Structural consideration of macrolide antibiotics in relation to the ribosomal interaction and drug design.

摘要: Macrolide antibiotics exert antimicrobial effects by binding to the peptidyl transferase center of 50S subunit bacterial ribosomes and inhibiting protein synthesis. Hence, structure macrolides their interaction with have been investigated in order understand structural mechanisms macrolide-ribosome interaction. Most found tom adopt a common conformation both crystal form solution, which is believed play an important role for as well representing bi-facial property essential excellent biological functions macrolides. Chemical footprinting mutant analysis offered topological information on at nucleotide level. Recently, structures ribosomal macrolide published. These provide much atomic level will enable structure-based drug design novel potent activity against resistant strains.