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

“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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