The control and mediation of the cell cycle is influenced by cell signals. Different types of cell signaling molecules: Proteins (growth factors), peptide hormones, amino acids, steroids, retenoids, fatty acid derivatives, and small gases can all act as signaling molecules. G- protein coupled receptors(GPCR) are heptahelical, serpentine receptors and are multi functional receptors having lot more clinical implications. Many reports have been clarified the basic mechanism of GPCR signal transduction, numerous laboratories have published on the clinical implication/application of GPCR. To name a few, dysfunction of GPCR signal pathway plays a role in cancer, autoimmunity, and diabetes. In this report, we will review the role of GPCR in cell signaling and impact of GPCR in clinical medicine,