Huang et al clarify the molecular mechanism of activation of adhesion G protein-coupled receptor GPR110 by synaptamide, the only small-molecule endogenous ligand known for this class of GPCR. They find through chemical cross-linking mass spectrometry, modeling and mutagenesis that synaptamide binds to residues in the GAIN domain and induces a conformational change triggering downstream signaling.
- Bill X. Huang
- Xin Hu
- Hee-Yong Kim
