Bruton tyrosine kinase represents a promising therapeutic target for treatment of chronic lymphocytic leukemia and is effectively targeted by PCI-32765

B-cell receptor (BCR) signaling is aberrantly activated in chronic lymphocytic leukemia (CLL). Bruton tyrosine kinase (BTK) is essential to BCR signaling and in knockout mouse models its mutation has a relatively B cell–specific phenotype. Herein, we demonstrate that BTK protein and mRNA are signifi...

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Bibliographic Details
Published in:	Blood Vol. 117; no. 23; pp. 6287 - 6296
Main Authors:	Herman, Sarah E.M., Gordon, Amber L., Hertlein, Erin, Ramanunni, Asha, Zhang, Xiaoli, Jaglowski, Samantha, Flynn, Joseph, Jones, Jeffrey, Blum, Kristie A., Buggy, Joseph J., Hamdy, Ahmed, Johnson, Amy J., Byrd, John C.
Format:	Journal Article
Language:	English
Published:	Washington, DC Elsevier Inc 09-06-2011 Americain Society of Hematology American Society of Hematology
Subjects:	Agammaglobulinaemia Tyrosine Kinase Animals Apoptosis - drug effects Apoptosis - genetics B-Cell Activating Factor - genetics B-Cell Activating Factor - metabolism B-Lymphocytes - enzymology Biological and medical sciences CD40 Ligand - genetics CD40 Ligand - metabolism Cell Line, Tumor Cell Proliferation - drug effects Cell Survival - drug effects Cell Survival - genetics Drug Screening Assays, Antitumor - methods Female Gene Expression Regulation, Enzymologic - drug effects Gene Expression Regulation, Enzymologic - genetics Gene Expression Regulation, Leukemic - drug effects Gene Expression Regulation, Leukemic - genetics Hematologic and hematopoietic diseases Humans Interleukin-4 - genetics Interleukin-4 - metabolism Interleukin-6 - genetics Interleukin-6 - metabolism Leukemia, Lymphocytic, Chronic, B-Cell - drug therapy Leukemia, Lymphocytic, Chronic, B-Cell - enzymology Leukemias. Malignant lymphomas. Malignant reticulosis. Myelofibrosis Lymphoid Neoplasia Male MAP Kinase Signaling System - drug effects MAP Kinase Signaling System - genetics Medical sciences Mice Mitogen-Activated Protein Kinase 1 - genetics Mitogen-Activated Protein Kinase 1 - metabolism Mitogen-Activated Protein Kinase 3 - genetics Mitogen-Activated Protein Kinase 3 - metabolism Neoplasm Proteins - antagonists & inhibitors Neoplasm Proteins - biosynthesis Neoplasm Proteins - genetics NF-kappa B - genetics NF-kappa B - metabolism Phosphatidylinositol 3-Kinases - genetics Phosphatidylinositol 3-Kinases - metabolism Protein-Tyrosine Kinases - antagonists & inhibitors Protein-Tyrosine Kinases - biosynthesis Protein-Tyrosine Kinases - genetics Pyrazoles - pharmacology Pyrimidines - pharmacology Receptors, Antigen, B-Cell - genetics Receptors, Antigen, B-Cell - metabolism T-Lymphocytes - enzymology Tumor Necrosis Factor-alpha - genetics Tumor Necrosis Factor-alpha - metabolism Chronic lymphocytic leukemia Bruton tyrosine kinase Treatment Targeting Hematology Targeted therapy Lymphoproliferative syndrome Malignant hemopathy Cancer
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