Podophyllotoxin analogues active versus Trypanosoma brucei
نویسندگان
چکیده
منابع مشابه
Trypanosoma brucei brucei
Protein synthesis in Trypanosoma brucei brucei was rapidly inhibited during polyamine depletion by DL-adifluoromethylornithine (DFMO) in vitro and in vivo. [3H]Leucine incorporation was depressed 30-40 % by 24 h and 80-90 % by 48 h of DFMO treatment. Concomitantly there was an apparent decrease in the synthesis of the variant-specific glycoprotein (VSG) in DFMO-treated trypanosomes, as measured...
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Diesters based on N-benzyloxycarbonyl-S-(2,4-dinitrophenyl) GSH (CBzGSDNP) containing linear alcohols 3 to 9, branched alcohols 10 to 20, or heteroatom linear alcohols 21 to 25, were investigated as in vitro inhibitors of pathogenic parasites. Diesters 3 to 25 were better inhibitors of Trypanosoma brucei rhodesiense than of T. brucei brucei and had low cytotoxicities. The most active compound h...
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Trypanosoma brucei is a digenetic protozoan parasite presenting a public health hazard in certain areas of Africa; it is transmitted between mammals (bloodstream form (BSF)) by tsetse flies (procyclic form (PCF)). We have an ongoing interest in small GTP proteins in T. brucei, and these are commonly isoprenylated. Many isoprenylated proteins belong to the rab family and include ras; the isopren...
متن کاملSUMOylation in Trypanosoma brucei
Small ubiquitin like modifier (SUMO) proteins are involved in many processes in eukaryotes. We here show that Trypanosoma brucei SUMO (Tb927.5.3210) modifies many proteins. The levels of SUMOylation were unaffected by temperature changes but were increased by severe oxidative stress. We obtained evidence that trypanosome homologues of the SUMO conjugating enzyme Ubc9 (Tb927.2.2460) and the SUMO...
متن کاملDevelopment of Simplified Heterocyclic Acetogenin Analogues as Potent and Selective Trypanosoma brucei Inhibitors
Neglected tropical diseases caused by parasitic infections are an ongoing and increasing concern. They are a burden to human and animal health, having the most devastating effect on the world's poorest countries. Building upon our previously reported triazole analogues, in this study we describe the synthesis and biological testing of other novel heterocyclic acetogenin-inspired derivatives, na...
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ژورنال
عنوان ژورنال: Bioorganic & Medicinal Chemistry Letters
سال: 2010
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2010.01.009