title: Live Cell Bioluminescence Imaging in Temporal Reaction of G Protein-Coupled Receptor for High-Throughput Screening and Analysis.
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.
authors.affiliation: Department of Chemistry, School of Science, The University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo, 113-0033, Japan.
authors.forename: Mitsuru
authors.initials: M
authors.lastname: Hattori
authors.affiliation: Department of Chemistry, School of Science, The University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo, 113-0033, Japan. ozawa@chem.s.u-tokyo.ac.jp.
authors.forename: Takeaki
authors.initials: T
authors.lastname: Ozawa
mesh_terms: D055808:Drug Discovery / Q000379:methods; D015870:Gene Expression; D017930:Genes, Reporter; D005822:Genetic Vectors / Q000235:genetics; D057166:High-Throughput Screening Assays; D008024:Ligands; D008163:Luminescent Measurements / Q000379:methods*; D057054:Molecular Imaging; D011485:Protein Binding; D025941:Protein Interaction Mapping; D043562:Receptors, G-Protein-Coupled / Q000235:genetics / Q000378:metabolism*; D059629:Signal-To-Noise Ratio
chemical_list: D008024:Ligands; D043562:Receptors, G-Protein-Coupled
keywords: Bioluminescence; Complementary technology; EM-CCD camera; G protein-coupled receptor; High-throughput screening; Protein–protein interaction