SNAP output for PDB entry 3cpw [SNAP web server]

PDB-id

3cpw; SNAP-derived features in text and JSON formats; DNAproDB

Class

ribosome

Method

X-ray (2.7 Å)

Summary

The structure of the antibiotic linezolid bound to the large ribosomal subunit of haloarcula marismortui

Reference

Ippolito JA, Kanyo ZK, Wang D, Franceschi FJ, Moore PB, Steitz TA, Duffy EM (2008): "Crystal Structure of the Oxazolidinone Antibiotic Linezolid Bound to the 50S Ribosomal Subunit." J.Med.Chem., 51, 3353-3356. 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.