Peptide Deformylase as an Antibacterial Drug Target: Target Validation and Resistance Development
نویسندگان
چکیده
منابع مشابه
Peptide deformylase as an antibacterial drug target: target validation and resistance development.
New inhibitors of peptide deformylase (PDF) which are very potent against the isolated enzyme and show a certain degree of antibacterial activity have recently been synthesized by our group. Several lines of experimental evidence indicate that these inhibitors indeed interfere with the target enzyme in the bacterial cell. (i) The inhibition of Escherichia coli growth could be counteracted by ov...
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The relatively rapid development of microbial resistance after the entry of every new antimicrobial into the marketplace necessitates a constant supply of new agents to maintain effective pharmacotherapy. Despite extensive efforts to identify novel lead compounds from molecular targets, only the peptide deformylase inhibitors (PDIs) have shown any real promise, with some advancing to phase I hu...
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متن کاملPeptide deformylase as an antibacterial drug target: assays for detection of its inhibition in Escherichia coli cell homogenates and intact cells.
An assay was developed to determine the activity of peptide deformylase (PDF) inhibitors under conditions as close as possible to the physiological situation. The assay principle is the detection of N-terminal [35S]methionine labeling of a protein that contains no internal methionine. If PDF is active, the deformylation of the methionine renders the peptide a substrate for methionine aminopepti...
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ژورنال
عنوان ژورنال: Antimicrobial Agents and Chemotherapy
سال: 2001
ISSN: 0066-4804,1098-6596
DOI: 10.1128/aac.45.4.1058-1064.2001