Abstract
Identification of the target proteins of bioactive small molecules isolated from phenotypic screens plays an important role in chemical biology and drug discovery. However, discovering the targets of small molecules is often the most challenging and time-consuming step for chemical biology researchers. To overcome the bottlenecks in target identification, many new approaches based on genomics, proteomics, and bioinformatics technologies have been developed. Here, we provide an overview of the current major methodologies for target deconvolution of bioactive small molecules. To obtain an integrated view of the mechanisms of action of small molecules, we propose a systematic approach that involves the combination of multi-omics-based target identification and validation and preclinical target validation.
| Original language | English |
|---|---|
| Pages (from-to) | 1627-1641 |
| Number of pages | 15 |
| Journal | Archives of Pharmacal Research |
| Volume | 38 |
| Issue number | 9 |
| DOIs | |
| Publication status | Published - 2015 Sep 22 |
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All Science Journal Classification (ASJC) codes
- Molecular Medicine
- Drug Discovery
- Organic Chemistry
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Target deconvolution of bioactive small molecules : The heart of chemical biology and drug discovery. / Jung, Hye Jin; Kwon, Ho Jeong.
In: Archives of Pharmacal Research, Vol. 38, No. 9, 22.09.2015, p. 1627-1641.Research output: Contribution to journal › Review article
TY - JOUR
T1 - Target deconvolution of bioactive small molecules
T2 - The heart of chemical biology and drug discovery
AU - Jung, Hye Jin
AU - Kwon, Ho Jeong
PY - 2015/9/22
Y1 - 2015/9/22
N2 - Identification of the target proteins of bioactive small molecules isolated from phenotypic screens plays an important role in chemical biology and drug discovery. However, discovering the targets of small molecules is often the most challenging and time-consuming step for chemical biology researchers. To overcome the bottlenecks in target identification, many new approaches based on genomics, proteomics, and bioinformatics technologies have been developed. Here, we provide an overview of the current major methodologies for target deconvolution of bioactive small molecules. To obtain an integrated view of the mechanisms of action of small molecules, we propose a systematic approach that involves the combination of multi-omics-based target identification and validation and preclinical target validation.
AB - Identification of the target proteins of bioactive small molecules isolated from phenotypic screens plays an important role in chemical biology and drug discovery. However, discovering the targets of small molecules is often the most challenging and time-consuming step for chemical biology researchers. To overcome the bottlenecks in target identification, many new approaches based on genomics, proteomics, and bioinformatics technologies have been developed. Here, we provide an overview of the current major methodologies for target deconvolution of bioactive small molecules. To obtain an integrated view of the mechanisms of action of small molecules, we propose a systematic approach that involves the combination of multi-omics-based target identification and validation and preclinical target validation.
UR - http://www.scopus.com/inward/record.url?scp=84941992624&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=84941992624&partnerID=8YFLogxK
U2 - 10.1007/s12272-015-0618-3
DO - 10.1007/s12272-015-0618-3
M3 - Review article
VL - 38
SP - 1627
EP - 1641
JO - Archives of Pharmacal Research
JF - Archives of Pharmacal Research
SN - 0253-6269
IS - 9
ER -