Evaluating the activity of the RNA polymerase inhibitor myxopyronin B against Staphylococcus aureus.
FEMS Microbiol Lett
; 319(2): 176-9, 2011 Jun.
Article
en En
| MEDLINE
| ID: mdl-21477256
ABSTRACT
Myxopyronin B (MyxB) binds to the switch region of RNA polymerase (RNAP) and inhibits transcriptional initiation. To evaluate the potential development of MyxB as a novel class of antibiotic, we characterized the antimicrobial activity of MyxB against Staphylococcus aureus. Spontaneous MyxB resistance in S. aureus occurred at a frequency of 8 × 10(-8) , similar to that of rifampin. The MyxB-resistant mutants were found to be altered in single amino acid residues in the RNAP subunits that form the MyxB-binding site. In the presence of human serum albumin, the MyxB minimum inhibitory concentration against S. aureus increased drastically (≥128-fold) and 99.5% of MyxB was protein bound. Because of the high serum protein binding and resistance rate, we conclude that MyxB is not a viable starting point for antibiotic development.
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Staphylococcus aureus
/
ARN Polimerasas Dirigidas por ADN
/
Inhibidores Enzimáticos
/
Lactonas
/
Antibacterianos
Límite:
Humans
Idioma:
En
Revista:
FEMS Microbiol Lett
Año:
2011
Tipo del documento:
Article
País de afiliación:
Estados Unidos