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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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| Asıl Yazarlar: | , , |
|---|---|
| Materyal Türü: | Artigo |
| Dil: | Inglês |
| Baskı/Yayın Bilgisi: |
American Chemical
Society
2014
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| Online Erişim: | https://ncbi.nlm.nih.gov/pmc/articles/PMC4113264/ https://ncbi.nlm.nih.gov/pubmed/24870364 https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/jm500345q |
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