Abstract
The protein kinase inhibitor imatinib, also known as Gleevec, has been a notable success in treating chronic myelogenous leukemia. A recent paper in BMC Structural Biology reports a 1.75 A crystal structure of imatinib bound to the oxidoreductase NQO2 and reveals insights into the binding specificity and the off-target effects of the inhibitor.
Publication types
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Research Support, N.I.H., Extramural
MeSH terms
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Animals
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Benzamides
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Fusion Proteins, bcr-abl / antagonists & inhibitors
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Humans
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Imatinib Mesylate
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Leukemia, Myelogenous, Chronic, BCR-ABL Positive / drug therapy
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Molecular Structure
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Piperazines / chemistry
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Piperazines / pharmacokinetics*
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Protein Kinase Inhibitors / chemistry
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Protein Kinase Inhibitors / pharmacokinetics
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Pyrimidines / chemistry
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Pyrimidines / pharmacokinetics*
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Quinone Reductases / antagonists & inhibitors
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Quinone Reductases / chemistry
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Structure-Activity Relationship
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Substrate Specificity
Substances
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Benzamides
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Piperazines
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Protein Kinase Inhibitors
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Pyrimidines
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Imatinib Mesylate
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NRH - quinone oxidoreductase2
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Quinone Reductases
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Fusion Proteins, bcr-abl