Cholecystokinin B receptor (CCKBR) (CCKBR)

The Cholecystokinin B receptor (CCKBR), also known as the CCK2 receptor or Gastrin receptor, is a G protein-coupled receptor primarily located in the central nervous system and the gastrointestinal tract (UniProt P32239). In the stomach, it is the principal mediator of gastrin-stimulated gastric acid secretion and has trophic effects on the gastric mucosa (NCBI Gene ID: 886). In the brain, CCKBR is widely distributed and plays a significant role in modulating anxiety, panic, and pain perception (PubMed: 15548710). Due to its involvement in promoting cell proliferation, the receptor is often overexpressed in various tumors, including medullary thyroid carcinoma and pancreatic cancer, making it a target for both imaging and therapy (PubMed: 21547383). Pharmacological targeting has focused on developing antagonists for treating acid-related disorders and anxiety, though clinical success in the latter has been limited (PubChem CID: 104749).

Other names

Cholecystokinin-2 receptorCCK2 receptorGastrin receptorCCK2RGASR

Antagonism of the CCKBR inhibits the binding of gastrin and cholecystokinin, thereby reducing gastric acid secretion and suppressing gastrin-dependent tumor growth (PubMed: 23832388).