Rotational-Echo Double-Resonance NMR Distance Measurements for the Tubulin-Bound Paclitaxel Conformation

摘要: The important anticancer drug Taxol (paclitaxel, PTX) owes its unique activity to ability bind tubulin in a stoichiometric ratio and promote assembly into microtubules. conformation of the microtubule-bound has been focus numerous research efforts, since inability polymerized form crystals precludes structure proof by X-ray crystallography. Likewise, although α,β-tubulin dimer solved electron crystallography, 3.7 A resolution is too low permit direct determination either ligand or binding pose. In this article, we present experimental results from 2H{19F} REDOR NMR that provide confirmation paclitaxel adopts T-shaped when it bound tubulin.