Genetic and proteomic approaches to identify cancer drug targets

被引：23

作者：

Roti, G. ^{[1
,2
]}

Stegmaier, K. ^{[1
,2
,3
,4
]}

机构：

[1] Harvard Univ, Sch Med, Childrens Hosp Boston, Dana Farber Canc Inst,Dept Pediat Oncol, Boston, MA 02215 USA

[2] Harvard Univ, Sch Med, Childrens Hosp Boston, Div Pediat Hematol Oncol, Boston, MA 02215 USA

[3] Harvard Univ, Broad Inst, Cambridge, MA 02142 USA

[4] MIT, Cambridge, MA 02142 USA

来源：

BRITISH JOURNAL OF CANCER | 2012年 / 106卷 / 02期

关键词：

drug discovery; protein target identification; chemical genomics; chemical proteomics; small-molecule library screening; cancer drug targets; DIVERSITY-ORIENTED SYNTHESIS; SMALL-MOLECULE MICROARRAYS; EXPRESSION PROFILES; CHEMICAL PROTEOMICS; CONNECTIVITY MAP; LEUKEMIA STEM; DISCOVERY; CELLS; DIFFERENTIATION; IDENTIFICATION;

D O I：

10.1038/bjc.2011.543

中图分类号：

R73 [肿瘤学];

学科分类号：

100214 ;

摘要：

While target-based small-molecule discovery has taken centre-stage in the pharmaceutical industry, there are many cancer-promoting proteins not easily addressed with a traditional target-based screening approach. In order to address this problem, as well as to identify modulators of biological states in the absence of knowing the protein target of the state switch, alternative phenotypic screening approaches, such as gene expression-based and high-content imaging, have been developed. With this renewed interest in phenotypic screening, however, comes the challenge of identifying the binding protein target(s) of small-molecule hits. Emerging technologies have the potential to improve the process of target identification. In this review, we discuss the application of genomic (gene expression-based), genetic (short hairpin RNA and open reading frame screening), and proteomic approaches to protein target identification. British Journal of Cancer (2012) 106, 254-261. doi:10.1038/bjc.2011.543 www.bjcancer.com Published online 13 December 2011 (C) 2012 Cancer Research UK

引用

页码：254 / 261

页数：8

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