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GSK2254232A

Development stage: Discontinued
Lead developer: GSK
Modality: Small Molecules
Administration: Intravenous

Overview

GSK2254232A is a novel benzoxaborole antibiotic developed by GSK that acts as a potent inhibitor of bacterial leucyl-tRNA synthetase (LeuRS). By binding to the editing site of the enzyme, it prevents the proper charging of tRNA with leucine, thereby inhibiting bacterial protein synthesis. The compound was specifically designed to target Gram-negative pathogens, including Pseudomonas aeruginosa. However, clinical development was halted during Phase 1 trials after observations of rapid resistance development in P. aeruginosa isolates, mediated by mutations in the LeuRS editing domain.

Targets

aaRS (Aminoacyl-tRNA synthetase family)

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