The g protein coupled receptors gpcrs and associated peripheral g proteins underpin a multitude of physiological processes the gpcrs represent one of the largest superfamilies in the human genome and are a significant target for bioactive and drug discovery programs it is estimated that greater than 50 of all drugs including those in development currently target gpcrs many of the characterized gpcrs have known ligands however approximately 20 of gpcrs are described as orphan gpcrs . The g protein coupled receptors gpcrs known to be one of the largest superfamilies in the human genome underpin a multitude of physiological processes and represent a significant target for bioactive and drug discovery programs in g protein coupled receptors in drug discovery methods and protocols experts in the field provide a range of classic and cutting edge laboratory protocols developed for gpcr research as well as several current review articles relevant to the area of high . The g protein coupled receptor gpcr superfamily consists of structurally similar proteins arranged into families classes and is one of the most abundant protein classes in the mammalian genome 1 5 gpcrs undertake a plethora of essential physiological functions and are targets for numerous novel drugs 45 their ligands are structurally heterogenous including natural odorants nucleotides amines peptides proteins and lipids 4 the conserved structure of gpcrs consists of seven . These structural and dynamic studies can provide a foundation for a wide range of applications including rational drug design and protein engineering in our laboratory the use of md simulations and network analysis assisted in the elucidation of the allosteric hotspots and intracellular signal transduction of g protein coupled receptors gpcrs primarily on one of the adenosine receptor subtypes a2a adenosine receptor a2aar in this chapter we describe a method for calculating the
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