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
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.