Vasoactive intestinal peptide receptor (VPAC)

Vasoactive intestinal peptide receptor (VPAC) is a class B G protein-coupled receptor that mediates the diverse biological actions of vasoactive intestinal peptide (VIP), a 28-amino acid neuropeptide. There are two main subtypes: VPAC1 and VPAC2, with a third receptor called PAC1 that preferentially binds pituitary adenylate cyclase-activating peptide (PACAP) but can also bind VIP with lower affinity[10]. VPAC receptors are widely distributed throughout the body and play important roles in various physiological processes including smooth muscle relaxation, secretion regulation, immune modulation, and glucose homeostasis. Their involvement in multiple disease processes makes them potential therapeutic targets for conditions including cancer, inflammatory diseases, neurodegenerative disorders, and type 2 diabetes. Current therapeutic development focuses on receptor-specific agonists and antagonists to maximize therapeutic benefits while minimizing side effects.

Other names

Vasoactive intestinal polypeptide receptorVIP receptorVPAC1 (VIP1)VPAC2 (VIP2)VIPR1 (gene name for VPAC1)

Drugs targeting VPAC receptors primarily modulate their coupling to the adenylyl cyclase pathway. For instance, VPAC2 agonists promote glucose-dependent insulin secretion and stimulate islet β-cell proliferation through the forkhead box M1 pathway.