Inhibitors of methionyl-tRNA synthetase have potent activity against Giardia intestinalis trophozoites

Antimicrobial Agents and Chemotherapy
Ranae M RanadeFrederick S Buckner

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.

Citations

Oct 28, 2016·European Journal of Medicinal Chemistry·Wenlin HuangErkang Fan
Aug 7, 2018·PLoS Neglected Tropical Diseases·Kelly M HennesseyKayode K Ojo
Aug 30, 2017·Antimicrobial Agents and Chemotherapy·Omeed FaghihFrederick S Buckner
Nov 7, 2019·Journal of Computer-aided Molecular Design·Galyna P VolynetsMichail A Tukalo
Feb 6, 2020·The Journal of Antimicrobial Chemotherapy·Samantha A MichaelsKayode K Ojo
Apr 16, 2021·The Journal of Biological Chemistry·Gustavo Fernando MercaldiCelso Eduardo Benedetti

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