Novel anti-infection agents: Small-molecule inhibitors of bacterial transcription factors

Structure-based drug design was utilized to identify potent small-molecule inhibitors of proteins within the AraC family of bacterial transcription factors, which control virulence in medically important microbes. These agents represent a novel approach to fight infectious disease and may be less likely to promote resistance development. These compounds lack intrinsic antibacterial activity in vitro and were able to limit a bacterial infection in a mouse model of urinary tract infection.

Inhibitors of AraC bacterial transcription factors are shown to limit infections by reducing virulence rather than halting growth of the organisms. This therapeutic approach is intended to prevent infection and minimize the development of bacterial resistance.Figure optionsDownload as PowerPoint slide