ATG7 E1 substrate-assisted covalent inhibitor

autophagy inhibition in vivo (150 mg/kg SC)

from focused HTS of adenosine sulfamates

Bioorg. Med. Chem., Aug. 4, 2020

Takeda, Cambridge, MA

Structure of compound 37

“compound 37” is an inhibitor of the ATG7 E1 ligase through an interesting substrate-assisted covalent mechanism. Rather than covalently modify ATG7 directly, the molecule reacts with the E1 ligase substrate,…

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