A common pharmacophore for epothilone and taxanes: Molecular basis for drug resistance conferred by tubulin mutations in human cancer cells

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A common pharmacophore for epothilone and taxanes: molecular basis for drug resistance conferred by tubulin mutations in human cancer cells.

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 ...

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A highly epothilone B-resistant A549 cell line with mutations in tubulin that confer drug dependence.

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ژورنال

عنوان ژورنال: Proceedings of the National Academy of Sciences

سال: 2000

ISSN: 0027-8424,1091-6490

DOI: 10.1073/pnas.040546297