A Dynamic, Split-Luciferase-Based Mini-G Protein Sensor to Functionally Characterize Ligands at All Four Histamine Receptor Subtypes.

ABSTRACT: In drug discovery, assays with proximal readout are of great importance to study target-specific effects of potential drug candidates. In the field of G protein-coupled receptors (GPCRs), the determination of GPCR-G protein interactions and G protein activation by means of radiolabeled GTP analogs ([³⁵S]GTPγS, [γ-³²P]GTP) has widely been used for this purpose. Since we were repeatedly faced with insufficient quality of radiolabeled nucleotides, there was a requirement to implement a novel proximal functional assay for the routine characterization of putative histamine receptor ligands. We applied the split-NanoLuc to the four histamine receptor subtypes (H₁R, H₂R, H₃R, H₄R) and recently engineered minimal G (mini-G) proteins

SUBMITTER: Horing C 

PROVIDER: S-EPMC7698210 | biostudies-literature | 2020 Nov

REPOSITORIES: biostudies-literature