Active site-targeted covalent irreversible inhibitors of USP7 impair the functions of Foxp3+ T-regulatory cells by promoting ubiquitination of Tip60
Fig 1
P217564 is a second generation USP7 inhibitor with increased potency that retains selectivity.
(A) Schematic representation of Ub- EKL isopeptidase reporter assay: cleavage by the isopeptidase at the carboxy-terminal glycine of the Ub releases catalytically active EKL, which liberates a quantifiable fluorescent product in the presence of its substrate. (B) P217564 demonstrates potent and specific inhibition of USP7 versus other purified DUBs and proteases.