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Publication Details
AFRICAN RESEARCH NEXUS
SHINING A SPOTLIGHT ON AFRICAN RESEARCH
biochemistry, genetics and molecular biology
A trypanosome oligopeptidase as a target for the trypanocidal agents pentamidine, diminazene and suramin
FEBS Letters, Volume 433, No. 3, Year 1998
Notification
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Description
African trypanosomes contain a cytosolic serine oligopeptidase, called OP-Tb, that is reversibly inhibited by the active principles of three of the five most commonly used trypanocidal drugs: pentamidine, diminazene and suramin. OP-Tb was inhibited by pentamidine in a competitive manner, and by suramin in a partial, non-competitive manner. The inhibition of OP-Tb by a variety of suramin analogues correlated with the trypanocidal efficacy of these analogues (P=0.03; by paired Student's t-test). Since intracellular (therapeutic) concentrations of pentamidine and suramin are reported to reach approximately 206Ki and 15Ki respectively, we suggest that these drugs may exert part of their trypanocidal activity through the inhibition of OP-Tb. © 1998 Federation of European Biochemical Societies.
Authors & Co-Authors
Morty, Rory Edward
South Africa, Durban
University of Kwazulu-natal
Troeberg, Linda
South Africa, Durban
University of Kwazulu-natal
Pike, Robert N.
Australia, Clayton
Monash University
Jones, Roy
United Kingdom, Cambridge
The Babraham Institute
Nickel, Peter
Germany, Bonn
Universität Bonn
Lonsdale-Eccles, John David
United States, Birmingham
Department of Biochemistry and Molecular Genetics
Coetzer, Theresa HT
South Africa, Durban
University of Kwazulu-natal
Statistics
Citations: 80
Authors: 7
Affiliations: 5
Identifiers
Doi:
10.1016/S0014-5793(98)00914-4
ISSN:
00145793
Research Areas
Infectious Diseases