Comparison of cefepime, cefpirome, and cefaclidine binding affinities for penicillin-binding proteins in Escherichia coli K-12 and Pseudomonas aeruginosa SC8329.
Article Details
- CitationCopy to clipboard
Pucci MJ, Boice-Sowek J, Kessler RE, Dougherty TJ
Comparison of cefepime, cefpirome, and cefaclidine binding affinities for penicillin-binding proteins in Escherichia coli K-12 and Pseudomonas aeruginosa SC8329.
Antimicrob Agents Chemother. 1991 Nov;35(11):2312-7. doi: 10.1128/AAC.35.11.2312.
- PubMed ID
- 1804003 [ View in PubMed]
- Abstract
The relative binding affinities of the extended-spectrum cephalosporins cefepime, cefpirome, and cefaclidine for the penicillin-binding proteins (PBPs) of Escherichia coli K-12 and Pseudomonas aeruginosa SC8329 were determined. Affinities were calculated from competition experiments between these antibiotics and [3H]benzylpenicillin in isolated membrane preparations. The concentrations which reduced binding to a PBP by 50% (IC50s) were determined. For E. coli, all three antibiotics displayed good PBP 3 binding (IC50s of 0.5 microgram/ml or less), and MICs roughly correlated with these values. Cefepime had a greater than 20-fold-lower IC50 for PBP 2 of E. coli than the other antibiotics. For P. aeruginosa, all of the antibiotics bound poorly (greater than 25 micrograms/ml) to PBP 2 but showed excellent pseudomonal (less than 0.0025 microgram/ml) PBP 3 binding. No correlations were seen between IC50s and MICs for P. aeruginosa. Despite differences in PBP binding, cefepime, cefpirome, and cefaclidine all displayed similar bactericidal activity for E. coli K-12 over the initial 3 h after antibiotic addition. All three caused E. coli to form filaments at values close to the MICs. In addition, cefepime induced "bleb" formation along the filaments at concentrations greater than 10x the MIC.
DrugBank Data that Cites this Article
- Drug Targets
Drug Target Kind Organism Pharmacological Action Actions Cefepime Penicillin-binding protein 1A Protein Escherichia coli (strain K12) YesInhibitorDetails Cefepime Penicillin-binding protein 1B Protein Escherichia coli (strain K12) YesInhibitorDetails Cefepime Penicillin-binding protein 1B Protein Pseudomonas aeruginosa YesInhibitorDetails Cefepime Penicillin-binding protein 2 Protein Escherichia coli (strain K12) YesInhibitorDetails Cefepime Penicillin-binding protein 2 Protein Pseudomonas aeruginosa UnknownInhibitorDetails Cefepime Penicillin-binding protein 3 Protein Pseudomonas aeruginosa YesInhibitorDetails Cefepime Peptidoglycan synthase FtsI Protein Escherichia coli (strain K12) YesInhibitorDetails