GPCRomics: GPCR Expression in Cancer Cells and Tumors Identifies New, Potential Biomarkers and Therapeutic Targets

Paul A. Insel* (Corresponding Author), Krishna Sriram, Shu Z. Wiley, Andrea Wilderman, Trishna Katakia, Thalia McCann, Hiroshi Yokouchi, Lingzhi Zhang, Ross Corriden, Dongling Liu, Michael Feigin, Randall P. French, Andrew M. Lowy, Fiona Murray

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

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G protein-coupled receptors (GPCRs), the largest family of targets for approved drugs, are rarely targeted for cancer treatment, except for certain endocrine and hormone-responsive tumors. Limited knowledge regarding GPCR expression in cancer cells likely has contributed to this lack of use of GPCR-targeted drugs as cancer therapeutics. We thus undertook GPCRomic studies to define the expression of endoGPCRs (which respond to endogenous hormones, neurotransmitters, and metabolites) in multiple types of cancer cells. Using TaqMan qPCR arrays to quantify the mRNA expression of ~340 such GPCRs, we found that human chronic lymphocytic leukemia (CLL) cells/stromal cells associated with CLL, breast cancer cell lines, colon cancer cell lines, pancreatic ductal adenocarcinoma (PDAC) cells, cancer associated fibroblasts (CAFs), and PDAC tumors express 50 to >100 GPCRs, including many orphan GPCRs (which lack known physiologic agonists). Limited prior data exist regarding the expression or function of most of the highly expressed GPCRs in these cancer cells and tumors. Independent results from cancer databases confirm the expression of such GPCRs. We propose that highly expressed GPCRs in cancer cells (for example, GPRC5A in PDAC and colon cancer cells and GPR68 in PDAC CAFs) may contribute to the malignant phenotype, serve as biomarkers and/or may be novel therapeutic targets for the treatment of cancer.
Original languageEnglish
Article number431
Number of pages11
JournalFrontiers in Pharmacology
Early online date22 May 2018
Publication statusPublished - 22 May 2018


  • breast cancer
  • Cancer microenvironment
  • chronic lymphocytic leukemia
  • Colon Cancer
  • GPCR array
  • Orphan receptors
  • Pancreatic Cancer


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