Frontiers in Biology

, Volume 8, Issue 2, pp 216-227

First online:

Current technologies to identify protein kinase substrates in high throughput

  • Liang XueAffiliated withDepartment of Biochemistry, Purdue University
  • , W. Andy TaoAffiliated withDepartment of Biochemistry, Purdue UniversityDepartment of Medicinal Chemistry & Molecular Pharmacology, Purdue UniversityDepartment of Chemistry, Purdue UniversityPurdue University Center for Cancer Research, Purdue University Email author 

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Since the discovery of protein phosphorylation as an important modulator of many cellular processes, the involvement of protein kinases in diseases, such as cancer, diabetes, cardiovascular diseases, and central nervous system pathologies, has been extensively documented. Our understanding of many disease pathologies at the molecular level, therefore, requires the comprehensive identification of substrates targeted by protein kinases. In this review, we focus on recent techniques for kinase substrate identification in high throughput, in particular on genetic and proteomic approaches. Each method with its inherent advantages and limitations is discussed.


phosphorylation kinase substrate in vitro kinase assay high throughput screening mass spectrometry phosphoproteomics