Structural Basis of the Activity of the Microtubule-Stabilizing Agent Epothilone A Studied by NMR Spectroscopy in Solution

M Reese, VM Sánchez-Pedregal, K Kubicek, J Meiler, MJJ Blommers, C Griesinger & T Carlomagno

Angewandte Chemie International Edition

Pages
1864–1868
Issue
11
Volume
46
Year
2007

Fits in a pocket: The binding mode of epothilone A (EpoA) to tubulin (see picture; rods: C gray, H white, N blue, O red, S yellow) is determined by NMR spectroscopy in aqueous solution. The results explain the existing structure–activity relationship data for epothilones with both native and mutant tubulins, and support the existence of a common pharmacophore for EpoA and paclitaxel.