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JAC Advance Access originally published online on December 22, 2005
Journal of Antimicrobial Chemotherapy 2006 57(2):245-251; doi:10.1093/jac/dki426
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© 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

Novel synthetic molecules targeting the bacterial RNA polymerase assembly

Estelle André1,{dagger}, Lionel Bastide2,{dagger}, Sylvie Michaux-Charachon3,4, Anne Gouby4, Philippe Villain-Guillot1, Jaqueline Latouche1, Aurélie Bouchet1, Maxime Gualtiéri2 and Jean-Paul Leonetti1,*

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; 4 Laboratoire de Bactériologie, CHU de Nîmes, Groupe hospitalo-universitaire de Caremeau, 30029 Nîmes Cedex 9, France

Received 11 March 2005; revised and accepted 28 October 2005

* Corresponding author. Tel: +33-4-67-54-86-07; Fax: +33-4-67-54-86-10; E-mail: jp.leonetti{at}ibph.pharma.univ-montp1.fr

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


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