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 …
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 …
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
Because nonopioid analgesics are much sought after, we computationally docked more
than 301 million virtual molecules against a validated pain target, the α2A-adrenergic …
than 301 million virtual molecules against a validated pain target, the α2A-adrenergic …
Common activation mechanism of class A GPCRs
Class A G-protein-coupled receptors (GPCRs) influence virtually every aspect of human
physiology. Understanding receptor activation mechanism is critical for discovering novel …
physiology. Understanding receptor activation mechanism is critical for discovering novel …
[PDF][PDF] A cardiovascular disease-linked gut microbial metabolite acts via adrenergic receptors
Summary Using untargeted metabolomics (n= 1,162 subjects), the plasma metabolite (m/z=
265.1188) phenylacetylglutamine (PAGln) was discovered and then shown in an …
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
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 …
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 …
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 …
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 …
including G protein-coupled receptors, ion channels, transporters and membrane-bound …
[PDF][PDF] Ligand recognition and allosteric regulation of DRD1-Gs signaling complexes
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 …
in a variety of neurological syndromes, as well as cardiovascular and kidney diseases. Here …