Article
Mutation in Abl kinase with altered drug-binding kinetics indicates a novel mechanism of imatinib resistance.
Proceedings of the National Academy of Sciences of the United States of America - 16 Nov 2021
Lyczek Agatha, Berger Benedict-Tilman, Rangwala Aziz M, Paung YiTing, Tom Jessica, Philipose Hannah, Guo Jiaye, Albanese Steven K, Robers Matthew B, Knapp Stefan, Chodera John D, Seeliger Markus A
Abstract excerpt
Protein kinase inhibitors are potent anticancer therapeutics. For example, the Bcr-Abl kinase inhibitor imatinib decreases mortality for chronic myeloid leukemia by 80%, but 22 to 41% of patients acquire resistance to imatinib. About 70% of relapsed patients harbor mutations in the Bcr-Abl kinase domain, where more than a hundred different mutations have been identified. Some mutations are located near the...
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