Glycolysis as a target for the design of new anti-trypanosome drugs

Citation
Clm. Verlinde et al., Glycolysis as a target for the design of new anti-trypanosome drugs, DRUG RESIST, 4(1), 2001, pp. 50-65
Citations number
105
Categorie Soggetti
Pharmacology & Toxicology
Journal title
DRUG RESISTANCE UPDATES
ISSN journal
13687646 → ACNP
Volume
4
Issue
1
Year of publication
2001
Pages
50 - 65
Database
ISI
SICI code
1368-7646(200102)4:1<50:GAATFT>2.0.ZU;2-N
Abstract
Glycolysis is perceived as a promising target for new drugs against parasit ic trypanosomatid protozoa because this pathway plays an essential role in their ATP supply, Trypanosomatid glycolysis is unique in that it is compart mentalized, and many of its enzymes display unique structural and kinetic f eatures. Structure- and catalytic mechanism-based approaches are applied to design compounds that inhibit the glycolytic enzymes of the parasites with out affecting the corresponding proteins of the human host. For some trypan osomatid enzymes, potent and selective inhibitors have already been develop ed that affect only the growth of cultured trypanosomatids, and not mammali an cells. (C) 2001 Harcourt Publishers Ltd.