What question did this study set out to answer?

Map the comprehensive drug-protein interaction profiles of imatinib, nilotinib, and dasatinib to predict potential adverse effects and identify new clinical applications.

August 25, 2007BloodOpen Access

Chemical proteomic profiles of the BCR-ABL inhibitors imatinib, nilotinib, and dasatinib reveal novel kinase and nonkinase targets

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Map the comprehensive drug-protein interaction profiles of imatinib, nilotinib, and dasatinib to predict potential adverse effects and identify new clinical applications.
Generated comprehensive drug-protein binding profiles using chemical proteomics for imatinib, nilotinib, and dasatinib.
Identified and cross-compared drug targets across tyrosine kinases, serine/threonine kinases, and nonkinase enzymes.
The three inhibitors displayed markedly different target profiles with minimal overlap beyond ABL kinases, with dasatinib binding over 30 tyrosine and serine/threonine kinases including immune regulators.
Nilotinib selectively engaged the receptor tyrosine kinase DDR1 as a major off-target interactor.
Imatinib and nilotinib bound and inhibited the oxidoreductase NQO2 at physiologically relevant concentrations, identifying the first known nonkinase target for these therapies.

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Implication

Chemical proteomic profiling reveals distinct kinase and nonkinase targets of BCR-ABL inhibitors, highlighting distinct off-target mechanisms and therapeutic possibilities.

Cite This Study

Rix et al. (2007) studied this question.

synapsesocial.com/papers/69dbd9455b363cdf1c836094 https://doi.org/10.1182/blood-2007-07-102061

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Implication

Chemical proteomic profiling reveals distinct kinase and nonkinase targets of BCR-ABL inhibitors, highlighting distinct off-target mechanisms and therapeutic possibilities.

Chemical proteomic profiles of the BCR-ABL inhibitors imatinib, nilotinib, and dasatinib reveal novel kinase and nonkinase targets

Key Points

Discussion

Implication

Cite This Study

Chemical proteomic profiles of the BCR-ABL inhibitors imatinib, nilotinib, and dasatinib reveal novel kinase and nonkinase targets

Key Points

Discussion

Implication

Cite This Study

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