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Target intelligence / Profile preview
Gastrin-releasing peptide receptor (GRPR)
- Target
- GRPR
- Molecular classification
- G protein-coupled receptor, GPCR, Bombesin receptor family
01
Overview
The Gastrin-releasing peptide receptor (GRPR) is a G protein-coupled receptor that mediates the effects of gastrin-releasing peptide (GRP) in the central nervous system and peripheral tissues. It plays a role in regulating gastrointestinal function, modulating immune responses, and influencing neurological processes. GRPR is overexpressed in several malignancies, making it an attractive target for imaging and therapy in oncology. It is also implicated in neurological disorders, itch transmission, and inflammation.
- Other names
- BB2BB2RBRS2
02
Mechanism of action
GRPR activation by agonists leads to stimulation of the phospholipase C pathway via Gq proteins, increasing intracellular calcium levels and downstream signaling.
03
Biological functions
Regulates gastrointestinal motilityGastric emptyingGastrin releasePancreatic enzyme secretionImmune response modulationMemory formationCircadian rhythm regulationEmotional response modulationFeeding behavior
04
Disease associations
CancerNeurodevelopmental disordersNeurological disordersItch transmissionInflammationPsychiatric conditions
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