Article
The HCK/BTK inhibitor KIN-8194 is active in MYD88-driven lymphomas and overcomes mutated BTKCys481 ibrutinib resistance.
Blood - 18 Nov 2021
Yang Guang, Wang Jinhua, Tan Li, Munshi Manit, Liu Xia, Kofides Amanda, Chen Jiaji G, Tsakmaklis Nicholas, Demos Maria G, Guerrera Maria Luisa, Xu Lian, Hunter Zachary R, Che Jinwei, Patterson Christopher J, Meid Kirsten, Castillo Jorge J, Munshi Nikhil C, Anderson Kenneth C, Cameron Michael, Buhrlage Sara J, Gray Nathanael S, Treon Steven P
Abstract excerpt
Activating mutations in MYD88 promote malignant cell growth and survival through hematopoietic cell kinase (HCK)-mediated activation of Bruton tyrosine kinase (BTK). Ibrutinib binds to BTKCys481 and is active in B-cell malignancies driven by mutated MYD88. Mutations in BTKCys481, particularly BTKCys481Ser, are common in patients with acquired ibrutinib resistance. We therefore performed an extensive medicinal...
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