Quantitative targeted proteomics for understanding the blood-brain barrier: Towards pharmacoproteomics

Sumio Ohtsuki, Mio Hirayama, Shingo Ito, Yasuo Uchida, Masanori Tachikawa, Tetsuya Terasaki

Research output: Contribution to journalReview articlepeer-review

36 Citations (Scopus)


The blood-brain barrier (BBB) is formed by brain capillary endothelial cells linked together via complex tight junctions, and serves to prevent entry of drugs into the brain. Multiple transporters are expressed at the BBB, where they control exchange of materials between the circulating blood and brain interstitial fluid, thereby supporting and protecting the CNS. An understanding of the BBB is necessary for efficient development of CNS-acting drugs and to identify potential drug targets for treatment of CNS diseases. Quantitative targeted proteomics can provide detailed information on protein expression levels at the BBB. The present review highlights the latest applications of quantitative targeted proteomics in BBB research, specifically to evaluate species and in vivo-in vitro differences, and to reconstruct in vivo transport activity. Such a BBB quantitative proteomics approach can be considered as pharmacoproteomics.

Original languageEnglish
Pages (from-to)303-313
Number of pages11
JournalExpert Review of Proteomics
Issue number3
Publication statusPublished - 2014 Jun


  • absolute quantification
  • blood brain barrier
  • brain capillary endothelial cells
  • multiple reaction monitoring
  • pharmacoproteomics
  • quantitative targeted proteomics
  • transporter

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology


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