Table 1 GPCRs in cancer
From: The authors' reply
Cancer | Receptor | Ligand | Process | Selected references |
|---|---|---|---|---|
Breast cancer | PAR1 | Thrombin | Growth; metastasis; angiogenesis | 12,132,133 |
EP2; EP4 | PGE2 | Growth; metastasis; angiogenesis | 42,44,134 | |
CXCR4 | SDF1 | Metastasis; angiogenesis | 70 | |
GPR30 | Oestrogen | Growth? Hormone-therapy resistance? | 23–26 | |
Colon cancer | EP2, EP4 | PGE2 | Growth; metastasis; angiogenesis | 30–34 |
LPA1 | LPA | Growth | 126 | |
ET receptors | Endothelin-1 | Survival | 41 | |
PAR1 | Thrombin | Growth; migration | 135 | |
Frizzleds | Wnts | Growth | 62 | |
Head and neck cancer | CXCR2 | IL8; GROα | Growth; metastasis; angiogenesis | 136 |
CXCR4 | SDF1 | Metastasis | 137 | |
EP receptors | PGE2 | Growth; angiogenesis; metastasis | 46 | |
GRPR | GRP | Growth; survival | 138 | |
PAR1 | Thrombin | Metastasis; angiogenesis | 13 | |
Small-cell lung cancer | GRPR | GRP | Growth | 3,16,17,139 |
NMB-R | Neuromedin B | Growth | 3,16,17 | |
CCK1; CCK2 | CCK | Growth; survival | 3 | |
CXCR4 | SDF1 | Growth; metastasis | 140 | |
Non-small-cell lung cancer | EP receptors | PGE2 | Growth; metastasis; angiogenesis | 45,141 |
CXCR2 | IL8; GROα | Growth; metastasis; angiogenesis | 142 | |
CXCR4 | SDF1 | Migration; metastasis | 143 | |
β1AR; β2AR | NNK | Growth? | 144 | |
Ovarian cancer | LPA1–LPA3 | LPA | Growth; metastasis; angiogenesis | 4,15 |
CXCR2 | GROα | Growth; angiogenesis | 15 | |
Pancreatic cancer | GRPR | GRP | Growth | 145 |
CCK1; CCK2 | CCK | Growth | 3 | |
Parathyroid gland cancer | CASR | Calcium | Growth | 146 |
Pituitary cancer | TSH receptor* | TSH‡ | Growth; survival | 51,147 |
ACTHR† | ACTH‡ | Growth | 147 | |
Prostate cancer | PAR1 | Thrombin | Growth; invasion | 14,89 |
ETA | Endothelin 1 | Growth; survival; metastasis | 14,18 | |
AT1 | Angiotensin II | Growth | 148 | |
EP2, EP4 | PGE2 | Growth; metastasis; angiogenesis | 27 | |
LPA1 | LPA | Growth; invasion | 14 | |
B1, B2 | Bradykinin | Growth; survival; invasion | 14,19 | |
GRPR | GRP | Growth; migration | 14 | |
Melanoma | MC1R | MSH | Sensitivity to UV-induced DNA damage | 50,149 |
CXCR2 | IL8; GROα | Growth; metastasis; angiogenesis | 150 | |
ETB | Endothelin-1/3 | Growth | 151 | |
Basal-cell carcinoma | Smoothened | Sonic hedgehog | Growth | 57,58,152 |
Testicular cancer | LH receptor | LH | Growth | 153 |
Thyroid cancer | TSH receptor | TSH | Growth | 51,56 |
Many G-protein-coupled receptors (GPCRs) contribute to the aberrant growth and survival of cancer cells, as well as to tumour-induced angiogenesis and metastasis. Examples of some of the GPCRs most frequently implicated in human cancer are listed. ACTHR, adrenocorticotropic hormone receptor; β1AR and β2AR, β1- and β2- adrenergic receptors; CASR, calcium sensing receptor; CCK, cholecystokinin; ETRA, endothelin receptor type A; ETRB, endothelin receptor type B; GPR30, G-protein- coupled receptor 30; GRPR, gastrin-releasing peptide receptor; IL8, interleukin 8; LH, luteinizing hormone; LPA, lysophosphatidic acid; MC1R, melanocortin 1 receptor; MSH, melanocortin 1; NMBR, neuromedin B receptor; NNK, 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone; PGE2, prostaglandin E2; SDF1, stromal cell-derived factor1; TSH, thyroid stimulating hormone.>*TSH acts on TSH receptor in the thyroid.†ACTH acts on ACTHR in the adrenal glands.‡Overproduced by pituitary tumours. | ||||
