Advances in identification and validation of protein targets of natural products without chemical modification

J. Chang, Y. Kim, H. J. Kwon

Research output: Contribution to journalReview articlepeer-review

87 Citations (Scopus)


Covering: up to February 2016 Identification of the target proteins of natural products is pivotal to understanding the mechanisms of action to develop natural products for use as molecular probes and potential therapeutic drugs. Affinity chromatography of immobilized natural products has been conventionally used to identify target proteins, and has yielded good results. However, this method has limitations, in that labeling or tagging for immobilization and affinity purification often result in reduced or altered activity of the natural product. New strategies have recently been developed and applied to identify the target proteins of natural products and synthetic small molecules without chemical modification of the natural product. These direct and indirect methods for target identification of label-free natural products include drug affinity responsive target stability (DARTS), stability of proteins from rates of oxidation (SPROX), cellular thermal shift assay (CETSA), thermal proteome profiling (TPP), and bioinformatics-based analysis of connectivity. This review focuses on and reports case studies of the latest advances in target protein identification methods for label-free natural products. The integration of newly developed technologies will provide new insights and highlight the value of natural products for use as biological probes and new drug candidates.

Original languageEnglish
Pages (from-to)719-730
Number of pages12
JournalNatural Product Reports
Issue number5
Publication statusPublished - 2016 May

Bibliographical note

Funding Information:
This work was partly supported by grants from the National Research Foundation of Korea, funded by the Korean government (MSIP; 2012M3A9D1054520, 2015M3A9B6027818, 2015K1A1A2028365, 2015M3A9C4076321) and Brain Korea 21 Plus Project, Republic of Korea.

Publisher Copyright:
© 2016 The Royal Society of Chemistry.

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Drug Discovery
  • Organic Chemistry


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