Human Gastrin Releasing Peptide Receptor (GRPR) Protein

Background

Gastrin Releasing Peptide Receptor (GRPR) is another GPCR within the bombesin-like receptor family that binds gastrin-releasing peptide (GRP). GRPR is expressed in the gastrointestinal tract, pancreas, and the central nervous system (CNS). In the gastrointestinal system, GRPR regulates gastric acid secretion and promotes pancreatic enzyme release, playing a vital role in digestion. It also enhances intestinal smooth muscle contraction, facilitating gastrointestinal motility. In the CNS, GRPR is involved in memory formation and fear conditioning, as it modulates pathways in the amygdala and hippocampus. Additionally, GRPR regulates feeding behavior and satiety, influencing energy homeostasis and food intake. GRPR signaling has garnered significant interest in oncology because it is overexpressed in several cancers, including prostate cancer, small cell lung cancer (SCLC), and gastrointestinal malignancies. Activation of GRPR stimulates tumor growth, cell proliferation, and angiogenesis, making it a key target for cancer diagnostics and therapeutics. Furthermore, GRPR has roles in pruritus (itch sensation), where it modulates spinal cord circuits related to itch and pain perception. Its multifaceted roles in neurobiology, digestion, and oncology position GRPR as a promising candidate for the development of novel treatments for metabolic disorders, neurological conditions, and cancer.