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READ-UP


Redox antimalarial drug discovery
EC contribution
: € 2.000.000
Duration
: 36 months
Starting date
: 01/12/2005
Funding scheme
: Specific Targeted Research Project
Keywords
: human parasitology, pharmaceutical chemistry, malaria, drug candidate, hit-to-lead optimisation, innovative Redox concept, developing countries
Contract/Grant agreement number
: LSHP-CT-2005-018602
Project web-site
: http://www.ird.fr/read-up/spip.php?rubrique3

Background:

The READ-UP project aims at identifying antimalarial drug candidates (one candidate and two back-ups). The project will begin with a hit identified in the first series, enlarging it, and designing other series through the different steps of drug discovery and hit-to-lead optimisation from the pilot scale production towards pre-clinical studies.

Artemisinin, the natural antimalarial product, and its derivatives are increasingly important in the treatment of drug-resistant malaria as they are the most potent antimalarials available, rapidly killing all blood stages of the malaria parasite. Artemisinins contain an endoperoxide bridge which plays a key role in the antimalarial activity with a mode of action starting from radical transient species initiated by the cleavage of this bridge. The READ-UP project starts from the unique mode of action of artemisinins to develop a completely new approach: initiate radical transient species within the parasitised red blood cell in such a way that no endoperoxide bridge is required.

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