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To accelerate progress in the development of therapeutics for protozoan parasitic diseases, we are studying enzymes active in co- and post-translational protein modification that are already the focus of drug development in other eukaryotic systems. Inhibitors of the protein farnesyltransferases (PFT) are well-established antitumour agents of low cytotoxicity and known pharmokinetic properties, while inhibitors of N-myristoyl transferase show both selectivity and specificity in the treatment of fungal infections. Here, we summarise the current evidence that supports the targeting of these ubiquitous eukaryotic enzymes for drug development against trypanosomatid infections and malaria.

Type

Journal article

Journal

Mol Biochem Parasitol

Publication Date

02/2003

Volume

126

Pages

155 - 163

Keywords

Acyltransferases, Alkyl and Aryl Transferases, Animals, Antimalarials, Chemistry, Pharmaceutical, Drug Design, Plasmodium, Protein Conformation, Trypanocidal Agents, Trypanosoma