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Identification of Dysregulated Expression of G Protein Coupled Receptors in Endocrine Tumors by Bioinformatics
Valentine Suteau1,2, Mathilde Munier1,2,3, Rym Ben Boubaker2
1Département d'Endocrinologie-Diabétologie Nutrition, Centre Hospitalier Universitaire (CHU) d'Angers, 49933 Angers, France.
Background:
Many studies link G protein-coupled receptors (GPCRs) to cancer. Some endocrine tumors are unresponsive to standard treatment and/or require long-term and poorly tolerated treatment. This study explored, by bioinformatics analysis, the tumoral profiling of the GPCR transcriptome to identify potential targets in these tumors aiming at drug repurposing.
Methods:
We explored the GPCR differentially expressed genes (DEGs) from public datasets (Gene Expression Omnibus (GEO) database and The Cancer Genome Atlas (TCGA)). The GEO datasets were available for two medullary thyroid cancers (MTCs), eighty-seven pheochromocytomas (PHEOs), sixty-one paragangliomas (PGLs), forty-seven pituitary adenomas and one-hundred-fifty adrenocortical cancers (ACCs). The TCGA dataset covered 92 ACCs. We identified GPCRs targeted by approved drugs from pharmacological databases (ChEMBL and DrugBank).
Results:
The profiling of dysregulated GPCRs was tumor specific. In MTC, we found 14 GPCR DEGs, including an upregulation of the dopamine receptor (DRD2) and adenosine receptor (ADORA2B), which were the target of many drugs. In PGL, seven GPCR genes were downregulated, including vasopressin receptor (AVPR1A) and PTH receptor (PTH1R), which were targeted by approved drugs. In ACC, PTH1R was also downregulated in both the GEO and TCGA datasets and was the target of osteoporosis drugs.
Conclusions:
We highlight specific GPCR signatures across the major endocrine tumors. These data could help to identify new opportunities for drug repurposing.
Insights
This study analyzed G protein-coupled receptor (GPCR) gene expression in endocrine tumors, identifying specific GPCR signatures for drug repurposing opportunities in medullary thyroid cancer and other rare tumors.
Area of Science:
- Endocrinology
- Oncology
- Pharmacology
- Bioinformatics
Background:
- G protein-coupled receptors (GPCRs) are implicated in various cancers.
- Endocrine tumors often exhibit resistance to standard treatments, necessitating novel therapeutic strategies.
Purpose of the Study:
- To perform a bioinformatics analysis of the GPCR transcriptome in endocrine tumors.
- To identify potential drug repurposing targets within these tumors.
Main Methods:
- Utilized public datasets from Gene Expression Omnibus (GEO) and The Cancer Genome Atlas (TCGA).
- Analyzed differentially expressed GPCR genes (DEGs) in medullary thyroid cancers (MTCs), pheochromocytomas (PHEOs), paragangliomas (PGLs), pituitary adenomas, and adrenocortical cancers (ACCs).
- Cross-referenced identified GPCRs with existing drug targets from pharmacological databases (ChEMBL, DrugBank).
Main Results:
- GPCR expression profiles were found to be tumor-specific.
- In MTC, upregulated GPCRs included dopamine receptor (DRD2) and adenosine receptor (ADORA2B).
- In PGL and ACC, downregulated GPCRs included vasopressin receptor (AVPR1A) and PTH receptor (PTH1R), with PTH1R targeted by osteoporosis drugs.
Conclusions:
- Specific GPCR signatures were identified across major endocrine tumors.
- These findings offer potential avenues for drug repurposing to improve treatment outcomes for endocrine malignancies.
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