Relationship between the structures of taxane derivatives and their microtubule polymerization activity. Hidaka, M., Koga, T., Kiyota, H., Horiguchi, T., Shi, Q., Hirose, K., & Uchida, T. Bioscience, Biotechnology and Biochemistry, 2012. abstract bibtex Paclitaxel (Taxol), one of the most potent anticancer drugs, is a microtubule-stabilizing compound that inhibits microtubule depolymerization within the cell. The structure of paclitaxel is composed of two key elements, a taxane ring and an N-benzoylphenylisoserine side chain at C-13. A number of natural and artificial compounds with taxane skeletons have been isolated, but almost none of their bioactivities have been evaluated. In this study, we focused on compounds having a taxane skeleton structure and examined their effects on tubulin dynamics. Although none of these compounds had an N-benzoylphenylisoserine side chain, three were found to promote tubulin assembly. On the other hand, one compound inhibited tubluin assembly in a way similar to nocodazole. These compounds exhibited novel structureactivity relationships of taxane compounds. © 2012 W. S. Maney & Son Ltd.
@article{
title = {Relationship between the structures of taxane derivatives and their microtubule polymerization activity},
type = {article},
year = {2012},
identifiers = {[object Object]},
keywords = {Cryo-electron microscopy (cryo-EM),Microtubule,Paclitaxel,Polymerization,Taxane},
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created = {2018-02-28T22:42:48.387Z},
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abstract = {Paclitaxel (Taxol), one of the most potent anticancer drugs, is a microtubule-stabilizing compound that inhibits microtubule depolymerization within the cell. The structure of paclitaxel is composed of two key elements, a taxane ring and an N-benzoylphenylisoserine side chain at C-13. A number of natural and artificial compounds with taxane skeletons have been isolated, but almost none of their bioactivities have been evaluated. In this study, we focused on compounds having a taxane skeleton structure and examined their effects on tubulin dynamics. Although none of these compounds had an N-benzoylphenylisoserine side chain, three were found to promote tubulin assembly. On the other hand, one compound inhibited tubluin assembly in a way similar to nocodazole. These compounds exhibited novel structureactivity relationships of taxane compounds. © 2012 W. S. Maney & Son Ltd.},
bibtype = {article},
author = {Hidaka, M. and Koga, T. and Kiyota, H. and Horiguchi, T. and Shi, Q.-W. and Hirose, K. and Uchida, T.},
journal = {Bioscience, Biotechnology and Biochemistry},
number = {2}
}
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