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J Med Chem. 2008 Jun 26;51(12):3353-6. doi: 10.1021/jm800379d.

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

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Department of Structure-Based Drug Design, Rib-X Pharmaceuticals Inc, 300 George Street, Suite 301, New Haven, CT 06511, USA.


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.

[Indexed for MEDLINE]

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