Article
CHZ868, a Type II JAK2 Inhibitor, Reverses Type I JAK Inhibitor Persistence and Demonstrates Efficacy in Myeloproliferative Neoplasms.
Cancer cell - 13 Jul 2015
Meyer Sara C, Keller Matthew D, Chiu Sophia, Koppikar Priya, Guryanova Olga A, Rapaport Franck, Xu Ke, Manova Katia, Pankov Dmitry, O'Reilly Richard J, Kleppe Maria, McKenney Anna Sophia, Shih Alan H, Shank Kaitlyn, Ahn Jihae, Papalexi Eftymia, Spitzer Barbara, Socci Nick, Viale Agnes, Mandon Emeline, Ebel Nicolas, Andraos Rita, Rubert Joëlle, Dammassa Ernesta, Romanet Vincent, Dölemeyer Arno, Zender Michael, Heinlein Melanie, Rampal Raajit, Weinberg Rona Singer, Hoffman Ronald, Sellers William R, Hofmann Francesco, Murakami Masato, Baffert Fabienne, Gaul Christoph, Radimerski Thomas, Levine Ross L
Abstract excerpt
Although clinically tested JAK inhibitors reduce splenomegaly and systemic symptoms, molecular responses are not observed in most myeloproliferative neoplasm (MPN) patients. We previously demonstrated that MPN cells become persistent to type I JAK inhibitors that bind the active conformation of JAK2. We investigated whether CHZ868, a type II JAK inhibitor, would demonstrate activity in JAK inhibitor persistent...
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