Galactosidase Enzyme Fragment Complementation as A Novel Technology for High Throughput Screening

Authors: Eglen R.M.; Singh R.

Source: Combinatorial Chemistry & High Throughput Screening, Volume 6, Number 4, June 2003 , pp. 381-387(7)

Publisher: Bentham Science Publishers

Abstract:

In this review, the applications of galactosidase complementation are described. Complementation is a naturally occurring process in bacteria and in engineered cells, and can also occur in eukaryotic cells. Two forms of complementation have been used in high throughput screening (HTS), in which interacting fragments complement with either low or high affinity. Low affinity complementation is used to monitor protein protein interactions, such as those occurring in homodimerization of the epidermal growth factor receptor (EGFR), and provides a robust screen for detection of EGFR inhibitors. High affinity complementation provides the basis for several HTS assays, in which analytes, such as cAMP or IP3, are detected in crude cell lysates. A development of the latter approach is protein labeling, providing for measurement of cell protein expression and trafficking. Collectively, the use of galactosidase complementation provides a novel and flexible technology for highly sensitive, homogeneous HTS assay development.

Keywords: enzyme fragment complementation; galactosidase; homogenous hts assays; protein:protein interactions; protein expression; g protein coupled receptors; proteases; receptor kinases

Language: English

Document Type: Review article

DOI: http://dx.doi.org/10.2174/138620703106298473

Publication date: 2003-06-01

• Combinatorial Chemistry & High Throughput Screening publishes full length original research articles and reviews describing various topics in combinatorial chemistry (e.g. small molecules, peptide, nucleic acid or phage display libraries) and/or high throughput screening (e.g. developmental, practical or theoretical). Ancillary subjects of key importance, such as robotics and informatics, will also be covered by the journal. In these respective subject areas, Combinatorial Chemistry & High Throughput Screening is intended to function as the most comprehensive and up-to-date medium available. The journal should be of value to individuals engaged in the process of drug discoveryand development, in the settings of industry, academia or government.

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• In this Subject: Pharmacology
• By this author: Eglen R.M. ;  Singh R.

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