Abstract
Bruton's tyrosine kinase (BTK) is a key component of B cell receptor (BCR) signalling and functions as an important regulator of cell proliferation and cell survival in various B cell malignancies. Small-molecule inhibitors of BTK have shown antitumour activity in animal models and, recently, in clinical studies. High response rates were reported in patients with chronic lymphocytic leukaemia and mantle cell lymphoma. Remarkably, BTK inhibitors have molecular effects that cannot be explained by the classic role of BTK in BCR signalling. In this Review, we highlight the importance of BTK in various signalling pathways in the context of its therapeutic inhibition.
Publication types
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Research Support, Non-U.S. Gov't
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Review
MeSH terms
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Agammaglobulinaemia Tyrosine Kinase
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Animals
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Antineoplastic Agents / pharmacology
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Antineoplastic Agents / therapeutic use
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Clinical Trials as Topic
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Enzyme Activation
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Humans
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Leukemia, B-Cell / drug therapy
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Leukemia, B-Cell / enzymology*
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Molecular Targeted Therapy
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Protein Kinase Inhibitors / pharmacology
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Protein Kinase Inhibitors / therapeutic use
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Protein Structure, Tertiary
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Protein-Tyrosine Kinases / antagonists & inhibitors
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Protein-Tyrosine Kinases / chemistry
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Protein-Tyrosine Kinases / metabolism*
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Signal Transduction
Substances
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Antineoplastic Agents
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Protein Kinase Inhibitors
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Protein-Tyrosine Kinases
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Agammaglobulinaemia Tyrosine Kinase
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BTK protein, human