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Structural Basis of the Activity of the Microtubule‐Stabilizing Agent Epothilone A Studied by NMR Spectroscopy in Solution
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Citations
25
References
2007
Year
Pharmaceutical ScienceNmr SpectroscopyQuantitative PharmacologySystem PharmacologyChemical BiologyTranslational PharmacologyMolecular PharmacologyMedicinal ChemistryMutant TubulinsStructural BasisBiophysicsBiochemistryMechanism Of ActionEpothilone ASolution Nmr SpectroscopyPharmacologyMolecular ModelingNatural SciencesRational Drug DesignMedicineDrug DiscoveryDrug Analysis
Fits in a pocket: The binding mode of epothilone A (EpoA) to tubulin (see picture; rods: C gray, H white, N blue, O red, S yellow) is determined by NMR spectroscopy in aqueous solution. The results explain the existing structure–activity relationship data for epothilones with both native and mutant tubulins, and support the existence of a common pharmacophore for EpoA and paclitaxel. Supporting information for this article is available on the WWW under http://www.wiley-vch.de/contents/jc_2002/2007/z604505_s.pdf or from the author. Please note: The publisher is not responsible for the content or functionality of any supporting information supplied by the authors. Any queries (other than missing content) should be directed to the corresponding author for the article.
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