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Sep. 18, 2021

Compound 37: An Inhibitor of the ATG7 E1 Ligase

"compound 37"

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

Drug Hunter Team

“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, Ubl, to form a Ubl-inhibitor adduct which non-covalently inhibits ATG7. This mechanism has been employed by Takeda successfully in the [...]



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