Journal of Medicinal Chemistry p. 9703 - 9717 (2019)
Update date:2022-07-30
Topics:
Cain, Ricky
Salimraj, Ramya
Punekar, Avinash S.
Bellini, Dom
Fishwick, Colin W. G.
Czaplewski, Lloyd
Scott, David J.
Harris, Gemma
Dowson, Christopher G.
Lloyd, Adrian J.
Roper, David I.
Aminoacyl-tRNA synthetases are ubiquitous and essential enzymes for protein synthesis and also a variety of other metabolic processes, especially in bacterial species. Bacterial aminoacyl-tRNA synthetases represent attractive and validated targets for antimicrobial drug discovery if issues of prokaryotic versus eukaryotic selectivity and antibiotic resistance generation can be addressed. We have determined high-resolution X-ray crystal structures of the Escherichia coli and Staphylococcus aureus seryl-tRNA synthetases in complex with aminoacyl adenylate analogues and applied a structure-based drug discovery approach to explore and identify a series of small molecule inhibitors that selectively inhibit bacterial seryl-tRNA synthetases with greater than 2 orders of magnitude compared to their human homologue, demonstrating a route to the selective chemical inhibition of these bacterial targets.
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