High-Content Analysis of Kinase Activity in Cells

Author(s): Fabio Gasparri, Francesco Sola, Tiziano Bandiera, Jurgen Moll, Arturo Galvani

Journal Name: Combinatorial Chemistry & High Throughput Screening
Accelerated Technologies for Biotechnology, Bioassays, Medicinal Chemistry and Natural Products Research

Volume 11 , Issue 7 , 2008

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Abstract:

High-content analysis (HCA) is a term used to describe techniques involving multiplexed analysis of fluorescent markers to measure multiple cellular responses to biological stimuli or drug treatment. HCA is usually based on automated microscopy or related technologies, and its value lies in providing multiparametric information on single cells within a population. During the last decade, several HCA approaches have been developed and applied to assess cellular mechanism of action of pharmacologically relevant compounds identified through biochemical screening or similar in vitro methods. With automation and instrument development, these approaches have evolved to the extent that the technique is now routinely used in screening applications, including primary HTS on compound collections. Here, we review the field and discuss in particular the application of HCA to the discovery of small molecule inhibitors targeting kinases which are implicated in Oncology.

Keywords: High-content screening, kinase, cell-based assays

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Article Details

VOLUME: 11
ISSUE: 7
Year: 2008
Page: [523 - 536]
Pages: 14
DOI: 10.2174/138620708785204126
Price: $65

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