Article
Identification of bacteria-selective threonyl-tRNA synthetase substrate inhibitors by structure-based design.
Journal of medicinal chemistry - 28 Feb 2013
Teng Min, Hilgers Mark T, Cunningham Mark L, Borchardt Allen, Locke Jeffrey B, Abraham Sunny, Haley Gregory, Kwan Bryan P, Hall Courtney, Hough Grayson W, Shaw Karen J, Finn John
Abstract excerpt
A series of potent and bacteria-selective threonyl-tRNA synthetase (ThrRS) inhibitors have been identified using structure-based drug design. These compounds occupied the substrate binding site of ThrRS and showed excellent binding affinities for all of the bacterial orthologues tested. Some of the compounds displayed greatly improved bacterial selectivity. Key residues responsible for potency and bacteria/human...
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