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Electrophilic Fragment-Based Design of Reversible Covalent Kinase Inhibitors

Fragment-based ligand design and covalent targeting of noncatalytic cysteines have been employed to develop potent and selective kinase inhibitors. Here, we combine these approaches, starting with a panel of low-molecular weight, heteroaryl-susbstituted cyanoacrylamides, which we have previously sho...

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Detalhes bibliográficos
Main Authors: Miller, Rand M., Paavilainen, Ville O., Krishnan, Shyam, Serafimova, Iana M., Taunton, Jack
Formato: Artigo
Idioma:Inglês
Publicado em: 2013
Assuntos:
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC3665406/
https://ncbi.nlm.nih.gov/pubmed/23540679
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/ja401221b
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