Isolation, Crystal and Solution Structure Determination, and Biosynthesis of Tubulysins—Powerful Inhibitors of Tubulin Polymerization from Myxobacteria

Heinrich Steinmetz(Gesellschaft zur Förderung von Medizin-, Bio- und Umwelttechnologien), Nicole Glaser(Helmholtz Centre for Infection Research), Eberhardt Herdtweck(Technical University of Munich), Florenz Sasse(Gesellschaft zur Förderung von Medizin-, Bio- und Umwelttechnologien), Hans Reichenbach(Helmholtz Centre for Infection Research), Gerhard Höfle(Gesellschaft zur Förderung von Medizin-, Bio- und Umwelttechnologien)
Angewandte Chemie International Edition
September 16, 2004
Cited by 162

Abstract

Myxobacteria have it both ways: Whereas the epothilones stabilize the tubulin cytoskeleton and build microtubuli, tubulysins, which have now been isolated from Archangium gephyra and Angiococcus disciformis, have exactly the opposite effect. They induce the disintegration of the microtubuli, and even picomolar concentrations can cause cell death by apoptosis. Their effect on cell cultures exceeds that of the most active epothilones by 50-fold. Supporting information for this article is available on the WWW under http://www.wiley-vch.de/contents/jc_2002/2004/z460147_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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