...
  • 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>Current topics in medicinal chemistry >Alternate strategies of Hsp90 modulation for the treatment of cancer and other diseases
【24h】

Alternate strategies of Hsp90 modulation for the treatment of cancer and other diseases

机译：Hsp90调节的替代策略，用于治疗癌症和其他疾病

获取原文
获取原文并翻译 | 示例
           
页面导航
  • 摘要
  • 著录项
  • 相似文献
  • 相关主题

摘要

The 90 kDa heat shock protein (Hsp90) has become a validated target for the development of anti-cancer agents. Several Hsp90 inhibitors are currently under clinical trial investigation for the treatment of cancer. All of these agents inhibit Hsp90's protein folding activity by binding to the N-terminal ATP binding site of the Hsp90 molecular chaperone. Administration of these investigational drugs elicits induction of the heat shock response, or the overexpression of several Hsps, which exhibit antiapoptotic and pro-survival effects that may complicate the application of these inhibitors. To circumvent this issue, alternate mechanisms for Hsp90 inhibition that do not elicit the heat shock response have been identified and pursued. After providing background on the structure, function, and mechanism of the Hsp90 protein folding machinery, this review describes several mechanisms of Hsp90 modulation via small molecules that do not induce the heat shock response.
机译：90 kDa热激蛋白（Hsp90）已成为开发抗癌药物的有效靶标。几种Hsp90抑制剂目前正在临床试验研究中，用于治疗癌症。所有这些试剂都通过与Hsp90分子伴侣的N末端ATP结合位点结合而抑制Hsp90的蛋白质折叠活性。给予这些研究药物会引起热休克反应的诱导或几种Hsps的过度表达，这些表现出抗凋亡和促生存作用，可能会使这些抑制剂的应用复杂化。为了规避此问题，已经确定并寻求了不引起热休克反应的Hsp90抑制的替代机制。在提供有关Hsp90蛋白质折叠机制的结构，功能和机制的背景知识之后，本综述描述了通过不诱导热激反应的小分子进行Hsp90调节的几种机制。

著录项

相似文献

  • 外文文献
  • 中文文献
  • 专利
获取原文

客服邮箱：kefu@zhangqiaokeyan.com

京公网安备：11010802029741号 ICP备案号：京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有

  • 客服微信

  • 服务号