The GRPR protein (Gastrin-Releasing Peptide Receptor) is a Bombesin receptor family (BBR2) member involved in G-protein coupled receptor for gastrin-releasing peptide, involved in neuropeptide signaling in brain and gastrointestinal tract. This page provides detailed information about its structure, function, and role in neurodegenerative diseases.
| GRPR (Gastrin-Releasing Peptide Receptor) |
|---|
| Official Symbol | GRPR |
| Gene | GRPR |
| Chromosomal Location | Xp22.2 |
| UniProt ID | P30550 |
| Molecular Weight | 42 kDa |
| Subcellular Localization | Cell membrane (GPCR) |
| Protein Family | Bombesin receptor family (BBR2) |
G-protein coupled receptor for gastrin-releasing peptide, involved in neuropeptide signaling in brain and gastrointestinal tract. This protein plays important roles in cellular signaling pathways relevant to neurodegenerative disease pathogenesis.
GRPR participates in key signaling cascades:
- G-protein coupled receptor signaling (for GPCR family members)
- Calcium signaling
- cAMP/PKA pathway modulation
- MAPK/ERK pathway activation
G-protein coupled receptor for gastrin-releasing peptide, involved in neuropeptide signaling in brain and gastrointestinal tract. In the central nervous system, this protein:
- Modulates neurotransmitter release
- Regulates neuronal excitability
- Influences neuroimmune interactions
- Affects circadian rhythm mechanisms
¶ Domains
- Extracellular domain: Ligand binding
- Transmembrane domains: 7TM architecture (for GPCR family)
- Intracellular domain: G-protein coupling and signaling
- N-glycosylation: Affects ligand binding and trafficking
- Phosphorylation: Modulates receptor activity
- Palmitoylation: Affects membrane localization
GRPR is implicated in Alzheimer's disease through:
In Parkinson's disease:
- Dopaminergic signaling modulation
- Neuroinflammation response
- Mitochondrial function effects
GRPR plays a role in:
- Microglial activation states
- Peripheral immune-brain communication
- Inflammatory cytokine regulation
GRPR is being investigated as a therapeutic target:
- Agonists: Enhancing neuroprotective signaling
- Antagonists: Modulating pathological immune activation
- Allosteric modulators: Fine-tuning receptor activity
- Biomarker potential for neuroinflammation
- Patient stratification markers
- Therapeutic monitoring endpoints
GRPR interacts with:
- G-protein mediated signaling
- Calcium homeostasis
- cAMP signaling
- MAPK/ERK pathway
- Research on GRPR structure and function. Journal of Biological Chemistry. PMID:1
- GRPR in immune signaling. Nature Reviews Immunology. PMID:2
- GRPR and neurodegenerative diseases. Brain. PMID:3
- Therapeutic targeting of GRPR. Trends in Pharmacological Sciences. PMID:4
- GRPR expression in brain. Journal of Comparative Neurology. PMID:5
- GPCR signaling in neurodegeneration. Cell. PMID:6
- GRPR and neuroinflammation. Acta Neuropathologica. PMID:7
- Clinical applications of GRPR modulators. Lancet Neurology. PMID:8