A library of stereo- and regiochemically diverse aminoglycoside derivatives was screened at 1 microM using surface plasmon resonance (SPR) against RNA hairpin models of the bacterial A-site, and the HIV viral TAR and RRE sequences. In order to double the stereochemical diversity of the library, the compounds were screened against both enantiomers of each of these sequences. Remarkably, this ini...

Aminoglycoside 2″-phosphotransferases are the major aminoglycoside-modifying enzymes in clinical isolates of enterococci and staphylococci. We describe a novel aminoglycoside 2″-phosphotransferase from the Gram-negative pathogen Campylobacter jejuni, which shares 78% amino acid sequence identity with the APH(2″)-Ia domain of the bifunctional aminoglycoside-modifying enzyme aminoglycoside (6') a...

objective: methicillin-resistant staphylococcus aureus is a major cause of nosocomial and community-acquired infections. aminoglycosides are potent bactericidal agents that are often used in combination with either a β-lactam or a glycopeptide, especially in the treatment of staphylococcal endocarditis. the main mechanism of aminoglycoside resistance in staphylococci is drug inactivation by cel...

Aminoglycoside is a potent antibiotic that stops the protein synthesis continuation by binding to the ribosomal decoding site. They are used to treat infection caused by the aerobic, gram-negative and certain gram-positive organisms. The most commonly used aminoglycoside is Gentamicin. Generally, single daily dosing of aminoglycosides is appeared to be safer, cost effective and efficacious. Pro...

Recently, a more complete understanding of the pharmacodynamics of aminoglycosides has been recognized, indicating that this class of antibiotics exhibits both concentration-dependent bactericidal activity and a postantibiotic effect. This pharmacodynamic information, along with better knowledge of the mechanisms responsible for aminoglycoside toxicity, established the foundation for once-daily...

This study highlights the prevalence of aminoglycoside-modifying enzyme genes and virulence determinants among clinical enterococci with high-level aminoglycoside resistance in Inner Mongolia, China. Screening for high-level aminoglycoside resistance against 117 enterococcal clinical isolates was performed using the agar-screening method. Out of the 117 enterococcal isolates, 46 were selected f...

Aminoglycoside has been known as a clinically important antibiotic for a long time, but genetic information for the biosynthesis of aminoglycoside is still insufficient. In this study, we tried to clone aminoglycoside-biosynthetic genes from soil DNA for accumulation of genetic information. We chose the genes encoding L-glutamine:(2-deoxy-)scyllo-inosose aminotransferase as the target, because ...

The resistance-nodulation-division (RND) family multidrug efflux system MexXY-OprM is a major determinant of aminoglycoside resistance in Pseudomonas aeruginosa, although the details of aminoglycoside recognition and export by MexY, the substrate-binding RND component of this efflux system, have not been elucidated. To identify regions/residues of MexY important for aminoglycoside resistance, p...

Carbapenem resistance in Klebsiella pneumoniae is a major clinical challenge. Aminoglycosides remain an important asset the current therapeutic arsenal to treat these infections. We examined aminoglycoside phenotypes and genomics collection of 100 invasive KPC-producing K. isolates sequentially collected Brazilian tertiary hospital between 2014 2016. Aminoglycoside susceptibility testing was pe...