Target intelligence / Profile preview

Cholecystokinin A receptor (CCKAR)

Target
CCKAR
Molecular classification
G protein-coupled receptor, Receptor
01

Overview

The cholecystokinin A receptor (CCKAR), also known as CCK1 or CCK1R, is a G protein-coupled receptor (GPCR) that primarily binds sulfated members of the cholecystokinin (CCK) family of peptide hormones. It plays a central role in mediating physiological responses to CCK, especially in the gastrointestinal tract and select regions of the central nervous system.

Other names
CCK1Type I cholecystokinin receptorCCK1R
02

Mechanism of action

Agonist binding leads to activation of Gq proteins, increasing intracellular calcium via IP₃-sensitive stores. At high agonist concentrations, coupling with Gs proteins can occur, increasing cAMP levels. Coupling with G13 has also been observed, activating RhoA pathways.

03

Biological functions

Signal transductionPancreatic enzyme secretionGallbladder contractionRegulation of gut motilitySatiety regulation
04

Interacting drugs

Proglumide

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