调控主调节因子：将热休克因子1作为一种化疗方法进行调控。
Regulating the master regulator: Controlling heat shock factor 1 as a chemotherapy approach.
作者信息
McConnell Jeanette R, Buckton Laura K, McAlpine Shelli R
机构信息
Department of Chemistry, University of New South Wales, Sydney, NSW 2052, Australia.
Department of Chemistry, University of New South Wales, Sydney, NSW 2052, Australia.
出版信息
Bioorg Med Chem Lett. 2015 Sep 1;25(17):3409-14. doi: 10.1016/j.bmcl.2015.06.052. Epub 2015 Jun 20.
Described is the role that heat shock factor 1 (HSF1) plays in regulating cellular stress. Focusing on the current state of the HSF1 field in chemotherapeutics we outline the cytoprotective role of HSF1 in the cell. Summarizing the mechanism by which HSF1 regulates the unfolded proteins that are generated under stress conditions provides the background on why HSF1, the master regulator, is such an important protein in cancer cell growth. Summarizing siRNA knockdown results and current inhibitors provides a comprehensive evaluation on HSF1 and its current state. One set of molecules stands out, in that they completely obliterate the levels of HSF1, while simultaneously inhibiting heat shock protein 90 (Hsp90). These molecules are extremely promising as chemotherapeutic agents and as tools that may ultimately provide the connection between Hsp90 inhibition and HSF1 protein levels.
本文描述了热休克因子1（HSF1）在调节细胞应激中所起的作用。着眼于HSF1在化疗领域的当前研究状况，我们概述了HSF1在细胞中的细胞保护作用。总结HSF1调节应激条件下产生的未折叠蛋白的机制，为HSF1（主要调节因子）为何在癌细胞生长中是如此重要的蛋白质提供了背景信息。总结小干扰RNA（siRNA）敲低结果和当前的抑制剂，对HSF1及其当前状况进行了全面评估。有一组分子脱颖而出，因为它们能完全消除HSF1的水平，同时抑制热休克蛋白90（Hsp90）。这些分子作为化疗药物以及最终可能提供Hsp90抑制与HSF1蛋白水平之间联系的工具，极具前景。
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