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Titelbild: 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 (Angew. Chem. 22/2003)

✍ Scribed by Teresa Carlomagno; Marcel J. J. Blommers; Jens Meiler; Wolfgang Jahnke; Thomas Schupp; Frank Petersen; Dieter Schinzer; Karl-Heinz Altmann; Christian Griesinger

Publisher
John Wiley and Sons
Year
2003
Tongue
English
Weight
22 KB
Volume
115
Category
Article
ISSN
0044-8249

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✦ Synopsis

Leistungsstarke Tumortherapeutika der Epothilon‐Familie wirken durch Bindung an Tubulin und Beeinflussung der Microtubuli‐Entwicklung. Bisher sind keine hochaufgelösten Strukturen von Tubulin‐Epothilon‐Komplexen verfügbar, doch ließen sich NMR‐spektroskopisch zwei größere Konformationsänderungen bei Tubulin‐gebundenem Epothilon A gegenüber freiem nachweisen. Die Strukturdaten stimmen gut mit den Resultaten chemischer Derivatisierungsexperimente überein. Diese Ergebnisse und neue NMR‐Techniken schildern Carlomagno et al. in den Zuschriften auf S. 2615–2621.

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