2. Academic Validation
  3. Crystal structure of the oxazolidinone antibiotic linezolid bound to the 50S ribosomal subunit

Crystal structure of the oxazolidinone antibiotic linezolid bound to the 50S ribosomal subunit

  • J Med Chem. 2008 Jun 26;51(12):3353-6. doi: 10.1021/jm800379d.
Joseph A Ippolito 1,  Zoltan F Kanyo,  Deping Wang,  Francois J Franceschi,  Peter B Moore,  Thomas A Steitz,  Erin M Duffy
Affiliations

Affiliation

  • 1 Department of Structure-Based Drug Design, Rib-X Pharmaceuticals Inc, 300 George Street, Suite 301, New Haven, CT 06511, USA.
PMID: 18494460 DOI: 10.1021/jm800379d
Abstract

The Oxazolidinone antibacterials target the 50S subunit of prokaryotic ribosomes. To gain insight into their mechanism of action, the crystal structure of the canonical Oxazolidinone, linezolid, has been determined bound to the Haloarcula marismortui 50S subunit. Linezolid binds the 50S A-site, near the catalytic center, which suggests that inhibition involves competition with incoming A-site substrates. These results provide a structural basis for the discovery of improved oxazolidinones active against emerging drug-resistant clinical strains.

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