Bruton tyrosine kinase degradation as a therapeutic strategy for cancer

The covalent Bruton tyrosine kinase (BTK) inhibitor ibrutinib is highly efficacious against multiple B-cell malignancies. However, it is not selective for BTK, and multiple mechanisms of resistance, including the C481S-BTK mutation, can compromise its efficacy. We hypothesized that small-molecule-in...

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Veröffentlicht in:	Blood Jg. 133; H. 9; S. 952
Hauptverfasser:	Dobrovolsky, Dennis, Wang, Eric S, Morrow, Sara, Leahy, Catharine, Faust, Tyler, Nowak, Radosław P, Donovan, Katherine A, Yang, Guang, Li, Zhengnian, Fischer, Eric S, Treon, Steven P, Weinstock, David M, Gray, Nathanael S
Format:	Journal Article
Sprache:	Englisch
Veröffentlicht:	United States 28.02.2019
Schlagworte:	Agammaglobulinaemia Tyrosine Kinase - metabolism Animals Antineoplastic Agents - pharmacology Cell Proliferation - drug effects Humans Ikaros Transcription Factor - metabolism Lymphoma, Mantle-Cell - drug therapy Lymphoma, Mantle-Cell - enzymology Lymphoma, Mantle-Cell - pathology Mice Mice, Inbred NOD Mice, SCID Proteolysis Pyrazoles - pharmacology Pyrimidines - pharmacology Signal Transduction Small Molecule Libraries - pharmacology Tumor Cells, Cultured Xenograft Model Antitumor Assays
ISSN:	1528-0020, 1528-0020
Online-Zugang:	Weitere Angaben
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