The Tubulin-Bound Structure of the Antimitotic Drug Tubulysin

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Authors

KUBICEK Karel GRIMM S. Kaspar ORTS Julien SASSE Florenz CARLOMAGNO Teresa

Year of publication 2010
Type Article in Periodical
Magazine / Source Angewandte Chemie International Edition
MU Faculty or unit

Faculty of Science

Citation
Web http://onlinelibrary.wiley.com/doi/10.1002/anie.200906828/abstract
Field Biophysics
Keywords conformation analysis;cytotoxicity;microtubules;NMR spectroscopy;tubulysin
Description Bound to be active: The solution structure of tubulin-bound tubulysin A is determined from transferred NOE data (see picture; blue N, red O, yellow S, green C), and this bioactive conformation is compared to the unbound conformation. The binding site on tubulin is examined on the basis of the interligand NOEs observed between epothilone A and tubulysin A in the presence of tubulin.
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