Details

Autor(en) / Beteiligte

• Ippolito, Joseph A
• Kanyo, Zoltan F
• Wang, Deping
• Franceschi, Francois J
• Moore, Peter B
• Steitz, Thomas A
• Duffy, Erin M

Titel

Crystal Structure of the Oxazolidinone Antibiotic Linezolid Bound to the 50S Ribosomal Subunit

Ist Teil von

• Journal of medicinal chemistry, 2008-06, Vol.51 (12), p.3353-3356

Ort / Verlag

Washington, DC: American Chemical Society

Erscheinungsjahr

2008

Link zum Volltext

Quelle

MEDLINE

Beschreibungen/Notizen

• 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.