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Current Medicinal Chemistry


ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

6-Phosphogluconate Dehydrogenase: A Target for Drugs in African Trypanosomes

Author(s): Stefania Hanau, Eliana Rinaldi, Franco Dallocchio, Ian H. Gilbert, Christophe Dardonville, Margaret J. Adams, Sheila Gover and Michael P. Barrett

Volume 11 , Issue 19 , 2004

Page: [2639 - 2650] Pages: 12

DOI: 10.2174/0929867043364441

Price: $65


New drugs are urgently required for Human African Trypanosomiasis (sleeping sickness), a disease which has re-emerged as a major health threat in Sub-Saharan Africa. The third enzyme of the pentose phosphate pathway, 6-phosphogluconate dehydrogenase, has been shown to be a good target for drugs. The enzyme is essential to the trypanosomes that causes sleeping sickness and structural differences when compared to its mammalian counterpart allow for selective inhibition. Three series of inhibitors have been designed, these include phosphorylated carbohydrate substrate and transition state analogues, noncarbohydrate substrate analogues and also triphenylmethane-based compounds. All have shown selective inhibition of the trypanosomal 6-phosphogluconate dehydrogenase and representatives of each have trypanocidal activity.

Keywords: human african trypanosomiasis, sleeping sickness, chemotherapy, drugs, pentose phosphate pathway, 6- phosphogluconate dehydrogenase, transition state inhibitor, triphenylmethane

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