泛素连接酶抑制剂的鉴定策略。
Strategies for the identification of ubiquitin ligase inhibitors.
机构信息
Progenra Inc., 271A Great Valley Parkway, Malvern, PA 19355, USA.
出版信息
Biochem Soc Trans. 2010 Feb;38(Pt 1):132-6. doi: 10.1042/BST0380132.
Abstract
Dysregulation of the UPS (ubiquitin-proteasome system) 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; however, toxicity with this target remains high. E3s (Ub-protein ligases) represent an alternative attractive therapeutic target in the UPS. In this paper, we will discuss current platforms that report on E3 ligase activity and can detect E3 inhibitors, and underline the advantages and disadvantages of each approach.
摘要
UPS（泛素-蛋白酶体系统）的失调与多种疾病有关，包括癌症、神经退行性疾病和病毒感染。抑制蛋白酶体已被证明是人类的一种有效治疗策略；然而，该靶点的毒性仍然很高。E3s（泛素蛋白连接酶）是 UPS 中另一个有吸引力的治疗靶点。在本文中，我们将讨论目前报告 E3 连接酶活性并能检测 E3 抑制剂的平台，并强调每种方法的优缺点。
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