1nwy

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1nwy, resolution 3.30Å

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COMPLEX OF THE LARGE RIBOSOMAL SUBUNIT FROM DEINOCOCCUS RADIODURANS WITH AZITHROMYCIN

Overview

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.

About this Structure

1NWY is a Protein complex structure of sequences from Deinococcus radiodurans with ZIT as ligand. Full crystallographic information is available from OCA.

Reference

Structural basis for the antibiotic activity of ketolides and azalides., Schlunzen F, Harms JM, Franceschi F, Hansen HA, Bartels H, Zarivach R, Yonath A, Structure. 2003 Mar;11(3):329-38. PMID:12623020

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