The High-Resolution Solution Structure of Epothilone A Bound to Tubulin: An Understanding of the Structure-Activity Relationships for a Powerful Class of Antitumor Agents

The tubulin‐bound structure of epothilone A (shown in green) differs substantially from its free conformation (determined by X‐ray crystallography, shown in gray). The new structural data correlate well with results from chemical modification experiments, giving a consistent picture of the functiona...

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Bibliographic Details
Published in:Angewandte Chemie International Edition 2003-06, Vol.42 (22), p.2511-2515
Main Authors: Carlomagno, Teresa, Blommers, Marcel J. J., Meiler, Jens, Jahnke, Wolfgang, Schupp, Thomas, Petersen, Frank, Schinzer, Dieter, Altmann, Karl-Heinz, Griesinger, Christian
Format: Article
Language:English
Subjects:
Animals
Antineoplastic Agents - chemistry
Cattle
Epothilones - chemistry
Models, Molecular
Molecular Conformation
Molecular Structure
natural products
NMR spectroscopy
Nuclear Magnetic Resonance, Biomolecular
Solutions - chemistry
structure elucidation
Structure-Activity Relationship
structure-activity relationships
tubulin
Tubulin - chemistry
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Summary:The tubulin‐bound structure of epothilone A (shown in green) differs substantially from its free conformation (determined by X‐ray crystallography, shown in gray). The new structural data correlate well with results from chemical modification experiments, giving a consistent picture of the functionally important regions of epothilone.
ISSN:1433-7851
1521-3773
DOI:10.1002/anie.200351276