ArticleChemMedChem2012
Design, synthesis and biological evaluation of Trypanosoma brucei trypanothione synthetase inhibitors.
Article in ChemMedChem, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
17 citing papers in PubMed, 44 citations in OpenAlex.
- Targeting Trypanothione Metabolism in Trypanosomatids.Molecules (Basel, Switzerland) · 2024Review
- Drug-like molecules with anti-trypanothione synthetase activity identified by high throughput screening.Journal of enzyme inhibition and medicinal chemistry · 2022Article
- Novel 3-chloro-6-nitro-1Journal of enzyme inhibition and medicinal chemistry · 2022Article
- Ensemble learning application to discover new trypanothione synthetase inhibitors.Molecular diversity · 2021Article
- Mechanistic and biological characterisation of novelJournal of enzyme inhibition and medicinal chemistry · 2020Article
- Future Prospects in the Treatment of Parasitic Diseases: 2-Amino-1,3,4-Thiadiazoles in Leishmaniasis.Molecules (Basel, Switzerland) · 2019Review
- Discovery and Genetic Validation of Chemotherapeutic Targets for Chagas' Disease.Frontiers in cellular and infection microbiology · 2018Review
- Inhibition of Leishmania infantum trypanothione reductase by diaryl sulfide derivatives.Journal of enzyme inhibition and medicinal chemistry · 2017Article
- Anti-trypanosomatid drug discovery: an ongoing challenge and a continuing need.Nature reviews. Microbiology · 2017Review
- Trypanosoma brucei DHFR-TS Revisited: Characterisation of a Bifunctional and Highly Unstable Recombinant Dihydrofolate Reductase-Thymidylate Synthase.PLoS neglected tropical diseases · 2016Article
- Identification of Novel Chemical Scaffolds Inhibiting Trypanothione Synthetase from Pathogenic Trypanosomatids.PLoS neglected tropical diseases · 2016Article
- Genetic validation of Trypanosoma brucei glutathione synthetase as an essential enzyme.Eukaryotic cell · 2014Article
- Application of fundamental organometallic chemistry to the development of a gold-catalyzed synthesis of sulfinate derivatives.Angewandte Chemie (International ed. in English) · 2014Article
- Target-based drug discovery for human African trypanosomiasis: selection of molecular target and chemical matter.Parasitology · 2014Review
- Drug discovery for neglected diseases: molecular target-based and phenotypic approaches.Journal of medicinal chemistry · 2013Review
- Product feedback regulation implicated in translational control of the Trypanosoma brucei S-adenosylmethionine decarboxylase regulatory subunit prozyme.Molecular microbiology · 2013Article
- Trypanosoma brucei S-adenosylmethionine decarboxylase N terminus is essential for allosteric activation by the regulatory subunit prozyme.The Journal of biological chemistry · 2013Article
Corrections and comments
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Authors and funding
9 authors at 1 institution in 2 countries.
Funding
Abstract
Trypanothione synthetase (TryS) is essential for the survival of the protozoan parasite Trypanosoma brucei, which causes human African trypanosomiasis. It is one of only a handful of chemically validated targets for T. brucei in vivo. To identify novel inhibitors of TbTryS we screened our in-house diverse compound library that contains 62,000 compounds. This resulted in the identification of six novel hit series of TbTryS inhibitors. Herein we describe the SAR exploration of these hit series, which gave rise to one common series with potency against the enzyme target. Cellular studies on these inhibitors confirmed on-target activity, and the compounds have proven to be very useful tools for further study of the trypanothione pathway in kinetoplastids.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.