Target intelligence / Profile preview

Cholecystokinin receptor 2 (CCK2R)

Target
CCK2R
Molecular classification
G protein-coupled receptor, Receptor
01

Overview

Cholecystokinin receptor 2 (CCK2R), also known as the cholecystokinin B receptor or gastrin receptor, is a G protein-coupled receptor (GPCR) with seven transmembrane domains that mediates the physiological actions of both cholecystokinin (CCK) and gastrin peptides. CCK2R is expressed primarily in the gastric mucosa (particularly in acid-secreting parietal cells) and widely in the central nervous system. It regulates key biological processes including gastric acid secretion, appetite, gastrointestinal motility, and cellular proliferation. CCK2R is distinguished from the CCK1R subtype by its similar affinity for CCK and gastrin (including both sulfated and non-sulfated forms), while CCK1R is more selective for sulfated CCK. CCK2R plays a role in a variety of pathological states, including gastrointestinal and neuroendocrine cancers, as well as potential roles in psychiatric and neurological diseases. Multiple small-molecule and peptide agonists and antagonists targeting CCK2R have been developed for research and potential therapeutic use[1][3][4][5][6][7][8].

Other names
CCK2 receptorCholecystokinin B receptorCCK-B receptorGastrin receptorCCKBR
02

Mechanism of action

Antagonism of CCK2R to inhibit gastric acid secretion or modulate tumor growth; Agonism to stimulate acid secretion or GI motility (experimental); Inhibition of signal transduction pathways mediated by gastrin and cholecystokinin[4][5][6]

03

Biological functions

Signal transductionRegulation of gastric acid secretionModulation of gastrointestinal motilityAppetite regulationCentral nervous system signalingCell proliferation
04

Disease associations

CancerNeuropsychiatric disordersGastrointestinal disordersOther
05

Safety considerations

Central nervous system effects (e.g., anxiety, panic, seizures at high CCK2R activity)Acid-base disturbances (e.g., hypochlorhydria or achlorhydria with antagonists)Potential for off-target effects on cell proliferation in tumors[5][7]
06

Interacting drugs

Netazepide

5 more in the full profile.

07

Biomarkers

CCK2R expression (for certain gastrointestinal or neuroendocrine tumors)Gastrin levels (indirect, related to activity)Use in PET imaging ligands for tumor localization (research)[5]

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