Silent agonists for α7 nicotinic acetylcholine receptors
Pharmacological Research, 2023 We discuss models for the activation and desensitization of α7 nicotinic acetylcholine receptors (nAChRs) and the effects of efficacious type II positive allosteric modulators (PAMs) that destabilize α7 desensitized states.
Roger L. Papke +2 more
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Phosphocholine-Modified Lipooligosaccharides of Haemophilus influenzae Inhibit ATP-Induced IL-1β Release by Pulmonary Epithelial Cells [PDF]
Molecules, 2018 Phosphocholine-modified bacterial cell wall components are virulence factors enabling immune evasion and permanent colonization of the mammalian host, by mechanisms that are poorly understood.
Katrin Richter +11 more
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Conformational dynamics of a nicotinic receptor neurotransmitter site [PDF]
eLifeAgonists enhance receptor activity by providing net-favorable binding energy to active over resting conformations, with efficiency (η) linking binding energy to gating.
Mrityunjay Singh +4 more
doaj +2 more sources
Molecular insights into the α6β4 nicotinic acetylcholine receptor function and ligand recognition [PDF]
Nature CommunicationsThe α6β4 nicotinic acetylcholine receptor (nAChR) is found in the sensory neurons of dorsal root ganglia. It is a promising therapeutic target for pain.
Jiawei Su +10 more
doaj +2 more sources
New Therapeutic Approaches for the Treatment of Rheumatoid Arthritis may Rise from the Cholinergic Anti-Inflammatory Pathway and Antinociceptive Pathway [PDF]
The Scientific World Journal, 2010 Due to the complex etiology of rheumatoid arthritis (RA), it is difficult to be completely cured at the current stage although many approaches have been applied in clinics, especially the wide application of nonsteroidal anti-inflammatory drugs (NSAIDs ...
Xiao Hua Pan +5 more
doaj +2 more sources
Agonist efficiency links binding and gating in a nicotinic receptor
eLife, 2023 Receptors signal by switching between resting (C) and active (O) shapes (‘gating’) under the influence of agonists. The receptor’s maximum response depends on the difference in agonist binding energy, O minus C.
Dinesh C Indurthi, Anthony Auerbach
doaj +3 more sources
S5‐01–02: Nicotine and nicotine agonists [PDF]
Alzheimer's & Dementia, 2008 Paul Newhouse
openalex +3 more sources
eLife, 2022 Nicotinic partial agonists provide an accepted aid for smoking cessation and thus contribute to decreasing tobacco-related disease. Improved drugs constitute a continued area of study. However, there remains no reductionist method to examine the cellular
Aaron L Nichols +18 more
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Nicotinic acetylcholine receptor agonists attenuate septic acute kidney injury in mice by suppressing inflammation and proteasome activity. [PDF]
PLoS ONE, 2012 Sepsis is one of the leading causes of acute kidney injury (AKI). Septic patients who develop acute kidney injury (AKI) are at increased risk of death. To date there is no effective treatment for AKI or septic AKI.
Prodyot K Chatterjee +6 more
doaj +1 more source
Acute activation, desensitization and smoldering activation of human acetylcholine receptors. [PDF]
PLoS ONE, 2013 The behavioral effects of nicotine and other nicotinic agonists are mediated by AChRs in the brain. The relative contribution of acute activation versus chronic desensitization of AChRs is unknown. Sustained "smoldering activation" occurs over a range of
Barbara G Campling +2 more
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