The Tubulin-Bound Structure of the Antimitotic Drug Tubulysin

K Kubicek, SK Grimm, J Orts, F Sasse & T Carlomagno

Angewandte Chemie International Edition

Pages
4809–4812
Issue
28
Volume
49
Year
2010

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.