G protein-coupled receptors (GPCRs), which include ~900 members, represent the most leading family of validated drug targets in biomedicine. G protein-coupled receptors (GPCRs) have an important role in multiple diseases, including the development of cancer and cancer metastasis, and that's what makes GPCRs perfect drug targets for modern medicinal drugs.
When some GPCRs ligands such as chemokine, thrombin, lysophosphatidic acid (LPA), gastrin-releasing peptide and endothelin bind to their receptors, it causes a comformational change in G protein-coupled receptors (GPCRs) , which are involved in two signal transduction pathways: cAMP signaling pathway and phosphatidylinositol signaling pathway.
Recently, G protein-coupled receptors (GPCRs) have been an uprising star in drug therapy. One example of such GPCRs is chemokine receptor type 4 (CXCR4) which has great potential in drug target research. CXCR4 is thought to be involved in many disease states including more than 23 types of cancer and several immunodeficiency disorders, including head and neck cancer, breast cancer, small-cell lung cancer, non-small-cell lung cancer and Acquired Immune Deficiency Syndrome (AIDS).