Strategies for the identification of ubiquitin ligase inhibitors.
Strategies for the identification of ubiquitin ligase inhibitors.
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DOI：
10.1042/bst0380132
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发表时间：
2010-02
影响因子：
3.9
通讯作者：
Nicholson B
中科院分区：
文献类型：
--
作者：
Goldenberg SJ;Marblestone JG;Mattern MR;Nicholson B
泛素蛋白酶体系统 (UPS) 的失调与多种病理学有关，包括癌症、神经退行性变和病毒感染。抑制蛋白酶体已被证明是人类有效的治疗策略；然而该目标的毒性仍然很高。泛素连接酶 (E3) 是 UPS 中另一种有吸引力的治疗靶点。在这里，我们将讨论当前报告 E3 连接酶活性并可以检测 E3 抑制剂的平台，同时强调每种方法的优点和缺点。
Dysregulation of the ubiquitin-proteasome system (UPS) has been implicated in a wide range of pathologies including cancer, neurodegeneration, and viral infection. Inhibiting the proteasome has been shown to be an effective therapeutic strategy in humans; yet toxicity with this target remains high. Ubiquitin Ligases (E3s) represent an alternative attractive therapeutic target in the UPS. Here we will discuss current platforms that report on E3 ligase activity and can detect E3 inhibitors, while underlining the advantages and disadvantages of each approach.