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.
Highlights
Use of antimicrobial drugs over the last 60 years in medicine and veterinary has triggered a development of very efficient genetic and biochemical mechanisms within bacteria enabling them to live in the antibiotic-containing environments
The list of antibiotics available for efficient treatment of community-acquired and nosocomial infections caused by methicillin-resistant Staphylococcus aureus (MRSA), vancomycin-resistant Enterococcus, extended-spectrum β-lactamase (ESBL)-producing Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, carbapenemase-producing Acinetobacter baumannii became dramatically short
Tigecycline is the first antimicrobial of glycylcycline class, recently approved for use in the clinical practice for the treatment of adult complicated skin and skin-structure infections, complicated intra-abdominal infections, and community-acquired bacterial pneumonia (CABP) [1,2] and introduced during the past two decades into clinical practice [1]
Summary
Use of antimicrobial drugs over the last 60 years in medicine and veterinary has triggered a development of very efficient genetic and biochemical mechanisms within bacteria enabling them to live in the antibiotic-containing environments. It has been proposed that either higher affinity of tigecycline to Tet-1 binding site compared to tetracycline and its derivatives or its unique orientation, when bound to ribosome, could prevent tigecycline from dissociation via the action of ribosome protection proteins in tetracycline-resistant bacteria [10].
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