mechanism-based SAE E1 ligase inhibitor

first-in-class, Ph. II (IV) for adv. solid tumors

from phenotypic screen and scaffold hop

J. Med. Chem., Feb. 25, 2021

Millenium/Takeda, Cambridge, MA

Chemical structure of molecule TAK-981 Subasumstat

5. The Millenium/Takeda SUMO-activating enzyme (SAE) inhibitor TAK-981 is a mechanism-based inhibitor that covalently forms a SUMO substrate-inhibitor adduct that potently inhibits SAE, rather than reacting with SAE directly.…

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