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Discovery of a First-In-Class Covalent Allosteric Inhibitor of SUMO E1 Activating Enzyme.

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SUMOylation is a post-translational modification with important roles in normal physiology and whose dysregulation is associated with human diseases. In this issue of Cell Chemical Biology, Li et al. (2019) describe… Click to show full abstract

SUMOylation is a post-translational modification with important roles in normal physiology and whose dysregulation is associated with human diseases. In this issue of Cell Chemical Biology, Li et al. (2019) describe a covalent, allosteric inhibitor of the SUMO E1 enzyme and demonstrate its anti-tumor activity in preclinical models of colorectal cancer.

Keywords: covalent allosteric; allosteric inhibitor; biology; inhibitor sumo

Journal Title: Cell chemical biology
Year Published: 2019

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