CDK HIV-1 Integrase protease HAT GPCR Retniblastoma

G-Protein Coupled Receptor (GPCR)

Role of GPCR in CNS Disorder
  Human G protein-coupled receptor (GPCR) families have more than 800 seven-transmembrane receptors representing the largest class of membrane proteins in the human genome.There has been a exceptional growth in the field of GPCR biology during the past two decades. The prominent landmark includes cloning of first GPCR genes and the sequencing of the human genome exposing the size of the GPCR family. Besides that there is a growing recognition of GPCR regulation is much more complex than primitively anticipated and includes signaling through G protein independent pathways. Despite of the fact that the outstanding advances in the biology and the pharmacology of GPCRs, progress in crystallizing the membrane protein is limited. They are involved in signal transduction pathways and responsible for metabolic, physiological and neurological maintenance [3]and linked to various diseases like cancer, diabetes, cardiovascular diseases, inflammation and several kinds of neurological diseases offers the richest source of target for the pharmaceutical industry almost 50-60% drugs in the market targeting the GPCR family.
Effect of Allosteric modulaters on CNS Disorder
  Even though the proven success of GPCR drug targets much intensive effort made by scientist to develop the selective drug candidates for GPCR have failed. Conventionally the drugs that target the same site where the endogenous ligand bind either to activate or inhibit the receptor. In many cases the endogenous ligand cannot be modified to get the drug like properties because many amino acids and peptide like molecules unable to cross the blood-brain barrier easily. Nowadays the CNS drug discovery focusing on developing the allosteric modulators which bind to the allosteric site that is distant from the conventional orthosteric site. The allosteric modulators offer lots of advantages over the conventional drug designing approach. The understanding of allosteric modulators gives a great momentum and the allosteric modulators marketed for the treatment of HIV infections and hyperthyroidism. However many allosteric modulators are entered into clinical trials in the treatment of CNS disorder that opens the new avenue for the CNS disorder treatment.