RNA 结合唑烷酮衍生物的构效关系研究。
Structure-activity studies of RNA-binding oxazolidinone derivatives.
机构信息
Department of Chemistry and Biochemistry, Ohio University, Athens, OH 45701, USA.
出版信息
Bioorg Med Chem Lett. 2011 Aug 1;21(15):4524-7. doi: 10.1016/j.bmcl.2011.05.130. Epub 2011 Jun 15.
Abstract
The structure-activity relationship of a series of oxazolidinones binding to T-box riboswitch antiterminator RNA has been investigated. Oxazolidinones differentially substituted at C-5 were prepared and the ligand-induced fluorescence resonance energy transfer (FRET) changes in FRET-labeled antiterminator model RNA were assayed. Both qualitative and quantitative analysis of the structure-activity relationship indicate that hydrogen bonding and hydrophobic properties play a significant role in ligand binding.
摘要
研究了一系列与 T 型框核糖体开关抗终止子 RNA 结合的恶唑烷酮的结构-活性关系。合成了在 C-5 位不同取代的恶唑烷酮，并测定了在 FRET 标记的抗终止子模型 RNA 中配体诱导的荧光共振能量转移 (FRET)变化。结构-活性关系的定性和定量分析表明，氢键和疏水性在配体结合中起着重要作用。
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