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Science. 2004 Aug 6;305(5685):866-9.

The binding mode of epothilone A on alpha,beta-tubulin by electron crystallography.

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  • 1Molecular and Systems Pharmacology, Emory University, Atlanta, GA 30322, USA.


The structure of epothilone A, bound to alpha,beta-tubulin in zinc-stabilized sheets, was determined by a combination of electron crystallography at 2.89 angstrom resolution and nuclear magnetic resonance-based conformational analysis. The complex explains both the broad-based epothilone structure-activity relationship and the known mutational resistance profile. Comparison with Taxol shows that the longstanding expectation of a common pharmacophore is not met, because each ligand exploits the tubulin-binding pocket in a unique and independent manner.

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