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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.

Type

Journal article

Journal

FEBS Lett

Publication Date

21/08/1998

Volume

433

Pages

251 - 256

Keywords

Animals, Diminazene, Pentamidine, Serine Endopeptidases, Serine Proteinase Inhibitors, Structure-Activity Relationship, Suramin, Trypanocidal Agents, Trypanosoma