ADGRF5

ADGRF5, officially Adhesion G Protein-Coupled Receptor F5 (common alias GPR116), belongs to the adhesion GPCR superfamily. It undergoes autoproteolytic cleavage at the GPCR proteolysis site (GPS), generating N-terminal (NTF) and C-terminal (CTF) fragments. Activation—via NTF dissociation or ligand binding—triggers coupling to Gαs and Gαq proteins, modulating cyclic AMP (cAMP) and calcium signaling to regulate cell adhesion, migration, and tissue homeostasis.
Dysregulated ADGRF5 expression is linked to pulmonary fibrosis, where it may drive fibroblast activation and extracellular matrix deposition. Preclinical studies explore ADGRF5 modulators as potential anti-fibrotic therapies, though no candidates have entered clinical trials. It also influences renal function and immune cell regulation, making it a promising target for fibrotic and inflammatory disorder research.