Molecular signatures of G-protein-coupled receptors

AJ Venkatakrishnan, X Deupi, G Lebon, CG Tate… - Nature, 2013 - nature.com
G-protein-coupled receptors (GPCRs) are physiologically important membrane proteins that
sense signalling molecules such as hormones and neurotransmitters, and are the targets of …

Biased signaling of G protein coupled receptors (GPCRs): Molecular determinants of GPCR/transducer selectivity and therapeutic potential

M Seyedabadi, MH Ghahremani, PR Albert - Pharmacology & therapeutics, 2019 - Elsevier
G protein coupled receptors (GPCRs) convey signals across membranes via interaction with
G proteins. Originally, an individual GPCR was thought to signal through one G protein …

Structure of the µ-opioid receptor–Gi protein complex

A Koehl, H Hu, S Maeda, Y Zhang, Q Qu, JM Paggi… - Nature, 2018 - nature.com
The μ-opioid receptor (μOR) is a G-protein-coupled receptor (GPCR) and the target of most
clinically and recreationally used opioids. The induced positive effects of analgesia and …

Structures of the M1 and M2 muscarinic acetylcholine receptor/G-protein complexes

S Maeda, Q Qu, MJ Robertson, G Skiniotis, BK Kobilka - Science, 2019 - science.org
Muscarinic acetylcholine receptors are G protein–coupled receptors that respond to
acetylcholine and play important signaling roles in the nervous system. There are five …

Single-molecule analysis of ligand efficacy in β2AR–G-protein activation

GG Gregorio, M Masureel, D Hilger, DS Terry, M Juette… - Nature, 2017 - nature.com
G-protein-coupled receptor (GPCR)-mediated signal transduction is central to human
physiology and disease intervention, yet the molecular mechanisms responsible for ligand …

Single-molecule imaging reveals receptor–G protein interactions at cell surface hot spots

T Sungkaworn, ML Jobin, K Burnecki, A Weron… - Nature, 2017 - nature.com
G-protein-coupled receptors mediate the biological effects of many hormones and
neurotransmitters and are important pharmacological targets. They transmit their signals to …

The mechanism for ligand activation of the GPCR–G protein complex

A Mafi, SK Kim, WA Goddard III - Proceedings of the National Academy of …, 2022 - pnas.org
G protein–coupled receptors (GPCRs) activate cellular responses ranging from odorants to
neurotransmitters. Binding an agonist leads to activation of a heterotrimeric G protein (GP) …

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 …

Allosteric regulation of G-protein-coupled receptors: from diversity of molecular mechanisms to multiple allosteric sites and their ligands

AO Shpakov - International Journal of Molecular Sciences, 2023 - mdpi.com
Allosteric regulation is critical for the functioning of G protein-coupled receptors (GPCRs)
and their signaling pathways. Endogenous allosteric regulators of GPCRs are simple ions …