title: Structural insight into the antibiotic action of telithromycin against resistant mutants.
abstract: The crystal structure of the ketolide telithromycin bound to the Deinococcus radiodurans large ribosomal subunit shows that telithromycin blocks the ribosomal exit tunnel and interacts with domains II and V of the 23S RNA. Comparisons to other clinically relevant macrolides provided structural insights into its enhanced activity against macrolide-resistant strains.
authors.affiliation: Max-Planck-Research Unit for Ribosomal Structure, Hamburg, Germany.
authors.forename: Rita
authors.initials: R
authors.lastname: Berisio
authors.forename: Joerg
authors.initials: J
authors.lastname: Harms
authors.forename: Frank
authors.initials: F
authors.lastname: Schluenzen
authors.forename: Raz
authors.initials: R
authors.lastname: Zarivach
authors.forename: Harly A S
authors.initials: HA
authors.lastname: Hansen
authors.forename: Paola
authors.initials: P
authors.lastname: Fucini
authors.forename: Ada
authors.initials: A
authors.lastname: Yonath
mesh_terms: D000900:Anti-Bacterial Agents / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D001665:Binding Sites; D003460:Crystallization; D018360:Crystallography, X-Ray; D034301:Deinococcus / Q000187:drug effects* / Q000235:genetics / Q000378:metabolism; D024881:Drug Resistance, Bacterial; D004917:Erythromycin / Q000031:analogs & derivatives* / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D006801:Humans; D048628:Ketolides; D018942:Macrolides; D008958:Models, Molecular; D008969:Molecular Sequence Data; D012338:RNA, Ribosomal, 23S / Q000235:genetics / Q000378:metabolism
chemical_list: D000900:Anti-Bacterial Agents; D048628:Ketolides; D018942:Macrolides; D012338:RNA, Ribosomal, 23S; D004917:Erythromycin; C405499:cethromycin; C106791:telithromycin