First Solution Structures of Seven-Transmembrane Helical Proteins

摘要

Seven-transmembrane (7-TM) helical proteins constitute a biologically important class of membrane proteins. The most prominent members of this class are the G-protein coupled receptors (GPCRs). These proteins are involved in transmitting the signal from the extracellular space into cells, and therefore play a pivotal role in biology. Not astonishingly, about 30% of all drugs target GPCRs. Despite their prime pharmacological importance still little high-resolution structural knowledge is available, although we have witnessed significant progress in this area over the last decade. Following the structure of bovine rhodopsin in 2000 a number of other GPCR structures were determined by crystallography, including the β1 and β2 adrenergic receptors, the dopamine D3, the adenosine A_(2A), the histamine H1 and the chemokine CXCR4 receptors.