[HTML][HTML] Mechanistic insights into allosteric regulation of the A2A adenosine G protein-coupled receptor by physiological cations
Cations play key roles in regulating G-protein-coupled receptors (GPCRs), although their
mechanisms are poorly understood. Here, 19F NMR is used to delineate the effects of …
mechanisms are poorly understood. Here, 19F NMR is used to delineate the effects of …
[HTML][HTML] The role of a sodium ion binding site in the allosteric modulation of the A2A adenosine G protein-coupled receptor
The function of G protein-coupled receptors (GPCRs) can be modulated by a number of
endogenous allosteric molecules. In this study, we used molecular dynamics, radioligand …
endogenous allosteric molecules. In this study, we used molecular dynamics, radioligand …
[HTML][HTML] Delineating the conformational landscape of the adenosine A2A receptor during G protein coupling
G-protein-coupled receptors (GPCRs) represent a ubiquitous membrane protein family and
are important drug targets. Their diverse signaling pathways are driven by complex …
are important drug targets. Their diverse signaling pathways are driven by complex …
[HTML][HTML] Allosteric coupling of drug binding and intracellular signaling in the A2A adenosine receptor
Signaling across cellular membranes, the 826 human G protein-coupled receptors (GPCRs)
govern a wide range of vital physiological processes, making GPCRs prominent drug …
govern a wide range of vital physiological processes, making GPCRs prominent drug …
[HTML][HTML] Single-molecule visualization of human A2A adenosine receptor activation by a G protein and constitutively activating mutations
Mutations that constitutively activate G protein-coupled receptors (GPCRs), known as
constitutively activating mutations (CAMs), modify cell signaling and interfere with drugs …
constitutively activating mutations (CAMs), modify cell signaling and interfere with drugs …
[HTML][HTML] Intermediate-state-trapped mutants pinpoint G protein-coupled receptor conformational allostery
X Wang, C Neale, SK Kim, WA Goddard… - Nature Communications, 2023 - nature.com
Understanding the roles of intermediate states in signaling is pivotal to unraveling the
activation processes of G protein-coupled receptors (GPCRs). However, the field is still …
activation processes of G protein-coupled receptors (GPCRs). However, the field is still …
Allosteric interactions at adenosine A1 and A3 receptors: new insights into the role of small molecules and receptor dimerization
The purine nucleoside adenosine is present in all cells in tightly regulated concentrations. It
is released under a variety of physiological and pathophysiological conditions to facilitate …
is released under a variety of physiological and pathophysiological conditions to facilitate …
Structural basis for allosteric regulation of GPCRs by sodium ions
Pharmacological responses of G protein–coupled receptors (GPCRs) can be fine-tuned by
allosteric modulators. Structural studies of such effects have been limited due to the medium …
allosteric modulators. Structural studies of such effects have been limited due to the medium …
[HTML][HTML] Anionic phospholipids control mechanisms of GPCR-G protein recognition
G protein-coupled receptors (GPCRs) are embedded in phospholipids that strongly
influence drug-stimulated signaling. Anionic lipids are particularly important for GPCR …
influence drug-stimulated signaling. Anionic lipids are particularly important for GPCR …
The role of the second and third extracellular loops of the adenosine A1 receptor in activation and allosteric modulation
MC Peeters, LE Wisse, A Dinaj, B Vroling… - Biochemical …, 2012 - Elsevier
The adenosine A1 receptor is a member of the large membrane protein family that signals
through G proteins, the G protein-coupled receptors (GPCRs). GPCRs consist of seven …
through G proteins, the G protein-coupled receptors (GPCRs). GPCRs consist of seven …
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