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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Vydáno v:Nat Chem Biol
Hlavní autoři: 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
Médium: Artigo
Jazyk:Inglês
Vydáno: 2015
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Article
On-line přístup: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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