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Updated: May 9, 2026

Genetically-encoded Molecular Probes to Study G Protein-coupled Receptors
Published on: September 13, 2013
Harnessing the genome for characterization of G-protein coupled receptors in cancer pathogenesis
1Cold Spring Harbor Laboratory, NY, USA.
Abstract:
G-protein coupled receptors (GPCRs) mediate numerous physiological processes and represent the targets for a vast array of therapeutics for diseases ranging from depression to hypertension to reflux. Despite the recognition that GPCRs can act as oncogenes and tumour suppressors by regulating oncogenic signalling networks, few drugs targeting GPCRs are utilized in cancer therapy. Recent large-scale genome-wide analyses of multiple human tumours have uncovered novel GPCRs altered in cancer. However, work aiming to determine which GPCRs from these lists are the drivers of tumourigenesis, and hence valid therapeutic targets, comprises a formidable challenge. The present review highlights recent studies providing evidence that GPCRs are relevant targets for cancer therapy through their effects on known cancer signalling pathways, tumour progression, invasion and metastasis, and the microenvironment. Furthermore, the review also explores how genomic analysis is beginning to highlight GPCRs as therapeutic targets in the age of personalized medicine.
Insights
G-protein coupled receptors (GPCRs) are increasingly recognized as crucial in cancer. This review highlights GPCRs as promising therapeutic targets for cancer treatment and personalized medicine.
Area of Science:
- Oncology
- Pharmacology
- Molecular Biology
Background:
- G-protein coupled receptors (GPCRs) are vital in physiological processes and drug development.
- GPCRs can function as oncogenes or tumor suppressors by influencing cancer signaling networks.
- Despite their known roles, GPCR-targeted drugs are underutilized in cancer therapy.
Purpose of the Study:
- To review evidence supporting GPCRs as viable targets for cancer therapy.
- To explore the role of GPCRs in cancer signaling, progression, and the tumor microenvironment.
- To discuss the potential of GPCRs as therapeutic targets in personalized cancer medicine.
Main Methods:
- Review of recent studies and large-scale genome-wide analyses of human tumors.
- Analysis of GPCR alterations in cancer.
- Evaluation of GPCRs' impact on cancer signaling pathways, tumor progression, invasion, metastasis, and the microenvironment.
Main Results:
- Recent genomic analyses have identified novel GPCRs altered in various human cancers.
- Evidence suggests GPCRs significantly influence cancer signaling pathways, tumor progression, invasion, and metastasis.
- GPCRs play a role in modulating the tumor microenvironment.
Conclusions:
- GPCRs are relevant and promising therapeutic targets for cancer treatment.
- Genomic analysis is identifying specific GPCRs as targets for personalized cancer medicine.
- Further research into GPCRs can lead to novel cancer therapies.
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