Mapping the Putative G Protein-coupled Receptor (GPCR) Docking Site on GPCR Kinase 2

Expanding the Concept of G Protein-Coupled Receptor (GPCR) Dimer Asymmetry towards GPCR-Interacting Proteins

G protein-coupled receptors (GPCRs), major targets of drug discovery, are organized in dimeric and/or oligomeric clusters. The minimal oligomeric unit, the dimer, is composed of two protomers, which can behave differently within the dimer. Several examples of GPCR asymmetry within dimers at the level of ligand binding, ligandpromoted conformational changes, conformational changes within transme...

GPCR-OKB: the G Protein Coupled Receptor Oligomer Knowledge Base

SUMMARY Rapid expansion of available data about G Protein Coupled Receptor (GPCR) dimers/oligomers over the past few years requires an effective system to organize this information electronically. Based on an ontology derived from a community dialog involving colleagues using experimental and computational methodologies, we developed the GPCR-Oligomerization Knowledge Base (GPCR-OKB). GPCR-OKB ...

Detection of G protein-selective G protein-coupled receptor (GPCR) conformations in live cells.

Although several recent studies have reported that GPCRs adopt multiple conformations, it remains unclear how subtle conformational changes are translated into divergent downstream responses. In this study, we report on a novel class of FRET-based sensors that can detect the ligand/mutagenic stabilization of GPCR conformations that promote interactions with G proteins in live cells. These senso...

G-protein-coupled Receptors Gpcr Structure and Function

Potential role of G protein-coupled receptor (GPCR) heterodimerization in neuropsychiatric disorders: a focus on depression.

G protein-coupled receptors (GPCRs) represent the largest family of membrane proteins in the human genome and are the target of approximately half of all therapeutic drugs. For many years, GPCRs were thought to exist and function as monomeric units. However, during the past two decades, substantial biochemical, structural and functional evidence have indicated that GPCRs can associate and form ...