Conformational basis of G protein-coupled receptor signaling versatility
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 …
Imaging neurotransmitter and neuromodulator dynamics in vivo with genetically encoded indicators
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 …
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 …
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 …
[HTML][HTML] 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 …
[HTML][HTML] 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 …
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 …
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 …
Pharmacology and therapeutics of bronchodilators revisited
Bronchodilators remain the cornerstone of the treatment of airway disorders such as asthma
and chronic obstructive pulmonary disease (COPD). There is therefore considerable interest …
and chronic obstructive pulmonary disease (COPD). There is therefore considerable interest …