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NEDDylation 抑制活性检测方法综述。

Review of NEDDylation inhibition activity detection methods.

机构信息

School of Basic Medical Science, Zhengzhou University, Zhengzhou 450001, China; The Academy of Medical Science, Zhengzhou University, Zhengzhou 450001, China.

School of Basic Medical Science, Zhengzhou University, Zhengzhou 450001, China; School of Pharmaceutical Sciences & Collaborative Innovation Center of New Drug Research and Safety Evaluation, Zhengzhou University, Zhengzhou 450001, China.

出版信息

Bioorg Med Chem. 2021 Jan 1;29:115875. doi: 10.1016/j.bmc.2020.115875. Epub 2020 Nov 16.

Abstract

NEDDylation is a post-translational modification of a protein, which transfers Ubiquitin like protein NEDD8 (Neuronal Precursor Cell-expressed Developmentally Down-regulated Protein 8) to the lysine residue of the product through a three-stage enzymatic reaction, and widely regulates many biological processes, such as cell cycle signal transduction and immune recognition. In the past ten years, we have witnessed tremendous progress in the study of protein ubiquitination modification, from modification mechanisms to drug development. Which suggests that inhibition of NEDDylation is an effective way to inhibit tumor. A variety of biological detection methods have been developed during the development of the inhibitor. In this review, we briefly introduced the modification process and substrates of NEDDylation, and discussed detection methods of NEDDylation activity in detail. This review will provide an up-to-date and comprehensive review of the methods for detecting NEDDylation activity that will contribute to NEDDylation inhibitor development.

摘要

NEDDylation 是一种蛋白质的翻译后修饰,通过三阶段酶反应将泛素样蛋白 NEDD8(神经元前体细胞表达的发育下调蛋白 8)转移到产物的赖氨酸残基上,并广泛调节许多生物过程,如细胞周期信号转导和免疫识别。在过去的十年中,我们见证了蛋白质泛素化修饰研究的巨大进展,从修饰机制到药物开发。这表明抑制 NEDDylation 是抑制肿瘤的有效方法。在抑制剂的开发过程中,已经开发出了多种生物检测方法。在这篇综述中,我们简要介绍了 NEDDylation 的修饰过程和底物,并详细讨论了 NEDDylation 活性的检测方法。这篇综述将提供对 NEDDylation 活性检测方法的最新和全面的综述,这将有助于 NEDDylation 抑制剂的开发。

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