The structures of antibiotics bound to the E site region of the 50 S ribosomal subunit of Haloarcula marismortui: 13-deoxytedanolide and girodazole

J Mol Biol. 2007 Apr 13;367(5):1471-9. doi: 10.1016/j.jmb.2007.01.081. Epub 2007 Feb 7.

Abstract

Crystal structures of the 50 S ribosomal subunit from Haloarcula marismortui complexed with two antibiotics have identified new sites at which antibiotics interact with the ribosome and inhibit protein synthesis. 13-Deoxytedanolide binds to the E site of the 50 S subunit at the same location as the CCA of tRNA, and thus appears to inhibit protein synthesis by competing with deacylated tRNAs for E site binding. Girodazole binds near the E site region, but is somewhat buried and may inhibit tRNA binding by interfering with conformational changes that occur at the E site. The specificity of 13-deoxytedanolide for eukaryotic ribosomes is explained by its extensive interactions with protein L44e, which is an E site component of archaeal and eukaryotic ribosomes, but not of eubacterial ribosomes. In addition, protein L28, which is unique to the eubacterial E site, overlaps the site occupied by 13-deoxytedanolide, precluding its binding to eubacterial ribosomes. Girodazole is specific for eukarytes and archaea because it makes interactions with L15 that are not possible in eubacteria.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / metabolism
  • Binding, Competitive
  • Haloarcula marismortui*
  • Hydrophobic and Hydrophilic Interactions
  • Imidazoles / chemistry*
  • Imidazoles / metabolism*
  • Macrolides / chemistry*
  • Macrolides / metabolism*
  • Models, Molecular
  • Propanolamines / chemistry*
  • Propanolamines / metabolism*
  • Protein Binding
  • Protein Structure, Tertiary
  • Protein Subunits / chemistry
  • Protein Subunits / metabolism
  • Ribosomal Proteins / chemistry
  • Ribosomal Proteins / metabolism*

Substances

  • 13-deoxytedanolide
  • Anti-Bacterial Agents
  • Imidazoles
  • Macrolides
  • Propanolamines
  • Protein Subunits
  • Ribosomal Proteins
  • girodazole

Associated data

  • PDB/2OTJ
  • PDB/2OTL