Update on Hsp90 inhibitors in clinical trial.
Update on Hsp90 inhibitors in clinical trial.
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DOI：
10.2174/156802609789895728
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发表时间：
2009
影响因子：
3.4
通讯作者：
Trepel JB
中科院分区：
文献类型：
--
作者：
Kim YS;Alarcon SV;Lee S;Lee MJ;Giaccone G;Neckers L;Trepel JB
25年前，第一批小分子Hsp90抑制剂被发现。在这中间的几年里，在对Hsp90伴侣机制的基本科学理解和Hsp90在恶性肿瘤中的作用方面取得了戏剧性的进展。首屈一指的Hsp90抑制剂17-AAG于1999年进入I期临床试验。目前有13种Hsp90抑制剂在临床试验中，代表多个药物类别，数百名患者已在成人肿瘤学和儿童肿瘤学试验中接受治疗。这篇综述将提供到目前为止临床试验结果的概述。此外，还将讨论Hsp90抑制剂作为抗癌药物进一步开发的关键问题。
Twenty-five years ago the first small molecule inhibitors of Hsp90 were identified. In the intervening years there has been dramatic progress in basic scientific understanding of the Hsp90 chaperone machinery and in the role of Hsp90 in malignancy. The first-in-class Hsp90 inhibitor 17-AAG entered into Phase I clinical trials in 1999. There are now 13 Hsp90 inhibitors in clinical trial, representing multiple drug classes, and hundreds of patients have been treated in adult oncology and pediatric oncology trials. This review will provide an overview of the clinical trial results thus far. In addition, pivotal issues in further development of Hsp90 inhibitors as anticancer drugs will be discussed.