生物活性 | |||
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描述 | TAK-981 is a new small molecule inhibitor of sumoylation. Through intravenous administration, TAK-981 targets and covalently binds to the small ubiquitin-like modifier (SUMO; small ubiquitin-related modifier) protein, preventing SUMO conjugation to lysine residues on target proteins and abrogating many sumoylated protein-mediated cellular processes that play key roles in tumor cells, including proliferation, DNA repair, metastasis and survival. Through preventing sumoylation, TAK-981 is able to increase the production of type 1 IFN and thereby increases type 1 IFN-mediated signaling, activates innate effector cells and enhances the antitumor innate immune responses. This may further increase tumor cell killing. These suggest TAK-981 may have potential immune-activating and antineoplastic activities. | ||
作用机制 | TAK-981 could covalently bind to SUMO protein and form an adduct with SUMO protein, which prevents the transfer of SUMO from the SUMO-activating enzyme (SAE) to SUMO-conjugating enzyme UBC9.[1] |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.73mL 0.35mL 0.17mL |
8.65mL 1.73mL 0.86mL |
17.30mL 3.46mL 1.73mL |
参考文献 |
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