The current status of anti-GPCR drugs against different cancers

G protein coupled receptors (GPCRs) have emerged as the most potential target for a number of drug discovery programs ranging from control of blood pressure, diabetes, cure for genetic diseases to treatment of cancer. A panel of different ligands including hormones, peptides, ions and small molecules is responsible for activation of these receptors. Molecular genetics has identified key GPCRs, whose mutations or altered expressions are linked with tumorgenicity. In this review, we discussed recent advances regarding the involvement of GPCRs in the development of cancers and approaches to manipulating the mechanism behind GPCRs involved tumor growth and metastasis to treat different types of human cancer. This review provides an insight into the current scenario of GPCR-targeted therapy, progress to date and the challenges in the development of anticancer drugs.
Graphical abstract GPCRs based drugs against different cancers.Image 1
Highlights • An association of GPCRs in tumor growth and metastasis is confirmed in different types of cancers. • Despite the incredible potential of GPCRs in cancer therapy, only a few anti-GPCR drugs has been approved for clinical use. • Advancement in studying the association of cancer with GPCRs is inevitable to manipulate these receptors for cancer therapy.