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

GAT107, the (+)-enantiomer of racemic 4-(4-bromophenyl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-8-sulfonamide, is a strong positive allosteric modulator (PAM) of α7 nicotinic acetylcholine receptor (nAChR) activation by orthosteric agonists with intrinsic allosteric agonist activities. The di...

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Autors principals: Papke, Roger L., Horenstein, Nicole A., Kulkarni, Abhijit R., Stokes, Clare, Corrie, Lu W., Maeng, Cheol-Young, Thakur, Ganesh A.
Format: Artigo
Idioma:Inglês
Publicat: American Society for Biochemistry and Molecular Biology 2014
Matèries:
Molecular Biophysics
Accés en línia:https://ncbi.nlm.nih.gov/pmc/articles/PMC3924313/
https://ncbi.nlm.nih.gov/pubmed/24362025
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1074/jbc.M113.524603
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