GPCRs are known to play an essential role in the coordination of cellular communication, and they can activate signaling pathways that control gene expression and cell proliferation. Aberrant GPCR signaling, either through activating inherited or acquired mutations within the GPCRs or due to the overexpression of GPCRs or their respective ligands, may lead to transformation, thus contributing to the onset or progression of oncogenesis. Because the role of GPCRs in the development of cancer is becoming apparent, GPCRs are emerging targets for therapeutic interventions to treat cancer.

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