S105: Utilizing resistance enzymes for generating new aminoglycoside antibiotics

Aminoglycosides are broad-spectrum antibiotics commonly used for the treatment of serious bacterial infections. Decades of intensive clinical use of aminoglycosides have led to the emergence of bacterial resistance to this family of drugs. A highly prevalent mode of bacterial resistance to aminoglycosides evolved through the acquisition of enzymes that modify the antibiotics. These perform three chemical alterations of the drug: N-acetylation by acetyltransferases (AACs), adenylation by adenyltransferases (ANTs), or phosphorylation by phosphotransferases (APHs). Development of novel methodologies utilizing resistance enzymes for the preparation of aminoglycoside antibiotics will be discussed.