Prolonged and tunable residence time using reversible covalent kinase inhibitors

Drugs with prolonged, on-target residence time often show superior efficacy, yet general strategies for optimizing drug-target residence time are lacking. Here, we demonstrate progress toward this elusive goal by targeting a noncatalytic cysteine in Bruton's tyrosine kinase (BTK) with reversibl...

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Detalhes bibliográficos
Publicado no:Nat Chem Biol
Main Authors: Bradshaw, J. Michael, McFarland, Jesse M., Paavilainen, Ville O., Bisconte, Angelina, Tam, Danny, Phan, Vernon T., Romanov, Sergei, Finkle, David, Shu, Jin, Patel, Vaishali, Ton, Tony, Li, Xiaoyan, Loughhead, David G., Nunn, Philip A., Karr, Dane E., Gerritsen, Mary E., Funk, Jens Oliver, Owens, Timothy D., Verner, Erik, Brameld, Ken A., Hill, Ronald J., Goldstein, David M., Taunton, Jack
Formato: Artigo
Idioma:Inglês
Publicado em: 2015
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Article
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC4472506/
https://ncbi.nlm.nih.gov/pubmed/26006010
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1038/nchembio.1817
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