Abstract:
:Trypanothione reductase (TR) is a major enzyme in trypanosomatids. Its substrate, trypanothione is a molecule containing a tripeptide (L-glutamic acid-cysteine-glycine) coupled to a polyamine, spermidine. This redox system (TR/Trypanothione) is vital for parasite survival within the host cell and has been described as a good target for chemotherapy anti-Leishmania. The use of tripeptides analogs of glutathione would result in a decrease in trypanothione synthesis and as a consequence in TR activity. In this work, besides the enzyme potential inhibition, it also evaluated the influence of those analogs on parasite growth and on its infective capacity. The results showed a significant effect on parasite growth and infectivity and in addition TR activity was highly inhibited. These results are very promising, suggesting a potential use of those analogs as therapeutic drugs against experimental diseases caused by trypanosomatids.
journal_name
J Enzyme Inhib Med Chemjournal_title
Journal of enzyme inhibition and medicinal chemistryauthors
Castro-Pinto DB,Lima EL,Cunha AS,Genestra M,De Léo RM,Monteiro F,Leon LLdoi
10.1080/14756360600920180subject
Has Abstractpub_date
2007-02-01 00:00:00pages
71-5issue
1eissn
1475-6366issn
1475-6374journal_volume
22pub_type
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journal_title:Journal of enzyme inhibition and medicinal chemistry
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