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Review
. 2020:35:17-34.
doi: 10.21775/cimb.035.017. Epub 2019 Aug 18.

Progress in the Discovery of Small Molecule Modulators of DeSUMOylation

Shiyao Chen  1 , Duoling Dong  1 , Weixiang Xin  1 , Huchen Zhou  1
Affiliations
Free article
Review

Progress in the Discovery of Small Molecule Modulators of DeSUMOylation

Shiyao Chen et al. Curr Issues Mol Biol. 2020.
Free article

Abstract

SUMOylation and DeSUMOylation are reversible protein post-translational modification (PTM) processes involving small ubiquitin-like modifier (SUMO) proteins. These processes have indispensable roles in various cellular processes, such as subcellular localization, gene transcription, and DNA replication and repair. Over the past decade, increasing attention has been given to SUMO-related pathways as potential therapeutic targets. The Sentrin/SUMO-specific protease (SENP), which is responsible for deSUMOylation, has been proposed as a potential therapeutic target in the treatment of cancers and cardiac disorders. Unfortunately, no SENP inhibitor has yet reached clinical trials. In this review, we focus on advances in the development of SENP inhibitors in the past decade.

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