Article
A common pharmacophore for epothilone and taxanes: molecular basis for drug resistance conferred by tubulin mutations in human cancer cells.
Proceedings of the National Academy of Sciences of the United States of America - 14 Mar 2000
Giannakakou P, Gussio R, Nogales E, Downing K H, Zaharevitz D, Bollbuck B, Poy G, Sackett D, Nicolaou K C, Fojo T
Abstract excerpt
The epothilones are naturally occurring antimitotic drugs that share with the taxanes a similar mechanism of action without apparent structural similarity. Although photoaffinity labeling and electron crystallographic studies have identified the taxane-binding site on beta-tubulin, similar data are not available for epothilones. To identify tubulin residues important for epothilone binding, we have isolated two...
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