The Structural Basis of G-Protein-Coupled Receptor Signaling (Nobel Lecture)

The structural basis of G-protein-coupled receptor signaling (Nobel Lecture).

Complex organisms require a sophisticated communication network to maintain homeostasis. Cells from different parts of our bodies communicate with each other using chemical messengers in the form of hormones and neurotransmitters. Cells process information encoded in these chemical messages using G-protein-coupled receptors (GPCRs) located in the plasma membrane. GPCRs also mediate communicatio...

G-protein Coupled Receptor Dimerization

A growing body of evidence suggests that GPCRs exist and function as dimers or higher oligomers. The evidence for GPCR dimerization comes from biochemical, biophysical and functional studies. In addition, researchers have shown the occurrence of heterodimerization between different members of the GPCR family. Two receptors can interact with each other to make a dimer through their extracellular...

A brief history of G-protein coupled receptors (Nobel Lecture).

Molecular basis for activation of G protein-coupled receptor kinases.

G protein-coupled receptor (GPCR) kinases (GRKs) selectively recognize and are allosterically regulated by activated GPCRs, but the molecular basis for this interaction is not understood. Herein, we report crystal structures of GRK6 in which regions known to be critical for receptor phosphorylation have coalesced to stabilize the kinase domain in a closed state and to form a likely receptor doc...

Structural Basis for Tailor-Made Modulation of G Protein Coupled Receptor Functionality