Imatinib bound to Abelson Tyrosine Kinase (1FPU)
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Imatinib (STI-571) is a tyrosine kinase inhibitor used for chronic myelogenous leukaemia (CML). CML causes undesirable activation of the Abelson tyrosine kinase (Abl). The activity of Abl in pateinets with CML is uncontrolled. Using an inhibitor, such as imatinib, decreases the activivity of the enzyme, mitigating some of the pathophysiology. (DOI: 10.1126/science.289.5486.1938) NB: The inhibitor in the crystallised structure is missing a piperazinyl group. This is not involved in target binding but effects the pharmacokinetics of the inhibitor (including solubility). Supplementary information: DOI: 10.1016/s0959-8049(02)80599-8
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