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
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
收藏
页码:466 / 479
页数:14
相关论文
共 150 条
[1]   CypHer 5: A generic approach for measuring the activation and trafficking of G protein-coupled receptors in live cells [J].
Adie, EJ ;
Francis, MJ ;
Davies, J ;
Smith, L ;
Marenghi, A ;
Hather, C ;
Hadingham, K ;
Michael, NP ;
Milligan, G ;
Gamel, S .
ASSAY AND DRUG DEVELOPMENT TECHNOLOGIES, 2003, 1 (02) :251-259
[2]   Nuclear export inhibitors and kinase inhibitors identified using a MAPK-activated protein kinase 2 Redistribution® screen [J].
Almholt, DLC ;
Loechel, F ;
Nielsen, SJ ;
Krog-Jensen, C ;
Terry, R ;
Bjorn, SP ;
Pedersen, HC ;
Præstegaard, M ;
Moller, S ;
Heide, M ;
Pagliaro, L ;
Mason, AJ ;
Butcher, S ;
Dahl, SW .
ASSAY AND DRUG DEVELOPMENT TECHNOLOGIES, 2004, 2 (01) :7-20
[3]  
AULD DS, 1999, PROTEOLYTIC ENZYMES, P30
[4]   Resveratrol inhibits firefly luciferase [J].
Bakhtiarova, Adel ;
Taslimi, Paul ;
Elliman, Stephen J. ;
Kosinski, Penelope A. ;
Hubbard, Brian ;
Kavana, Michael ;
Kemp, Daniel M. .
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 2006, 351 (02) :481-484
[5]   High-throughput drug screen targeted to the 5′ untranslated region of Alzheimer amyloid precursor protein mRNA [J].
Bandyopadhyay, Sanghamitra ;
Ni, Jake ;
Ruggiero, Amy ;
Walshe, Karen ;
Rogers, Mark S. ;
Chattopadhyay, Naibedya ;
Glicksman, Marcie A. ;
Rogers, Jack T. .
JOURNAL OF BIOMOLECULAR SCREENING, 2006, 11 (05) :469-480
[6]   Identification and characterization of pleckstrin-homology-domain-dependent and isoenzyme-specific Akt inhibitors [J].
Barnett, SF ;
Defeo-Jones, D ;
Fu, S ;
Hancock, PJ ;
Haskell, KM ;
Jones, RE ;
Kahana, JA ;
Kral, AM ;
Leander, K ;
Lee, LL ;
Malinowski, J ;
McAvoy, EM ;
Nahas, DD ;
Robinson, RG ;
Huber, HE .
BIOCHEMICAL JOURNAL, 2005, 385 :399-408
[7]  
Behan D P, 2001, Curr Opin Drug Discov Devel, V4, P548
[8]   Pharmacological chaperones:: potential treatment for conformational diseases [J].
Bernier, V ;
Lagacé, M ;
Bichet, DG ;
Bouvier, M .
TRENDS IN ENDOCRINOLOGY AND METABOLISM, 2004, 15 (05) :222-228
[9]   A novel HIV-1 antiviral high throughput screening approach for the discovery of HIV-1 inhibitors [J].
Blair, WS ;
Isaacson, J ;
Li, XQ ;
Cao, J ;
Peng, QH ;
Kong, GFZ ;
Patick, AK .
ANTIVIRAL RESEARCH, 2005, 65 (02) :107-116
[10]   Application of laser-scanning fluorescence microplate cytometry in high content screening [J].
Bowen, Wayne P. ;
Wylie, Paul G. .
ASSAY AND DRUG DEVELOPMENT TECHNOLOGIES, 2006, 4 (02) :209-221