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A Fragment-Based Method to Discover Irreversible Covalent Inhibitors of Cysteine Proteases

[Image: see text] A novel fragment-based drug discovery approach is reported which irreversibly tethers drug-like fragments to catalytic cysteines. We attached an electrophile to 100 fragments without significant alterations in the reactivity of the electrophile. A mass spectrometry assay discovered...

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Detalles Bibliográficos
Autores principales:	Kathman, Stefan G., Xu, Ziyang, Statsyuk, Alexander V.
Formato:	Online Artículo Texto
Lenguaje:	English
Publicado:	American Chemical Society 2014
Acceso en línea:	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4113264/ https://www.ncbi.nlm.nih.gov/pubmed/24870364 http://dx.doi.org/10.1021/jm500345q

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