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SUMOylation is a post-translation modification responsible for the regulation of many nuclear processes. Dysregulation can lead to various diseases, so the discovery of the mechanisms and players behind the (de)SUMOylation cycle is crucial. Here, we describe a linear SPPS approach to obtain SUMO2/3-based activity probes and their application in assessing the activity of deSUMOylases, ultimately aiding in the identification of small molecules that target this system. These probes can be utilized in assays to characterize the activity of the SUMO machinery, providing insights into its regulation and potential therapeutics.

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Synthesis and Application of SUMO-Based Probes for SUMO Protease Profiling

  • 实验方案

  • 发表日期：

    2025年

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  • Matthew D. Maletic,
  • Monique P. C. Mulder

摘要

SUMOylation is a post-translation modification responsible for the regulation of many nuclear processes. Dysregulation can lead to various diseases, so the discovery of the mechanisms and players behind the (de)SUMOylation cycle is crucial. Here, we describe a linear SPPS approach to obtain SUMO2/3-based activity probes and their application in assessing the activity of deSUMOylases, ultimately aiding in the identification of small molecules that target this system. These probes can be utilized in assays to characterize the activity of the SUMO machinery, providing insights into its regulation and potential therapeutics.