Gastrin releasing peptidesecreted by The gastrin-releasing peptide receptor (GRPR) is a crucial protein involved in various physiological and pathological processes, particularly in the gastrointestinal and nervous systems, and increasingly recognized for its role in cancer. As a G protein-coupled receptor (GPCR), GRPR mediates the effects of gastrin-releasing peptide (GRP), a neuropeptide that plays a significant role in regulating numerous bodily functionsBB 2 receptor. The overexpression of GRPR in various cancers, including prostate, breast, and small cell lung cancer, has positioned it as a promising target for diagnostic imaging and therapeutic interventionsGRPRgastrin-releasing peptide receptor. Synonyms: Species: HumanGRPR(2925), MouseGrpr(14829), RatGrpr(24938), Zebrafishgrpr(567289), naked mole-rat ....
The gastrin-releasing peptide receptor, also known by its abbreviation GRPR or as the BB2 receptor, is a transmembrane protein belonging to the bombesin receptor family. It is activated by gastrin-releasing peptide (GRP) and related bombesin-like peptides. GRP itself is a neuropeptide that influences a wide array of functions, including the release of gastrointestinal hormones, regulation of food intake, and sensory perception, such as the transmission of itch signals.Gastrin-Releasing Peptide Receptor Imaging and Therapy in ... The interaction between GRP and GRPR triggers intracellular signaling pathways, leading to diverse cellular responsesGastrin peptide-relatedreceptor(GRPR) is one of the highly expressed genes in c-met-mutated organoids (126), a major target in GB (127). Indeed, the ....
One of the most significant areas of research concerning GRPR is its aberrant overexpression in several types of human cancers. This includes, but is not limited to, prostate cancer, breast cancer, small cell lung cancer, and head and neck tumors. In these malignancies, GRPR signaling can drive tumor growth and metastatic behavior.GRPRgastrin-releasing peptide receptor. Synonyms: Species: HumanGRPR(2925), MouseGrpr(14829), RatGrpr(24938), Zebrafishgrpr(567289), naked mole-rat ... This overexpression makes GRPR an attractive target for developing novel cancer therapies and diagnostic tools. The ability to specifically target GRPR allows for the selective delivery of cytotoxic drugs or imaging agents to cancer cells, potentially minimizing damage to healthy tissuesPhysiology, Gastrin - StatPearls - NCBI Bookshelf.
The overexpression of GRPR in various cancers has spurred significant interest in GRPR-targeted cancer therapy. Researchers are developing radioligands and other molecular agents that can bind specifically to GRPR on cancer cells. These agents can be used for molecular imaging, enabling precise visualization and staging of tumors, including the detection of lymph node and bone metastases in prostate cancer. Furthermore, these targeted agents can be equipped with therapeutic payloads, such as radioisotopes for targeted radiotherapy or cytotoxic drugs, to directly combat cancer cells. This dual capability of imaging and therapy, known as theranostics, holds great promise for personalized medicine in oncology.
Beyond its role in cancer, GRPR is integral to normal physiological processes. In the gastrointestinal system, it is involved in the regulation of gastrin release, which is essential for digestion.作者：C Morgat·2025·被引用次数：1—Gastrin-releasing peptide receptorimaging and therapy in the era of personalized medicine. Clément Morgat, Andrei Iagaru and Elif Hindié. In the central nervous system (CNS), GRP acting through GRPR can modulate feeding behavior and sensory pathwaysGRPR - Gastrin-releasing peptide receptor. Understanding these normal functions is crucial for evaluating potential side effects of GRPR-targeting therapies and for a comprehensive understanding of the receptor's overall biological significance.
While the potential of GRPR as a therapeutic and diagnostic target is substantial, ongoing research continues to refine targeting strategies. Developing highly selective ligands that bind effectively to GRPR while minimizing off-target effects remains a key focusGastrin-Releasing Peptide Receptor - an overview. The structural elucidation of human GRPR has provided valuable insights for designing more potent and specific therapeutic agents. Further investigation into the diverse signaling pathways activated by GRPR will also contribute to the development of more sophisticated treatment approaches for cancers that overexpress this receptorGastrin-Releasing Peptide Receptor Imaging and Therapy in ....
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