptors, G-Protein-Coupled / agonists*
  • Receptors, G-Protein-Coupled / antagonists & inhibitors
  • Receptors, G-Protein-Coupled / metabolism
  • beta-Arrestins / metabolism

Substances

  • Benzothiazoles
  • D-luciferin
  • GPR35 protein, human
  • Receptors, G-Protein-Coupled
  • beta-Arrestins