Development and evaluation of a highly reliable assay for SUMO-specific protease inhibitors

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• 作者：Wenjuan Xie ; Zhongli Wang ; Jianchen Zhang ; Lie Wang ; Yaxue Zhao ; Huchen Zhou ; ^{hczhou@sjtu.edu.cn" class="auth_mail" title="E-mail the corresponding author}
• 关键词：SUMO ; SENP ; DeSUMOlyation ; Inhibitor ; Assay
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：1 May 2016
• 年：2016
• 卷：26
• 期：9
• 页码：2124-2128
• 全文大小：916 K

文摘

SUMOylation, as a post-translational modification of proteins, plays essential regulatory roles in a variety of pathological conditions. In the dynamic process of SUMOylation and deSUMOylation, SENPs (SUMO-specific proteases), in charge of deconjugation of SUMO (small ubiquitin-related modifier) from substrate proteins, have recently been found to be potential therapeutic targets for cancer treatment. A reliable and practical assay is much needed to accelerate the discovery of SENPs inhibitors. We established a quantitative assay based on readily available SDS–PAGE-Coomassie system using RanGAP-SUMO as the substrate, thus avoiding the use of expensive fluorescent dyes or the error-prone fluorescent reporter. Its reproducibility and reliability were also evaluated in this report.