Abstract
G protein-coupled receptors (GPCRs), also known as 7-transmembrane domain receptors, represent the most druggable target for diseases in the human genome. Novel approaches to targeting GPCRs have been possible due to available structures of these proteins on the Protein Data Bank (PDB). Moreover, structures that contain ligands bound to allosteric sites on GPCRs have been useful in the development of allosteric modulators. Because allosteric modulators bind to GPCR receptor sites that do not interfere with the endogenous ligand, they do not drastically affect the physiological function of the receptor but rather modulate their effects. In this chapter we will look at specific allosteric binding sites on GPCRs that have been discovered via crystallography or computational methods.
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