5HKV

The crystal structure of the large ribosomal subunit of Staphylococcus aureus in complex with lincomycin

Summary for 5HKV

• Entry DOI: 10.2210/pdb5hkv/pdb
• Related: 4WCE 4WF9 4WFA 4WFB
• Descriptor: 23s ribosomal RNA, 50S ribosomal protein L15, 50S ribosomal protein L16, ... (34 entities in total)
• Functional Keywords: ribosome, rna, lincomycin, antibiotics
• Biological source: Staphylococcus aureus subsp. aureus NCTC 8325; More
• Total number of polymer chains: 27
• Total formula weight: 1364953.90

Authors

Yonath, A.,Matzov, D.,Eyal, Z.,Ben Hamou, R.,Zimmerman, E.,Rozenberg, H.,Bashan, A.,Fridman, M. (deposition date: 2016-01-14, release date: 2017-05-03, Last modification date: 2024-01-10)

Primary citation

Matzov, D.,Eyal, Z.,Benhamou, R.I.,Shalev-Benami, M.,Halfon, Y.,Krupkin, M.,Zimmerman, E.,Rozenberg, H.,Bashan, A.,Fridman, M.,Yonath, A.
Structural insights of lincosamides targeting the ribosome of Staphylococcus aureus.
Nucleic Acids Res., 45:10284-10292, 2017

PubMed 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.

PubMed: 28973455
DOI: 10.1093/nar/gkx658

Experimental method

X-RAY DIFFRACTION (3.66 Å)