[HTML][HTML] Erlotinib effectively inhibits JAK2V617F activity and polycythemia vera cell growth
Z Li, M Xu, S Xing, WT Ho, T Ishii, Q Li, X Fu… - Journal of biological …, 2007 - ASBMB
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 (Tarceva™) is a potent inhibitor of JAK2 V617F activity. In
vitro colony culture assays revealed that erlotinib at micro-molar concentrations effectively …
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 (Tarceva™) is a potent inhibitor of JAK2 V617F activity. In
vitro colony culture assays revealed that erlotinib at micro-molar concentrations effectively …