Target intelligence / Profile preview

Cholecystokinin type 1 receptor (CCK‑1R)

Target
CCK‑1R
Molecular classification
G protein-coupled receptor, GPCR, Receptor
01

Overview

The cholecystokinin type 1 receptor (CCK‑1R), also known as CCKAR or the cholecystokinin A receptor, is a G protein-coupled receptor (GPCR) that binds sulfated members of the cholecystokinin (CCK) family of peptide hormones. It is primarily involved in mediating physiological responses to CCK, especially in the gastrointestinal tract and nervous system. It plays a role in gallbladder contraction, pancreatic exocrine secretion, gastric acid secretion, gastric emptying, and satiety.

Other names
CCKARCholecystokinin A receptor
02

Mechanism of action

Agonist or antagonist binding to CCK-1R modulates downstream signaling pathways involving G proteins, phospholipases, protein kinases, and intracellular calcium levels, ultimately affecting gastrointestinal functions and appetite regulation.

03

Biological functions

Signal transductionRegulation of gallbladder contractionRegulation of pancreatic exocrine secretionRegulation of gastric acid secretionRegulation of gastric emptyingRegulation of satietyAppetite suppressionModulates release of beta‐endorphinModulates release of dopamine
04

Disease associations

ObesityMetabolic syndrome
05

Safety considerations

Limited clinical use of ligands targeting this receptor.Therapeutic challenges in developing selective partial agonists/allosteric modulators.
06

Interacting drugs

Cholecystokinin peptides (e.g., CCK‐8)

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