Antibiotic target discovery by integrated phenotypic and activity-based profiling of electrophilic fragments.

Abstract excerpt

The emergence of antibiotic resistance necessitates the discovery of novel bacterial targets and antimicrobial agents. Here, we present a bacterial target discovery framework that integrates phenotypic screening of cysteine-reactive fragments with competitive activity-based protein profiling to map and functionally characterize the targets of screening hits. Using this approach, we identify β-ketoacyl-acyl...

Topics

• Anti-Bacterial Agents
• Drug Discovery
• Shigella flexneri
• 3-Oxoacyl-(Acyl-Carrier-Protein) Synthase
• Bacterial Proteins
• Microbial Sensitivity Tests