Skip Navigation



JAC Advance Access published online on December 22, 2005
Journal of Antimicrobial Chemotherapy, doi:10.1093/jac/dki426
This Article
Right arrow FREE Full Text (PDF) Freely available
Right arrow All Versions of this Article:
57/2/245    most recent
dki426v1
Right arrow Alert me when this article is cited
Right arrow Alert me if a correction is posted
Services
Right arrow Email this article to a friend
Right arrow Similar articles in this journal
Right arrow Similar articles in PubMed
Right arrow Alert me to new issues of the journal
Right arrow Add to My Personal Archive
Right arrow Download to citation manager
Right arrowRequest Permissions
Right arrow Disclaimer
Google Scholar
Right arrow Articles by André, E.
Right arrow Articles by Leonetti, J.-P.
Right arrow Search for Related Content
PubMed
Right arrow PubMed Citation
Right arrow Articles by André, E.
Right arrow Articles by Leonetti, J.-P.
Social Bookmarking
Add to CiteULike   Add to Connotea   Add to Del.icio.us  
What's this?

© The Author 2005. Published by Oxford University Press on behalf of the British Society for Antimicrobial Chemotherapy. All rights reserved. For Permissions, please e-mail: journals.permissions@oxfordjournals.org
Received March 11, 2005
Revised October 28, 2005
Accepted October 28, 2005

Original article

Novel synthetic molecules targeting the bacterial RNA polymerase assembly

Estelle André 1 {dagger}, Lionel Bastide 2 {dagger}, Sylvie Michaux-Charachon 3, Anne Gouby 4, Philippe Villain-Guillot 1, Jaqueline Latouche 1, Aurélie Bouchet 1, Maxime Gualtiéri 2, and Jean-Paul Leonetti 1 *

1 CPBS CNRS UMR 5160, Faculté de Pharmacie 15 Avenue Charles Flahault, BP 14491, 34093 Montpellier Cedex 5, France
2 Selectbiotics, 69 Rue G Besse, Parc scientifique G Besse, 30000 Nîmes, France
3 INSERM U-431, Faculté de Médecine, Avenue Kennedy, 30900 Nîmes, France; Laboratoire de Bactériologie, CHU de Nîmes, Groupe hospitalo-universitaire de Caremeau, 30029 Nîmes Cedex 9, France
4 Laboratoire de Bactériologie, CHU de Nîmes, Groupe hospitalo-universitaire de Caremeau, 30029 Nîmes Cedex 9, France

* To whom correspondence should be addressed.
Jean-Paul Leonetti, E-mail: jp.leonetti{at}ibph.pharma.univ-montp1.fr


  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.

Keywords: transcription; antibacterial drug screening; antibacterials; antibiotic resistance; anti-infective agents.
{dagger}These authors contributed equally to this work.
Add to CiteULike CiteULike   Add to Connotea Connotea   Add to Del.icio.us Del.icio.us    What's this?


This article has been cited by other articles:


Home page
 Antimicrob. Agents Chemother.Home page
P. Villain-Guillot, M. Gualtieri, L. Bastide, and J.-P. Leonetti
In Vitro Activities of Different Inhibitors of Bacterial Transcription against Staphylococcus epidermidis Biofilm
Antimicrob. Agents Chemother., September 1, 2007; 51(9): 3117 - 3121.
[Abstract] [Full Text] [PDF]

Home page
 J Antimicrob ChemotherHome page
M. Gualtieri, L. Bastide, P. Villain-Guillot, S. Michaux-Charachon, J. Latouche, and J.-P. Leonetti
In vitro activity of a new antibacterial rhodanine derivative against Staphylococcus epidermidis biofilms
J. Antimicrob. Chemother., October 1, 2006; 58(4): 778 - 783.
[Abstract] [Full Text] [PDF]


Disclaimer: Please note that abstracts for content published before 1996 were created through digital scanning and may therefore not exactly replicate the text of the original print issues. All efforts have been made to ensure accuracy, but the Publisher will not be held responsible for any remaining inaccuracies. If you require any further clarification, please contact our Customer Services Department.