NMR Structures of Thiostrepton Derivatives for Characterization of the Ribosomal Binding Site

NMR Structures of Thiostrepton Derivatives for Characterization of the Ribosomal Binding Site
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DOI：
10.1002/anie.201003582
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发表时间：
2011-01-01
期刊：
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
影响因子：
16.6
通讯作者：
Arndt, Hans-Dieter
Arndt, Hans-Dieter
中科院分区：
化学1区
文献类型：
--
作者：
Jonker, Hendrik R. A.;Baumann, Sascha;Arndt, Hans-Dieter

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结构探测：通过使用半合成、NMR结构测定、对接（见图）和生物学评价以综合方式在其核糖体结合位点测定具有靶向形状变化的硫链丝菌素和衍生物的活性。这种组合揭示了靶点（复合RNA-蛋白质复合物）嵌入的药基内分子识别的重要元素。版权所有© 2011 WILEY-VCH Verlag GmbH & Co. KGaA，魏因海姆。
Structural probing: The activity of thiostrepton and derivatives with targeted shape changes was determined at their ribosomal binding site by using semisynthesis, NMR structure determination, docking (see picture), and biological evaluation in an integrated fashion. This combination revealed important elements of molecular recognition within the embedded pharmocophore of the target, a composite RNA-protein complex. Copyright© 2011 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.