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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Библиографические подробности
Опубликовано в: :Nat Chem Biol
Главные авторы: 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
Формат: Artigo
Язык:Inglês
Опубликовано: 2015
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Article
Online-ссылка: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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