Established and In-trail GPCR Families in Clinical Trials: A Review for Target Selection.

The key down player remains for drug industries is the selection of biological target currently attracting huge investments to validate them in patient subsets in order to study potential drugs. GPCRs are one such druggable target wherein non-olfactory GPCRs are encoded by 50% of the human genome-encoded which are therapeutically unexploited. The concept of ploypharmacology has become essential part of therapeutics for complex diseases like schizophrenia, cancer etc and considering the promiscuity and selectivity GPCRs could emerge as novel targets. The availability of 44 crystal structures of unique receptors and 205 ligand receptor complexes now presents a strong foundation structure-based drug discovery and design. Further, 34% of all the drugs approved by the US Food and Drug Administration FDA act at 108 unique GPCRs which indicates the benefits of considering the correct target in drug designing. The important GPCR families currently in clinical trials can offer huge understanding towards the drug designing prospects including "off-target" effects reducing economical resource and time. This review will concentrate on the established and in-trail GPCR families in clinical trials. The druggability of GPCR protein families and critical roles played by them in complex diseases are explained for considering them as targets for novel drug discovery ventures.