About: Molecular Mechanisms of Methoctramine Binding and Selectivity at Muscarinic Acetylcholine Receptors     Goto   Sponge   NotDistinct   Permalink

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  • We demonstrate that methoctramine high affinity binding to the M2 receptors involves simultaneous interaction with both the orthosteric binding site and the allosteric binding site located between the second and third extracellular loops. Lysine 523 in the third extracellular loop of the M3 receptors forms a hydrogen bond with glutamate 219 of the second extracellular loop that hinders methoctramine binding to the allosteric site at this receptor subtype and results in low affinity of M3 receptor for methoctramine
  • We demonstrate that methoctramine high affinity binding to the M2 receptors involves simultaneous interaction with both the orthosteric binding site and the allosteric binding site located between the second and third extracellular loops. Lysine 523 in the third extracellular loop of the M3 receptors forms a hydrogen bond with glutamate 219 of the second extracellular loop that hinders methoctramine binding to the allosteric site at this receptor subtype and results in low affinity of M3 receptor for methoctramine (en)
Title
  • Molecular Mechanisms of Methoctramine Binding and Selectivity at Muscarinic Acetylcholine Receptors
  • Molecular Mechanisms of Methoctramine Binding and Selectivity at Muscarinic Acetylcholine Receptors (en)
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  • Molecular Mechanisms of Methoctramine Binding and Selectivity at Muscarinic Acetylcholine Receptors
  • Molecular Mechanisms of Methoctramine Binding and Selectivity at Muscarinic Acetylcholine Receptors (en)
skos:notation
  • RIV/67985823:_____/14:00431597!RIV15-GA0-67985823
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  • I, P(GA305/09/0681), P(GAP304/12/0259), Z(AV0Z50110509)
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  • 2
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  • 30294
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  • RIV/67985823:_____/14:00431597
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  • muscarinic receptors; selectivity; methoctramine; allosteric; FRET (en)
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  • US - Spojené státy americké
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  • [7D46B1C2A7CC]
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  • Molecular Pharmacology
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  • 86
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  • Doležal, Vladimír
  • El-Fakahany, E. E.
  • Jakubík, Jan
  • Randáková, Alena
  • Zimčík, Pavel
  • Fuksová, Květoslava
http://linked.open...ain/vavai/riv/wos
  • 000339267500006
http://linked.open...n/vavai/riv/zamer
issn
  • 0026-895X
number of pages
http://bibframe.org/vocab/doi
  • 10.1124/mol.114.093310
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