Adhesion G protein-coupled receptor A1 (ADGRA1)

Adhesion G protein-coupled receptor A1 (ADGRA1, also known as GPR123) is a member of the adhesion GPCR family, broadly conserved in vertebrates. Unlike other adhesion GPCRs, ADGRA1 lacks the canonical GAIN domain and other common N-terminal motifs, but contains a long C-terminal region with a PDZ-binding motif possibly relevant for protein–protein interactions. ADGRA1 is expressed most abundantly in the central nervous system, especially the hypothalamus, and is primarily localized to neuronal membranes. It plays important roles in neuronal signal transduction and homeostatic regulation of energy expenditure and thermogenesis, as demonstrated in animal models. The full physiological function in humans is still being elucidated, and its involvement in disease is inferred from family-level associations with neurological disorders and cancer.

Other names

ADGRA1GPR123KIAA1828G-protein coupled receptor 123probable G-protein coupled receptor 123

no drugs characterized; based on family, the mechanism may involve modulation of G protein-mediated signaling, and signal transduction cascades such as PI3K/AKT/GSK3β and MEK/ERK