Chemical biology
High-throughput ABPP of DUB inhibitors in lysates
Open access · cc by · source: Europe PMC
A ubiquitin-propargylamine activity probe plus MS screens how selective DUB inhibitors are in a cellular protein matrix.
Key findings
Without fractionation ~30–40 DUBs are quantified; with fractionation they previously reached 74 DUBs in MCF-7 (similar to 78 transcripts). The HT format maps concentration dependence and selectivity of several inhibitors across cell types.
Methodology
Authors labeled MCF-7/SH-SY5Y (and mouse tissue) lysates with HA-Ub-PA, immunopurified adducts, and quantified DUBs by MS with or without inhibitors (including USP30 compounds), using short incubations so the covalent probe does not outcompete tight inhibitors.
Limitations
This is lysate ABPP, not proof of in vivo efficacy or safety; probe occupancy is a surrogate for inhibition and can displace some inhibitors if incubation is too long.
How this study connects
Role on claims
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A ubiquitin-propargylamine activity probe plus MS screens how selective DUB inhibitors are in a cellular protein matrix.
Evidence for the claim as stated.
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