A Gq Biased Small Molecule Active at the TSH Receptor

G protein coupled receptors (GPCRs) can lead to G protein and non-G protein initiated signals. 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 Gq/11. To identify allosteric modulators inducing selective signaling of the...