Gz Enhanced Signal Transduction assaY (G_ZESTY) for GPCR deorphanization.

ABSTRACT: G protein-coupled receptors (GPCRs) are key pharmacological targets, yet many remain underutilized due to unknown activation mechanisms and ligands. Orphan GPCRs, lacking identified natural ligands, are a high priority for research, as identifying their ligands will aid in understanding their functions and potential as drug targets. Most GPCRs, including orphans, couple to G_i/o/z family members, however current assays to detect their activation are limited, hindering ligand identification efforts. We introduce G_ZESTY, a highly sensitive, cell-based assay developed in an easily deliverable format designed to study the pharmacology of G_i/o/z-coupled GPCRs and assist in deorphanization. We optimized assay conditions and developed an all-in-one vector employing

SUBMITTER: Franchini L 

PROVIDER: S-EPMC11291178 | biostudies-literature | 2024 Jul

REPOSITORIES: biostudies-literature