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
Combinatorial Chemistry & High Throughput Screening
Title: High-Content Analysis of Kinase Activity in Cells
Volume: 11 Issue: 7
Author(s): Fabio Gasparri, Francesco Sola, Tiziano Bandiera, Jurgen Moll and Arturo Galvani
Affiliation:
Keywords: High-content screening, kinase, cell-based assays
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.
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Cite this article as:
Gasparri Fabio, Sola Francesco, Bandiera Tiziano, Moll Jurgen and Galvani Arturo, High-Content Analysis of Kinase Activity in Cells, Combinatorial Chemistry & High Throughput Screening 2008; 11 (7) . https://dx.doi.org/10.2174/138620708785204126
DOI https://dx.doi.org/10.2174/138620708785204126 |
Print ISSN 1386-2073 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5402 |
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