G protein-coupled receptors (GPCRs) comprise the largest family of cell surface receptors in the human genome, regulating a plethora of physiological responses and serving as frequent drug targets. Four main groups of GPCRs are recognized and classified according to their pharmacological properties: Class A is rhodopsin-like; Class B is secretin-like; Class C is comprised of metabotropic glutamate/pheromone; and Class D is comprised of frizzled receptors. While GPCRs regulate many aspects of tumorigenesis as well as many cancer-associated signaling pathways, only a few drugs aiming to inhibit GPCRs are currently used in cancer, these signal proteins are PARs, chemokine receptors, Gα12/13 proteins, lysophosphatidic acid (LPA), and GPCR-mediated pathways such as the WNT and Hippo signaling pathways.


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