Structures of Class B G Protein-Coupled Receptors: Prospects for Drug Discovery

摘要

Gprotein-coupled receptors (GPCRs) are the most important class of drug targets. GPCR structural biology has witnessed a revolution in the last five years, cumulating in the Nobel Prize in Chemistry 2012. While a consensus for the structural framework for the majority of GPCRs (the class A GPCRs) has now emerged, their more distantly related cousins of the class B GPCR family are structurally still poorly understood. Now two landmark publications by Hollenstein et al. and Siu et al. have presented the first class B GPCR structures providing the first highly resolved snapshots for this class of molecular signaling machines.