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Updated: Jul 9, 2026

Detection of G Protein-coupled Receptor Expression in Mouse Vagal Afferent Neurons using Multiplex In Situ Hybridization
Published on: September 20, 2021
GPR87 is an overexpressed G-protein coupled receptor in squamous cell carcinoma of the lung
Mathias Gugger1, Richard White, Susan Song
1Division of Cell Biology and Experimental Cancer Research, Institute of Pathology, University of Bern, Murtenstrasse 31, 3010 Bern, Switzerland.
Abstract:
Lung cancer is the leading cause of cancer death worldwide. The overall 5-year survival after therapy is about 16% and there is a clear need for better treatment options, such as therapies targeting specific molecular structures. G-protein coupled receptors (GPCRs), as the largest family of cell surface receptors, represent an important group of potential targets for diagnostics and therapy. We therefore used laser capture microdissection and GPCR-focused Affymetrix microarrays to examine the expression of 929 GPCR transcripts in tissue samples of 10 patients with squamous cell carcinoma and 7 with adenocarcinoma in order to identify novel targets in non-small cell lung carcinoma (NSCLC). The relative gene expression levels were calculated in tumour samples compared to samples of the neighbouring alveolar tissue in every patient. Based on this unique study design, we identified 5 significantly overexpressed GPCRs in squamous cell carcinoma, in the following decreasing order of expression: GPR87 > CMKOR1 > FZD10 > LGR4 > P2RY11. All are non-olfactory and GRAFS (glutamate, rhodopsin, adhesion, frizzled/taste2, secretin family) classified. GPR87, LGR4 and CMKOR1 are orphan receptors. GPR87 stands out as a candidate for further target validation due to its marked overexpression and correlation on a mutation-based level to squamous cell carcinoma.
Insights
Researchers identified novel molecular targets for non-small cell lung carcinoma (NSCLC). Five G-protein coupled receptors (GPCRs) were significantly overexpressed in squamous cell carcinoma, with GPR87 showing the most promise for future lung cancer therapies.
Area of Science:
- Oncology
- Molecular Biology
- Genomics
Background:
- Lung cancer is a leading cause of cancer mortality globally, with a low 5-year survival rate, highlighting the need for improved therapeutic strategies.
- G-protein coupled receptors (GPCRs), the largest family of cell surface receptors, are crucial for cellular communication and represent promising targets for cancer diagnostics and treatments.
Purpose of the Study:
- To identify novel molecular targets for non-small cell lung carcinoma (NSCLC) by examining the expression of G-protein coupled receptors (GPCRs).
- To investigate differential GPCR expression in squamous cell carcinoma and adenocarcinoma subtypes of NSCLC.
Main Methods:
- Utilized laser capture microdissection to isolate tumor and adjacent normal tissue samples from NSCLC patients.
- Employed GPCR-focused Affymetrix microarrays to analyze the expression of 929 GPCR transcripts.
- Calculated relative gene expression levels by comparing tumor tissue to neighboring alveolar tissue within each patient.
Main Results:
- Identified five significantly overexpressed GPCRs in squamous cell carcinoma compared to normal lung tissue: GPR87, CMKOR1, FZD10, LGR4, and P2RY11.
- GPR87 demonstrated the highest level of overexpression and showed a correlation with squamous cell carcinoma on a mutation-based level.
- The identified GPCRs belong to non-olfactory families (GRAFS classification), including orphan receptors like GPR87, LGR4, and CMKOR1.
Conclusions:
- GPR87 is a highly promising candidate for further investigation and validation as a therapeutic target in squamous cell carcinoma.
- This study provides a foundation for developing targeted therapies for NSCLC by identifying novel GPCRs involved in tumor development.
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