Journal
BIOCHEMICAL PHARMACOLOGY
Volume 80, Issue 5, Pages 739-747Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bcp.2010.03.027
Keywords
Phosphorylation; Phosphoproteomics; Mass spectrometry; Drug response; Drug resistance; Targeted therapy
Categories
Funding
- National Cancer Institute [P30-CA076292]
- Moffitt Foundation
- Florida Department of Health [06BS-02-9614]
- National Functional Genomics Center
- Melanoma Research Foundation
- Bankhead-Coley Research Program of the State of Florida [09BN-14]
- Donald A Adam Comprehensive Melanoma Research Center
- NATIONAL CANCER INSTITUTE [P30CA076292] Funding Source: NIH RePORTER
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Phosphorylation acts as a molecular switch for many regulatory events in signaling pathways that drive cell division, proliferation, and apoptosis. Because of the critical nature of these protein post-translational modifications in cancer, drug development programs often focus on inhibitors for kinases and phosphatases, which control protein phosphorylation. Numerous kinase inhibitors have entered clinical use, but prediction of their efficacy and a molecular basis for patient response remain uncertain. Chemical proteomics, the combination of drug affinity chromatography with mass spectrometry, identifies potential target proteins that bind to the drugs. Phosphorylation profiling can complement chemical proteomics by cataloging modifications in the target kinases and their downstream substrates using phosphopeptide enrichment and quantitative mass spectrometry. These experiments shed light on the mechanism of disease development and illuminate candidate biomarkers to guide personalized therapeutic strategies. In this review, commonly applied technologies and workflows are discussed to illustrate the role of proteomics in examining tumor biology and therapeutic intervention using kinase inhibitors. (C) 2010 Elsevier Inc. All rights reserved.
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