4.8 Article

A small-molecule SUMOylation inhibitor activates antitumor immune responses and potentiates immune therapies in preclinical models

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Summary: SUMOylation is a reversible post-translational modification that involves a cascaded enzymatic process and ATP-dependent activation, regulating protein function by attaching SUMO proteins covalently. TAK-981 is a mechanism-based inhibitor of SAE, optimized for selectivity against related enzymes and prolonged mean residence time of the inhibitory adduct, leading to potent cellular pathway inhibition and ultimately high efficacy in preclinical tumor models, resulting in the identification of the clinical molecule TAK-981.

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