Article
Activity of the Type II JAK2 Inhibitor CHZ868 in B Cell Acute Lymphoblastic Leukemia.
Cancer cell - 13 Jul 2015
Wu Shuo-Chieh, Li Loretta S, Kopp Nadja, Montero Joan, Chapuy Bjoern, Yoda Akinori, Christie Amanda L, Liu Huiyun, Christodoulou Alexandra, van Bodegom Diederik, van der Zwet Jordy, Layer Jacob V, Tivey Trevor, Lane Andrew A, Ryan Jeremy A, Ng Samuel Y, DeAngelo Daniel J, Stone Richard M, Steensma David, Wadleigh Martha, Harris Marian, Mandon Emeline, Ebel Nicolas, Andraos Rita, Romanet Vincent, Dölemeyer Arno, Sterker Dario, Zender Michael, Rodig Scott J, Murakami Masato, Hofmann Francesco, Kuo Frank, Eck Michael J, Silverman Lewis B, Sallan Stephen E, Letai Anthony, Baffert Fabienne, Vangrevelinghe Eric, Radimerski Thomas, Gaul Christoph, Weinstock David M
Abstract excerpt
A variety of cancers depend on JAK2 signaling, including the high-risk subset of B cell acute lymphoblastic leukemias (B-ALLs) with CRLF2 rearrangements. Type I JAK2 inhibitors induce paradoxical JAK2 hyperphosphorylation in these leukemias and have limited activity. To improve the efficacy of JAK2 inhibition in B-ALL, we developed the type II inhibitor CHZ868, which stabilizes JAK2 in an inactive conformation....
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