molecules of the month


USP30-sel. covalent DUB enzyme inhibitor

active in cells and selective vs. DUB panel

undisclosed, related to lit. DUB inhibitors

BioRXiV, Apr. 20, 2020

FORMA Therapeutics / U. Liverpool

1 min read

FT385 is a covalent inhibitor of the USP30 deubiquitinating enzyme with a cyanopyrrolidine warhead. Identifying selective active-site inhibitors of de-ubiquitinating enzymes has been challenging, and FT385 now provides a good tool compound to study USP30 biology. Some of my colleagues at Genentech recently published on the mechanism of cyanopyrrolidine inhibition of USP7, which proceeds through an interesting de-sulfhydration reaction.

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