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

S Ferré, V Casadó, LA Devi, M Filizola, R Jockers… - Pharmacological …, 2014 - Elsevier
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 …

Action of molecular switches in GPCRs-theoretical and experimental studies

B Trzaskowski, D Latek, S Yuan… - Current medicinal …, 2012 - ingentaconnect.com
G protein coupled receptors (GPCRs), also called 7TM receptors, form a huge superfamily of
membrane proteins that, upon activation by extracellular agonists, pass the signal to the cell …

Crystal structure of the µ-opioid receptor bound to a morphinan antagonist

A Manglik, AC Kruse, TS Kobilka, FS Thian… - Nature, 2012 - nature.com
Opium is one of the world's oldest drugs, and its derivatives morphine and codeine are
among the most used clinical drugs to relieve severe pain. These prototypical opioids …

Single-molecule analysis of fluorescently labeled G-protein–coupled receptors reveals complexes with distinct dynamics and organization

D Calebiro, F Rieken, J Wagner, T Sungkaworn… - Proceedings of the …, 2013 - pnas.org
G-protein–coupled receptors (GPCRs) constitute the largest family of receptors and major
pharmacological targets. Whereas many GPCRs have been shown to form di-/oligomers, the …

Fluorescence/bioluminescence resonance energy transfer techniques to study G-protein-coupled receptor activation and signaling

MJ Lohse, S Nuber, C Hoffmann - Pharmacological reviews, 2012 - Elsevier
Fluorescence and bioluminescence resonance energy transfer (FRET and BRET)
techniques allow the sensitive monitoring of distances between two labels at the nanometer …

A new approach to analyze cell surface protein complexes reveals specific heterodimeric metabotropic glutamate receptors

E Doumazane, P Scholler, JM Zwier… - The FASEB …, 2011 - Wiley Online Library
G‐protein‐coupled receptors (GPCRs) can form heteromeric complexes. Herein'we describe
a new approach to test the heteromerization of 2 receptors' or 2 receptor subunits' and to …

Conformational selection or induced fit? 50 years of debate resolved

JP Changeux, S Edelstein - F1000 biology reports, 2011 - pmc.ncbi.nlm.nih.gov
Exactly 50 years ago, biochemists raised the question of the mechanism of the
conformational change that mediates “allosteric” interactions between regulatory sites and …

Crystal structure of oligomeric β1-adrenergic G protein–coupled receptors in ligand-free basal state

J Huang, S Chen, JJ Zhang, XY Huang - Nature structural & molecular …, 2013 - nature.com
G protein–coupled receptors (GPCRs) mediate transmembrane signaling. Before ligand
binding, GPCRs exist in a basal state. Crystal structures of several GPCRs bound with …

Apo-ghrelin receptor forms heteromers with DRD2 in hypothalamic neurons and is essential for anorexigenic effects of DRD2 agonism

A Kern, R Albarran-Zeckler, HE Walsh, RG Smith - Neuron, 2012 - cell.com
We identified subsets of neurons in the brain that coexpress the dopamine receptor subtype-
2 (DRD2) and the ghrelin receptor (GHSR1a). Combination of FRET confocal microscopy …

[HTML][HTML] The endocannabinoid system as a target in cancer diseases: are we there yet?

E Moreno, M Cavic, A Krivokuca, V Casadó… - Frontiers in …, 2019 - frontiersin.org
The endocannabinoid system (ECS) has been placed in the anti-cancer spotlight in the last
decade. The immense data load published on its dual role in both tumorigenesis and …