Gα Protein Signaling Bias at Serotonin 1A Receptor.

ABSTRACT: Serotonin 1A receptor (5-HT1AR) is a clinically relevant target because of its involvement in several central and peripheral functions, including sleep, temperature homeostasis, processing of emotions, and response to stress. As a G protein coupled receptor (GPCR) activating numerous Gα _i/o/z family members, 5-HT1AR can potentially modulate multiple intracellular signaling pathways in response to different therapeutics. Here, we applied a cell-based bioluminescence resonance energy transfer assay to quantify how ten structurally diverse 5-HT1AR agonists exert biased signaling by differentially stimulating Gα _i/o/z family members. Our concentration-response analysis of the activation of each Gα _i/o/z protein revealed unique potency and e

SUBMITTER: Alabdali R 

PROVIDER: S-EPMC10586511 | biostudies-literature | 2023 Nov

REPOSITORIES: biostudies-literature