Cover Picture: Switching Futile para‐Quinone to Efficient Reactive Oxygen Species Generator: Ubiquitin‐Specific Protease‐2 Inhibition, Electrocatalysis, and Quantification (ChemBioChem 17/2017). (16th August 2017)

• Record Type: Journal Article
• Authors: Gopinath, Pushparathinam; Mahammed, Atif; Eilon‐Shaffer, Tal; Nawatha, Mickal; Ohayon, Shimrit; Shabat, Doron; Gross, Zeev; Brik, Ashraf
• Is Part Of: Chembiochem. Volume 18:Number 17(2017)
• Page Start: 1669
• Page End: 1669
• Publication Date: 2017-08-16
• Subjects: drug design -- enzymes -- heterocycles -- inhibitors -- structure–activity relationships; Biochemistry -- Periodicals; Molecular biology -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1002/cbic.201700431
• Languages: English
• ISSNs: 1439-4227

Abstract

Abstract : 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. onpage 1683 in Issue 17, 2017 (DOI:10.1002/cbic.201700330 ).