Discovery of Novel Irreversible Inhibitors of Interleukin (IL)-2-inducible Tyrosine Kinase (Itk) by Targeting Cysteine 442 in the ATP Pocket

IL-2-inducible tyrosine kinase (Itk) plays a key role in antigen receptor signaling in T cells and is considered an important target for anti-inflammatory drug discovery. In order to generate inhibitors with the necessary potency and selectivity, a compound that targeted cysteine 442 in the ATP bind...

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Main Authors: Harling, John D., Deakin, Angela M., Campos, Sébastien, Grimley, Rachel, Chaudry, Laiq, Nye, Catherine, Polyakova, Oxana, Bessant, Christina M., Barton, Nick, Somers, Don, Barrett, John, Graves, Rebecca H., Hanns, Laura, Kerr, William J., Solari, Roberto
Formato: Artigo
Idioma:Inglês
Publicado: American Society for Biochemistry and Molecular Biology 2013
Assuntos:
Enzymology
Acceso en liña:https://ncbi.nlm.nih.gov/pmc/articles/PMC3784729/
https://ncbi.nlm.nih.gov/pubmed/23935099
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1074/jbc.M113.474114
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