The Molecular Basis of Ubiquitin-Conjugating Enzymes (E2s) as a Potential Target for Cancer Therapy.
The Molecular Basis of Ubiquitin-Conjugating Enzymes (E2s) as a Potential Target for Cancer Therapy.
复制标题
泛素偶联酶（E2s）作为癌症治疗潜在靶点的分子基础。
DOI：
10.3390/ijms22073440
复制
发表时间：
2021-03-26
影响因子：
5.6
通讯作者：
Yang G
中科院分区：
文献类型：
--
作者：
Du X;Song H;Shen N;Hua R;Yang G
泛素结合酶（E2）是泛素-蛋白酶体途径所需的三种酶之一，通过泛素连接酶将活化的泛素连接到靶蛋白。E2决定了泛素链的连接类型，不同类型的泛素链调节底物蛋白的稳定性和活性。因此，E2参与各种生物过程的调节。近年来，E2在人类健康和疾病中的重要性特别受到重视。研究表明，E2在多种癌症中表达异常，因此它可能是一个潜在的治疗靶点。然而，E2 s作为治疗靶点的分子基础尚未系统地描述。本文从E2 s在泛素-蛋白酶体通路中的特殊地位和作用、E2 s的结构及其参与的生物学过程等方面对E2 s的研究进展进行了综述。此外，还对E2的抑制剂和microRNA进行了综述。本文不仅为开发有效药物提供了方向，也为今后进一步研究该酶奠定了基础。
Ubiquitin-conjugating enzymes (E2s) are one of the three enzymes required by the ubiquitin-proteasome pathway to connect activated ubiquitin to target proteins via ubiquitin ligases. E2s determine the connection type of the ubiquitin chains, and different types of ubiquitin chains regulate the stability and activity of substrate proteins. Thus, E2s participate in the regulation of a variety of biological processes. In recent years, the importance of E2s in human health and diseases has been particularly emphasized. Studies have shown that E2s are dysregulated in variety of cancers, thus it might be a potential therapeutic target. However, the molecular basis of E2s as a therapeutic target has not been described systematically. We reviewed this issue from the perspective of the special position and role of E2s in the ubiquitin-proteasome pathway, the structure of E2s and biological processes they are involved in. In addition, the inhibitors and microRNAs targeting E2s are also summarized. This article not only provides a direction for the development of effective drugs but also lays a foundation for further study on this enzyme in the future.
登录
查看更多内容
影响因子：
62.1
作者：
Cappadocia L;Lima CD
通讯作者：
Lima CD
影响因子：
16.6
作者：
Bellail, Anita C.;Olson, Jeffrey J.;Hao, Chunhai
通讯作者：
Hao, Chunhai
影响因子：
16
作者：
Bartke, T;Pohl, C;Jentsch, S
通讯作者：
Jentsch, S
影响因子：
4.6
作者：
Cacciola, Nunzio Antonio;Calabrese, Chiara;Pallante, Pierlorenzo
通讯作者：
Pallante, Pierlorenzo
影响因子：
4.8
作者：
Ben-Eliezer, Inbal;Pomerantz, Yael;Dekel, Nava
通讯作者：
Dekel, Nava