酿酒酵母、克氏锥虫、卡氏肺孢子虫和拟南芥的氧化鲨烯环化酶在酵母中的表达：一种新型抗寄生虫药物开发的模型。

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

机构信息

Dipartimento di Scienza e Tecnologia del Farmaco, Università di Torino, via P. Giuria 9, 10125 Torino, Italy.

出版信息

Bioorg Med Chem Lett. 2009 Feb 1;19(3):718-23. doi: 10.1016/j.bmcl.2008.12.040. Epub 2008 Dec 14.

DOI:10.1016/j.bmcl.2008.12.040

PMID:19119009

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.

摘要

一系列 25 种化合物，其中一些先前被描述为抑制人肝微粒体角鲨烯环氧化酶 (OSC) 的化合物，被测试为抑制酿酒酵母、克氏锥虫、卡氏肺孢子虫和拟南芥 OSCs 的抑制剂，这些 OSCs 在酿酒酵母的 OSC 缺陷株中表达。筛选鉴定出三种衍生物特别有希望开发新型抗锥虫药物，八种衍生物有希望开发新型抗肺孢子虫药物。