Robust and systematic drug screening method using chemical arrays and the protein library: Identification of novel inhibitors of carbonic anhydrase II

Isao Miyazaki, Siro Simizu, Harumi Ichimiya, Makoto Kawatani, Hiroyuki Osada

Research output: Contribution to journalArticle

28 Citations (Scopus)


The identification of specific interactions between small molecules and human proteins of interest is a fundamental step in chemical biology and drug development. Here we describe an efficient method to obtain novel binding ligands of human proteins by a chemical array approach. Our method includes large-scale ligand screening with two libraries, proteins and chemicals, the use of cell lysates that express proteins of interest fused with red fluorescent protein, and high-throughput screening by merged display analysis, which removes false positive signals from array experiments. Using our systematic platform, we detected novel inhibitors of carbonic anhydrase II. It is suggested that our systematic platform is a rapid and robust approach to screen novel ligands for human proteins of interest.

Original languageEnglish
Pages (from-to)2739-2749
Number of pages11
JournalBioscience, Biotechnology and Biochemistry
Issue number10
Publication statusPublished - 2008 Nov 5



  • Carbonic anhydrase II
  • Chemical array
  • Protein library
  • Small molecule inhibitor

ASJC Scopus subject areas

  • Biotechnology
  • Analytical Chemistry
  • Biochemistry
  • Applied Microbiology and Biotechnology
  • Molecular Biology
  • Organic Chemistry

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