High-throughput screening assays for the identification of chemical probes

被引：437

作者：

Inglese, James ^{[1
]}

Johnson, Ronald L. ^{[1
]}

Simeonov, Anton ^{[1
]}

Xia, Menghang ^{[1
]}

Zheng, Wei ^{[1
]}

Austin, Christopher P. ^{[1
]}

Auld, Douglas S. ^{[1
]}

机构：

[1] US Natl Inst Hlth, Chem Genom Ctr, Bethesda, MD 20892 USA

来源：

NATURE CHEMICAL BIOLOGY | 2007年 / 3卷 / 08期

关键词：

D O I：

10.1038/nchembio.2007.17

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：

High-throughput screening (HTS) assays enable the testing of large numbers of chemical substances for activity in diverse areas of biology. The biological responses measured in HTS assays span isolated biochemical systems containing purified receptors or enzymes to signal transduction pathways and complex networks functioning in cellular environments. This Review addresses factors that need to be considered when implementing assays for HTS and is aimed particularly at investigators new to this field. We discuss assay design strategies, the major detection technologies and examples of HTS assays for common target classes, cellular pathways and simple cellular phenotypes. We conclude with special considerations for configuring sensitive, robust, informative and economically feasible HTS assays.

引用

页码：466 / 479

页数：14

共 150 条

[21] A cell-based assay for IκBα stabilization using a two-color dual luciferase-based sensor [J].

Davis, R. Eric ;

Zhang, Ya-Qin ;

Southall, Noel ;

Staudt, Louis M. ;

Austin, Christopher P. ;

Inglese, James ;

Auld, Douglas S. .

ASSAY AND DRUG DEVELOPMENT TECHNOLOGIES, 2007, 5 (01) :85-103

[22] Substrate capacity considerations in developing kinase assays [J].

DeForge, LE ;

Cochran, AG ;

Yeh, SH ;

Robinson, BS ;

Billeci, KL ;

Wong, WLT .

ASSAY AND DRUG DEVELOPMENT TECHNOLOGIES, 2004, 2 (02) :131-140

[23]

DINGER MC, 2004, MOL BIOL MED CHEM, P73

[24]

*E LILL COMP NIH C, 2005, ASS GUID MAN VERS 4

[25] The minimum significant ratio: A statistical parameter to characterize the reproducibility of potency estimates from concentration-response assays and estimation by replicate-experiment studies [J].

Eastwood, BJ ;

Farmen, MW ;

Iversen, PW ;

Craft, TJ ;

Smallwood, JK ;

Garbison, KE ;

Delapp, NW ;

Smith, GF .

JOURNAL OF BIOMOLECULAR SCREENING, 2006, 11 (03) :253-261

[26] Emerging concepts of guanine nucleotide-binding protein-coupled receptor (GPCR) function and implications for high throughput screening [J].

Eglen, Richard M. ;

Bosse, Roger ;

Reisine, Terry .

ASSAY AND DRUG DEVELOPMENT TECHNOLOGIES, 2007, 5 (03) :425-451

[27]

Eglen RM, 2003, COMB CHEM HIGH T SCR, V6, P381

[28] Bioluminescent assays for high-throughput screening [J].

Fan, Frank ;

Wood, Keith V. .

ASSAY AND DRUG DEVELOPMENT TECHNOLOGIES, 2007, 5 (01) :127-136

[29] A high-throughput screen for aggregation-based inhibition in a large compound library [J].

Feng, Brian Y. ;

Simeonov, Anton ;

Jadhav, Ajit ;

Babaoglu, Kerim ;

Inglese, James ;

Shoichet, Brian K. ;

Austin, Christopher P. .

JOURNAL OF MEDICINAL CHEMISTRY, 2007, 50 (10) :2385-2390

[30] Miniaturizable homogenous time-resolved fluorescence assay for carboxypeptidase B activity [J].

Ferrer, M ;

Zuck, P ;

Kolodin, G ;

Mao, SS ;

Peltier, RR ;

Bailey, C ;

Gardell, SJ ;

Strulovici, B ;

Inglese, J .

ANALYTICAL BIOCHEMISTRY, 2003, 317 (01) :94-98

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