Author(s): Cook BN, Bentzien J, White A, Nemoto PA, Wang J,
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Abstract Interleukin-2 inducible T-cell kinase (ITK) is a member of the Tec kinase family and is involved with T-cell activation and proliferation. Due to its critical role in acting as a modulator of T-cells, ITK inhibitors could provide a novel route to anti-inflammatory therapy. This work describes the discovery of ITK inhibitors through structure-based design where high-resolution crystal structural information was used to optimize interactions within the kinase specificity pocket of the enzyme to improve both potency and selectivity.
This article was published in Bioorg Med Chem Lett
and referenced in Journal of Clinical & Cellular Immunology