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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

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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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