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Constraining regulatory domain dynamics of the Src kinase Fgr increases ATP-site inhibitor sensitivity and impairs bone marrow engraftment

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Acute myeloid leukemia is often associated with constitutive activation of the Src-family kinases, Hck, Lyn, and Fgr. Their modular SH3 and SH2 domains regulate kinase activity and signal transduction. Here, we show that regulatory domain dynamics critically i... ...