Article
Establishing a chemical genetic link between Bruton tyrosine kinase activity in malignant B cells and cell functions involved in the micro-environmental dialogue.
British journal of haematology - 1 Sept 2017
Göckeritz Elisa, Vondey Verena, Guastafierro Anna, Pizevska Maja, Hassenrück Floyd, Neumann Lars, Hallek Michael, Krause Günter
Abstract excerpt
To elucidate their mechanism of action, inhibitors of Bruton tyrosine kinase (BTK) and resistant BTK mutants were employed to dissect target-dependent cellular functions. BTK-C481S and -T474I, expressed in Ramos and NALM-6 cells, maintained BTK auto-phosphorylation under treatment with ibrutinib or dasatinib, respectively, which showed only modest cytotoxicity. Retained activity of BTK-T474 partially rescued cell...
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