A non-covalent inhibitor XMU-MP-3 overrides ibrutinib-resistant BtkC481S mutation in B-cell malignancies.
Fu GuiJie JiangZhixiang HeLi LiYunzhan LiZhou DengYue LuXinrui WuGuyue ChenJingyi SuSiyang SongYue-Ming ZhangCai-Hong YunXin HuangEllen WeisbergJianming ZhangXianming DengPublished in: British journal of pharmacology (2019)
XMU-MP-3 directly targets the BTK signalling pathway in B-cell lymphoma. These findings establish XMU-MP-3 as a novel inhibitor of BTK, which could serve as both a tool compound and a lead for further drug development in BTK relevant B-cell malignancies, especially those with the acquired ibrutinib-resistant C481S mutation.