G Protein–Coupled Receptor Heteromers

Understanding the Added Value of G-Protein-Coupled Receptor Heteromers

G-protein-coupled receptors (GPCRs) constitute the most populated family of proteins within the human genome. Since the early sixties work on GPCRs and on GPCR-mediated signaling has led to a number of awards, the most recent being the Nobel Prize in Chemistry for 2012. The future of GPCRs research is surely based on their capacity for heteromerization. Receptor heteromers offer a series of cha...

A direct and functional interaction between the trimeric G protein Go and Rab5 in G proteincoupled receptor signaling

Allostery at G protein-coupled receptor homo- and heteromers: uncharted pharmacological landscapes.

For many years seven transmembrane domain G protein-coupled receptors (GPCRs) were thought to exist and function exclusively as monomeric units. However, evidence both from native cells and heterologous expression systems has demonstrated that GPCRs can both traffic and signal within higher-order complexes. As for other protein-protein interactions, conformational changes in one polypeptide, in...

ASSOCIATE EDITOR: DAVID SIBLEY Allostery at G Protein-Coupled Receptor Homo- and Heteromers: Uncharted Pharmacological Landscapes

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Receptor and Channel Heteromers as Pain Targets

Recent discoveries indicate that many G-protein coupled receptors (GPCRs) and channels involved in pain modulation are able to form receptor heteromers. Receptor and channel heteromers often display distinct signaling characteristics, pharmacological properties and physiological function in comparison to monomer/homomer receptor or ion channel counterparts. It may be possible to capitalize on s...