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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)

Erlotinib Effectively Inhibits JAK2V617F Activity and Polycythemia Vera Cell Growth.

JAK2(V617F), a mutant of tyrosine kinase JAK2, is found in most patients with polycythemia vera (PV) and a substantial proportion of patients with idiopathic myelofibrosis or essential thrombocythemia. The JAK2 mutant displays a much increased kinase activity and generates a PV-like phenotype in mouse bone marrow transplant models. This study shows that the anti-cancer drug erlotinib (Tarcevatrade mark) is a potent inhibitor of JAK2(V617F) activity. In vitro colony culture assays revealed that erlotinib at micro-molar concentrations effectively suppresses the growth and expansion of PV hematopoietic progenitor cells while having little effect on normal cells. Furthermore, JAK2(V617F)-positive cells from PV patients show greater susceptibility to the inhibitor than their negative counterparts. Similar inhibitory effects were found with the JAK2(V617F)-positive human erythroleukemia HEL cell line. These data suggest that erlotinib may be used for treatment of JAK2(V617F)-positive PV and other myeloproliferative disorders.[1]


  1. Erlotinib Effectively Inhibits JAK2V617F Activity and Polycythemia Vera Cell Growth. Li, Z., Xu, M., Xing, S., Ho, W.T., Ishii, T., Li, Q., Fu, X., Zhao, Z.J. J. Biol. Chem. (2007) [Pubmed]
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