G protein–coupled receptor oligomerization revisited: functional and pharmacological perspectives

S Ferré, V Casadó, LA Devi, M Filizola, R Jockers… - Pharmacological …, 2014 - ASPET
Most evidence indicates that, as for family CG protein–coupled receptors (GPCRs), family A
GPCRs form homo-and heteromers. Homodimers seem to be a predominant species, with …

G-protein-coupled receptor oligomerization and its potential for drug discovery

SR George, BF O'Dowd, SP Lee - Nature reviews Drug discovery, 2002 - nature.com
G-protein-coupled receptors (GPCRs) represent by far the largest class of targets for modern
drugs. Virtually all therapeutics that are directed towards GPCRs have been designed using …

Heterodimerization of G-protein-coupled receptors: pharmacology, signaling and trafficking

LA Devi - Trends in pharmacological sciences, 2001 - cell.com
Although classical models predict that G-protein-coupled receptors (GPCRs) function as
monomers, several recent studies acknowledge that GPCRs exist as dimeric or oligomeric …

G-protein-coupled receptor dimerization: modulation of receptor function

CD Rios, BA Jordan, I Gomes, LA Devi - Pharmacology & therapeutics, 2001 - Elsevier
G-protein-coupled receptors (GPCRs) comprise the largest family of transmembrane
receptors in the human genome that respond to a plethora of signals, including …

Roles of G‐protein‐coupled receptor dimerization: From ontogeny to signalling regulation

S Terrillon, M Bouvier - EMBO reports, 2004 - embopress.org
The classical idea that G‐protein‐coupled receptors (GPCRs) function as monomeric
entities has been unsettled by the emerging concept of GPCR dimerization. Recent findings …

The impact of G‐protein‐coupled receptor hetero‐oligomerization on function and pharmacology

R Maggio, F Novi, M Scarselli, GU Corsini - The FEBS journal, 2005 - Wiley Online Library
Although highly controversial just a few years ago, the idea that G‐protein‐coupled
receptors (GPCRs) may undergo homo‐oligomerization or hetero‐oligomerization has …

Asymmetry of GPCR oligomers supports their functional relevance

P Maurice, M Kamal, R Jockers - Trends in pharmacological sciences, 2011 - cell.com
G protein-coupled receptors (GPCRs) can exist as dimers or as larger oligomeric clusters
that enable intercommunication between different receptor protomers within the same …

The apparent cooperativity of some GPCRs does not necessarily imply dimerization

M Chabre, P Deterre, B Antonny - Trends in pharmacological sciences, 2009 - cell.com
When the binding of one ligand to its receptor is influenced by a second ligand acting on a
different receptor, one might assume that the receptors dimerize, enabling allosteric …

Contribution of heteromerization to G protein-coupled receptor function

SA Gaitonde, J González-Maeso - Current opinion in pharmacology, 2017 - Elsevier
Highlights•Family A GPCRs can function as monomers but they also form higher order
complexes.•These complexes are involved in almost every step of the GPCR life cycle.•They …

Dimerization of G-protein-coupled receptors: roles in signal transduction

M Bai - Cellular signalling, 2004 - Elsevier
Recently, many G-protein-coupled receptors (GPCRs) have been demonstrated to form
constitutive dimers consisting of identical or distinct monomeric subunits. The discovery of …