1,3,5-Trihydroxy-13,13-dimethyl-2H-pyran [7,6-b] xanthone directly targets heat shock protein 27 in hepatocellular carcinoma
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摘要We previously showed that the small molecule 1,3,5-trihydroxy-13,13-dimethyl-2H-pyran [7,6-b] xanthone (TDP) induces apoptosis in hepatocellular carcinoma (HCC) by suppressing Hsp27 expression, although the mechanism is not fully understood. To investigate the functional association between TDP and Hsp27 protein in HCC, recombinant Hsp27 protein was incubated with TDP at room temperature, and assayed by mass spectrum (MS) and natural electrophoresis. TDP effectively stimulated Hsp27 to form aggregates ex vitro, leading to suppression of its chaperone activity. The aggregates were degraded by the ubiquitin-proteasome (UPS) pathway. TDP directly interacted with Asp17 and Phe55 in chain C of Hsp27 on the basis of bioinformatic prediction. In conclusion, Hsp27 is a direct target of TDP in its anti-cancer activity, which provides strong support for a clinical application.
著者Fu WM, Wang WM, Wang H, Zhu X, Liang Y, Kung HF, Zhang JF
期刊名稱Cell Biology International
出版年份2014
月份2
日期1
卷號38
期次2
出版社Wiley: 12 months
頁次272 - 276
國際標準期刊號1065-6995
電子國際標準期刊號1095-8355
語言英式英語
關鍵詞1,3,5-trihydroxy-13,13-dimethyl-2H-pyran [7,6-b] xanthone; Autodock; hepatocellular carcinoma; Hsp27; interaction
Web of Science 學科類別Cell Biology; CELL BIOLOGY

上次更新時間 2020-09-07 於 01:50