Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10591301 | Bioorganic & Medicinal Chemistry Letters | 2013 | 11 Pages |
Abstract
Inhibition of the non-receptor tyrosine kinase ITK, a component of the T-cell receptor signalling cascade, may represent a novel treatment for allergic asthma. Here we report the structure-based optimization of a series of benzothiazole amides that demonstrate sub-nanomolar inhibitory potency against ITK with good cellular activity and kinase selectivity. We also elucidate the binding mode of these inhibitors by solving the X-ray crystal structures of several inhibitor-ITK complexes.
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Authors
Colin H. MacKinnon, Kevin Lau, Jason D. Burch, Yuan Chen, Jonathon Dines, Xiao Ding, Charles Eigenbrot, Alexander Heifetz, Allan Jaochico, Adam Johnson, Joachim Kraemer, Susanne Kruger, Thomas M. Krülle, Marya Liimatta, Justin Ly, Rosemary Maghames,