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Recent advances in methods to assess the activity of the kinome
F1000Res. 2017 Jun;6 :1004
PMID: 28713564 PMCID: PMC5490475
AbstractProtein and lipid kinases are deregulated in most, if not all, cancers and are among the most valuable therapeutic targets in these diseases. Despite the introduction of dozens of effective kinase inhibitors into clinical practice, the development of drug resistance remains a major barrier to treatment because of adaption of cellular signaling pathways to bypass targeted kinases. So that the basal and adaptive responses of kinases in cancer can be better understood, new methods have emerged that allow simultaneous and unbiased measurement of the activation state of a substantial fraction of the entire kinome. Here, we discuss such kinome-profiling methodologies, emphasizing the relative strengths and weaknesses of each approach.
NotesRadu, Maria Orcid: 0000-0002-8316-5331 Chernoff, Jonathan Orcid: 0000-0002-4803-7836 Journal Article Review England F1000Res. 2017 Jun 26;6:1004. doi: 10.12688/f1000research.10962.1. eCollection 2017.