Recent advances in target identification of bioactive natural products

Biosci Biotechnol Biochem. 2019 Jan;83(1):1-9. doi: 10.1080/09168451.2018.1533804. Epub 2018 Oct 21.


Natural products are a tremendous source of tool discovery for basic science and drug discovery for clinical uses. In contrast to the large number of compounds isolated from nature, however, the number of compounds whose target molecules have been identified so far is fairly limited. Elucidation of the mechanism of how bioactive small molecules act in cells to induce biological activity (mode of action) is an attractive but challenging field of basic biology. At the same time, this is the major bottleneck for drug development of compounds identified in cell-based and phenotype-based screening. Although researchers' experience and inspiration have been crucial for successful target identification, recent advancements in genomics, proteomics, and chemical genomics have made this challenging task possible in a systematic fashion.

Keywords: Chemical genetics; mode of action; profiling; target molecule; yeast genetics.

Publication types

  • Review

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Anti-Bacterial Agents / chemical synthesis
  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology
  • Antifungal Agents / chemical synthesis
  • Antifungal Agents / chemistry
  • Antifungal Agents / pharmacology
  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology
  • Biological Products / chemical synthesis*
  • Biological Products / chemistry
  • Biological Products / pharmacology
  • Drug Development / methods
  • Drug Development / trends*
  • Drug Discovery*
  • Drug Evaluation, Preclinical
  • Drug Interactions
  • Genomics
  • Humans
  • Phenotype
  • Proteomics
  • Small Molecule Libraries


  • Anti-Bacterial Agents
  • Antifungal Agents
  • Antineoplastic Agents
  • Biological Products
  • Small Molecule Libraries