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Updated: Jul 16, 2026

A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
Published on: February 20, 2018
Potential inhibition of the neuro-neoplastic interactions: the clue of a GPCR-targeted therapy
1Institut de Physiologie et de Biologie Cellulaires, CNRS UMR6187, Pôle Biologie-Santé, Université de Poitiers, Poitiers, France.
Abstract:
Other sections of this monograph, dedicated to neuronal activities in tumor tissue, have highlight the chief influence of neurotrophins, neurotransmitters, adhesion, guidance molecules and different nerve cell markers in the progression, but also for the prognostic, therapy and survey of cancers. The G-protein-coupled receptors (GPCR) are among the most successful and promising target proteins for drug discovery and therapeutic research. GPCR are frequently overexpressed in cancer cells, an interesting property for tumor imaging or for a targeted radiotherapy, using radiolabeled ligand derivatives. The tumor microenvironment contains a number of GPCR ligands (e.g., bioactive peptides, biogenic amines, purins, chemokines), known to regulate the proliferation, migration or survival of both tumoral and neural cells and that may be key actors of the neuro-neoplastic interactions. Here will be reviewed the potential utilization of substances that target a selected choice of GPCR, especially neuropeptide receptors, for a novel concept of therapy, concerning the numerous types of cancers where neurons infiltrate the tumoral mass or those where the malignant cells invade nerve branches (perineural invasion). Some molecular mechanisms linked to these GPCR (or linking GPCR to other types of membrane receptors or co-receptors), involved in these processes, will also be considered.
Insights
Targeting G-protein-coupled receptors (GPCR) offers a novel cancer therapy approach. By targeting GPCRs, particularly neuropeptide receptors, researchers aim to treat cancers involving neuro-neoplastic interactions and perineural invasion.
Area of Science:
- Oncology
- Neuroscience
- Pharmacology
Background:
- Neurotrophins, neurotransmitters, and guidance molecules influence cancer progression and prognosis.
- G-protein-coupled receptors (GPCRs) are crucial drug targets, often overexpressed in cancer cells, making them valuable for imaging and targeted radiotherapy.
- The tumor microenvironment features GPCR ligands that regulate tumor cell proliferation, migration, and survival, mediating neuro-neoplastic interactions.
Purpose of the Study:
- To review the potential of targeting specific GPCRs, especially neuropeptide receptors, for novel cancer therapies.
- To explore therapeutic strategies for cancers with neuronal infiltration or perineural invasion.
- To consider molecular mechanisms involving GPCRs in neuro-neoplastic processes.
Main Methods:
- Literature review focusing on GPCRs in cancer and neuro-neoplastic interactions.
- Analysis of GPCR ligands within the tumor microenvironment.
- Examination of molecular mechanisms linking GPCRs to cancer progression.
Main Results:
- GPCRs are implicated in regulating tumor cell behavior and mediating interactions between neural and neoplastic cells.
- Targeting GPCRs, particularly neuropeptide receptors, presents a promising avenue for cancer therapy.
- Understanding GPCRs' role is key for developing treatments for cancers with neural involvement.
Conclusions:
- Targeting GPCRs offers a novel therapeutic strategy for various cancers, especially those with neuro-neoplastic interactions or perineural invasion.
- Further research into GPCRs and their ligands can lead to advanced cancer treatments and imaging techniques.
- The study highlights the importance of neuro-neoplastic crosstalk in cancer and the therapeutic potential of targeting GPCRs.
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