Structural Basis of the Activity of the Microtubule-Stabilizing Agent Epothilone A Studied by NMR Spectroscopy in Solution
| Autor: | Jens Meiler, Karel Kubíček, Víctor M. Sánchez-Pedregal, Teresa Carlomagno, Christian Griesinger, Marcel Reese, Marcel J. J. Blommers |
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| Rok vydání: | 2007 |
| Předmět: |
Models
Molecular Epothilones Magnetic Resonance Spectroscopy Stereochemistry Antineoplastic Agents macromolecular substances Epothilone Microtubules Catalysis Structure-Activity Relationship Tubulin Microtubule medicine Structure–activity relationship Magnesium Aqueous solution biology Chemistry General Medicine General Chemistry Nuclear magnetic resonance spectroscopy Solutions biology.protein Pharmacophore medicine.drug |
| Zdroj: | Angewandte Chemie International Edition. 46:1864-1868 |
| ISSN: | 1521-3773 1433-7851 |
| Popis: | Fits in a pocket: The binding mode of epothilone A (EpoA) to tubulin 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. |
| Databáze: | OpenAIRE |
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