Structural basis of the action of pulvomycin and GE2270 A on elongation factor Tu

Biochemistry. 2006 Jun 6;45(22):6846-57. doi: 10.1021/bi0525122.

Abstract

Pulvomycin inhibits protein synthesis by preventing the formation of the ternary complex between elongation factor Tu (EF-Tu) x GTP and aa-tRNA. In this work, the crystal structure of Thermus thermophilus EF-Tu x pulvomycin in complex with the GTP analogue guanylyl imino diphosphate (GDPNP) at 1.4 A resolution reveals an antibiotic binding site extending from the domain 1-3 interface to domain 2, overlapping the domain 1-2-3 junction. Pulvomycin binding interferes with the binding of the 3'-aminoacyl group, the acceptor stem, and 5' end of tRNA. Only part of pulvomycin overlaps the binding site of GE2270 A, a domain 2-bound antibiotic of a structure unrelated to pulvomycin, which also hinders aa-tRNA binding. The structure of the T. thermophilus EF-Tu x GDPNP x GE2270 A complex at 1.6 A resolution shows that GE2270 A interferes with the binding of the 3'-aminoacyl group and part of the acceptor stem of aa-tRNA but not with the 5' end. Both compounds, pulvomycin more markedly, hinder the correct positioning of domain 1 over domains 2 and 3 that characterizes the active form of EF-Tu, while they affect the domain 1 switch regions that control the EF-Tu x GDP/GTP transitions in different ways. This work reveals how two antibiotics with different structures and binding modes can employ a similar mechanism of action.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aminoglycosides / chemistry*
  • Aminoglycosides / pharmacology
  • Anti-Bacterial Agents / chemistry*
  • Anti-Bacterial Agents / pharmacology
  • Crystallography
  • Peptide Elongation Factor Tu / chemistry*
  • Peptide Elongation Factor Tu / drug effects
  • Peptides, Cyclic / chemistry
  • Peptides, Cyclic / pharmacology*
  • Phenylalanine-tRNA Ligase / chemistry
  • Protein Conformation
  • Thermus thermophilus / drug effects
  • Thermus thermophilus / metabolism
  • Thiazoles / chemistry
  • Thiazoles / pharmacology

Substances

  • Aminoglycosides
  • Anti-Bacterial Agents
  • Peptides, Cyclic
  • Thiazoles
  • pulvomycin
  • Peptide Elongation Factor Tu
  • Phenylalanine-tRNA Ligase
  • GE 2270 A

Associated data

  • PDB/2C77
  • PDB/2C78