Progress in Anticancer Drug Development Targeting Ubiquitination-Related Factors.

Progress in Anticancer Drug Development Targeting Ubiquitination-Related Factors.
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针对泛素化相关因子的抗癌药物开发进展。

DOI:
10.3390/ijms232315104
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发表时间:
2022-12-01
影响因子:
5.6
通讯作者:
--
中科院分区:
生物学2区
文献类型:
--
作者:

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泛素化通过监测蛋白质稳定性、亚细胞定位和活性,广泛参与关键信号通路。这一过程的失调会导致包括恶性癌症在内的严重疾病。开发靶向泛素化相关因子的药物是实现人类疾病更好治疗的研究热点。泛素化由Ub活化酶E1、Ub偶联酶E2和Ub连接酶E3介导的三个连续反应组成。正如预期的那样,多种泛素化酶因其在肿瘤发生和癌症进展中的主导作用而成为抗癌药物开发的靶点。本文综述了近年来针对酶机制成分的抗癌药物的研究进展。
Ubiquitination is extensively involved in critical signaling pathways through monitoring protein stability, subcellular localization, and activity. Dysregulation of this process results in severe diseases including malignant cancers. To develop drugs targeting ubiquitination-related factors is a hotspot in research to realize better therapy of human diseases. Ubiquitination comprises three successive reactions mediated by Ub-activating enzyme E1, Ub-conjugating enzyme E2, and Ub ligase E3. As expected, multiple ubiquitination enzymes have been highlighted as targets for anticancer drug development due to their dominant effect on tumorigenesis and cancer progression. In this review, we discuss recent progresses in anticancer drug development targeting enzymatic machinery components.
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