ArticlePLoS neglected tropical diseases2016
Validation of N-myristoyltransferase as Potential Chemotherapeutic Target in Mammal-Dwelling Stages of Trypanosoma cruzi.
Article in PLoS neglected tropical diseases, 2016. 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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Who cites it
17 citing papers in PubMed, 27 citations in OpenAlex.
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- Drug discovery in leishmaniasis using protein lipidation as a target.Biophysical reviews · 2021Review
- A Not-So-Ancient Grease History: Click Chemistry and Protein Lipid Modifications.Chemical reviews · 2021Review
- Article
- NMT1 and NMT2 are lysine myristoyltransferases regulating the ARF6 GTPase cycle.Nature communications · 2020Article
- Exploring NovelACS omega · 2019Article
- Exploring protein myristoylation in Toxoplasma gondii.Experimental parasitology · 2019Article
- Validation and Invalidation of Chemical Probes for the Human N-myristoyltransferases.Cell chemical biology · 2019Article
- Pharmacological Validation of N-Myristoyltransferase as a Drug Target in Leishmania donovani.ACS infectious diseases · 2019Article
- Treatment of Trypanosoma cruzi with 2-bromopalmitate alters morphology, endocytosis, differentiation and infectivity.BMC cell biology · 2018Article
- Virtual screening to identify Leishmania braziliensis N-myristoyltransferase inhibitors: pharmacophore models, docking, and molecular dynamics.Journal of molecular modeling · 2018Article
- Protein Lipidation: Occurrence, Mechanisms, Biological Functions, and Enabling Technologies.Chemical reviews · 2018Article
- Design and Synthesis of Brain Penetrant Trypanocidal N-Myristoyltransferase Inhibitors.Journal of medicinal chemistry · 2017Article
- Dynamic protein S-palmitoylation mediates parasite life cycle progression and diverse mechanisms of virulence.Critical reviews in biochemistry and molecular biology · 2017Review
- Structure and Functional Diversity of GCN5-Related N-Acetyltransferases (GNAT).International journal of molecular sciences · 2016Review
Corrections and comments
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Authors and funding
13 authors at 2 institutions in 2 countries.
Funding
Abstract
backgroundTrypanosoma cruzi causes Chagas disease, an endemic and debilitating illness in Latin America. Lately, owing to extensive population movements, this neglected tropical disease has become a global health concern. The two clinically available drugs for the chemotherapy of Chagas disease have rather high toxicity and limited efficacy in the chronic phase of the disease, and may induce parasite resistance. The development of new anti-T. cruzi agents is therefore imperative. The enzyme N-myristoyltransferase (NMT) has recently been biochemically characterized, shown to be essential in Leishmania major, Trypanosoma brucei, and T. cruzi¸ and proposed as promising chemotherapeutic target in these trypanosomatids. METHODOLOGY/PRINCIPAL
findingsHere, using high-content imaging we assayed eight known trypanosomatid NMT inhibitors, against mammal-dwelling intracellular amastigote and trypomastigote stages and demonstrated that three of them (compounds 1, 5, and 8) have potent anti-proliferative effect at submicromolar concentrations against T. cruzi, with very low toxicity against human epithelial cells. Moreover, metabolic labeling using myristic acid, azide showed a considerable decrease in the myristoylation of proteins in parasites treated with NMT inhibitors, providing evidence of the on-target activity of the inhibitors. CONCLUSIONS/SIGNIFICANCE: Taken together, our data point out to the potential use of NMT inhibitors as anti-T. cruzi chemotherapy.
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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.