Mechanisms of antibiotics inhibiting bacterial RNA polymerase

Biochem Soc Trans. 2019 Feb 28;47(1):339-350. doi: 10.1042/BST20180499. Epub 2019 Jan 15.


Transcription, the first phase of gene expression, is performed by the multi-subunit RNA polymerase (RNAP). Bacterial RNAP is a validated target for clinical antibiotics. Many natural and synthetic compounds are now known to target RNAP, inhibiting various stages of the transcription cycle. However, very few RNAP inhibitors are used clinically. A detailed knowledge of inhibitors and their mechanisms of action (MOA) is vital for the future development of efficacious antibiotics. Moreover, inhibitors of RNAP are often useful tools with which to dissect RNAP function. Here, we review the MOA of antimicrobial transcription inhibitors.

Keywords: RNA polymerase; antibiotic resistance; antibiotics; mechanism of action of antibiotics; rifampicin; transcription.

Publication types

  • Review

MeSH terms

  • Anti-Bacterial Agents / pharmacology*
  • Bacteria / enzymology*
  • Bacterial Proteins / antagonists & inhibitors*
  • Bacterial Proteins / chemistry
  • DNA-Directed RNA Polymerases / antagonists & inhibitors*
  • DNA-Directed RNA Polymerases / chemistry
  • Enzyme Inhibitors / pharmacology*


  • Anti-Bacterial Agents
  • Bacterial Proteins
  • Enzyme Inhibitors
  • DNA-Directed RNA Polymerases