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Updated: Aug 14, 2026
A Method for Screening and Validation of Resistant Mutations Against Kinase Inhibitors
Published on: December 7, 2014
Identification of differentially expressed proteins in imatinib mesylate-resistant chronic myelogenous cells
Jungeun Park1, Sangmi Kim, Jong K Oh
1Division of Molecular Genomic Medicine and #Cancer Research Institute, College of Medicine, Seoul National University, Yongon-Dong, Seoul 110-799, Korea.
Abstract:
Resistance to imatinib mesylate (also known as Gleevec, Glivec, and STI571) often becomes a barrier to the treatment of chronic myelogenous leukemia (CML). In order to identify markers of the action of imatinib mesylate, we used a mass spectrometry approach to compare protein expression profiles in human leukemia cells (K562) and in imatinib mesylate-resistant human leukemia cells (K562-R) in the presence and absence of imatinib mesylate. We identified 118 differentially regulated proteins in these two leukemia cell-lines, with and without a 1 microM imatinib mesylate challenge. Nine proteins of unknown function were discovered. This is the first comprehensive report regarding differential protein expression in imatinib mesylate-treated CML cells.
Insights
This study identifies protein markers associated with imatinib mesylate resistance in chronic myelogenous leukemia (CML) cells. Understanding these proteins could lead to better CML treatment strategies.
Area of Science:
- Proteomics
- Oncology
- Molecular Biology
Background:
- Imatinib mesylate is a key treatment for chronic myelogenous leukemia (CML).
- Resistance to imatinib mesylate is a significant challenge in CML therapy.
- Identifying molecular markers of imatinib action is crucial for overcoming resistance.
Purpose of the Study:
- To identify protein expression profiles associated with imatinib mesylate action.
- To discover potential biomarkers for imatinib mesylate resistance in CML.
- To compare protein expression between sensitive and resistant CML cell lines.
Main Methods:
- Utilized mass spectrometry to analyze protein expression.
- Compared protein profiles in K562 (CML) and K562-R (resistant CML) cell lines.
- Analyzed cells in the presence and absence of 1 microM imatinib mesylate.
Main Results:
- Identified 118 differentially regulated proteins between the two cell lines under imatinib treatment.
- Discovered nine novel proteins with unknown functions.
- This represents the first comprehensive report on differential protein expression in imatinib-treated CML cells.
Conclusions:
- Differential protein expression is linked to imatinib mesylate resistance in CML.
- The identified proteins may serve as biomarkers for predicting or overcoming resistance.
- Further research into these proteins could advance CML treatment strategies.
