Pseudouridimycin: The First Nucleoside Analogue That Selectively Inhibits Bacterial RNA Polymerase

Angew Chem Int Ed Engl. 2017 Oct 16;56(43):13184-13186. doi: 10.1002/anie.201708133. Epub 2017 Sep 12.

Abstract

Seek, and ye shall find: After years of focusing research on synthetic antibiotics out of fear that all the useful natural ones had already been found, a novel antibacterial compound has been discovered through conventional microbial extract screening. The broad-spectrum nucleoside-analogue inhibitor pseudouridimycin is selective for bacterial RNA polymerase and elicits very low resistance rates.

Keywords: RNA polymerase; antibiotics; medicinal chemistry; natural products; nucleoside analogues.

MeSH terms

  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / metabolism*
  • Anti-Bacterial Agents / pharmacology
  • Bacteria / enzymology*
  • Bacterial Proteins / antagonists & inhibitors
  • Bacterial Proteins / metabolism*
  • DNA-Directed RNA Polymerases / antagonists & inhibitors
  • DNA-Directed RNA Polymerases / metabolism*
  • Gram-Negative Bacteria / drug effects
  • Nucleosides / analogs & derivatives*
  • Nucleosides / chemistry
  • Nucleosides / metabolism
  • Nucleosides / pharmacology
  • Structure-Activity Relationship

Substances

  • Anti-Bacterial Agents
  • Bacterial Proteins
  • Nucleosides
  • pseudouridimycin
  • DNA-Directed RNA Polymerases