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MetabolomicsSmall Polar Hits against S. aureus: Screening, Initial Hit Optimization, and Metabolomic Studies
The global prevalence of antibacterial resistance requires new antibacterial drugs with novel chemical scaffolds and modes of action. It is also vital to design compounds with optimal physicochemical properties to permeate the bacterial cell envelope. We described an approach of combining and integr...
2021-11-04 | MTBLS788 | MetaboLights
MetabolomicsUntargeted Metabolomics To Ascertain Antibiotic Modes of Action
Deciphering the mode of action (MOA) of new antibiotics discovered through phenotypic screening is of increasing importance. Metabolomics offers a potentially rapid and cost-effective means of identifying modes of action of drugs whose effects are mediated through changes in metabolism. Metabolomics...
2017-06-16 | MTBLS464 | MetaboLights
MetabolomicsUntargeted Metabolomics Reveals a Lack Of Synergy between Nifurtimox and Eflornithine against Trypanosoma brucei
A non-targeted metabolomics-based approach is presented that enables the study of pathways in response to drug action with the aim of defining the mode of action of trypanocides. Eflornithine, a polyamine pathway inhibitor, and nifurtimox, whose mode of action involves its metabolic activation, are ...
2017-06-07 | MTBLS459 | MetaboLights
MetabolomicsMetabolomics identifies multiple candidate biomarkers to diagnose and stage human African trypanosomiasis
Treatment for human African trypanosomiasis is dependent on the species of trypanosome causing the disease and the stage of the disease (stage 1 defined by parasites being present in blood and lymphatics whilst for stage 2, parasites are found beyond the blood-brain barrier in the cerebrospinal flui...
2018-01-24 | MTBLS413 | MetaboLights
MetabolomicsHost-parasite co-metabolic activation of antitrypanosomal aminomethyl-benzoxaboroles
Recent development of benzoxaborole-based chemistry gave rise to a collection of compounds with great potential in targeting diverse infectious diseases, including human African Trypanosomiasis (HAT), a devastating neglected tropical disease. However, further medicinal development is largely restric...
2018-02-12 | MTBLS452 | MetaboLights
MetabolomicsMetabolomic profiling of macrophages determines the discrete metabolomic signature and metabolomic interactome triggered by polarising immune stimuli
Priming and activating immune stimuli have profound effects on macrophages, however, studies generally evaluate stimuli in isolation rather than in combination. In this study we have investigated the effects of pro-inflammatory and anti-inflammatory stimuli either alone or in combination on macropha...
2018-03-13 | MTBLS570 | MetaboLights
MetabolomicsVeterinary trypanocidal benzoxaboroles are peptidase-activated prodrugs (T. congolense assay)

Livestock diseases caused by Trypanosoma congolense, T. vivax and T. brucei, collectively known as nagana, are responsible for billions of dollars in lost food production annually. There is an urgent need for novel therapeutics. Encouragingly, promising antitrypanosomal benzoxaboroles are under v...

2020-10-22 | MTBLS1309 | MetaboLights
MetabolomicsVeterinary trypanocidal benzoxaboroles are peptidase-activated prodrugs (T. brucei assay)

Livestock diseases caused by Trypanosoma congolense, T. vivax and T. brucei, collectively known as nagana, are responsible for billions of dollars in lost food production annually. There is an urgent need for novel therapeutics. Encouragingly, promising antitrypanosomal benzoxaboroles are under v...

2020-09-23 | MTBLS1474 | MetaboLights
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