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

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.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Ippolito JA,Kanyo ZF,Wang D,Franceschi FJ,Moore PB,Steitz TA,Duffy EM

doi

10.1021/jm800379d

subject

Has Abstract

pub_date

2008-06-26 00:00:00

pages

3353-6

issue

12

eissn

0022-2623

issn

1520-4804

journal_volume

51

pub_type

杂志文章

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