Molecular Mechanism of Action of Microtubule-Stabilizing Anticancer Agents

• DOI: 10.1126/science.1230582
• Publication Date: 2013-01-04T05:46:42Z
• Authors: Andrea E. Prota; Katja Bargsten; Didier Zurwerra; Jessica J. Field; José Fernando Díaz; Karl-Heinz Altmann; Michel O. Steinmetz
• Keywords: Bridged-Ring Compounds; 0301 basic medicine; 1000 Multidisciplinary; 0303 health sciences; Binding Sites; SX20 Research, Technology and Development Projects; Antineoplastic Agents; Crystallography, X-Ray; Microtubules; Protein Structure, Secondary; Tubulin Modulators; 3. Good health; 03 medical and health sciences; SX00 SystemsX.ch; SX25 Bridge 2 Industry Projects; Epothilones; Tubulin; 570 Life sciences; biology; Animals; Cattle; Taxoids; Macrolides; Chickens

Dissecting Microtubule Stability

Microtubule-stabilizing agents (MSAs), like taxol, inhibit cell division and are widely used in cancer chemotherapy.

Prota et al.

(p. 587 , published online 3 January) present structural data on the molecular mechanism of action of antimitotic drugs. Tubulin structures in complex with the MSAs zampanolide and epothilone A, revealed a general mechanism for how MSAs promote microtubule assembly and stability by affecting lateral tubulin interactions.