Conformational basis of G protein-coupled receptor signaling versatility

LM Wingler, RJ Lefkowitz - Trends in cell biology, 2020 - cell.com
G protein-coupled receptors (GPCRs) are privileged structural scaffolds in biology that have
the versatility to regulate diverse physiological processes. Interestingly, many GPCR ligands …

[PDF][PDF] Imaging neurotransmitter and neuromodulator dynamics in vivo with genetically encoded indicators

BL Sabatini, L Tian - Neuron, 2020 - cell.com
The actions of neuromodulation are thought to mediate the ability of the mammalian brain to
dynamically adjust its functional state in response to changes in the environment. Altered …

Structure-based discovery of nonopioid analgesics acting through the α2A-adrenergic receptor

EA Fink, J Xu, H Hübner, JM Braz, P Seemann, C Avet… - Science, 2022 - science.org
Because nonopioid analgesics are much sought after, we computationally docked more
than 301 million virtual molecules against a validated pain target, the α2A-adrenergic …

Common activation mechanism of class A GPCRs

Q Zhou, D Yang, M Wu, Y Guo, W Guo, L Zhong, X Cai… - Elife, 2019 - elifesciences.org
Class A G-protein-coupled receptors (GPCRs) influence virtually every aspect of human
physiology. Understanding receptor activation mechanism is critical for discovering novel …

[PDF][PDF] A cardiovascular disease-linked gut microbial metabolite acts via adrenergic receptors

I Nemet, PP Saha, N Gupta, W Zhu, KA Romano… - Cell, 2020 - cell.com
Summary Using untargeted metabolomics (n= 1,162 subjects), the plasma metabolite (m/z=
265.1188) phenylacetylglutamine (PAGln) was discovered and then shown in an …

[PDF][PDF] Structural insights into the human D1 and D2 dopamine receptor signaling complexes

Y Zhuang, P Xu, C Mao, L Wang, B Krumm, XE Zhou… - Cell, 2021 - cell.com
Summary The D1-and D2-dopamine receptors (D1R and D2R), which signal through G s
and G i, respectively, represent the principal stimulatory and inhibitory dopamine receptors …

Molecular basis of β-arrestin coupling to formoterol-bound β1-adrenoceptor

Y Lee, T Warne, R Nehmé, S Pandey… - Nature, 2020 - nature.com
Abstract The β1-adrenoceptor (β1AR) is a G-protein-coupled receptor (GPCR) that couples
to the heterotrimeric G protein Gs. G-protein-mediated signalling is terminated by …

[HTML][HTML] Structural basis of α1A-adrenergic receptor activation and recognition by an extracellular nanobody

Y Toyoda, A Zhu, F Kong, S Shan, J Zhao… - Nature …, 2023 - nature.com
The α1A-adrenergic receptor (α1AAR) belongs to the family of G protein-coupled receptors
that respond to adrenaline and noradrenaline. α1AAR is involved in smooth muscle …

Ligand binding at the protein–lipid interface: strategic considerations for drug design

J Payandeh, M Volgraf - Nature Reviews Drug Discovery, 2021 - nature.com
Many drug targets are embedded within the phospholipid bilayer of cellular membranes,
including G protein-coupled receptors, ion channels, transporters and membrane-bound …

[PDF][PDF] Ligand recognition and allosteric regulation of DRD1-Gs signaling complexes

P Xiao, W Yan, L Gou, YN Zhong, L Kong, C Wu… - Cell, 2021 - cell.com
Dopamine receptors, including D1-and D2-like receptors, are important therapeutic targets
in a variety of neurological syndromes, as well as cardiovascular and kidney diseases. Here …