title: Tigecycline - how powerful is it in the fight against antibiotic-resistant bacteria?
abstract: Tigecycline is a semisynthetic analogue of earlier tetracyclines and represents the first member of a novel class of antimicrobials - glycylcyclines - recently approved for clinical use. It is active against a broad range of gram-negative and gram-positive bacterial species including clinically important multidrug-resistant nosocomial and community-acquired bacterial pathogens. The exact molecular basis of tigecycline action is not clear at present, although similarly to the tetracyclines, it has been shown to inhibit the translation elongation step by binding to the ribosome 30S subunit and preventing aminoacylated tRNAs to accommodate in the ribosomal A site. Importantly, tigecycline overcomes the action of ribosomal protection proteins and is not a substrate for tetracycline efflux pumps of most bacteria - well-known and prevalent cellular mechanisms of microbial tetracycline resistance. The present review summarizes current knowledge on the molecular mechanism of the tigecycline action, antibacterial activity against various bacteria, clinical application, development of resistance to glycylcyclines.
authors.affiliation: Department of Biochemistry and Biophysics, Faculty of Natural Sciences, Vilnius University, 03101 Vilnius, Lithuania.
authors.forename: Vaida
authors.initials: V
authors.lastname: Seputiene
authors.forename: Justas
authors.initials: J
authors.lastname: Povilonis
authors.forename: Julija
authors.initials: J
authors.lastname: Armalyte
authors.forename: Kestutis
authors.initials: K
authors.lastname: Suziedelis
authors.forename: Alvydas
authors.initials: A
authors.lastname: Pavilonis
authors.forename: Edita
authors.initials: E
authors.lastname: Suziedeliene
mesh_terms: D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D017326:Clinical Trials, Phase III as Topic; D024901:Drug Resistance, Multiple, Bacterial / Q000187:drug effects; D006090:Gram-Negative Bacteria / Q000187:drug effects; D006094:Gram-Positive Bacteria / Q000187:drug effects; D006801:Humans; D008826:Microbial Sensitivity Tests; D008911:Minocycline / Q000031:analogs & derivatives* / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D015337:Multicenter Studies as Topic; D009154:Mutation; D016032:Randomized Controlled Trials as Topic; D013211:Staphylococcus aureus / Q000187:drug effects / Q000235:genetics; D013753:Tetracycline Resistance / Q000187:drug effects*; D013754:Tetracyclines / Q000494:pharmacology; D000078304:Tigecycline; D014481:United States; D014486:United States Food and Drug Administration
chemical_list: D000900:Anti-Bacterial Agents; D013754:Tetracyclines; C087533:CL 331002; D000078304:Tigecycline; D008911:Minocycline