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PMID: 26364198 Published · ppublish English Journal Article Research Support, Non-U.S. Gov't Review

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

Journal of industrial microbiology & biotechnology ·Vol. 43 ·No. 2-3 ·2016-03-00 ·Pages 221-31

Chang J, Kwon HJ

Abstract

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.

Keywords
Drug discovery Mode of action Natural products Phenotypic screening Target identification
MeSH Terms
Aminoglycosides/pharmacology Animals Biological Products/pharmacology Bridged Bicyclo Compounds/pharmacology Drug Evaluation, Preclinical/methods Humans Molecular Targeted Therapy Peptides, Cyclic/pharmacology Proteomics
Chemicals
Aminoglycosides Biological Products Bridged Bicyclo Compounds Peptides, Cyclic ecumicin glucopiericidin A terpestacin
Authors & Affiliations
2 authors, click to expand affiliations / ORCID
Chang Junghwa
Department of Biotechnology, Translational Research Center for Protein Function Control, College of Life Science and Biotechnology, Yonsei University, Seoul, 120-749, Republic of Korea.
Kwon Ho Jeong ORCID
Department of Biotechnology, Translational Research Center for Protein Function Control, College of Life Science and Biotechnology, Yonsei University, Seoul, 120-749, Republic of Korea. [email protected]. | Department of Internal Medicine, College of Medicine, Yonsei University, Seoul, 120-752, Republic of Korea. [email protected].
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Article Info
Journal
Journal of industrial microbiology & biotechnology
Abbr.
J Ind Microbiol Biotechnol
ISSN
1476-5535
DOI
10.1007/s10295-015-1681-y
Email
[email protected]
Published
2016-03-00
Epub
2015-00-12
Pages
221-31
Language
English
Region
Germany
NLM ID
9705544
Subset
IM
External Links
PubMed source DOI: 10.1007/s10295-015-1681-y View journal details
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