The natural diterpene tonantzitlolone A and its synthetic enantiomer inhibit cell proliferation and kinesin-5 function
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- 作者：Tobias J. Pfeffera ; 1 ; Florenz Sasseb ; Christoph F. Schmidtc ; Stefan Lakä ; mperc ; 2 ; Andreas Kirschningd ; Tim Scholza ; scholz.tim@mh-hannover.de" class="auth_mail" title="E-mail the corresponding author
- 关键词：Inhibitor ; Cytostatic ; Diterpene ; Kinesin spindle protein ; Monoaster ; Cancer
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：13 April 2016
- 年：2016
- 卷：112
- 期：Complete
- 页码：164-170
- 全文大小：1330 K
文摘
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The natural compound tonantzitlolone A shows cytostatic activity on tumor cells.
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In dividing cells, tonantzitlolone A induces monoastral half-spindle formation suggesting kinesin-5 inhibition.
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The impact of tonantzitlolone A's synthetic enantiomer on cell proliferation is enhanced.
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Both enantiomers inhibit kinesin-5 function in single-molecule motility assays, the synthetic enantiomer even stronger.
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Both enantiomers are no general kinesin inhibitors as they do not affect neuronal kinesin-1 function.