The activity of GAT107, an allosteric activator and positive modulator of α7 nicotinic acetylcholine receptors (nAChR), is regulated by aromatic amino acids that span the subunit interface.
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Structurally similar allosteric modulators of α7 nicotinic acetylcholine receptors exhibit five distinct pharmacological effects.Functional Impact of 14 Single Nucleotide Polymorphisms Causing Missense Mutations of Human α7 Nicotinic Receptor.The influence of allosteric modulators and transmembrane mutations on desensitisation and activation of α7 nicotinic acetylcholine receptorsCritical Molecular Determinants of α7 Nicotinic Acetylcholine Receptor Allosteric Activation: SEPARATION OF DIRECT ALLOSTERIC ACTIVATION AND POSITIVE ALLOSTERIC MODULATION.Persistent activation of α7 nicotinic ACh receptors associated with stable induction of different desensitized states.The α7 nicotinic receptor dual allosteric agonist and positive allosteric modulator GAT107 reverses nociception in mouse models of inflammatory and neuropathic pain.An Unaltered Orthosteric Site and a Network of Long-Range Allosteric Interactions for PNU-120596 in α7 Nicotinic Acetylcholine Receptors.The interaction between alpha 7 nicotinic acetylcholine receptor and nuclear peroxisome proliferator-activated receptor-α represents a new antinociceptive signaling pathway in mice.New Insights on Neuronal Nicotinic Acetylcholine Receptors as Targets for Pain and Inflammation: A Focus on α7 nAChRs.The current agonists and positive allosteric modulators of α7 nAChR for CNS indications in clinical trials.Nicotinic acetylcholine receptors in neuropathic and inflammatory pain.Diversity of Nicotinic Acetylcholine Receptor Positive Allosteric Modulators Revealed by Mutagenesis and a Revised Structural Model.High-Throughput Screening for Positive Allosteric Modulators Identified Potential Therapeutics against Acetylcholinesterase Inhibition.
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The activity of GAT107, an allosteric activator and positive modulator of α7 nicotinic acetylcholine receptors (nAChR), is regulated by aromatic amino acids that span the subunit interface.
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article científic
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article scientifique
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articolo scientifico
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artigo científico
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bilimsel makale
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scientific article published on 20 December 2013
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vedecký článok
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vetenskaplig artikel
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videnskabelig artikel
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vědecký článek
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name
The activity of GAT107, an all ...... at span the subunit interface.
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The activity of GAT107, an all ...... at span the subunit interface.
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type
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The activity of GAT107, an all ...... at span the subunit interface.
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The activity of GAT107, an all ...... at span the subunit interface.
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prefLabel
The activity of GAT107, an all ...... at span the subunit interface.
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The activity of GAT107, an all ...... at span the subunit interface.
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P2093
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P356
P1476
The activity of GAT107, an all ...... at span the subunit interface.
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Abhijit R Kulkarni
Cheol-Young Maeng
Clare Stokes
Ganesh A Thakur
Lu W Corrie
Nicole A Horenstein
Roger L Papke
P2860
P304
P356
10.1074/JBC.M113.524603
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P577
2013-12-20T00:00:00Z