6-phosphogluconate dehydrogenase: A target for drugs in African trypanosomes

Stefania Hanau; Eliana Rinaldi; Franco Dallocchio; Ian H. Gilbert; Christophe Dardonville; Margaret J. Adams; Sheila Gover; Michael P.  Barrett

doi:10.2174/0929867043364441

6-phosphogluconate dehydrogenase: A target for drugs in African trypanosomes

Stefania Hanau
, Eliana Rinaldi
, Franco Dallocchio
, Ian H. Gilbert
, Christophe Dardonville
, Margaret J. Adams
, Sheila Gover
, Michael P. Barrett

Research output: Contribution to journal › Review article › peer-review

30 Citations (Scopus)

Abstract

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.

Original language	English
Pages (from-to)	2639-2650
Number of pages	12
Journal	Current Topics in Medicinal Chemistry
Volume	11
Issue number	19
DOIs	https://doi.org/10.2174/0929867043364441
Publication status	Published - Oct 2004

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

SDG 3 Good Health and Well-being

Access to Document

10.2174/0929867043364441

Cite this

@article{3d29aae0bc4d4159ac9bc45132dc144a,

title = "6-phosphogluconate dehydrogenase: A target for drugs in African trypanosomes",

abstract = "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.",

author = "Stefania Hanau and Eliana Rinaldi and Franco Dallocchio and Gilbert, \{Ian H.\} and Christophe Dardonville and Adams, \{Margaret J.\} and Sheila Gover and Barrett, \{Michael P.\}",

year = "2004",

month = oct,

doi = "10.2174/0929867043364441",

language = "English",

volume = "11",

pages = "2639--2650",

journal = "Current Topics in Medicinal Chemistry",

issn = "1873-4294",

publisher = "Bentham Science Publishers",

number = "19",

}

TY - JOUR

T1 - 6-phosphogluconate dehydrogenase

T2 - A target for drugs in African trypanosomes

AU - Hanau, Stefania

AU - Rinaldi, Eliana

AU - Dallocchio, Franco

AU - Gilbert, Ian H.

AU - Dardonville, Christophe

AU - Adams, Margaret J.

AU - Gover, Sheila

AU - Barrett, Michael P.

PY - 2004/10

Y1 - 2004/10

N2 - 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.

AB - 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.

U2 - 10.2174/0929867043364441

DO - 10.2174/0929867043364441

M3 - Review article

SN - 1873-4294

VL - 11

SP - 2639

EP - 2650

JO - Current Topics in Medicinal Chemistry

JF - Current Topics in Medicinal Chemistry

IS - 19

ER -

6-phosphogluconate dehydrogenase: A target for drugs in African trypanosomes

Abstract

UN SDGs

Access to Document

Fingerprint

Cite this