Structural insight into the antibiotic action of telithromycin against resistant mutants

被引:140
作者
Berisio, R
Harms, J
Schluenzen, F
Zarivach, R
Hansen, HAS
Fucini, P
Yonath, A [1 ]
机构
[1] Weizmann Inst Sci, Dept Biol Struct, IL-76100 Rehovot, Israel
[2] Max Planck Inst Mol Genet, Berlin, Germany
[3] Max Planck Res Unit Ribosomal Struct, Hamburg, Germany
[4] CNR, Inst Biostruct & Bioimaging, Naples, Italy
关键词
D O I
10.1128/JB.185.14.4276-4279.2003
中图分类号
Q93 [微生物学];
学科分类号
071005 ; 100705 ;
摘要
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.
引用
收藏
页码:4276 / 4279
页数:4
相关论文
共 19 条
[1]   Methods used in the structure determination of bovine mitochondrial F-1 ATPase [J].
Abrahams, JP ;
Leslie, AGW .
ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY, 1996, 52 :30-42
[2]   THE CCP4 SUITE - PROGRAMS FOR PROTEIN CRYSTALLOGRAPHY [J].
BAILEY, S .
ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY, 1994, 50 :760-763
[3]   Structural insight into the role of the ribosomal tunnel in cellular regulation [J].
Berisio, R ;
Schluenzen, F ;
Harms, J ;
Bashan, A ;
Auerbach, T ;
Baram, D ;
Yonath, A .
NATURE STRUCTURAL BIOLOGY, 2003, 10 (05) :366-370
[4]   Crystallography & NMR system:: A new software suite for macromolecular structure determination [J].
Brunger, AT ;
Adams, PD ;
Clore, GM ;
DeLano, WL ;
Gros, P ;
Grosse-Kunstleve, RW ;
Jiang, JS ;
Kuszewski, J ;
Nilges, M ;
Pannu, NS ;
Read, RJ ;
Rice, LM ;
Simonson, T ;
Warren, GL .
ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY, 1998, 54 :905-921
[5]   Ribbons [J].
Carson, M .
MACROMOLECULAR CRYSTALLOGRAPHY, PT B, 1997, 277 :493-505
[6]   Macrolide-ketolide inhibition of MLS-resistant ribosomes is improved by alternative drug interaction with domain II of 23S rRNA [J].
Douthwaite, S ;
Hansen, LH ;
Mauvais, P .
MOLECULAR MICROBIOLOGY, 2000, 36 (01) :183-192
[7]   ROLE OF PROTONATED AND NEUTRAL FORMS OF MACROLIDES IN BINDING TO RIBOSOMES FROM GRAM-POSITIVE AND GRAM-NEGATIVE BACTERIA [J].
GOLDMAN, RC ;
FESIK, SW ;
DORAN, CC .
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 1990, 34 (03) :426-431
[8]   High resolution structure of the large ribosomal subunit from a mesophilic Eubacterium [J].
Harms, J ;
Schluenzen, F ;
Zarivach, R ;
Bashan, A ;
Gat, S ;
Agmon, I ;
Bartels, H ;
Franceschi, F ;
Yonath, A .
CELL, 2001, 107 (05) :679-688
[9]   IMPROVED METHODS FOR BUILDING PROTEIN MODELS IN ELECTRON-DENSITY MAPS AND THE LOCATION OF ERRORS IN THESE MODELS [J].
JONES, TA ;
ZOU, JY ;
COWAN, SW ;
KJELDGAARD, M .
ACTA CRYSTALLOGRAPHICA SECTION A, 1991, 47 :110-119
[10]   Activity of the ketolide telithromycin is refractory to erm monomethylation of bacterial rRNA [J].
Liu, MF ;
Douthwaite, S .
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 2002, 46 (06) :1629-1633