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Turning the tables on drug discovery

EUREKA project E! 2314 O'SCREEN reverses the traditional screening process used to discover potentially active new pharmaceutical compounds. Testing single, targeted molecules rather than tens of thousands it promises vastly increased efficiency in drug discovery.

Until now, new molecules with the potential to be developed as drugs have been discovered by screening thousands of candidate new molecules and developing those showing potential activity in some therapeutic area. But the process is extremely expensive and wasteful. Now, a radical new option couples this unique approach with bioinformatics resources.

Reverse approach
Project coordinator Dr Jean-Yves Berthon from French pharmaceuticals company Greentech explains the way this 'reverse approach' developed. "We have a large database of 30,000 plants, with information on their botany, physiology, chemical components and their applications; also another database on 300,000 natural molecules coming from plants. We reasoned that if we had an idea of what molecules would have a particular pharmaceutical effect, we could find a natural source in our databases." Greentech's partner in the project was Drug Discovery Ltd, part of the natural products business of the Strathclyde Institute for Drug Research in Scotland, which has focused on identifying lead molecules from natural sources for drug development.

The method starts with knowledge of the key enzymes involved in particular diseases, such as acetylcholinesterase in the case of Alzheimer's disease. Project team biochemists researched and identified what chemical entities (ligands) could be attached to the enzyme to alter its behaviour. They then consulted the databases of plant-derived molecules and plants to discover the natural sources of the ligands which could influence the enzyme. Identified in this way substances can then be extracted from the identified plant material and subjected to early-stage potentiality testing.
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Contact: Shiels
catherine.shiels@es.eureka.be
322-770-0969
EUREKA
24-May-2006


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