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ID: ALA3797135

Journal: Bioorg Med Chem Lett

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

Authors: Xie W, Wang Z, Zhang J, Wang L, Zhao Y, Zhou H.

Abstract: 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.

CiteXplore: 27032332

DOI: 10.1016/j.bmcl.2016.03.080