Discovery of a Potent and Selective Covalent Inhibitor and Activity-Based Probe for the Deubiquitylating Enzyme UCHL1, with Antifibrotic Activity

[Image: see text] Ubiquitin carboxy-terminal hydrolase L1 (UCHL1) is a deubiquitylating enzyme that is proposed as a potential therapeutic target in neurodegeneration, cancer, and liver and lung fibrosis. Herein we report the discovery of the most potent and selective UCHL1 probe (IMP-1710) to date...

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Veröffentlicht in:J Am Chem Soc
Hauptverfasser: Panyain, Nattawadee, Godinat, Aurélien, Lanyon-Hogg, Thomas, Lachiondo-Ortega, Sofía, Will, Edward J., Soudy, Christelle, Mondal, Milon, Mason, Katie, Elkhalifa, Sarah, Smith, Lisa M., Harrigan, Jeanine A., Tate, Edward W.
Format: Artigo
Sprache:Inglês
Veröffentlicht: American Chemical Society 2020
Online Zugang:https://ncbi.nlm.nih.gov/pmc/articles/PMC7366380/
https://ncbi.nlm.nih.gov/pubmed/32579346
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/jacs.0c04527
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