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GRPR

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All listed services and products are For Research Use Only. Do Not use in any diagnostic or therapeutic applications.

Background

Gastrin releasing peptide receptor (GRPR) is a seven-transmembrane Gq-coupled GPCR encoded by the GRPR gene, expressed on neuroendocrine, epithelial and transformed tumor cells, localized exclusively to plasma lipid bilayers. Distinct from other bombesin family receptors, GRPR selectively binds gastrin-releasing peptide ligands to trigger intracellular calcium mobilization and proliferative transcriptional cascades. Under physiological neuroendocrine balance, basal GRPR activity sustains moderate gastrointestinal hormone secretion without aberrant cell growth. Upon ligand overabundance or malignant transformation, sustained GRPR signaling amplifies proliferative and migratory programs driving tumor expansion. Instead of ubiquitous peptide receptors, GRPR bears neuroendocrine tissue-specific proliferative regulatory functions that cannot be fully substituted by related bombesin receptors, linking neuropeptide ligand binding directly to tumor growth pathways. Loss of balanced GRPR signaling restrains proliferative potential, while receptor overexpression accelerates neoplastic progression, establishing GRPR as a core research target for neuropeptide GPCR biology and anti-proliferative compound screening.

GRPR executes Gq-mediated signal transduction function embedded within cell surface membranes, utilizing extracellular ligand-binding pockets to capture gastrin-releasing peptide neuropeptides. Conserved binding cavities distinguish its ligand selectivity from other bombesin receptor paralogs distributed across neural tissue. GRPR-mediated peptide sensing bridges extracellular neuropeptide stimulation and intracellular calcium-dependent proliferative signaling, balancing neuroendocrine secretion and cell growth according to ligand concentration. GRPR participates in gastrointestinal hormone release, neural sensory signaling and neuroendocrine tumor proliferation. Deficient GRPR expression blunts peptide-driven proliferative responses. Therefore, GRPR represents a pivotal research target for bombesin GPCR study and neuroendocrine anti-tumor compound screening.

Fig. 1 Schematic of GRPR-specific imaging probe assembly and receptor binding complex structure. (OA Literature)Fig. 1 Structural construction of GRPR-targeted ProCA1 fluorescent probes and specific binding interaction between targeting peptide and cell membrane GRPR receptor.1

GRPR Protein Function: Core Roles in Gastrin-Releasing Peptide Sensing and Proliferative Tuning

The biological functions of GRPR are focused on neuropeptide ligand binding, Gq calcium signaling and cell growth control:

  • Gastrin-Releasing Peptide Recognition: Selectively binds GRP neuropeptides via extracellular receptor domains.
  • Gq-Mediated Calcium Mobilization: Activates intracellular calcium release to trigger downstream signaling cascades.
  • Neuroendocrine Homeostasis: Maintains baseline gastrointestinal peptide secretion under resting physiological status.
  • Tumor Proliferation Modulation: Amplifies cell growth and migratory signals upon sustained ligand stimulation.
  • Disease Relevance: GRPR overexpression drives neuroendocrine tumor progression, while inhibited signaling limits neoplastic expansion.

GRPR Protein Product

Creative Biolabs offers high-quality GRPR proteins through optimized expression systems. These products retain native neuropeptide binding and Gq signaling biological activity, suitable for ligand-receptor interaction and anti-tumor modulator screening. All GRPR proteins undergo strict quality control to ensure consistent performance and reliable application across diverse research platforms.

GRPR Protein Product

Not finding the membrane protein product you need? Contact us to start your one-stop custom service!

GRPR Stable Cell Line Product

Creative Biolabs provides custom-engineered GRPR stable cell lines, including overexpression and blank control models. These cell lines are optimized for bombesin GPCR profiling and calcium proliferative signal functional analysis. Each cell line undergoes stringent validation to ensure stable expression profiles and consistent functional performance in diverse experimental contexts.

GRPR Stable Cell Line Product

Not finding the stable cell line product you need? Contact us to start your one-stop custom service!

GRPR Recombinant Antibody Product

High-specificity recombinant antibodies targeting GRPR are developed via advanced antibody engineering technologies, with no cross-reactivity with other bombesin GPCR family members. These antibodies are validated for neuroendocrine cell membrane localization detection and tumor tissue expression profiling, and can be combined with neuropeptide marker reagents to analyze complete GRP-GRPR signaling complexes in neuroendocrine cell models.

GRPR Recombinant Antibody Product

Not finding the recombinant antibody product you need? Contact us to start your one-stop custom service!

Product Features

  • Native GRP Ligand Binding & Gq Signaling Activity: Preserves intact neuropeptide recognition and calcium signal capacity for neuroendocrine research.
  • Bombesin Receptor Specificity: Eliminates non-specific cross-recognition of other GRP-family GPCRs.
  • Neuroendocrine Tumor Compatibility: Optimized reagent series for proliferative therapeutic screening workflows.
  • Comprehensive Customization Support: Facilitates end-to-end development of customized proteins, antibodies and stable cell lines to address bombesin receptor research demands.

Custom GRPR Research Services

Beyond catalog products, Creative Biolabs offers specialized custom services for GRPR research:

  • Custom GRPR Protein Production: Tailored expression of mutant and tagged GRPR constructs for neuropeptide ligand binding analysis.
  • Custom Antibody Development: Generation of GRPR-specific antibodies for neuroendocrine membrane immunostaining.
  • Stable Cell Line Engineering: Construction of GRPR-modified cell models for calcium proliferative signaling research.
  • Functional Assay Development: Custom design of ligand binding and intracellular calcium detection workflows.

Frequently Asked Questions (FAQ)

  1. What is the primary function of GRPR?

    GRPR is a Gq-coupled GPCR binding gastrin-releasing peptide to trigger calcium mobilization and drive neuroendocrine cell proliferation.

  2. Why is GRPR a significant research target?

    GRPR links neuropeptide hormone signaling to neuroendocrine tumor growth, serving as a tumor biomarker and therapeutic target.

  3. Are Creative Biolabs' GRPR products suitable for clinical use?

    No, all GRPR products and services are strictly for research use only, not intended for clinical diagnosis or treatment.

  4. What types of GRPR products does Creative Biolabs offer?

    Offerings include full-length GRPR GPCR proteins, isoform-specific detection antibodies and custom stable cell lines for neuroendocrine tumor research.

  5. How are GRPR proteins validated for activity?

    GRPR proteins are validated via gastrin-releasing peptide ligand binding and calcium signal functional testing.

Reference
  1. Pu, Fan, et al. "GRPR-targeted protein contrast agents for molecular imaging of receptor expression in cancers by MRI." Scientific reports 5.1 (2015): 16214. Under Open Access license CC BY 4.0, without modification. https://doi.org/10.1038/srep16214
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