Exploring a role for heteromerization in GPCR signalling specificity

R Rozenfeld, LA Devi - Biochemical Journal, 2011 - portlandpress.com
The critical involvement of GPCRs (G-protein-coupled receptors) in nearly all physiological
processes, and the presence of these receptors at the interface between the extracellular …

Functional selectivity in GPCR signaling: understanding the full spectrum of receptor conformations

E Goupil, SA Laporte, TE Hebert - Mini reviews in medicinal …, 2012 - ingentaconnect.com
The great versatility of G protein-coupled receptors (GPCRs), in terms of both their ability to
bind different types of ligands and initiate a large number of distinct cellular signaling events …

Functional crosstalk between GPCRs: with or without oligomerization

L Prezeau, ML Rives, L Comps-Agrar, D Maurel… - Current opinion in …, 2010 - Elsevier
Communication between cells requires key and specialized signaling systems, like G-
protein-coupled receptors (GPCRs). Cells coexpress a large number of different GPCRs, the …

Functional consequences of GPCR heterodimerization: GPCRs as allosteric modulators

KKV Haack, NA McCarty - Pharmaceuticals, 2011 - mdpi.com
G Protein Coupled Receptors (GPCRs) represent the largest family of membrane proteins in
the human genome, are the targets of approximately 25% of all marketed pharmaceuticals …

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 …

Emerging structural insights into biased GPCR signaling

AK Shukla, G Singh, E Ghosh - Trends in biochemical sciences, 2014 - cell.com
The discovery of biased signaling at G protein-coupled receptors (GPCRs), the largest class
of cell surface receptors and primary drug targets for numerous human diseases, has …

Emerging concepts in GPCR function--the influence of cell phenotype on GPCR pharmacology.

RM Eglen - Proceedings of the Western Pharmacology Society, 2005 - europepmc.org
G protein coupled receptors (GPCRs) are an important class of ligand-activated proteins that
regulate cellular metabolism. It is now appears that GPCR function is highly dependent upon …

Compartmentalization of GPCR signalling controls unique cellular responses

AM Ellisdon, ML Halls - Biochemical Society Transactions, 2016 - portlandpress.com
With> 800 members, G protein-coupled receptors (GPCRs) are the largest class of cell-
surface signalling proteins, and their activation mediates diverse physiological processes …

How ligands illuminate GPCR molecular pharmacology

D Wacker, RC Stevens, BL Roth - Cell, 2017 - cell.com
G protein-coupled receptors (GPCRs), which are modulated by a variety of endogenous and
synthetic ligands, represent the largest family of druggable targets in the human genome …

An update on the physiological and therapeutic relevance of GPCR oligomers

B Farran - Pharmacological research, 2017 - Elsevier
The traditional view on GPCRs held that they function as single monomeric units composed
of identical subunits. This notion was overturned by the discovery that GPCRs can form …