Comparison of fortimicins with other aminoglycosides and effects on bacterial ribosome and protein synthesis.
Fortimicins are bicyclic aminoglycoside antibiotics that contain a fortamine moiety instead of the deoxystreptamine found in other aminoglysides. Fortimicin A had a bactericidal effect on Escherichia coli and Staphylococcus epidermidis and was found to inhibit protein synthesis in vivo. In vitro, fortimicin A inhibited polyuridylic acid-directed phenylalanine polymerization and induced misreading, as shown by leucine incorporation. In contrast, fortimicin B had no effect on either polymerization or misreading. In assays programmed with natural mRNA, only a weak polymerization inhibition effect was observed with fortimicin A, whereas a strong stimulation was seen in the presence of fortimicin B. Both fortimicins A and B inhibited dissociation of 70S ribosomes into their subunits and neither was able to displace [3H]dihydrostreptomycin, [3H]tobramycin, or [3H]gentamicin from their respective binding sites on the 70S particle.
D000617:Aminoglycosides / Q000494:pharmacology; D000900:Anti-Bacterial Agents / Q000494:pharmacology*; D001426:Bacterial Proteins / Q000096:biosynthesis*; D001667:Binding, Competitive; D004352:Drug Resistance, Microbial; D004926:Escherichia coli / Q000187:drug effects / Q000254:growth & development / Q000378:metabolism; D012269:Ribosomal Proteins / Q000096:biosynthesis*; D012270:Ribosomes / Q000187:drug effects / Q000378:metabolism; D013212:Staphylococcus epidermidis / Q000187:drug effects / Q000254:growth & development
D000617:Aminoglycosides; D000900:Anti-Bacterial Agents; D001426:Bacterial Proteins; D012269:Ribosomal Proteins; C023521:fortimicins; C023384:fortimicin A