| | GPCR mRNA expression in cancer | Source of mRNA data | Cancer type studied |
| GPCRs frequently upregulated in most cancer types: FPR3, F2RL1, GPR160, GPR143, P2RY6, APLNR, OPN3CXCR3, CCR1, FZD2, LPAR5, CELSR3, ADORA2B, CCR5, PTAFR, GRP39, F2R, C3AR1, GP5CA, and CELSR1
GPCRs frequently downregulated in most cancer types: GABBR1, GRP146, ACKR1, MRGPRF, LTB4R, SIPR1, ADGRA2, PTGIR, FZD4, ADGRL4, LPAR1, EDNRB, GRP4, MC1R, ADGRD1, ADGRF5, VIPR1, ACKR3, LPAR6, and ADORA2A | TCGA data for tumors vs. GTEx database for normal tissue expression | Adrenocortical cancer, bladder cancer, breast cancer, cervical cancer, colon adenocarcinoma, esophageal cancer, kidney cancer, liver hepatocellular carcinoma, lung cancer, ovarian cancer, pancreatic cancer, prostate adenocarcinoma, skin cutaneous melanoma, stomach adenocarcinoma, testicular cancer, thyroid cancer, uterine carcinosarcoma [24] |
| GPCRs frequently upregulated in B-CLL cell lines: CXCR4, EBI2, CCR7, ADRB2, PTGER4, GABBR1, CNR2, CELSR1, and LPAR5
GPCRs frequently upregulated in breast cancer cell lines: FZD6, GPR126, P2RY11, CD97, GPRC5B, FZD1, GPR153, OXTR, BAI2, FZD4, LPHN2, GPR161, FZD2, FZD7, TBXA2R, F2R, GABBR1, MC1R, ADORA2B, GPR125, GPR135, OPN3, and EDG3
GPCRs frequently upregulated in colon cancer cell lines: F2RL1, ADORA2B, VIPR1, OXER1, LPAR2, GPR160, and GPRC5A
GPCRs frequently upregulated in pancreatic ductal adenocarcinoma tumors: GPRC5A and GPR68 | (1) TaqMan GPCR arrays
(2) TCGA data for tumors vs. GTEx database for normal tissue expression
(3) EBI database | B-cell chronic lymphocytic leukemia cell lines, colon cancer cell lines, triple-negative breast cancer cell lines, pancreatic ductal adenocarcinoma tumors [187] |
| | PAR (1-4) family of GPCRs has high expression in cancer, with frequent upregulation of PAR1 and PAR3 in multiple cancers | Protease-activated receptors in TCGA data for tumors vs. GTEx database for normal tissue expression | Pancreatic adenocarcinoma, esophageal carcinoma, stomach adenocarcinoma, breast invasive carcinoma, head and neck squamous carcinoma, and kidney renal clear cell carcinoma [188] |
| | More than 1.5-fold expression was observed for ~18 GPCRs in prostate cancer and ~30 in breast cancer. AGTR1, F2R, and FPR1 were predicted as targets for prostate cancer and CCR7, CXCR3, GPR18, GPR19, GPR37, GPR171, and GPR171 for breast cancer | Analysis was done using the GEO repository | Prostate cancer and breast cancer [189] |
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