对泰利霉素针对耐药突变体的抗生素作用的结构洞察。
Structural insight into the antibiotic action of telithromycin against resistant mutants.
作者信息
Berisio Rita, Harms Joerg, Schluenzen Frank, Zarivach Raz, Hansen Harly A S, Fucini Paola, Yonath Ada
机构信息
Max-Planck-Research Unit for Ribosomal Structure, Hamburg, Germany.
出版信息
J Bacteriol. 2003 Jul;185(14):4276-9. doi: 10.1128/JB.185.14.4276-4279.2003.
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.
摘要
与耐辐射球菌大核糖体亚基结合的酮内酯类药物泰利霉素的晶体结构表明，泰利霉素阻断核糖体出口通道，并与23S RNA的结构域II和V相互作用。与其他临床相关大环内酯类药物的比较为其对大环内酯耐药菌株增强活性提供了结构上的见解。
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本文引用的文献
1
Processing of X-ray diffraction data collected in oscillation mode.振荡模式下收集的X射线衍射数据的处理。
Methods Enzymol. 1997;276:307-26. doi: 10.1016/S0076-6879(97)76066-X.
2
Ribbons.丝带。
Methods Enzymol. 1997;277:493-505.
3
Methods used in the structure determination of bovine mitochondrial F1 ATPase.用于牛线粒体F1 ATP合酶结构测定的方法。
Acta Crystallogr D Biol Crystallogr. 1996 Jan 1;52(Pt 1):30-42. doi: 10.1107/S0907444995008754.
4
The CCP4 suite: programs for protein crystallography.CCP4软件包：用于蛋白质晶体学的程序。
Acta Crystallogr D Biol Crystallogr. 1994 Sep 1;50(Pt 5):760-3. doi: 10.1107/S0907444994003112.
5
Structural insight into the role of the ribosomal tunnel in cellular regulation.核糖体通道在细胞调控中作用的结构洞察。
Nat Struct Biol. 2003 May;10(5):366-70. doi: 10.1038/nsb915.
6
Structural basis for the antibiotic activity of ketolides and azalides.酮内酯类和氮杂内酯类抗生素活性的结构基础。
Structure. 2003 Mar;11(3):329-38. doi: 10.1016/s0969-2126(03)00022-4.
7
Activity of the ketolide telithromycin is refractory to Erm monomethylation of bacterial rRNA.酮内酯类药物泰利霉素的活性对细菌核糖体RNA的Erm单甲基化具有耐药性。
Antimicrob Agents Chemother. 2002 Jun;46(6):1629-33. doi: 10.1128/AAC.46.6.1629-1633.2002.
8
Telithromycin: the first of the ketolides.泰利霉素：首个酮内酯类药物。
Ann Pharmacother. 2002 Mar;36(3):452-64. doi: 10.1345/aph.1A038.
9
High resolution structure of the large ribosomal subunit from a mesophilic eubacterium.来自嗜温真细菌的大核糖体亚基的高分辨率结构。
Cell. 2001 Nov 30;107(5):679-88. doi: 10.1016/s0092-8674(01)00546-3.
10
Structural basis for the interaction of antibiotics with the peptidyl transferase centre in eubacteria.抗生素与真细菌肽基转移酶中心相互作用的结构基础。
Nature. 2001 Oct 25;413(6858):814-21. doi: 10.1038/35101544.
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