Unraveling the antitrypanosomal mechanism of benznidazole and related 2‐nitroimidazoles: From prodrug activation to DNA damage

Nitroheterocycles represent an important class of compound used to treat trypanosomiasis. They often function as prodrugs and can undergo type I nitroreductase (NTR1)‐mediated activation before promoting their antiparasitic activities although the nature of these downstream effects has yet to be det...

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Veröffentlicht in:	Molecular microbiology 2021-08, Vol.116 (2), p.674-689
Hauptverfasser:	Dattani, Ambika, Drammeh, Isatou, Mahmood, Aishah, Rahman, Mahbubur, Szular, Joanna, Wilkinson, Shane R.
Format:	Artikel
Sprache:	eng
Schlagworte:	Activation, Metabolic - physiology Antiparasitic agents Benznidazole CRISPR gene editing Damage Deoxyribonucleic acid DNA DNA Breaks, Double-Stranded - drug effects DNA damage DNA repair DNA Repair - drug effects DNA Repair - genetics Drug development Eukaryotes fluorescence profiling gene deletion Genome, Protozoan - drug effects Genome, Protozoan - genetics Genomes Homologous recombination Homology Lesions Nitroimidazole Nitroimidazoles - pharmacology Nitroreductase Nitroreductases - metabolism Nucleotide excision repair Nucleotide sequence Nucleotides prodrug activation Prodrugs Prodrugs - chemistry Repair Transcription Trypanocidal Agents - pharmacology Trypanosoma brucei brucei - drug effects Trypanosoma brucei brucei - genetics Trypanosoma brucei brucei - metabolism Trypanosome Trypanosomiasis Trypanosomiasis, African - drug therapy Vector-borne diseases
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