Kinase activity signature of breast cancer using peptide phosphosensors.

2012 
27 Background: Improper control of phosphorylation networks represents one of the most relevant regulator and biomarkers of cell dysfunctions leading to cancer. Surprisingly however, measuring the phosphorylation activity of kinases, and potentially monitoring the functionality of the entire kinome at once, remains largely unexplored. Specifically, a highly convenient tool for clinical applications or research purposes would be the advent of a microarray-like chip to comprehensively map phosphorylation networks. While developing such a kinase-sensing platform, we had to establish a library of probes capable of reporting on the catalytic activity of kinases. We present here strategies and results supporting such methodology. Methods: The devised kinase activity-sensing system we are currently exploiting, relies on peptide probes that act as beacons to evaluate enzymes functionality, which emit distinctive signals before and after (de-)phosphorylation. As presented below, computational and molecular biology...
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