Title: Crystal structures of the b2-adrenergic receptor

Abstract:

G protein coupled receptors (GPCRs) constitute the largest family of membrane proteins in the human genome, and are responsible for the majority of signal transduction events involving hormones and neurotransmitters across the cell membrane. GPCRs that bind to diffusible ligands have low natural abundance, are relatively unstable in detergents, and display basal G protein activation even in the absence of ligands. I will describe approaches that have led to crystal structures of the beta2-adrenergic receptor. These structures, along with several other GPCRs, have provided insights into the basal activity of the receptor, the structural features that enable binding of diffusible ligands, and the coupling between ligand binding and G-protein activation.