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
TAK-981
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.…