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Prolonged and tunable residence time using reversible covalent kinase inhibitors
- 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
Published Web Location
https://doi.org/10.1038/nchembio.1817Abstract
Structural changes in the capping groups of inverted cyanoacrylamide-based kinase inhibitors resulted in alterations in residence time, with some compounds exhibiting sustained pharmacological effects in vivo.
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