Identification and validation of bioactive small molecule target through phenotypic screening

被引:24
作者
Cho, Yoon Sun [1 ]
Kwon, Ho Jeong [1 ]
机构
[1] Yonsei Univ, Chem Genom Natl Res Lab, Dept Biotechnol, Translat Res Ctr Prot Funct Control,Coll Life Sci, Seoul 120749, South Korea
基金
新加坡国家研究基金会;
关键词
Phenotypic screening; Target identification; Small molecule; Chemical genomics; Chemical proteomics; DRUG-DISCOVERY; CHEMICAL GENETICS; GENOMICS; ANGIOGENESIS; INHIBITORS;
D O I
10.1016/j.bmc.2011.11.021
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
For effective bioactive small molecule discovery and development into new therapeutic drug, a systematic screening and target protein identification is required. Different from the conventional screening system, herein phenotypic screening in combination with multi-omics-based target identification and validation (MOTIV) is introduced. First, phenotypic screening provides visual effect of bioactive small molecules in the cell or organism level. It is important to know the effect on the cell or organism level since small molecules affect not only a single target but the entire cellular mechanism within a cell or organism. Secondly, MOTIV provides systemic approach to discover the target protein of bioactive small molecule. With the chemical genomics and proteomics approach of target identification methods, various target protein candidates are identified. Then network analysis and validations of these candidates result in identifying the biologically relevant target protein and cellular mechanism. Overall, the combination of phenotypic screening and MOTIV will provide an effective approach to discover new bioactive small molecules and their target protein and mechanism identification. (C) 2011 Elsevier Ltd. All rights reserved.
引用
收藏
页码:1922 / 1928
页数:7
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