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Updated: May 8, 2026

Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding
Published on: June 9, 2017
G-protein-coupled receptors and cancer
Robert T Dorsam1, J Silvio Gutkind
1Oral and Pharyngeal Cancer Branch, National Institute of Dental and Craniofacial Research, National Institutes of Health, Bethesda, Maryland 20892-4330, USA.
Abstract:
G-protein-coupled receptors (GPCRs), the largest family of cell-surface molecules involved in signal transmission, have recently emerged as crucial players in tumour growth and metastasis. Malignant cells often hijack the normal physiological functions of GPCRs to survive, proliferate autonomously, evade the immune system, increase their blood supply, invade their surrounding tissues and disseminate to other organs. This Review will address our current understanding of the many roles of GPCRs and their signalling circuitry in tumour progression and metastasis. We will also discuss how interfering with GPCRs might provide unique opportunities for cancer prevention and treatment.
Insights
G-protein-coupled receptors (GPCRs) are vital in cancer progression and metastasis. Targeting GPCRs offers potential new strategies for cancer prevention and treatment.
Area of Science:
- Oncology
- Molecular Biology
- Cell Biology
Background:
- G-protein-coupled receptors (GPCRs) are the largest family of cell-surface receptors.
- GPCRs are critical for normal physiological signal transmission.
- Emerging evidence highlights GPCRs' significant roles in cancer development.
Purpose of the Study:
- To review the multifaceted roles of GPCRs in tumor progression.
- To elucidate the involvement of GPCR signaling in metastasis.
- To explore therapeutic and preventive strategies targeting GPCRs in cancer.
Main Methods:
- Literature review of current research on GPCRs in cancer.
- Analysis of signaling pathways utilized by GPCRs in malignant cells.
- Synthesis of data on GPCR functions in tumor growth, survival, and dissemination.
Main Results:
- Malignant cells exploit GPCRs for autonomous proliferation and survival.
- GPCRs facilitate immune evasion and angiogenesis in tumors.
- GPCR signaling contributes to tissue invasion and distant metastasis.
Conclusions:
- GPCRs are key drivers of tumor progression and metastasis.
- Understanding GPCR circuitry is crucial for cancer research.
- Targeting GPCRs presents promising avenues for novel cancer therapies.
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