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Target intelligence / Profile preview
Cholecystokinin 2 Receptor (CCK2R)
- Target
- CCK2R
- Molecular classification
- G protein-coupled receptor, Receptor
01
Overview
The cholecystokinin 2 receptor (CCK2R) is a G protein-coupled receptor predominantly found in the central nervous system and stomach. It binds cholecystokinin and gastrin with similar affinity and is involved in regulating gastric acid secretion, pain perception, anxiety responses, and memory formation. Overexpression has been reported in various cancers, making it a target for diagnostic imaging and potential therapies. Several synthetic antagonists have been developed, but clinical use is limited.
- Other names
- CCKBRGastrin receptor
02
Mechanism of action
Agonists bind to the CCK2R receptor, activating Gq/G11 protein signaling pathways, which in turn activate phospholipase C, leading to production of inositol phosphates (IPs) and an increase in intracellular calcium levels. Antagonists bind to the receptor and prevent activation by endogenous ligands.
03
Biological functions
Signal transductionRegulation of gastric acid secretionDifferentiation of gastric mucosaModulation of pain perception/nociceptionModulation of anxietyInfluence on memory formationHunger controlThermoregulation
04
Disease associations
Gastric adenocarcinomaMedullary thyroid carcinomaColorectal carcinomaSmall cell lung carcinomaPancreatic carcinomaGastrointestinal disordersNeurological disordersPsychiatric conditionsPain conditions
05
Safety considerations
Differences between preclinical models and human biology leading to limited clinical efficacy of antagonists for pain reliefPotential for neuropsychiatric effects
06
Interacting drugs
L‑365,260
1 more in the full profile.
07
Biomarkers
CCK2R expression levels in tumor tissues
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