Cover Picture The High-Resolution Solution Structure of Epothilone A Bound to Tubulin An Understanding of the StructureЦActivity Relationships for a Powerful Class of Antitumor Agents (Angew. Chem. Int. Ed. 222003)код для вставкиСкачать
Cover Picture Teresa Carlomagno,* Marcel J. J. Blommers,* Jens Meiler, Wolfgang Jahnke, Thomas Schupp, Frank Petersen, Dieter Schinzer, Karl-Heinz Altmann, and Christian Griesinger* The powerful antitumor agents, the epothilones, bind to tubulin and interfere with microtubule dynamics. Until now, no high-resolution structure for the tubulin– epothilone complex was available. NMR spectroscopy studies provide a highresolution structure of epothilone bound to tubulin and show two major conformational changes of epothilone relative to the free conformation. These results correlate well with chemical-modification data. These findings and NMR techniques are discussed in the Communications by Carlomagno and co-workers on pp. 2511 – 2517.