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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]

Melanoma

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]

Cholangiocarcinoma

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