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Biochemical characterization of tirabrutinib and other irreversible inhibitors of Bruton's tyrosine kinase reveals differences in on - and off - target inhibition

Albert Liclican, Loredana Serafini, Weimei Xing, Gregg Czerwieniec, Bart Steiner, Ting Wang, Katherine M. Brendza, Justin D. Lutz, Kathleen S. Keegan, Adrian S. Ray,

Biochimica et Biophysica Acta (BBA) - General Subjects · 2020 · 89 citations · 23 references

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Abstract

This is the first study that offers a detailed side-by-side comparison of four clinically-relevant BTK inhibitors with respect to their inactivation of BTK and related kinases.

References

23

A quantitative analysis of kinase inhibitor selectivity

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Targeting BTK with Ibrutinib in Relapsed Chronic Lymphocytic Leukemia

John C. Byrd, Richard R. Furman, Steven Coutré et al. · New England Journal of Medicine · 2013 · 2.2K citations · Full text

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Ibrutinib versus Ofatumumab in Previously Treated Chronic Lymphoid Leukemia

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The Bruton tyrosine kinase inhibitor PCI-32765 blocks B-cell activation and is efficacious in models of autoimmune disease and B-cell malignancy

Lee Honigberg, Ashley M. Smith, Mint Sirisawad et al. · Proceedings of the National Academy of Sciences · 2010 · 1.5K citations · Full text

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