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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Detalles Bibliográficos
Autores principales: 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: Online Artículo Texto
Lenguaje:English
Publicado: 2015
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4472506/
https://www.ncbi.nlm.nih.gov/pubmed/26006010
http://dx.doi.org/10.1038/nchembio.1817

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