MPT0B002, a novel microtubule inhibitor, downregulates T315I mutant Bcr-Abl and induces apoptosis of imatinib-resistant chronic myeloid leukemia cells

Summary Chronic myeloid leukemia (CML) is a hematopoietic malignancy caused by the constitutive activation of Bcr-Abl tyrosine kinase. The Bcr-Abl inhibitor imatinib and other second-generation tyrosine kinase inhibitors such as dasatinib and nilotinib have remarkable efficacy in CML treatment. Howe...

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Veröffentlicht in:	Investigational new drugs 2017-08, Vol.35 (4), p.427-435
Hauptverfasser:	Yeh, Yi-Yen, Liou, Jing-Ping, Lee, Yueh-Lun, Lin, John Yi-Chung, Huang, Huei-Mei
Format:	Artikel
Sprache:	eng
Schlagworte:	Apoptosis Apoptosis - drug effects BCR-ABL protein Caspase Caspase-3 Cell cycle Cell Line, Tumor Cell proliferation Cells, Cultured Chronic myeloid leukemia Down-Regulation Drug resistance Drug Resistance, Neoplasm - drug effects Endothelial cells Enzyme inhibitors Fusion protein Fusion Proteins, bcr-abl - antagonists & inhibitors Fusion Proteins, bcr-abl - genetics GTP-binding protein Human Umbilical Vein Endothelial Cells Humans Imatinib Imatinib Mesylate - pharmacology Inhibitor drugs Inhibitors Kinases Leukemia Leukemia, Myelogenous, Chronic, BCR-ABL Positive - metabolism Malignancy Medicine Medicine & Public Health mRNA Mutation Myeloid leukemia Oncology Pharmacology/Toxicology Point mutation Poly(ADP-ribose) polymerase Polymerization Preclinical Studies Protein Kinase Inhibitors - pharmacology Protein-tyrosine kinase Studies Targeted cancer therapy Tubulin Tubulin - metabolism Tubulin Modulators - pharmacology Tyrosine Umbilical vein
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