Discovery of novel drug targets and their functions using phenotypic screening of natural products

Junghwa Chang, Ho Jeong Kwon

Research output: Contribution to journalArticlepeer-review

15 Citations (Scopus)


Natural products are valuable resources that provide a variety of bioactive compounds and natural pharmacophores in modern drug discovery. Discovery of biologically active natural products and unraveling their target proteins to understand their mode of action have always been critical hurdles for their development into clinical drugs. For effective discovery and development of bioactive natural products into novel therapeutic drugs, comprehensive screening and identification of target proteins are indispensable. In this review, a systematic approach to understanding the mode of action of natural products isolated using phenotypic screening involving chemical proteomics-based target identification is introduced. This review highlights three natural products recently discovered via phenotypic screening, namely glucopiericidin A, ecumicin, and terpestacin, as representative case studies to revisit the pivotal role of natural products as powerful tools in discovering the novel functions and druggability of targets in biological systems and pathological diseases of interest.

Original languageEnglish
Pages (from-to)221-231
Number of pages11
JournalJournal of Industrial Microbiology and Biotechnology
Issue number2-3
Publication statusPublished - 2016 Mar 1

Bibliographical note

Funding Information:
This work was partly supported by grants from the National Research Foundation of Korea funded by the Korean Government (MSIP, 2010-0017984 and 2012M3A9D1054520), the Translational Research Center for Protein Function Control, NRF (2009-0083522), the Ministry of Health and Welfare (0620360-1), and the Brain Korea 21 Plus Project, Republic of Korea.

Publisher Copyright:
© 2015, Society for Industrial Microbiology and Biotechnology.

All Science Journal Classification (ASJC) codes

  • Biotechnology
  • Bioengineering
  • Applied Microbiology and Biotechnology


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