GPCR Partners as Cancer Driver Genes: Association with PH-Signal Proteins in a Distinctive Signaling Network

The essential role of G-protein coupled receptors (GPCRs) in tumor growth is recognized, yet a GPCR based drug in cancer is rare. Understanding the molecular path of a tumor driver gene may lead to the design and development of an effective drug. For example, in members of protease-activated receptor (PAR) family (e.g., PAR(1) and PAR(2)), a novel PH-binding motif is allocated as critical for tumor growth. Animal models have indicated the generation of large tumors in the presence of PAR(1) or PAR(2) oncogenes. These tumors showed effective inhibition when the PH-binding motif was either modified or were inhibited by a specific inhibitor targeted to the PH-binding motif. In the second part of the review we discuss several aspects of some cardinal GPCRs in tumor angiogenesis.

Automated summary

The essential role of G-protein coupled receptors (GPCRs) in tumor growth is recognized, yet GPCR based drugs in cancer are rare. Understanding the molecular path of a tumor driver gene may lead to the design and development of effective drugs. Several aspects of some cardinal GPCRs in tumor angiogenesis are also discussed.