title: Novel synthetic molecules targeting the bacterial RNA polymerase assembly.
abstract: OBJECTIVE
  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.
authors.affiliation: CPBS CNRS UMR 5160, Faculté de Pharmacie 15 Avenue Charles Flahault, BP 14491, 34093 Montpellier Cedex 5, France.
authors.forename: Estelle
authors.initials: E
authors.lastname: André
authors.forename: Lionel
authors.initials: L
authors.lastname: Bastide
authors.forename: Sylvie
authors.initials: S
authors.lastname: Michaux-Charachon
authors.forename: Anne
authors.initials: A
authors.lastname: Gouby
authors.forename: Philippe
authors.initials: P
authors.lastname: Villain-Guillot
authors.forename: Jaqueline
authors.initials: J
authors.lastname: Latouche
authors.forename: Aurélie
authors.initials: A
authors.lastname: Bouchet
authors.forename: Maxime
authors.initials: M
authors.lastname: Gualtiéri
authors.forename: Jean-Paul
authors.initials: JP
authors.lastname: Leonetti
mesh_terms: D000900:Anti-Bacterial Agents / Q000494:pharmacology*; D001408:Bacillus anthracis / Q000187:drug effects; D001409:Bacillus cereus / Q000187:drug effects; D001419:Bacteria / Q000187:drug effects* / Q000201:enzymology*; D012321:DNA-Directed RNA Polymerases / Q000187:drug effects*; D024881:Drug Resistance, Bacterial; D004797:Enzyme-Linked Immunosorbent Assay; D006090:Gram-Negative Bacteria / Q000187:drug effects; D006094:Gram-Positive Bacteria / Q000187:drug effects; D047468:Immunoprecipitation; D008826:Microbial Sensitivity Tests; D013212:Staphylococcus epidermidis / Q000187:drug effects; D013296:Streptococcus pneumoniae / Q000187:drug effects; D014158:Transcription, Genetic / Q000187:drug effects
chemical_list: D000900:Anti-Bacterial Agents; D012321:DNA-Directed RNA Polymerases