Three-dimensional representations of G protein-coupled receptor structures and mechanisms.

Publisher Summary G protein-coupled receptors (GPCRs) have been grouped into five somewhat distinct families: one resembling rhodopsin, another identified with the secretin receptor, a class related to the metabotropic glutamate receptor, another to the fungal pheromone receptor, and a class of CAMP receptors. The recent breakthrough in determining the crystal structure of rhodopsin has confirmed the general expectation that GPCRs are composed of seven helical transmembrane segments connected by intracellular and extracellular loop segments, as well as the expected topology of an extracellular N terminus and an intracellular C terminus. This chapter describes the construction, evaluation, and use of the three-dimensional (3D) molecular models of GPCRs from the various families reflects the general current understanding of their architecture. This understanding is implemented in the 3D receptor models based on a variety of direct experimental data, as well as results from various approaches from computational genomics, biophysics, and bioinformatics.