Re-evaluating the mechanism of action of α,β-unsaturated carbonyl DUB inhibitors b-AP15 and VLX1570: a paradigmatic example of unspecific protein crosslinking with Michael acceptor motif-containing drugs

Deubiquitinating enzymes are a growing target class across multiple disease states, with several inhibitors now report-ed. b-AP15 and VLX1570 are two structurally related USP14/UCH-37 inhibitors. Through a proteomic approach, we demonstrate that these compounds target a diverse range of proteins, re...

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Bibliographic Details
Main Authors: Ward, JA, Pinto-Fernandez, A, Cornelissen, L, Bonham, S, Díaz-Sáez, L, Riant, O, Huber, KVM, Kessler, BM, Feron, O, Tate, EW
Format: Journal article
Language:English
Published: American Chemical Society 2020