Journal
MOLECULAR AND BIOCHEMICAL PARASITOLOGY
Volume 126, Issue 2, Pages 155-163Publisher
ELSEVIER SCIENCE BV
DOI: 10.1016/S0166-6851(02)00282-7
Keywords
protein farnesyl transferase; N-myristoyl transferase; protein prenylation
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Funding
- NCI NIH HHS [CA52874] Funding Source: Medline
- Wellcome Trust [061343] Funding Source: Medline
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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 (FIT) 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. (C) 2002 Elsevier Science B.V. All rights reserved.
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