Exploring a New Frontier in Cancer Treatment: Targeting the Ubiquitin and Ubiquitin-like Activating Enzymes
Exploring a New Frontier in Cancer Treatment: Targeting the Ubiquitin and Ubiquitin-like Activating Enzymes
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DOI：
10.1021/jm301420b
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发表时间：
2013-03-28
影响因子：
7.3
通讯作者：
Gunning, Patrick T.
中科院分区：
文献类型：
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作者：
da Silva, Sara R.;Paiva, Stacey-Lynn;Gunning, Patrick T.
用小泛素（Ub）和泛素样（Ubl）修饰剂标记蛋白质可以调节细胞内的大量活动，如蛋白质循环、细胞周期修饰和蛋白质易位。这些过程通常在病变细胞中过度活跃，导致不受调节的细胞生长和疾病进展。因此，在Ub/Ubl蛋白标记失调的系统中，选择性和有效破坏Ub/Ubl蛋白标记的药物的开发提供了一种靶向分子方法来致敏这些患病细胞。本展望概述了针对Ub/Ubl通路的抑制剂开发的进展。
The labeling of proteins with small ubiquitin (Ub) and ubiquitin-like (Ubl) modifiers regulates a plethora of activities within the cell, such as protein recycling, cell cycle modifications, and protein translocation. These processes are often overactive in diseased cells, leading to unregulated cell growth and disease progression. Therefore, in systems where Ub/Ubl protein labeling is dysregulated, the development of drugs to selectively and potently disrupt Ub/Ubl protein labeling offers a targeted molecular approach for sensitizing these diseased cells. This Perspective outlines the progress that has been made in the context of inhibitor development for targeting Ub/Ubl pathways.