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Deoxyuridine Triphosphate Nucleotidohydrolase as a drug target against Malaria

Objective

There are around 500 million clinical cases of malaria each year and about 1-2 million people die from this debilitating disease. There is an urgent need for the development of new drugs owing to problems with drug resistance. New drugs should have novel mechanisms of action to prevent cross-resistance with existing drugs. We have discovered some novel, drug-like and selective inhibitors of the Plasmodium enzyme, deoxyuridine triphosphate nucleotidohydrolase (dUTPase). The role of the enzyme is to hydrolyse dUTP to dUMP, maintaining a low dUTP:dTTP ratio. The aim of this project is to optimise these early lead molecules to generate preclinical drug candidates. The project will consist of: medicinal chemistry to prepare and optimise lead compounds; ADME-Tox assays to ensure that the compounds have correct 'drug-like' properties; assays to determine the efficacy of the compounds; mode of action studies; crystallography of inhibitors with the enzyme active site to assist in the drug design process.'

Call for proposal

FP6-2005-LIFESCIHEALTH-7
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Coordinator

UNIVERSITY OF DUNDEE
Address
Nethergate
Dundee
United Kingdom

Participants (4)

MEDIVIR AB
Sweden
Address
Lunastigen 7
Huddinge
AGENCIA ESTATAL CONSEJO SUPERIOR DE INVESTIGACIONES CIENTIFICAS
Spain
Address
Serrano 117
Madrid
UNIVERSITY OF YORK
United Kingdom
Address
Heslington
York
SWISS TROPICAL INSTITUTE
Switzerland
Address
Socinstrasse 57
Basel