ArticleThe Biochemical journal2014
Biochemical and genetic characterization of Trypanosoma cruzi N-myristoyltransferase.
Article in The Biochemical journal, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 25 papers.
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Who cites it
25 citing papers in PubMed, 34 citations in OpenAlex.
- Trypanosoma cruzi cell atlas as a single-cell resource for understanding parasite population heterogeneity and differentiation.Nature communications · 2026Article
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- Untargeted metabolomics for triaging of cytochrome b inhibitors during Chagas' disease drug discovery.PLoS neglected tropical diseases · 2026Article
- Structure guided modification of 2-chloro-5-(ethyl-phenyl-sulfamoyl)-N-[2-(2-oxo-pyrrolidin-1-yl)-phenyl]-benzamide to afford selective inhibitors of Cryptosporidium parvum N-myristoyltransferase.Bioorganic & medicinal chemistry letters · 2025Article
- AdvancingFrontiers in molecular biosciences · 2025Article
- A versatile 2A peptide-based strategy for ectopic expression and endogenous gene tagging inHeliyon · 2024Article
- Identification of and Structural Insights into Hit Compounds TargetingACS infectious diseases · 2023Article
- Identification of a Proteasome-Targeting Arylsulfonamide with Potential for the Treatment of Chagas' Disease.Antimicrobial agents and chemotherapy · 2022Article
- Live-imaging rate-of-kill compound profiling for Chagas disease drug discovery with a new automated high-content assay.PLoS neglected tropical diseases · 2021Article
- A Not-So-Ancient Grease History: Click Chemistry and Protein Lipid Modifications.Chemical reviews · 2021Review
- Defeating the trypanosomatid trio: proteomics of the protozoan parasites causing neglected tropical diseases.RSC medicinal chemistry · 2020Review
- The QACS infectious diseases · 2020Article
- Advances in preclinical approaches to Chagas disease drug discovery.Expert opinion on drug discovery · 2019Review
- Phenotypic Screens Reveal Posaconazole as a Rapidly Acting Amebicidal Combination Partner for Treatment of Primary Amoebic Meningoencephalitis.The Journal of infectious diseases · 2019Article
- Pharmacological Validation of N-Myristoyltransferase as a Drug Target in Leishmania donovani.ACS infectious diseases · 2019Article
- Genetically Validated Drug Targets in Leishmania: Current Knowledge and Future Prospects.ACS infectious diseases · 2018Review
- The N-myristoylome of Trypanosoma cruzi.Scientific reports · 2016Article
- Global Profiling and Inhibition of Protein Lipidation in Vector and Host Stages of the Sleeping Sickness ParasiteACS infectious diseases · 2016Article
- Validation of N-myristoyltransferase as Potential Chemotherapeutic Target in Mammal-Dwelling Stages of Trypanosoma cruzi.PLoS neglected tropical diseases · 2016Article
- Analyses of the Binding between Water Soluble C60 Derivatives and Potential Drug Targets through a Molecular Docking Approach.PloS one · 2016Article
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
Abstract
Co- and post-translational N-myristoylation is known to play a role in the correct subcellular localization of specific proteins in eukaryotes. The enzyme that catalyses this reaction, NMT (N-myristoyltransferase), has been pharmacologically validated as a drug target in the African trypanosome, Trypanosoma brucei. In the present study, we evaluate NMT as a potential drug target in Trypanosoma cruzi, the causative agent of Chagas' disease, using chemical and genetic approaches. Replacement of both allelic copies of TcNMT (T. cruzi NMT) was only possible in the presence of a constitutively expressed ectopic copy of the gene, indicating that this gene is essential for survival of T. cruzi epimastigotes. The pyrazole sulphonamide NMT inhibitor DDD85646 is 13-23-fold less potent against recombinant TcNMT than TbNMT (T. brucei NMT), with Ki values of 12.7 and 22.8 nM respectively, by scintillation proximity or coupled assay methods. DDD85646 also inhibits growth of T. cruzi epimastigotes (EC50=6.9 μM), but is ~1000-fold less potent than that reported for T. brucei. On-target activity is demonstrated by shifts in cell potency in lines that over- and under-express NMT and by inhibition of intracellular N-myristoylation of several proteins in a dose-dependent manner. Collectively, our findings suggest that N-myristoylation is an essential and druggable target in T. cruzi.
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