This chapter provides an overview of the field of structural biology of GPCRs. Rhodopsin is the most extensively studied GPCR to date and serves as the central theme of this chapter which describes some of the most important method developments and results that has led to our current understanding of the structures and dynamics of GPCRs. Nuclear magnetic resonance (NMR) spectroscopy has served as a primary tool in this effort, with some of the earliest studies carried out more than 30 years ago. Advances in NMR including solution and solid-state methods yielded results that, in combination with other biophysical methods (e.g., electron paramagnetic resonance, x-ray crystallography), applications of biochemical innovations (e.g., site-directed mutagenesis, recombinant protein expression), and computational modeling, revealed high-resolution structural details of the mechanisms of signal transduction for rhodopsin. The highly conserved seven-transmembrane (7TM) architectures of GPCRs allow this knowledge to be extended in light of studies on other receptors in this family (also reviewed here) to provide overall models of the structure and dynamics of GPCRs in general.

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