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

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.

authors

Ranade RM,Zhang Z,Gillespie JR,Shibata S,Verlinde CL,Hol WG,Fan E,Buckner FS

doi

10.1128/AAC.01573-15

subject

Has Abstract

pub_date

2015-11-01 00:00:00

pages

7128-31

issue

11

eissn

0066-4804

issn

1098-6596

pii

AAC.01573-15

journal_volume

59

pub_type

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