Projektnummer

0050578

Zusammenfassung

In this project it is intended to investigate the basis of the conformational changes induced in tubulin by tubulin-binding agents. Changes in tubulin conformation interfere with the tubulin polymerization equilibrium, therefore with the cell cycle and ultimately with cell viability. Epothilones bind to tubulin in the taxane binding pocket, stabilize the microtubular form of the protein and possess strong cytotoxic activity. Despite the determination of two tubulin-bound conformations of epitholone A by NMR sprectroscopy and electron crystallography and the synthesis of more than 500 ...