A Gq Biased Small Molecule Active at the TSH Receptor.

ABSTRACT: G protein coupled receptors (GPCRs) can lead to G protein and non-G protein initiated signals. By virtue of its structural property, the TSH receptor (TSHR) has a unique ability to engage different G proteins making it highly amenable to selective signaling. In this study, we describe the identification and characterization of a novel small molecule agonist to the TSHR which induces primary engagement with G_αq/11. To identify allosteric modulators inducing selective signaling of the TSHR we used a transcriptional-based luciferase assay system with CHO-TSHR cells stably expressing response elements (CRE, NFAT, SRF, or SRE) that were capable of measuring signals emanating from the coupling of G_αs , G_αq/11, G_βγ, and G_α12/13,

SUBMITTER: Latif R 

PROVIDER: S-EPMC7333667 | biostudies-literature | 2020

REPOSITORIES: biostudies-literature