1NWX

COMPLEX OF THE LARGE RIBOSOMAL SUBUNIT FROM DEINOCOCCUS RADIODURANS WITH ABT-773

1NWX の概要

• エントリーDOI: 10.2210/pdb1nwx/pdb
• 分子名称: 23S RIBOSOMAL RNA, ribosomal protein L13, ribosomal protein L14, ... (32 entities in total)
• 機能のキーワード: abt-773, macrolide, ketolide, ribosome, 50s, ribosomal subunit
• 由来する生物種: Deinococcus radiodurans; 詳細
• タンパク質・核酸の鎖数: 31
• 化学式量合計: 1380428.28

構造登録者

Schluenzen, F.,Harms, J.,Franceschi, F.,Hansen, H.A.S.,Bartels, H.,Zarivach, R.,Yonath, A. (登録日: 2003-02-07, 公開日: 2003-03-18, 最終更新日: 2023-08-16)

主引用文献

Schlunzen, F.,Harms, J.M.,Franceschi, F.,Hansen, H.A.,Bartels, H.,Zarivach, R.,Yonath, A.
Structural basis for the antibiotic activity of ketolides and azalides.
Structure, 11:329-338, 2003

PubMed Abstract: The azalide azithromycin and the ketolide ABT-773, which were derived by chemical modifications of erythromycin, exhibit elevated activity against a number of penicillin- and macrolide-resistant pathogenic bacteria. Analysis of the crystal structures of the large ribosomal subunit from Deinococcus radiodurans complexed with azithromycin or ABT-773 indicates that, despite differences in the number and nature of their contacts with the ribosome, both compounds exert their antimicrobial activity by blocking the protein exit tunnel. In contrast to all macrolides studied so far, two molecules of azithromycin bind simultaneously to the tunnel. The additional molecule also interacts with two proteins, L4 and L22, implicated in macrolide resistance. These studies illuminated and rationalized the enhanced activity of the drugs against specific macrolide-resistant bacteria.

PubMed: 12623020
DOI: 10.1016/S0969-2126(03)00022-4

実験手法

X-RAY DIFFRACTION (3.5 Å)