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Table 1 The regulation of YAP/TAZ activity by GPCR-associated signaling in human malignancies

From: YAP and endothelin-1 signaling: an emerging alliance in cancer

GPCRs Coupling Protein Cancer Type Drugs References
LPA receptors Gα12/13 Gαq/11 Ovarian cancer Phosphatase-resistant LPA analogues Monoclonal antibodies for LPA [68, 84,85,86]
S1P receptors Gα12/13 Ovarian cancer, Hepatocellular carcinoma Monoclonal antibodies for S1P [69, 72, 85, 86]
G protein-coupled estrogen receptor (GPER) Gαq/11 Breast cancer GPER inhibitors (agonist analogous, G15) [74]
Protease-activated receptors (PARs) Gα12/13 Gαq/11 Breast cancer RhoA GTPase inhibitors (C3 transferase) [75, 76]
Colon cancer
Lung cancer
Pancreatic cancer
Prostate cancer
Squamous cell carcinoma of the head and neck
Angiotensin II Receptor (AT1) Gαq/11 Prostate cancer Angiotensin receptor blockers (losartan) [77, 78]
Prostaglandin E2 receptor (EP2) Gαq/11 Colon cancer Prostaglandin synthetase blockers (indomethacin) [79, 80]
Hepatocellular carcinoma
Head and neck cancer
Non-small cell lung cancer
Chemochine (C-X-C motif) receptor 4 (CXCR4) Gα12/13 Gαq/11 Non-small cell lung cancer CXCR4 antagonists (WZ811) [81]
Breast cancer
Oral squamous carcinoma
Chronic Myelogenous leukemia
Free Fatty Acid receptor 1 (FFAR1) Gαq/11 Prostate cancer Docosahexaenoic acid (DHA) [82]
Wnt receptor (Frizzled, FRD) Gα12/13 Colorectal cancer RhoA GTPase inhibitors (C3 transferase) [83]
Prostate cancer
Hepatocellular carcinoma
Endothelin A receptor (ETAR) Gαq/11 Colon cancer Selective ETAR antagonists (BQ123) [87]
Endothelin A receptor (ETAR) β-arr1 Ovarian cancer Dual ET-1R antagonists (macitentan) [88, 89]
Breast cancer