The Tubulin-Bound Structure of the Antimitotic Drug Tubulysin
Angewandte Chemie International Edition 49, 4809–4812 (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.