Format

Send to

Choose Destination
J Antimicrob Chemother. 2006 Feb;57(2):245-51. Epub 2005 Dec 22.

Novel synthetic molecules targeting the bacterial RNA polymerase assembly.

Author information

1
CPBS CNRS UMR 5160, Faculté de Pharmacie 15 Avenue Charles Flahault, BP 14491, 34093 Montpellier Cedex 5, France.

Abstract

OBJECTIVES:

Despite extensive functional screening of the bacterial RNA polymerase (RNAP) over the past years, very few novel inhibitors have been reported. We have, therefore, decided to screen with a radically different, non-enzymic, protein-protein interaction assay. Our target is the highly conserved RNAP-sigma interaction that is essential for transcription.

METHODS:

Small molecule inhibitors of the RNAP-sigma interaction were tested for their activity on transcription and on bacteria.

RESULTS:

These compounds have antibacterial activity against Gram-positive bacteria including multiresistant clinical isolates.

CONCLUSIONS:

This is, to our knowledge, the first example of a small molecule inhibitor of this interaction.

PMID:
16373430
DOI:
10.1093/jac/dki426
[Indexed for MEDLINE]

Supplemental Content

Full text links

Icon for Silverchair Information Systems
Loading ...
Support Center