Halogenated tryptophan derivatives disrupt essential transamination mechanisms in bloodstream form Trypanosoma brucei.
Peter E CockramEmily A DickieMichael P BarrettTerry K SmithPublished in: PLoS neglected tropical diseases (2020)
Amino acid metabolism within Trypanosoma brucei, the causative agent of human African trypanosomiasis, is critical for parasite survival and virulence. Of these metabolic processes, the transamination of aromatic amino acids is one of the most important. In this study, a series of halogenated tryptophan analogues were investigated for their anti-parasitic potency. Several of these analogues showed significant trypanocidal activity. Metabolomics analysis of compound-treated parasites revealed key differences occurring within aromatic amino acid metabolism, particularly within the widely reported and essential transamination processes of this parasite.
Keyphrases
- amino acid
- plasmodium falciparum
- structure activity relationship
- molecular docking
- endothelial cells
- toxoplasma gondii
- escherichia coli
- mass spectrometry
- staphylococcus aureus
- trypanosoma cruzi
- pseudomonas aeruginosa
- antimicrobial resistance
- induced pluripotent stem cells
- single cell
- klebsiella pneumoniae
- multidrug resistant
- pluripotent stem cells
- free survival
- newly diagnosed
- molecular dynamics simulations
- candida albicans