Affiliation:
1. Schering-Plough Research Institute, Kenilworth, New Jersey 07033
Abstract
ABSTRACT
Evernimicin (SCH 27899) is a new antibiotic with activity against a wide spectrum of gram-positive bacteria and activity against some gram-negative bacteria. Previous metabolic labeling studies indicated that evernimicin specifically inhibited protein synthesis in
Staphylococcus aureus
. Using a susceptible
Escherichia coli
strain, we demonstrated that evernimicin also inhibited protein synthesis in
E. coli
. In cell-free translation assays with extracts from either
E. coli
or
S. aureus
, evernimicin had a 50% inhibitory concentration of approximately 125 nM. In contrast, cell-free systems derived from wheat germ and rabbit reticulocytes were inhibited only by very high levels of evernimicin. Evernimicin did not promote transcript misreading. [
14
C]evernimicin specifically bound to the 50S subunit from
E. coli
. Nonlinear regression analysis of binding data generated with 70S ribosomes from
E. coli
and
S. aureus
and 50S subunits from
E. coli
returned dissociation constants of 84, 86, and 160 nM, respectively. In binding experiments, performed in the presence of excess quantities of a selection of antibiotics known to bind to the 50S subunit, only the structurally similar drug avilamycin blocked binding of [
14
C]evernimicin to ribosomes.
Publisher
American Society for Microbiology
Subject
Infectious Diseases,Pharmacology (medical),Pharmacology
Cited by
61 articles.
订阅此论文施引文献
订阅此论文施引文献,注册后可以免费订阅5篇论文的施引文献,订阅后可以查看论文全部施引文献