Target identification of bioactive compounds

Etsu Tashiro, Masaya Imoto

Research output: Contribution to journalArticlepeer-review

25 Citations (Scopus)


To fully understand the regulation of cellular events, functional analysis of each protein involved in the regulatory systems is required. Among a variety of methods to uncover protein function, chemical genetics is a remarkable approach in which small molecular compounds are used as probes to elucidate protein functions within signaling pathways. However, identifying the target of small molecular bioactive compounds isolated by cell-based assays represents a crucial hurdle that must be overcome before chemical genetic studies can commence. A variety of methods and technologies for identifying target proteins have been reported. This review therefore aims to describe approaches for identifying these molecular targets.

Original languageEnglish
Pages (from-to)1910-1921
Number of pages12
JournalBioorganic and Medicinal Chemistry
Issue number6
Publication statusPublished - 2012 Mar 15


  • Bioactive compounds
  • Chemical genetics
  • Protein function
  • Target identification

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry


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