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Updated: Dec 23, 2025
In Vitro Drug Screening Against All Life Cycle Stages of Trypanosoma cruzi Using Parasites Expressing β-galactosidase
Published on: November 5, 2021
High-throughput screening affords novel and selective trypanothione reductase inhibitors with anti-trypanosomal
Derek C Martyn1, Deuan C Jones, Alan H Fairlamb
1Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA, USA.
Abstract:
Trypanothione reductase (TR), an enzyme that buffers oxidative stress in trypanosomatid parasites, was screened against commercial libraries containing approximately 134,500 compounds. After secondary screening, four chemotypes were identified as screening positives with selectivity for TR over human glutathione reductase. Thirteen compounds from these four chemotypes were purchased, and their in vitro activity against TR and Trypanosoma brucei is described.
