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Epothilones: From Discovery to Clinical Trials

[ Vol. 14 , Issue. 20 ]

Author(s):

Stefano Forli   Pages 2312 - 2321 ( 10 )

Abstract:


Epothilones are natural compounds isolated from a myxobacterium at the beginning of the 1990s, and showed a remarkable anti-neoplastic activity. They act through the same mechanism of action of paclitaxel, by stabilizing microtubules and inducing apoptosis. Although, their chemical structure, simpler than taxanes, makes them more suitable for derivatization. Their interesting pharmacokinetic and bioavailabilty profiles, and the activity against paclitaxel-resistant cell lines make them interesting therapeutic agents. Here a brief historical perspective of epothilones is presented, since their isolation, the identification of their mechanism of action and activity, to the recent clinical trials.

Keywords:

Cancer, Drug design, MDR, Microtubules MSAA, Pharmacophore, SAR, Tubulin.

Affiliation:

Molecular Graphics Laboratory, Dept. of Integrative Structural and Computational Biology, MB-112F The Scripps Research Institute, 10550 North Torrey Pines Road La Jolla, CA 92037-1000, USA.

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