Department of Chemistry, Indian Institute of Science Education and Research (IISER), Pune, India.
Curr Protoc Nucleic Acid Chem. 2020 Jun;81(1):e106. doi: 10.1002/cpnc.106.
Development of efficient tools that would enable direct correlation of nucleic acid structure and recognition in solution and in solid state at atomic resolution is highly desired. In this context, we recently developed dual-purpose nucleoside probes made of a 5-selenophene-modified uracil core, which serves both as a conformation-sensitive fluorophore and as an X-ray crystallography phasing agent. In this article, we provide a detailed synthetic procedure to synthesize the phosphoramidites of 5-selenophene-modified 2'-deoxyuridine and 5-selenophene-modified uridine analogs. We also describe their site-specific incorporation into therapeutically relevant DNA and RNA oligonucleotide motifs by an automated solid support synthesis protocol. The dual-purpose and minimally invasive nature of the probes enables efficient analysis of the conformation and ligand binding abilities of bacterial decoding site RNA (A-site) and G-quadruplex structures of the human telomeric overhang in real time by fluorescence and in 3D by X-ray crystallography. © 2020 by John Wiley & Sons, Inc. Basic Protocol 1: Synthesis of 5-selenophene-2'-deoxyuridine 2 and its phosphoramidite 5 Support Protocol 1: Synthesis of 2-(tri-n-butylstannyl) selenophene Support Protocol 2: Synthesis of 5'-O-DMT-protected 5-iodo-2'-deoxyuridine 3 Basic Protocol 2: Synthesis of 5-selenophene-modified uridine 7 and its phosphoramidite 11 Basic Protocol 3: Synthesis of DNA oligonucleotides containing 5-selenophene-modified 2'-deoxyuridine 2 Basic Protocol 4: Synthesis of an RNA oligonucleotide containing 5-selenophene-modified uridine 7.
开发能够将核酸结构与溶液中和固态中的识别直接相关联的高效工具,分辨率达到原子水平,这是非常需要的。在这种情况下,我们最近开发了一种双用途核苷探针,由 5-硒吩修饰的尿嘧啶核心制成,它既可以作为构象敏感的荧光团,也可以作为 X 射线晶体学相位分析剂。在本文中,我们提供了详细的合成步骤,用于合成 5-硒吩修饰的 2'-脱氧尿苷和 5-硒吩修饰的尿嘧啶类似物的磷酰胺。我们还描述了它们通过自动化固相合成方案在治疗相关 DNA 和 RNA 寡核苷酸基序中的定点掺入。探针的双重用途和微创性质使得能够通过荧光和 X 射线晶体学实时有效地分析细菌解码位点 RNA(A 位)的构象和配体结合能力以及人类端粒突出的 G-四链体结构。©2020 年由 John Wiley & Sons, Inc. 基本方案 1:5-硒吩-2'-脱氧尿苷 2 的合成及其磷酰胺 5 的合成 支持方案 1:2-(三丁基锡基)硒吩的合成 支持方案 2:5'-O-DMT-保护的 5-碘-2'-脱氧尿苷 3 的合成 基本方案 2:5-硒吩修饰的尿嘧啶 7 的合成及其磷酰胺 11 的合成 基本方案 3:含有 5-硒吩修饰的 2'-脱氧尿苷 2 的 DNA 寡核苷酸的合成 基本方案 4:含有 5-硒吩修饰的尿嘧啶 7 的 RNA 寡核苷酸的合成。