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Updated: May 3, 2026

Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding
Published on: June 9, 2017
Novel insights into G protein and G protein-coupled receptor signaling in cancer
Morgan O'Hayre1, Maria S Degese1, J Silvio Gutkind1
1Oral and Pharyngeal Cancer Branch, Dental and Craniofacial Research, National Institutes of Health, Bethesda, MD 20892, USA.
Abstract:
G protein-coupled receptors (GPCRs) play a central role in signal transmission, thereby controlling many facets of cellular function. Overwhelming evidence now implicates GPCRs, G proteins and their downstream signaling targets in cancer initiation and progression, where they can influence aberrant cell growth and survival, largely through activation of AKT/mTOR, MAPKs, and Hippo signaling pathways. GPCRs also play critical roles in the invasion and metastasis of cancer cells via activation of Rho GTPases and cytoskeletal changes, and angiogenesis to supply the tumor with nutrients and provide routes for metastasis. Lastly, GPCRs contribute to the establishment and maintenance of a permissive tumor microenvironment. Understanding GPCR involvement in cancer malignancy may help identify novel therapeutic opportunities for cancer prevention and treatment.
Insights
G protein-coupled receptors (GPCRs) are crucial in cell signaling and cancer development. Targeting GPCRs offers potential for novel cancer therapies by influencing tumor growth, spread, and the tumor microenvironment.
Area of Science:
- Molecular biology
- Cellular signaling
- Oncology
Background:
- G protein-coupled receptors (GPCRs) are integral membrane proteins that mediate cellular responses to external stimuli.
- GPCRs are implicated in various physiological processes, including cell growth, survival, migration, and angiogenesis.
- Dysregulation of GPCR signaling pathways is increasingly recognized in cancer development and progression.
Purpose of the Study:
- To elucidate the multifaceted roles of GPCRs in cancer initiation, progression, and metastasis.
- To highlight the involvement of GPCRs in key cancer-related signaling pathways.
- To explore the potential of targeting GPCRs for cancer therapeutic strategies.
Main Methods:
- Review of existing literature and evidence on GPCRs in cancer.
- Analysis of GPCR involvement in signaling pathways such as AKT/mTOR, MAPKs, and Hippo.
- Examination of GPCR roles in cancer cell invasion, metastasis, angiogenesis, and the tumor microenvironment.
Main Results:
- GPCRs influence cancer cell proliferation and survival through pathways like AKT/mTOR, MAPKs, and Hippo.
- GPCRs promote cancer cell invasion and metastasis via Rho GTPase activation and cytoskeletal remodeling.
- GPCRs contribute to tumor angiogenesis and the establishment of a pro-tumorigenic microenvironment.
Conclusions:
- GPCRs are critical regulators of multiple hallmarks of cancer.
- Understanding GPCR signaling in malignancy provides a basis for developing novel cancer treatments.
- Targeting GPCRs represents a promising avenue for cancer prevention and therapy.
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