Mutations in the G-domain of elongation factor G from Thermus thermophilus affect both its interaction with GTP and fusidic acid

J Biol Chem. 2001 Aug 3;276(31):28774-8. doi: 10.1074/jbc.M102023200. Epub 2001 May 22.

Abstract

Two hypersensitive and two resistant variants of elongation factor-G (EF-G) toward fusidic acid are studied in comparison with the wild type factor. All mutated proteins are active in a cell-free translation system and ribosome-dependent GTP hydrolysis. The EF-G variants with the Thr-84-->Ala or Asp-109-->Lys mutations bring about a strong resistance of EF-G to the antibiotic, whereas the EF-Gs with substitutions Gly-16-->Val or Glu-119-->Lys are the first examples of fusidic acid-hypersensitive factors. A correlation between fusidic acid resistance of EF-G mutants and their affinity to GTP are revealed in this study, although their interactions with GDP are not changed. Thus, fusidic acid-hypersensitive mutants have the high affinity to an uncleavable GTP analog, but the association of resistant mutants with GTP is decreased. The effects of either fusidic acid-sensitive or resistant mutations can be explained by the conformational changes in the EF-G molecule, which influence its GTP-binding center. The results presented in this paper indicate that fusidic acid-sensitive mutant factors have a conformation favorable for GTP binding and subsequent interaction with the ribosomes.

Publication types

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

MeSH terms

  • Alanine
  • Aspartic Acid
  • Binding Sites
  • Cell-Free System
  • Fusidic Acid / metabolism*
  • Genetic Variation
  • Guanosine Diphosphate / metabolism
  • Guanosine Triphosphate / metabolism*
  • Guanylyl Imidodiphosphate / metabolism
  • Kinetics
  • Lysine
  • Models, Molecular
  • Mutagenesis, Site-Directed
  • Peptide Elongation Factor G / chemistry*
  • Peptide Elongation Factor G / genetics
  • Peptide Elongation Factor G / metabolism*
  • Poly U / metabolism
  • Protein Biosynthesis
  • Protein Structure, Tertiary
  • Recombinant Proteins / chemistry
  • Recombinant Proteins / isolation & purification
  • Recombinant Proteins / metabolism
  • Thermus thermophilus / genetics
  • Thermus thermophilus / metabolism*
  • Threonine

Substances

  • Peptide Elongation Factor G
  • Recombinant Proteins
  • Guanosine Diphosphate
  • Poly U
  • Threonine
  • Aspartic Acid
  • Guanylyl Imidodiphosphate
  • Fusidic Acid
  • Guanosine Triphosphate
  • Lysine
  • Alanine