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Mini-Review Article

新HSP90抑制剂的发现进展:2014年更新

卷 21, 期 3, 2020

页: [302 - 317] 页: 16

弟呕挨: 10.2174/1389450120666190829162544

价格: $65

摘要

HSP90是热休克蛋白家族中的一员，负责将蛋白折叠成成熟的构象，从而维持其在细胞中的生物学功能。由于HSP90涉及癌症的所有特征，它被认为是一种有希望的癌症治疗药物靶点。18种HSP90抑制剂已经进入临床试验，但是没有一种被FDA批准。HSP90抑制剂具有较强的抗癌活性和良好的安全性，仍有很大的需求。在过去的几年里，许多新的分子被鉴定为HSP90抑制剂，其中一些在临床前评估中显示了有希望的药理概况。本文综述了2014年至今发现的HSP90抑制剂，并对其设计策略、化学结构和生物活性进行了综述。这些抑制剂根据其不同的靶区和选择性分为n端、c端和亚型选择性HSP90抑制剂。

关键词: HSP90，抗癌，药物设计，HSP90抑制剂，HSP90β，GRP94，先导物优化。

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图形摘要

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