Progress in targeting bacterial transcription

The bacterial RNA polymerase (RNAP) is an essential enzyme that is responsible for making RNA from a DNA template and is targeted by several antibiotics. Rifampicin was the first of such antibiotics to be described and is one of the most efficient anti-tuberculosis drugs in use. In the past five yea...

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Bibliographic Details
Published in:Drug discovery today 2007-03, Vol.12 (5), p.200-208
Main Authors: Villain-Guillot, Philippe, Bastide, Lionel, Gualtieri, Maxime, Leonetti, Jean-Paul
Format: Article
Language:English
Subjects:
Anti-Bacterial Agents
Anti-Bacterial Agents - pharmacology
Antibiotics, Antitubercular
Antibiotics, Antitubercular - pharmacology
Bacteria
Binding Sites
Binding Sites - genetics
Cellular Biology
DNA-Directed RNA Polymerases
Drug Delivery Systems
Drug Design
Humans
Life Sciences
Protein Subunits
Protein Subunits - genetics
Rifampin
Rifampin - pharmacology
RNA, Bacterial
RNA, Bacterial - drug effects
Structure-Activity Relationship
Transcription, Genetic
Transcription, Genetic - drug effects
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Summary:The bacterial RNA polymerase (RNAP) is an essential enzyme that is responsible for making RNA from a DNA template and is targeted by several antibiotics. Rifampicin was the first of such antibiotics to be described and is one of the most efficient anti-tuberculosis drugs in use. In the past five years, structural studies of bacterial RNAP and the resolution of several complexes of drugs bound to RNAP subunits have revealed molecular details of the drug-binding sites and the mechanism of drug action. This knowledge opens avenues for the development of antibiotics. Here these drugs are reviewed, together with their mechanisms and their potential interest for therapeutic applications.
ISSN:1359-6446
1878-5832
DOI:10.1016/j.drudis.2007.01.005