Re-Evaluating the Mechanism of Action of α,β-Unsaturated Carbonyl DUB Inhibitors b-AP15 and VLX1570: A Paradigmatic Example of Unspecific Protein Cross-linking with Michael Acceptor Motif-Containing Drugs

[Image: see text] Deubiquitinating enzymes (DUBs) are a growing target class across multiple disease states, with several inhibitors now reported. b-AP15 and VLX1570 are two structurally related USP14/UCH-37 inhibitors. Through a proteomic approach, we demonstrate that these compounds target a diver...

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Detalles Bibliográficos
Autores principales: Ward, Jennifer A., Pinto-Fernandez, Adan, Cornelissen, Loïc, Bonham, Sarah, Díaz-Sáez, Laura, Riant, Olivier, Huber, Kilian V. M., Kessler, Benedikt M., Feron, Olivier, Tate, Edward W.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2020
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7152998/
https://www.ncbi.nlm.nih.gov/pubmed/32109059
http://dx.doi.org/10.1021/acs.jmedchem.0c00144

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