About: The tubulin-bound conformation of discodermolide derived by NMR studies in solution supports a common pharmacophore model for epothilone and discodermolide     Goto   Sponge   Distinct   Permalink

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Description
  • Bound to have similarities: Although the overall shape of discodermolide bound to tubulin resembles the structure of the free ligand, the precise conformation and orientation of the lactone ring are different. A partially overlapping pharmacophore model supported by protein-mediated interligand NOE signals is proposed to explain the similar (but not fully equivalent) biological activity of discodermolide and epothilone A.
  • Bound to have similarities: Although the overall shape of discodermolide bound to tubulin resembles the structure of the free ligand, the precise conformation and orientation of the lactone ring are different. A partially overlapping pharmacophore model supported by protein-mediated interligand NOE signals is proposed to explain the similar (but not fully equivalent) biological activity of discodermolide and epothilone A. (en)
Title
  • The tubulin-bound conformation of discodermolide derived by NMR studies in solution supports a common pharmacophore model for epothilone and discodermolide
  • The tubulin-bound conformation of discodermolide derived by NMR studies in solution supports a common pharmacophore model for epothilone and discodermolide (en)
skos:prefLabel
  • The tubulin-bound conformation of discodermolide derived by NMR studies in solution supports a common pharmacophore model for epothilone and discodermolide
  • The tubulin-bound conformation of discodermolide derived by NMR studies in solution supports a common pharmacophore model for epothilone and discodermolide (en)
skos:notation
  • RIV/00216224:14310/06:00032342!RIV10-MSM-14310___
http://linked.open...avai/riv/aktivita
http://linked.open...avai/riv/aktivity
  • V
http://linked.open...iv/cisloPeriodika
  • 44
http://linked.open...vai/riv/dodaniDat
http://linked.open...aciTvurceVysledku
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http://linked.open...dnocenehoVysledku
  • 504522
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  • RIV/00216224:14310/06:00032342
http://linked.open...riv/jazykVysledku
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  • conformation analysis; discodermolide; NMR spectroscopy; structure-activity relationships; tubulin (en)
http://linked.open.../riv/klicoveSlovo
http://linked.open...odStatuVydavatele
  • DE - Spolková republika Německo
http://linked.open...ontrolniKodProRIV
  • [FA9EA57533FF]
http://linked.open...i/riv/nazevZdroje
  • Angewandte Chemie International Edition
http://linked.open...in/vavai/riv/obor
http://linked.open...ichTvurcuVysledku
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http://linked.open...UplatneniVysledku
http://linked.open...v/svazekPeriodika
  • 45
http://linked.open...iv/tvurceVysledku
  • Kubíček, Karel
  • Carlomagno, Teresa
  • Lyothier, Isabelle
  • Meiler, Jens
  • Paterson, Ian
  • Sanchez-Pedregal, Victor M
issn
  • 1433-7851
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  • 14310
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