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
N1 - Publisher Copyright:
© 2015 The Pharmaceutical Society of Korea.
Copyright:
Copyright 2017 Elsevier B.V., All rights reserved.
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
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U2 - 10.1007/s12272-015-0618-3
DO - 10.1007/s12272-015-0618-3
M3 - Review article
C2 - 26040984
AN - SCOPUS:84941992624
VL - 38
SP - 1627
EP - 1641
JO - Archives of Pharmacal Research
JF - Archives of Pharmacal Research
SN - 0253-6269
IS - 9
ER -