Positive allosteric modulation of the alpha7 nicotinic acetylcholine receptor: ligand interactions with distinct binding sites and evidence for a prominent role of the M2-M3 segment.
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The chimeric gene CHRFAM7A, a partial duplication of the CHRNA7 gene, is a dominant negative regulator of α7*nAChR functionThe human CHRNA7 and CHRFAM7A genes: A review of the genetics, regulation, and functionα7 nicotinic ACh receptors as a ligand-gated source of Ca(2+) ions: the search for a Ca(2+) optimumStructural basis for cooperative interactions of substituted 2-aminopyrimidines with the acetylcholine binding proteinSimilarities between the Binding Sites of SB-206553 at Serotonin Type 2 and Alpha7 Acetylcholine Nicotinic Receptors: Rationale for Its Polypharmacological ProfilePositive modulation of the α9α10 nicotinic cholinergic receptor by ascorbic acid.ELIC-α7 Nicotinic acetylcholine receptor (α7nAChR) chimeras reveal a prominent role of the extracellular-transmembrane domain interface in allosteric modulation.Tethered agonist analogs as site-specific probes for domains of the human α7 nicotinic acetylcholine receptor that differentially regulate activation and desensitization.Function of partially duplicated human α77 nicotinic receptor subunit CHRFAM7A gene: potential implications for the cholinergic anti-inflammatory response.The antidepressant bupropion is a negative allosteric modulator of serotonin type 3A receptors.An allosteric modulator of alpha7 nicotinic receptors, N-(5-Chloro-2,4-dimethoxyphenyl)-N'-(5-methyl-3-isoxazolyl)-urea (PNU-120596), causes conformational changes in the extracellular ligand binding domain similar to those caused by acetylcholine.Positive allosteric modulators as an approach to nicotinic acetylcholine receptor-targeted therapeutics: advantages and limitations.Single-channel and structural foundations of neuronal α7 acetylcholine receptor potentiation.Molecular blueprint of allosteric binding sites in a homologue of the agonist-binding domain of the α7 nicotinic acetylcholine receptor.Desformylflustrabromine (dFBr) and [3H]dFBr-Labeled Binding Sites in a Nicotinic Acetylcholine Receptor.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 receptorsEffects of α7 positive allosteric modulators in murine inflammatory and chronic neuropathic pain models.Dissection of N,N-diethyl-N'-phenylpiperazines as α7 nicotinic receptor silent agonistsCritical Molecular Determinants of α7 Nicotinic Acetylcholine Receptor Allosteric Activation: SEPARATION OF DIRECT ALLOSTERIC ACTIVATION AND POSITIVE ALLOSTERIC MODULATION.Point-to-point ligand-receptor interactions across the subunit interface modulate the induction and stabilization of conformational states of alpha7 nAChR by benzylidene anabaseines.The Ascaris suum nicotinic receptor, ACR-16, as a drug target: Four novel negative allosteric modulators from virtual screening.Pharmacological profile of Ascaris suum ACR-16, a new homomeric nicotinic acetylcholine receptor widely distributed in Ascaris tissuesColchicine: a novel positive allosteric modulator of the human 5-hydroxytryptamine3A receptorActivation and desensitization of nicotinic alpha7-type acetylcholine receptors by benzylidene anabaseines and nicotineSelective inhibition of acetylcholine-evoked responses of alpha7 neuronal nicotinic acetylcholine receptors by novel tris- and tetrakis-azaaromatic quaternary ammonium antagonists.Reducing cannabinoid abuse and preventing relapse by enhancing endogenous brain levels of kynurenic acid.Effects of asparagine mutagenesis of conserved aspartic acids in helix 2 (D2.50) and 3 (D3.32) of M1-M4 muscarinic receptors on the irreversible binding of nitrogen mustard analogs of acetylcholine and McN-A-343.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.NMR structures of the human α7 nAChR transmembrane domain and associated anesthetic binding sites.The structural basis of function in Cys-loop receptors.Alpha7 neuronal nicotinic receptors as a drug target in schizophrenia.Understanding the Bases of Function and Modulation of α7 Nicotinic Receptors: Implications for Drug Discovery.Competitive binding at a nicotinic receptor transmembrane site of two α7-selective positive allosteric modulators with differing effects on agonist-evoked desensitization.Nicotinic acetylcholine receptors at the single-channel level.Insights into nicotinic receptor signaling in nicotine addiction: Implications for prevention and treatment.Nicotinic acetylcholine receptor transmembrane mutations convert ivermectin from a positive to a negative allosteric modulator.An Unaltered Orthosteric Site and a Network of Long-Range Allosteric Interactions for PNU-120596 in α7 Nicotinic Acetylcholine Receptors.An allosteric binding site of the α7 nicotinic acetylcholine receptor revealed in a humanized acetylcholine binding protein.Molecular function of α7 nicotinic receptors as drug targets.
P2860
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P2860
Positive allosteric modulation of the alpha7 nicotinic acetylcholine receptor: ligand interactions with distinct binding sites and evidence for a prominent role of the M2-M3 segment.
description
2008 nî lūn-bûn
@nan
2008 թուականի Օգոստոսին հրատարակուած գիտական յօդուած
@hyw
2008 թվականի օգոստոսին հրատարակված գիտական հոդված
@hy
2008年の論文
@ja
2008年学术文章
@wuu
2008年学术文章
@zh-cn
2008年学术文章
@zh-hans
2008年学术文章
@zh-my
2008年学术文章
@zh-sg
2008年學術文章
@yue
name
Positive allosteric modulation ...... ent role of the M2-M3 segment.
@ast
Positive allosteric modulation ...... ent role of the M2-M3 segment.
@en
type
label
Positive allosteric modulation ...... ent role of the M2-M3 segment.
@ast
Positive allosteric modulation ...... ent role of the M2-M3 segment.
@en
prefLabel
Positive allosteric modulation ...... ent role of the M2-M3 segment.
@ast
Positive allosteric modulation ...... ent role of the M2-M3 segment.
@en
P2093
P356
P1476
Positive allosteric modulation ...... ent role of the M2-M3 segment.
@en
P2093
Daniel Bertrand
Earl Gubbins
M Gopalakrishnan
Sonia Bertrand
Steven Cassar
P304
P356
10.1124/MOL.107.042820
P577
2008-08-04T00:00:00Z