ArticleAntimicrobial agents and chemotherapy2015
Inhibitors of methionyl-tRNA synthetase have potent activity against Giardia intestinalis trophozoites.
Article in Antimicrobial agents and chemotherapy, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed, 21 citations in OpenAlex.
- ExploringPharmaceuticals (Basel, Switzerland) · 2023Article
- Identification of Fungus-Derived Natural Products as New Antigiardial Scaffolds.Microbiology spectrum · 2023Article
- Discovery of novel antituberculosis agents among 3-phenyl-5-(1-phenyl-1H-[1,2,3]triazol-4-yl)-[1,2,4]oxadiazole derivatives targeting aminoacyl-tRNA synthetases.Scientific reports · 2021Article
- Triazoxins: Novel nucleosides with anti-Giardia activity.Bioorganic & medicinal chemistry letters · 2020Article
- Methionyl-tRNA synthetase inhibitor has potent in vivo activity in a novel Giardia lamblia luciferase murine infection model.The Journal of antimicrobial chemotherapy · 2020Article
- Dual-target inhibitors of mycobacterial aminoacyl-tRNA synthetases amongMedChemComm · 2019Article
- Dual-targeted hit identification using pharmacophore screening.Journal of computer-aided molecular design · 2019Article
- Screening of the Pathogen Box for inhibitors with dual efficacy against Giardia lamblia and Cryptosporidium parvum.PLoS neglected tropical diseases · 2018Article
- Development of Methionyl-tRNA Synthetase Inhibitors as Antibiotics for Gram-Positive Bacterial Infections.Antimicrobial agents and chemotherapy · 2017Article
- From Cells to Mice to Target: Characterization of NEU-1053 (SB-443342) and Its Analogues for Treatment of Human African Trypanosomiasis.ACS infectious diseases · 2017Article
- Structure-guided design of novel Trypanosoma brucei Methionyl-tRNA synthetase inhibitors.European journal of medicinal chemistry · 2016Article
- 5-Fluoroimidazo[4,5-b]pyridine Is a Privileged Fragment That Conveys Bioavailability to Potent Trypanosomal Methionyl-tRNA Synthetase Inhibitors.ACS infectious diseases · 2016Article
- Brucella melitensis Methionyl-tRNA-Synthetase (MetRS), a Potential Drug Target for Brucellosis.PloS one · 2016Article
- Molecular basis for diaryldiamine selectivity and competition with tRNA in a type 2 methionyl-tRNA synthetase from a Gram-negative bacterium.The Journal of biological chemistryArticle
Corrections and comments
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Authors and funding
8 authors at 1 institution in 1 country.
Funding
Abstract
The methionyl-tRNA synthetase (MetRS) is a novel drug target for the protozoan pathogen Giardia intestinalis. This protist contains a single MetRS that is distinct from the human cytoplasmic MetRS. A panel of MetRS inhibitors was tested against recombinant Giardia MetRS, Giardia trophozoites, and mammalian cell lines. The best compounds inhibited trophozoite growth at 500 nM (metronidazole did so at ∼5,000 nM) and had low cytotoxicity against mammalian cells, indicating excellent potential for further development as anti-Giardia drugs.
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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.