Recently published X-ray structures of Class A and Class C G protein-coupled receptors (GPCRs) may afford the direct use of GPCR X-ray structures in structure-based drug design, provide more reliable homology modeling templates for many other ligand-mediated GPCR proteins, and help reveal the mechanism of GPCR activation. In this chapter, we assess the potential of some of the recent GPCR X-ray structures to provide insights into the mechanism of activation, and we provide a perspective of the emerging opportunities and possible limitations in the use of the new X-ray structures in structure-based drug design.

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