The roles of E3 ubiquitin ligases in cancer progression and targeted therapy.
The roles of E3 ubiquitin ligases in cancer progression and targeted therapy.
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E3 泛素连接酶在癌症进展和靶向治疗中的作用。
DOI：
10.1002/ctm2.1204
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发表时间：
2023-03
影响因子：
10.6
通讯作者：
中科院分区：
文献类型：
--
作者：
泛素化是最重要的翻译后修饰之一，在保持细胞蛋白的稳态中起着重要的作用。在泛素化过程中，泛素偶联到靶蛋白底物进行降解、易位或激活，其失调与包括各种类型癌症在内的几种疾病有关。E3泛素连接酶具有选择、结合和招募泛素化靶底物的能力，被认为是最具影响力的泛素酶。特别是，E3连接酶在癌症标志通路中起关键作用，它们作为肿瘤启动子或抑制子。E3连接酶的特异性以及它们在癌症标志中的含义促使了针对E3连接酶的化合物的开发，以用于癌症治疗。在这篇综述中，我们强调了E3连接酶在癌症标志中的作用，例如通过细胞周期进程持续增殖，免疫逃避和肿瘤促进炎症，以及逃避细胞凋亡。此外，我们总结了靶向E3连接酶的小化合物在癌症治疗中的应用和作用，以及靶向E3连接酶作为潜在癌症治疗的意义。E3泛素连接酶通过泛素化底物蛋白在癌症等疾病进展中的细胞过程中发挥重要作用。正因为如此，科学家们试图找到安全的、生物可利用的靶向E3连接酶的化合物。在这篇综述中，我们总结了E3连接酶在癌症相关通路中的作用，强调了小分子抑制剂的应用和临床意义，并讨论了进一步的研究方向。
Ubiquitination is one of the most important post‐translational modifications which plays a significant role in conserving the homeostasis of cellular proteins. In the ubiquitination process, ubiquitin is conjugated to target protein substrates for degradation, translocation or activation, dysregulation of which is linked to several diseases including various types of cancers. E3 ubiquitin ligases are regarded as the most influential ubiquitin enzyme owing to their ability to select, bind and recruit target substrates for ubiquitination. In particular, E3 ligases are pivotal in the cancer hallmarks pathways where they serve as tumour promoters or suppressors. The specificity of E3 ligases coupled with their implication in cancer hallmarks engendered the development of compounds that specifically target E3 ligases for cancer therapy. In this review, we highlight the role of E3 ligases in cancer hallmarks such as sustained proliferation via cell cycle progression, immune evasion and tumour promoting inflammation, and in the evasion of apoptosis. In addition, we summarise the application and the role of small compounds that target E3 ligases for cancer treatment along with the significance of targeting E3 ligases as potential cancer therapy. E3 ubiquitin ligases are important players in cellular processes by ubiquitinating substrate proteins in disease progression such as cancer. Owing to this, scientists attempt to identify safe and bioavailable compounds targeting E3 ligases. In this review, we summarise the roles of E3 ligases in cancer‐related pathways, highlight the application and clinical significance of small molecule inhibitors and discuss further directions .
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影响因子：
16.6
作者：
Alabi S;Jaime-Figueroa S;Yao Z;Gao Y;Hines J;Samarasinghe KTG;Vogt L;Rosen N;Crews CM
通讯作者：
Crews CM
致癌性CARMA1夫妇在扩散的大B细胞淋巴瘤中NF-κB和β-catenin信号传导。
影响因子：
8
作者：
Bognar MK;Vincendeau M;Erdmann T;Seeholzer T;Grau M;Linnemann JR;Ruland J;Scheel CH;Lenz P;Ott G;Lenz G;Hauck SM;Krappmann D
通讯作者：
Krappmann D
影响因子：
8
作者：
Argentini, M;Barboule, N;Wasylyk, B
通讯作者：
Wasylyk, B
影响因子：
32.4
作者：
Bertrand, Mathieu J. M.;Doiron, Karine;Saleh, Maya
通讯作者：
Saleh, Maya
影响因子：
4.8
作者：
Brenke, Jara K.;Popowicz, Grzegorz M.;Hadian, Kamyar
通讯作者：
Hadian, Kamyar