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Description
Background Information:
TAK-981 is a first-in-class selective small molecule inhibitor of
SUMOylation and an immuno-oncology agent. It targets and covalently
binds to the small ubiquitin-like modifier (SUMO) protein, forming an
adduct (TAK-981-SUMO adduct). This adduct prevents the transfer of SUMO
from the SUMO-activating enzyme (SAE) to SUMO-conjugating enzyme UBC9,
thus prevents SUMO conjugation to lysine residues on target proteins and
abrogates many sumoylated protein-mediated cellular processes that play
key roles in tumor cells, including proliferation, DNA repair,
metastasis and survival. In addition, by preventing sumoylation, TAK-981
is able to increase the production of type 1 interferon (IFN), thereby
increasing type 1 IFN-mediated signaling, activating innate effector
cells and enhancing the antitumor innate immune responses.
APIM050066: TAK-981
CAS No.: 1858276-04-6.
Molecular Formula: C25H28ClN5O5S2.
Molecular Weight: 578.1.
