
Merck & Co., Rahway, NJ undertook multiple strategies to discover new antibacterial leads and drugs, including screening natural product extracts and examining known but less-studied natural products with unknown mechanisms of action, namely the boxazomycins.
- Boxazomycin A is a potent broad-spectrum antibiotic that selectively inhibits bacterial protein synthesis by inhibiting leucine incorporation.
- Boxazomycin A's mechanism of action is distinct from other protein synthesis inhibitors, as it does not show cross-resistance.
- Boxazomycin A showed poor in vivo efficacy in a mouse infection model, likely due to rapid clearance.
Further optimization would be needed to develop it into a viable antibiotic lead.
Singh SB, Occi J, Ondeyka J, Barrett JF, Masurekar P, Motyl M, Gill C, Salituro G. Antibacterial and mechanism of action studies of boxazomycin A. J Antibiot (Tokyo). 2024 Oct;77(10):679-684. doi: 10.1038/s41429-024-00757-9. Epub 2024 Aug 1. PMID: 39090325. https://www.nature.com/articles/s41429-024-00757-9
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