Antitumor activity of a new HDAC inhibitor RF001 that enters the cell by macropinocytosis

来源 :2015医学前沿论坛暨第十四届全国肿瘤药理与化疗学术会议 | 被引量 : 0次 | 上传用户:dolan525
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  Recent studies demonstrate that macropinocytosis is selectively upregulated by cancer cells, especially those cells with k-ras mutation.In addition, overexpressed histone deacetylase (HDAC) activity has been linked with tumor initiation and progression.The novel compound RFOO1 is a trans-cinnamic acid (tCA) synthetic derivative.The present study is set to evaluate the antitumor activity of RF001 both in vitro and in vivo as well as its mechanism of action.As shown, RF001 entered human colon cancer cells (HT29 cells)intensively through macropinocytosis and the uptake of RF001 was significantly much higher than that of tCA.The IC50 value of RF001 for HT29 cell was 121.6 ± 9.6 μM which was significantly stronger than tCA.
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