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E3泛素连接酶及其在癌症中的治疗应用:叙述性综述

E3 Ubiquitin Ligases and Their Therapeutic Applications in Cancers: Narrative Review.

作者信息

Jamal Azfar

机构信息

Department of Biology, College of Science, Al-Zulfi-, Majmaah University, Majmaah, Riyadh, Saudi Arabia.

Health and Basic Science Research Centre, Majmaah University, Majmaah, Riyadh, Saudi Arabia.

出版信息

J Pharm Bioallied Sci. 2024 Jul;16(Suppl 3):S1984-S1986. doi: 10.4103/jpbs.jpbs_134_24. Epub 2024 Jun 7.

Abstract

E3 ubiquitin ligases are a class of enzymes, essential for maintaining the equilibrium of cells by binding ubiquitin molecules to substrates to mark them for destruction. Since many cancer-related proteins, including both oncogenic and tumor-suppressive ones, are controlled by the ubiquitin-proteasome system, E3 ligases have drawn a great deal of interest as potential targets for the creation of anti-cancer drugs. This is because E3 ligases function as modules that select the substrates that are intended for degradation, giving them the ability to particularly affect proteins that are connected to cancer. Their molecular properties and the ways in which they work serve as the basis for these distinctions. Investment in the creation of bioactive substances that can target E3 ligases is essential given the crucial roles they play in cancer. These substances have the potential to be powerful cancer-fighting tools. In this review, we explore the crucial roles that E3 ligases play in the biology of cancer. We also examine the current bioactive substances that have been created to target different E3 ligases, emphasizing their potential as candidates for treating the cancers.

摘要

E3泛素连接酶是一类酶,通过将泛素分子与底物结合以标记它们进行破坏,对于维持细胞平衡至关重要。由于许多与癌症相关的蛋白质,包括致癌蛋白和肿瘤抑制蛋白,都受泛素-蛋白酶体系统调控,E3连接酶作为抗癌药物潜在靶点已引起广泛关注。这是因为E3连接酶起着选择要降解底物的模块作用,使其能够特别影响与癌症相关的蛋白质。它们的分子特性及其作用方式构成了这些差异的基础。鉴于E3连接酶在癌症中发挥的关键作用,投资研发能够靶向E3连接酶的生物活性物质至关重要。这些物质有可能成为强大的抗癌工具。在本综述中,我们探讨了E3连接酶在癌症生物学中所起的关键作用。我们还研究了目前已研发出的针对不同E3连接酶的生物活性物质,强调它们作为癌症治疗候选药物的潜力。

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