Development of a chimeric c-Src kinase and HDAC inhibitor.
Development of a chimeric c-Src kinase and HDAC inhibitor.
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DOI:
10.1021/ml400175d
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发表时间:
2013-08-08
影响因子:
4.2
通讯作者:
Soellner, Matthew B.
中科院分区:
文献类型:
--
作者:
Ko, Kristin S.;Steffey, Michael E.;Brandvold, Kristoffer R.;Soellner, Matthew B.
On the basis of synergism observed between a selective c-Src kinase inhibitor with an HDAC inhibitor, the development of the first chimeric c-Src kinase and HDAC inhibitor is described. The optimized chimeric inhibitor is shown to be a potent c-Src and HDAC inhibitor. Chimeric inhibitor 4 is further shown to be highly efficacious in cancer cell lines and significantly more efficacious than a dual-targeting strategy using discrete c-Src and HDAC inhibitors.
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