منابع مشابه
Antagonism screen for inhibitors of bacterial cell wall biogenesis uncovers an inhibitor of undecaprenyl diphosphate synthase.
Drug combinations are valuable tools for studying biological systems. Although much attention has been given to synergistic interactions in revealing connections between cellular processes, antagonistic interactions can also have tremendous value in elucidating genetic networks and mechanisms of drug action. Here, we exploit the power of antagonism in a high-throughput screen for molecules that...
متن کاملA pathway-specific cell based screening system to detect bacterial cell wall inhibitors.
A pathway-specific cell-based screen is described to detect compounds that inhibit the biosynthesis of the cell wall of bacteria. The basis for detection is the discovery that the beta-lactamase gene from Citrobacterfreundii, cloned into Escherichia coli, is induced when cells are exposed to known cell wall inhibitors, and not just beta-lactam-based antibiotics. In a wild type host, cell wall i...
متن کاملBacterial Cell Wall-induced Immunosuppression
Asingle intraperitoneal injection of bacterial cell walls derived from groupA streptococci (SCW)' into susceptible rats results in the development of acute and chronic erosive polyarthritis (1, 2) . The pathology of the lesion leading to joint destruction has been shown to be aT cell-dependent, cell-mediated response to the deposition of the group A streptococcal peptidoglycan-polysaccharide po...
متن کاملScreening systems for detecting inhibitors of cell wall transglycosylation in Enterococcus. Cell wall transglycosylation inhibitors in Enterococcus.
We devised two screening systems to detect cell wall transglycosylation inhibitors. One screen utilizes a mutant of Enterococcus faecalis strain A256 that is dependent on vancomycin or moenomycin for growth. In the absence of transglycosylation inhibitors the strain fails to grow, while in the presence of inhibitors, cells are rescued. A second screening organism E. faecalis strain MDD212 utili...
متن کاملPolyphosphate-containing bisubstrate analogues as inhibitors of a bacterial cell wall thymidylyltransferase.
A series of polyphosphate containing sugar nucleotide analogues were synthesized and evaluated as bisubstrate inhibitors of α-D-glucose 1-phosphate thymidylyltransferase Cps2L, the first enzyme in Streptococcus pneumoniael-rhamnose biosynthesis, and a novel antibacterial target. WaterLOGSY NMR spectroscopy demonstrated binding of bisubstrate analogues to Cps2L and a spectrophotometric coupled a...
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ژورنال
عنوان ژورنال: ACS Medicinal Chemistry Letters
سال: 2012
ISSN: 1948-5875,1948-5875
DOI: 10.1021/ml2002746