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Bioorganic and Medicinal Chemistry Letters 2009-Feb

Oxidosqualene cyclase from Saccharomyces cerevisiae, Trypanosoma cruzi, Pneumocystis carinii and Arabidopsis thaliana expressed in yeast: a model for the development of novel antiparasitic agents.

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Gianni Balliano
Henrietta Dehmlow
Simonetta Oliaro-Bosso
Matilde Scaldaferri
Silvia Taramino
Franca Viola
Giulia Caron
Johannes Aebi
Jean Ackermann

Keywords

Abstract

A series of 25 compounds, some of which previously were described as inhibitors of human liver microsomal oxidosqualene cyclase (OSC), were tested as inhibitors of Saccharomyces cerevisiae, Trypanosoma cruzi, Pneumocystis carinii and Arabidopsis thaliana OSCs expressed in an OSC-defective strain of S. cerevisiae. The screening identified three derivatives particularly promising for the development of novel anti-Trypanosoma agents and eight derivatives for the development of novel anti-Pneumocystis agents.

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