Drug Target Identification Using a Trypanosome Overexpression Library

被引：25

作者：

Begolo, Daniela ^{[1
]}

Erben, Esteban ^{[1
]}

Clayton, Christine ^{[1
]}

机构：

[1] Heidelberg Univ, Zentrum Mol Biol, DKFZ ZMBH Alliance, Heidelberg, Germany

来源：

ANTIMICROBIAL AGENTS AND CHEMOTHERAPY | 2014年 / 58卷 / 10期

关键词：

N-MYRISTOYLTRANSFERASE INHIBITORS; RESISTANT LEISHMANIA; BLOOD-STREAM; PLASMODIUM-FALCIPARUM; BRUCEI; TRYPANOTHIONE; AMPLIFICATION; DISCOVERY; REDUCTASE; IDENTIFY;

D O I：

10.1128/AAC.03338-14

中图分类号：

Q93 [微生物学];

学科分类号：

071005 ; 100705 ;

摘要：

Elucidation of molecular targets is very important for lead optimization during the drug development process. We describe a direct method to find targets of antitrypanosomal compounds against Trypanosoma brucei using a trypanosome overexpression library. As proof of concept, we treated the library with difluoromethylornithine and DDD85646 and identified their respective targets, ornithine decarboxylase and N-myristoyltransferase. The overexpression library could be a useful tool to study the modes of action of novel antitrypanosomal drug candidates.

引用

页码：6260 / 6264

页数：5

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