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The Sound of Evolution
Melarsoprol
Mechanism of action:
Melarsoprol is an arsenical molecule. The trivalent arsenic (As3+) in Melarsoprol forms stable bonds with sulfhydryl (-SH) groups in parasite proteins, especially trypanothione and its related enzyme systems. Trypanosoma brucei depends on the trypanothione reductase system to maintain redox balance and eliminate reactive oxygen species. By inhibiting this system, Melarsoprol prevents the parasite from resisting oxidative stress.
Reference(s):
Zheng Y et al. (2023). Discovery of 5-Phenylpyrazolopyrimidinone Analogs as Potent Antitrypanosomal Agents with In Vivo Efficacy. Journal of Medicinal Chemistry.
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