Whole-Cell Screening Results

In May 2010, GlaxoSmithKlme (GSK), Tres Cantos, St. Jude Children s Research Hospital, Memphis, and Novartis - NITD/GNF - all published the full data from their combined malaria phenotypic screening efforts. Their data, on 

Organization Library size 3D7 Screening concentration No. of confirmed hits % Hit rate 

Additional screening has since been conducted with compound libraries from AstraZeneca, Pfizer, Sanofi, Evotec, Genzyme, the UK MRCT, the Biofocus Soft focus collection, and the Broad Institute. The summary of the published data is shown in Table 24.1. 

Repositioning of Clinical Candidates Developed for Other Indications 

The most rapid route to finding a clinically effective compound is to screen focused hbraries of compoimds that represent pharma clinical candidates - ideally that have been into volunteers or patients - but which have been halted due to lack of efficacy or a change in strategy. Since the achievable free plasma concentrations in man are known, it is relatively easy to triage such molecules for further clinical development An exercise such as this has been conducted 

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It should also be noted that both screening methods and selection methods have their own advantages and disadvantages. Screening involves physically or chemically interrogating every mutant protein in a library individually, and is often implemented in a 96-well plate format using plate readers. As a result, its throughput is relatively low (the size of the library that can be screened is limited to 10" ). However, because the screens are done in vitro with whole cells, cell... 

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