4U27

Crystal structure of the E. coli ribosome bound to flopristin and linopristin.

これはPDB形式変換不可エントリーです。

4U27 の概要

• エントリーDOI: 10.2210/pdb4u27/pdb
• 関連するBIRD辞書のPRD_ID: PRD_002101
• 分子名称: 16S rRNA, 30S ribosomal protein S10, 30S ribosomal protein S11, ... (58 entities in total)
• 機能のキーワード: protein biosynthesis, ribosome, rna, transfer, exit, peptidyl, 30s, 70s, 16s, ribosomal subunit, antibiotic, streptogramin
• 由来する生物種: Escherichia coli str. K-12 substr. MDS42; 詳細
• タンパク質・核酸の鎖数: 107
• 化学式量合計: 4270862.58

構造登録者

Noeske, J.,Huang, J.,Olivier, N.B.,Giacobbe, R.A.,Zambrowski, M.,Cate, J.H.D. (登録日: 2014-07-16, 公開日: 2014-07-30, 最終更新日: 2024-10-09)

主引用文献

Noeske, J.,Huang, J.,Olivier, N.B.,Giacobbe, R.A.,Zambrowski, M.,Cate, J.H.
Synergy of streptogramin antibiotics occurs independently of their effects on translation.
Antimicrob.Agents Chemother., 58:5269-5279, 2014

PubMed Abstract: Streptogramin antibiotics are divided into types A and B, which in combination can act synergistically. We compared the molecular interactions of the streptogramin combinations Synercid (type A, dalfopristin; type B, quinupristin) and NXL 103 (type A, flopristin; type B, linopristin) with the Escherichia coli 70S ribosome by X-ray crystallography. We further analyzed the activity of the streptogramin components individually and in combination. The streptogramin A and B components in Synercid and NXL 103 exhibit synergistic antimicrobial activity against certain pathogenic bacteria. However, in transcription-coupled translation assays, only combinations that include dalfopristin, the streptogramin A component of Synercid, show synergy. Notably, the diethylaminoethylsulfonyl group in dalfopristin reduces its activity but is the basis for synergy in transcription-coupled translation assays before its rapid hydrolysis from the depsipeptide core. Replacement of the diethylaminoethylsulfonyl group in dalfopristin by a nonhydrolyzable group may therefore be beneficial for synergy. The absence of general streptogramin synergy in transcription-coupled translation assays suggests that the synergistic antimicrobial activity of streptogramins can occur independently of the effects of streptogramin on translation.

PubMed: 24957822
DOI: 10.1128/AAC.03389-14

実験手法

X-RAY DIFFRACTION (2.8 Å)