Recent advances in methods to assess the activity of the kinome

Jonathan Chernoff, Maria Radu

Research output: Contribution to journalReview articlepeer-review

9 Scopus citations

Abstract

Protein 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.

Original languageEnglish
Article number1004
JournalF1000Research
Volume6
DOIs
StatePublished - 2017

Keywords

  • Assays
  • Cancer therapeutics
  • Enzymes
  • Kinome

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