Carba-sugars activate the glmS-riboswitch of Staphylococcus aureus

ACS Chem Biol. 2011 Jul 15;6(7):675-8. doi: 10.1021/cb200016d. Epub 2011 Apr 20.

Abstract

The glmS-riboswitch is unique among riboswitch families as it represents a metabolite-dependent ribozyme that undergoes self-cleavage upon recognition of glucosamin-6-phosphate. The glmS-riboswitch is located in the 5'-untranslated region of bacterial genes involved in cell wall biosynthesis. Therefore, this riboswitch represents a promising target for developing new antibiotics. We describe the metabolite-dependent glmS-riboswitch of pathologically relevant and vancomycin-resistant Staphylococcus aureus and the discovery and synthesis of a carba-sugar with potency similar to that of the native metabolite glucosamine-6-phosphate in modulating riboswitch activity. This compound represents a valuable lead structure for the development of antibiotics with a novel mode of action.

Publication types

  • Letter
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Bacterial Proteins / genetics
  • Bacterial Proteins / metabolism*
  • Carbasugars / chemistry*
  • Carbasugars / metabolism*
  • Glucosamine / analogs & derivatives
  • Glucosamine / metabolism
  • Glucose-6-Phosphate / analogs & derivatives
  • Glucose-6-Phosphate / metabolism
  • Magnesium / metabolism
  • RNA, Catalytic / physiology*
  • Riboswitch / physiology*
  • Staphylococcus aureus / genetics
  • Staphylococcus aureus / metabolism*
  • Vancomycin Resistance / genetics

Substances

  • Bacterial Proteins
  • Carbasugars
  • RNA, Catalytic
  • Riboswitch
  • component S, glutamate mutase protein, Bacteria
  • glucosamine 6-phosphate
  • Glucose-6-Phosphate
  • Magnesium
  • Glucosamine