GRPR Antibodies

Structure of GRPR

GRPR encodes a G protein-coupled receptor with a molecular weight of approximately 43 kDa. The molecular weight varies slightly among different species depending on the degree of glycosylation.

This receptor contains 384 amino acids and has a seven-transmembrane structure that forms a characteristic α-helical bundle. The extracellular region contains multiple N-glycosylation sites, which are involved in ligand recognition; the intracellular region is coupled to the Gq/11 protein and activates the phospholipase C signaling pathway. The third intracellular loop has multiple phosphorylation sites at the C-terminus, mediating receptor desensitization and internalization. The hydrophobic cavity formed by the transmembrane helices precisely recognizes the C-terminal amide structure of gastrin-releasing peptide, where the arginine residues in the transmembrane region directly form salt bridges with the ligand, and the histidine on the extracellular loop assists in stabilizing the binding conformation.

Fig. 1 Comparative Analysis of GRPR: Ligand Sequences, Activation Mechanism, and Predicted 3D Structure.¹

Key structural properties of GRPR:

• Seven transmembrane α -helical bundles
• Extracellular N-terminal glycosylation modification region
• Ligand-bound hydrophobic cavities
• Intracellular G protein-coupled domains
• The third intracellular loop contains phosphorylation sites

Functions of GRPR

The core function of GRPR is to mediate the gastrin-releasing peptide signal, regulating cell proliferation, smooth muscle contraction, and nerve conduction. It is also involved in various pathological physiological processes such as itch signal transduction, tumor growth, and inflammation regulation.

The dose-response curve of the binding of GRP to GRPR is in a typical S-shape. The ligand affinity is at the sub-nanomolar level. After receptor activation, it is rapidly internalized and desensitized. This characteristic makes it an ideal target for nuclear medicine molecular imaging and targeted radiotherapy.

Applications of GRPR and GRPR Antibody in Literature

1. D'Onofrio, Alice, et al. "GRPR-targeting radiotheranostics for breast cancer management." Frontiers in Medicine 10 (2023): 1250799. https://doi.org/10.3389/fmed.2023.1250799

This study focuses on the potential of gastrin-releasing peptide receptor (GRPR) as a new target for the diagnosis and treatment of breast cancer. Although previous related research has mainly concentrated on prostate cancer, given that GRPR is highly expressed in approximately 80% of estrogen receptor-positive breast cancers, this article systematically reviews the preclinical and clinical progress of radiopharmaceuticals targeting GRPR in breast cancer imaging and treatment, with the aim of providing a reference for subsequent translational applications.

2. Kim, Dong-Gun, et al. "GRPR Drives Metastasis via CRABP2 and FNDC4 Pathways in Lung Adenocarcinoma." Cells 13.24 (2024): 2128. https://doi.org/10.3390/cells13242128

This study reveals the crucial role of gastrin-releasing peptide receptor (GRPR) in the metastasis of lung adenocarcinoma (LUAD). High expression of GRPR is associated with poor prognosis in patients and promotes tumor cell invasion by upregulating CRABP2 and FNDC4. The results indicate that GRPR can serve as a potential prognostic marker and therapeutic target for inhibiting the metastasis of LUAD.

3. Ma, Yuze, and Feng Gao. "Advances of radiolabeled GRPR ligands for PET/CT imaging of cancers." Cancer Imaging 24.1 (2024): 19. https://doi.org/10.1186/s40644-024-00658-y

This study reveals that the gastrin-releasing peptide receptor (GRPR) is a transmembrane G protein-coupled receptor that is highly expressed in various types of cancers. This article systematically reviews the application progress and research breakthroughs of radiolabeled GRPR ligands in the imaging diagnosis, recurrence and metastasis monitoring of prostate cancer and breast cancer over the past two decades.

4. Liu, Jia-jia, et al. "Role of GRPR in acupuncture intervention in the "Itch-scratch vicious cycle" spinal circuit of chronic pruritus." Chinese Medicine 18.1 (2023): 2. https://doi.org/10.1186/s13020-022-00706-4

The research has found that the gastrin-releasing peptide receptor (GRPR) in the dorsal horn of the spinal cord is a key molecule that mediates the itching response, and it may become a new target for future acupuncture-based treatment of itching. This provides a new idea for intervening in the "itch-grooming cycle" at the spinal cord level to address chronic itching.

5. Abouzayed, Ayman, et al. "The GRPR antagonist [99mTc] Tc-maSSS-PEG2-RM26 towards Phase I Clinical Trial: Kit Preparation, characterization and toxicity." Diagnostics 13.9 (2023): 1611. https://doi.org/10.3390/diagnostics13091611

This study successfully developed a GRPR antagonist [99mTc]Tc-maSSS-PEG2-RM26 reagent kit for SPECT imaging of prostate cancer, achieving one-step labeling with a high labeling rate (>97%). The components of the kit are sterile and non-toxic, and the labeled product maintains its specific binding ability to GRPR, with a stability of 18 months, demonstrating potential for clinical application.

Creative Biolabs: GRPR Antibodies for Research

Creative Biolabs specializes in the production of high-quality GRPR antibodies for research and industrial applications. Our portfolio includes monoclonal and polyclonal antibodies tailored for ELISA, Flow Cytometry, Western blot, immunohistochemistry, and other diagnostic methodologies.

• Custom GRPR Antibody Development: Tailor-made solutions to meet specific research requirements.
• Bulk Production: Large-scale antibody manufacturing for industry partners.
• Technical Support: Expert consultation for protocol optimization and troubleshooting.
• Aliquoting Services: Conveniently sized aliquots for long-term storage and consistent experimental outcomes.

For more details on our GRPR antibodies, custom preparations, or technical support, contact us at email.