title: Drug target identification using a trypanosome overexpression library.
abstract: 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.
authors: Zentrum für Molekulare Biologie der Universität Heidelberg, DKFZ-ZMBH Alliance, Heidelberg, Germany d.begolo@zmbh.uni-heidelberg.de cclayton@zmbh.uni-heidelberg.de.
authors: Daniela
authors: D
authors: Begolo
authors: Zentrum für Molekulare Biologie der Universität Heidelberg, DKFZ-ZMBH Alliance, Heidelberg, Germany.
authors: Esteban
authors: E
authors: Erben
authors: Zentrum für Molekulare Biologie der Universität Heidelberg, DKFZ-ZMBH Alliance, Heidelberg, Germany d.begolo@zmbh.uni-heidelberg.de cclayton@zmbh.uni-heidelberg.de.
authors: Christine
authors: C
authors: Clayton
mesh_terms: D000217:Acyltransferases / Q000378:metabolism; D000631:Aminopyridines / Q000494:pharmacology; D000518:Eflornithine / Q000494:pharmacology; D009955:Ornithine Decarboxylase / Q000378:metabolism; D013449:Sulfonamides / Q000494:pharmacology; D014344:Trypanocidal Agents / Q000494:pharmacology*; D014346:Trypanosoma brucei brucei / Q000187:drug effects*; D000096926:Benzenesulfonamides
chemical_list: D000217:Acyltransferases; D000631:Aminopyridines; D000518:Eflornithine; D009955:Ornithine Decarboxylase; D013449:Sulfonamides; D014344:Trypanocidal Agents; C549249:DDD 85646; D000096926:Benzenesulfonamides; C050480:glycylpeptide N-tetradecanoyltransferase