Kinetics of drug-ribosome interactions defines the cidality of macrolide antibiotics.

ABSTRACT: Antibiotics can cause dormancy (bacteriostasis) or induce death (cidality) of the targeted bacteria. The bactericidal capacity is one of the most important properties of antibacterial agents. However, the understanding of the fundamental differences in the mode of action of bacteriostatic or bactericidal antibiotics, especially those belonging to the same chemical class, is very rudimentary. Here, by examining the activity and binding properties of chemically distinct macrolide inhibitors of translation, we have identified a key difference in their interaction with the ribosome, which correlates with their ability to cause cell death. While bacteriostatic and bactericidal macrolides bind in the nascent peptide exit tunnel of the large ribosomal subunit with comparable affinities, the bacte

SUBMITTER: Svetlov MS 

PROVIDER: S-EPMC5748224 | biostudies-literature | 2017 Dec

REPOSITORIES: biostudies-literature