Ibrutinib Resistance in Chronic Lymphocytic Leukemia

Ibrutinib, a Bruton's tyrosine kinase inhibitor, is active in CLL, but resistance may emerge. The authors observed the emergence of a CLL clone with a cysteine-to-serine change in amino acid 481 of the target protein that substantially weakens drug binding and leads to resistance. To the Editor...

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Veröffentlicht in:	The New England journal of medicine 2014-06, Vol.370 (24), p.2352-2354
Hauptverfasser:	Furman, Richard R, Cheng, Shuhua, Lu, Pin, Setty, Menu, Perez, Alexendar R, Guo, Ailin, Racchumi, Joelle, Xu, Guozhou, Wu, Hao, Ma, Jiao, Steggerda, Susanne M, Coleman, Morton, Leslie, Christina, Wang, Y. Lynn
Format:	Artikel
Sprache:	eng
Schlagworte:	Agammaglobulinaemia Tyrosine Kinase Amino acids Bruton's tyrosine kinase Chronic lymphocytic leukemia Drug Resistance, Neoplasm - genetics Female Humans Kinases Leukemia Leukemia, Lymphocytic, Chronic, B-Cell - drug therapy Leukemia, Lymphocytic, Chronic, B-Cell - genetics Lymphatic leukemia Lymphocytes Middle Aged Mutation Phosphorylation Point Mutation Protein-tyrosine kinase Protein-Tyrosine Kinases - antagonists & inhibitors Protein-Tyrosine Kinases - chemistry Protein-Tyrosine Kinases - metabolism Pyrazoles - metabolism Pyrazoles - therapeutic use Pyrimidines - metabolism Pyrimidines - therapeutic use Receptors, Antigen, B-Cell - metabolism Recurrence Sequence Analysis, DNA Serine
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