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Tag: Cys481

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What is the Binding Site of Ibrutinib? A Covalent Inhibitor's Precision Targeting

3 min read
Ibrutinib, a first-in-class, FDA-approved anticancer drug, is a potent tool in the fight against certain B-cell malignancies. Its therapeutic efficacy hinges on a highly specific molecular interaction, revealing exactly **what is the binding site of ibrutinib** on its target enzyme, Bruton's tyrosine kinase (BTK). This binding is an irreversible, covalent modification that effectively shuts down a critical signaling pathway in malignant B-cells.