当前位置: X-MOL 学术ChemBioChem › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Switching Futile para-Quinone to Efficient Reactive Oxygen Species Generator: Ubiquitin-Specific Protease-2 Inhibition, Electrocatalysis, and Quantification
ChemBioChem ( IF 3.2 ) Pub Date : 2017-08-16 06:50:48 , DOI: 10.1002/cbic.201700431
Pushparathinam Gopinath 1 , Atif Mahammed 1 , Tal Eilon-Shaffer 2 , Mickal Nawatha 1 , Shimrit Ohayon 1 , Doron Shabat 2 , Zeev Gross 1 , Ashraf Brik 1
Affiliation  

The cover picture shows that bicyclic para-quinones with a distinct “N-C=O-N” pattern are able to generate reactive oxygen species (ROS) catalyzing the reduction of oxygen, although minor changes in such a skeleton drastically alter its ROS-generating ability. In their article, the authors provide a structure–activity relationship study of these para-quinones and discuss their ability to inhibit ubiquitin-specific protease 2 through ROS production. The substantiation of the mode of action of these inhibitors is supported by cyclic voltammetry and hydrogen peroxide quantification studies. The knowledge acquired in this study should serve as an important guideline for future medicinal chemistry optimization of related structures so as to select the preferred mode of action of para-quinone-based inhibitors. More information can be found in the communication by D. Shabat, Z. Gross, A. Brik, et al. (DOI: 10.1002/cbic.201700330).

中文翻译:

将无用的对苯醌转换为高效的活性氧生成器:泛素特异性蛋白酶2抑制,电催化和定量

封面图片显示,具有独特“ NC = ON”模式的双环苯醌能够生成催化氧还原的活性氧(ROS),尽管此类骨架中的微小变化会极大地改变其ROS的产生能力。在他们的文章中,作者提供了对这些段落的结构-活动关系的研究。-醌,并讨论了它们通过ROS产生抑制泛素特异性蛋白酶2的能力。循环伏安法和过氧化氢定量研究支持了这些抑制剂作用方式的证实。在这项研究中获得的知识应作为将来有关结构的药物化学优化的重要指南,以便选择基于醌的抑制剂的优选作用方式。在D. Shabat,Z. Gross,A. Brik等人的来文中可以找到更多信息。(DOI:10.1002 / cbic.201700330)。
更新日期:2017-08-16
down
wechat
bug