Smaller is better for antibiotic discovery.
A recent study demonstrates the use of fragment-based drug discovery and virtual screening to develop inhibitors of biotin carboxylase that exhibit antibacterial activity. The work not only further validates biotin carboxylase as a target for antibiotic research but also provides a framework for using fragment-based drug discovery in antibiotic development.
Waldrop
Grover L
GL
Division of Biochemistry and Molecular Biology, Louisiana State University, Baton Rouge, Louisiana 70803, USA. gwaldro@lsu.edu
D000900:Anti-Bacterial Agents / Q000737:chemistry* / Q000494:pharmacology*; D001665:Binding Sites; D019731:Carbon-Nitrogen Ligases / Q000037:antagonists & inhibitors / Q000378:metabolism; D055808:Drug Discovery / Q000379:methods*; D004353:Drug Evaluation, Preclinical; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D008958:Models, Molecular; D015394:Molecular Structure; D008970:Molecular Weight; D054852:Small Molecule Libraries; D013329:Structure-Activity Relationship
D000900:Anti-Bacterial Agents; D004791:Enzyme Inhibitors; D054852:Small Molecule Libraries; D019731:Carbon-Nitrogen Ligases; C019791:biotin carboxylase