Live Cell Bioluminescence Imaging in Temporal Reaction of G Protein-Coupled Receptor for High-Throughput Screening and Analysis

Methods Mol Biol. 2016:1461:195-202. doi: 10.1007/978-1-4939-3813-1_16.

Abstract

G protein-coupled receptors (GPCRs) are notable targets of basic therapeutics. Many screening methods have been established to identify novel agents for GPCR signaling in a high-throughput manner. However, information related to the temporal reaction of GPCR with specific ligands remains poor. We recently developed a bioluminescence method for the quantitative detection of the interaction between GPCR and β-arrestin using split luciferase complementation. To monitor time-course variation of the interactions, a new imaging system contributes to the accurate evaluation of drugs for GPCRs in a high-throughput manner.

Keywords: Bioluminescence; Complementary technology; EM-CCD camera; G protein-coupled receptor; High-throughput screening; Protein–protein interaction.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Drug Discovery / methods
  • Gene Expression
  • Genes, Reporter
  • Genetic Vectors / genetics
  • High-Throughput Screening Assays*
  • Ligands*
  • Luminescent Measurements / methods*
  • Molecular Imaging*
  • Protein Binding
  • Protein Interaction Mapping
  • Receptors, G-Protein-Coupled / genetics
  • Receptors, G-Protein-Coupled / metabolism*
  • Signal-To-Noise Ratio

Substances

  • Ligands
  • Receptors, G-Protein-Coupled