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Imatinib functions by directly inhibiting the constant activity of tyrosine kinase. It achieves this by binding to the BCR-ABL kinase domain, which prevents the transfer of a phosphate group to tyrosine on the protein substrate. This action stops the subsequent activation of the phosphorylated protein. Consequently, the transmission of proliferative signals to the nucleus is blocked, leading to the induction of apoptosis in leukemic cells.
see also:
Bcr-Abl tyrosine-kinase inhibitors
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