Summary information and primary citation

PDB-id
5nrg; SNAP-derived features in text and JSON formats; DNAproDB
Class
ribosome
Method
X-ray (3.442 Å)
Summary
The crystal structure of the large ribosomal subunit of staphylococcus aureus in complex with rb02
Reference
Matzov D, Eyal Z, Benhamou RI, Shalev-Benami M, Halfon Y, Krupkin M, Zimmerman E, Rozenberg H, Bashan A, Fridman M, Yonath A (2017): "Structural insights of lincosamides targeting the ribosome of Staphylococcus aureus." Nucleic Acids Res., 45, 10284-10292. doi: 10.1093/nar/gkx658.
Abstract
Antimicrobial resistance within a wide range of pathogenic bacteria is an increasingly serious threat to global public health. Among these pathogenic bacteria are the highly resistant, versatile and possibly aggressive bacteria, Staphylococcus aureus. Lincosamide antibiotics were proved to be effective against this pathogen. This small, albeit important group of antibiotics is mostly active against Gram-positive bacteria, but also used against selected Gram-negative anaerobes and protozoa. S. aureus resistance to lincosamides can be acquired by modifications and/or mutations in the rRNA and rProteins. Here, we present the crystal structures of the large ribosomal subunit of S. aureus in complex with the lincosamides lincomycin and RB02, a novel semisynthetic derivative and discuss the biochemical aspects of the in vitro potency of various lincosamides. These results allow better understanding of the drugs selectivity as well as the importance of the various chemical moieties of the drug for binding and inhibition.

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