Cited by 289Chronic Myeloid Leukemia TreatmentsMast cells and histamineChronic Lymphocytic Leukemia Research

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The Btk tyrosine kinase is a major target of the Bcr-Abl inhibitor dasatinib

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Hantschel, Oliver, Rix, Uwe, Schmidt, Uwe, Bürckstümmer, Tilmann, Kneidinger, Michael, Schütze, Gregor, Colinge, Jacques, Bennett, Keiryn L., Ellmeier, Wilfried, Valent, Peter, Superti-Furga, Giulio·2007·Proceedings of the National Academy of Sciences

DOI 10.1073/pnas.0702654104PMC PMC1940229

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Abstract

Dasatinib is a small-molecule kinase inhibitor used for the treatment of imatinib-resistant chronic myelogenous leukemia (CML). We have analyzed the kinases targeted by dasatinib by using an unbiased chemical proteomics approach to detect binding proteins directly from lysates of CML cells. Besides Abl and Src kinases, we have identified the Tec kinases Btk and Tec, but not Itk, as major binders of dasatinib. The kinase activity of Btk and Tec, but not of Itk, was inhibited by nanomolar concentrations of dasatinib in vitro and in cultured cells. We identified the gatekeeper residue as the critical determinant of dasatinib susceptibility. Mutation of Thr-474 in Btk to Ile and Thr-442 in Tec to Ile conferred resistance to dasatinib, whereas mutation of the corresponding residue in Itk (Phe-435) to Thr sensitized the otherwise insensitive Itk to dasatinib. The configuration of this residue may be a predictor for dasatinib sensitivity across the kinome. Analysis of mast cells derived from Btk-deficient mice suggested that inhibition of Btk by dasatinib may be responsible for the observed reduction in histamine release upon dasatinib treatment. Furthermore, dasatinib inhibited histamine release in primary human basophils and secretion of proinflammatory cytokines in immune cells. The observed inhibition of Tec kinases by dasatinib predicts immunosuppressive (side) effects of this drug and may offer therapeutic opportunities for inflammatory and immunological disorders.

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Authors: Hantschel, O., Rix, U., Schmidt, U., Bürckstümmer, T., Kneidinger, M., Schütze, G., Colinge, J., Bennett, K. L., Ellmeier, W., Valent, P., & Superti-Furga, G.
Affiliations: Austrian Academy of Sciences (AT)
Medical University of Vienna (AT)
*Center for Molecular Medicine of the Austrian Academy of Sciences, Lazarettgasse 19, 1090 Vienna, Austria;
ORCID: Hantschel, Oliver
Rix, Uwe
Bürckstümmer, Tilmann
Colinge, Jacques
Bennett, Keiryn L.
Ellmeier, Wilfried
Valent, Peter
Venue: Proceedings of the National Academy of Sciences
Publisher: National Academy of Sciences
Published: 2007-08-14
Volume: 104
Issue: 33
Pages: 13283-13288
ISSN: 0027-8424 (ISSN-L)
1091-6490
DOI: 10.1073/pnas.0702654104
PMC: PMC1940229
OpenAlex: W1991795177
Cited by: 284
References: 38
Citations by year: 2026: 10 · 2025: 4 · 2024: 5 · 2023: 9 · 2022: 8 · 2021: 8 · 2020: 8 · 2019: 10 · 2018: 10 · 2017: 8 · 2016: 7 · 2015: 26 · 2014: 24 · 2013: 33 · 2012: 29
FWCI: 14.76
Type: journal article
Language: en
Open access: green
www.ncbi.nlm.nih.gov
Locations: Proceedings of the National Academy of Sciences (publishedVersion)
PubMed Central (publishedVersion)
PubMed (publishedVersion)
Infoscience (Ecole Polytechnique Fédérale de Lausanne) (submittedVersion)
Infoscience (Ecole Polytechnique Fédérale de Lausanne) (submittedVersion, cc-by-nc-nd)
Topics: Health Sciences › Medicine › Hematology › Chronic Myeloid Leukemia Treatments
Life Sciences › Immunology and Microbiology › Immunology › Mast cells and histamine
Health Sciences › Medicine › Hematology › Chronic Lymphocytic Leukemia Research
Keywords: dasatinib, Bruton's tyrosine kinase, Tec kinase, ITK, BCR-ABL tyrosine kinase inhibitors, chronic myeloid leukemia, imatinib resistance, kinase inhibitor binding, gatekeeper mutation, kinase inhibitor resistance, mast cells, histamine release, basophils, inflammatory cytokines, immunosuppression, chemoproteomics
MeSH terms: Dasatinib, Animals, Basophils, Enzyme-Linked Immunosorbent Assay, Histamine Release, Humans, Mice, Inbred C57BL, Protein-Tyrosine Kinases, Pyrimidines, Thiazoles, Fusion Proteins, bcr-abl, K562 Cells, U937 Cells, Protein Kinase Inhibitors, Mice

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The Btk tyrosine kinase is a major target of the Bcr-Abl inhibitor dasatinib

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