Antibiotic compositions and related screening methods
US8916540B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Jan 15, 2009 |
| Grant date | Dec 23, 2014 |
| Priority date | — |
| Expiry date | Feb 4, 2031 |
Classification
- Technology area (CPC Y)Emerging Cross-Sectional Technologies
- CPC primaryY02A50/30
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
Moenomycin inhibits bacterial growth by clocking the transglycosylase activity of class A penicillin-binding proteins (PBPs), which are key enzymes in bacterial cell wall synthesis. The binding affinities of moenomycin A with various truncated PBPs were compared showing that the transmembrane domain is important for moenomycin binding. Full-length class-A PBPs from 16 bacterial species were produced, and their binding activities showed a correlation with the antimicrobial activity of moenomycin against Enterococcus faecalis and Staphylococcus aureus. Moreover, a fluorescence anisotropy-based high-throughput assay was developed and used successfully for identification of transglycosylase inhibitors.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.