Tuning the Response of GPCR-Based Yeast Sensors Using Fluorescent Reporters.

ABSTRACT: G protein-coupled receptors (GPCRs) recognize ligands on the cell surface, initiating intracellular signaling pathways that control a variety of biological processes, from neurotransmission and hormone regulation to light detection and smell. As entryways into these pathways, GPCRs are key pharmacological targets, with 30% of FDA-approved drugs targeting them. High-throughput GPCR-based sensors in yeast are proven platforms for the identification of novel GPCR ligands. Most human GPCRs (hGPCRs), however, led to small increases in the signal after activation, hindering the development of high-throughput (HT) assays. To streamline the generation of HT assays for biomedically important hGPCRs, here we analyze five fluorescent reporters in the context of hGPCR-based sensors. Using the serotoni

SUBMITTER: Langevin R 

PROVIDER: S-EPMC12814776 | biostudies-literature | 2026 Jan

REPOSITORIES: biostudies-literature