相关实验视频

Updated: Jun 26, 2025

Protocol for the Solid-phase Synthesis of Oligomers of RNA Containing a 2'-O-thiophenylmethyl Modification and Characterization via Circular Dichroism

Protocol for the Solid-phase Synthesis of Oligomers of RNA Containing a 2'-O-thiophenylmethyl Modification and Characterization via Circular Dichroism

Published on: July 28, 2017

含有LNA-硫酸盐和硫酸胺脊柱连接的寡核酸的合成和特性

Belma Zengin Kurt^1,2, Debashis Dhara¹, Afaf H El-Sagheer^1,3

¹Department of Chemistry, Chemistry Research Laboratory, University of Oxford, Oxford OX1 3TA, U.K.

Organic letters

|May 8, 2024

概括

合成了具有降低电荷和改善细胞吸收的新型寡核酸类似物. 这些改性寡核酸具有较高的RNA亲和力和核酶抗性,解决了治疗应用的关键局限性.

科学领域:

药用化学医学化学
氧核酸治疗药物治疗药物
生物化学生物化学

背景情况:

寡核酸具有治疗潜力,但其生物可用性较差.
增强细胞吸收对于有效的寡核酸药物递送至关重要.

研究的目的:

合成和表征具有改善物理化学性质的新型寡核酸类比物.
调查低电荷连接的潜力,以提高治疗效用.

主要方法:

合成含有LNA-硫酸盐和硫酸胺链接的低电荷寡核酸.
加入2'-O-甲基糖和酸骨干.
物理研究来评估结合亲和力和核酶抵抗力.

主要成果:

成功合成了具有减少负电荷的新型寡核酸相似物.
已证明改性寡核酸对RNA标具有很高的结合亲和力.
确认了对核酶的优异耐药性,表明增强了稳定性.

结论:

带有人工链接的低电荷寡核酸为克服生物可用性挑战提供了一个有希望的策略.
这些类似物具有有利的特性,可作为下一代寡核酸治疗药物开发.

更多相关视频

Chemical Triphosphorylation of Oligonucleotides

Chemical Triphosphorylation of Oligonucleotides

Published on: June 2, 2022

Sequence-specific and Selective Recognition of Double-stranded RNAs over Single-stranded RNAs by Chemically Modified Peptide Nucleic Acids

Sequence-specific and Selective Recognition of Double-stranded RNAs over Single-stranded RNAs by Chemically Modified Peptide Nucleic Acids

Published on: September 21, 2017

相关概念视频

Nucleic Acid Structure

Nucleic Acid Structure

The pentose sugar in DNA is deoxyribose, while in RNA the pentose sugar is ribose. The difference between the sugars is the presence of the hydroxyl group on the ribose's second carbon and a hydrogen on the deoxyribose's second carbon. The phosphate residue attaches to the hydroxyl group of the 5′ carbon of one sugar and the hydroxyl group of the 3′ carbon of the sugar of the next nucleotide, which forms a 5′ to 3′ phosphodiester linkage.
DNA Structure
DNA...

Phosphodiester Linkages

Phosphodiester Linkages

Overview
Phosphodiester bond forms when a phosphoric acid molecule (H3PO4) links with two hydroxyl groups (–OH) of two other molecules, forming two ester bonds. Two water molecules are released in this process. The phosphodiester bond is commonly found in nucleic acids (DNA and RNA) and plays a critical role in their structure and function.
Phosphodiester Bonds Link Nucleotides Together
DNA and RNA are polynucleotides or long chains of nucleotides that are linked together. A nucleotide is...

Nucleic Acids

Nucleic Acids

Nucleic acids are the most important macromolecules for the continuity of life. They carry the cell's genetic blueprint and carry instructions for its functioning.
DNA and RNA
The two main types of nucleic acids are deoxyribonucleic acid (DNA) and ribonucleic acid (RNA). DNA is the genetic material in all living organisms, ranging from single-celled bacteria to multicellular mammals. It is in the nucleus of eukaryotes and in the organelles, chloroplasts, and mitochondria. In prokaryotes,...

Nucleic acids

Nucleic acids

Nucleic acids are the most important macromolecules for the continuity of life. They carry the cell's genetic blueprint and carry instructions for its functioning.
DNA and RNA
The two main types of nucleic acids are deoxyribonucleic acid (DNA) and ribonucleic acid (RNA). DNA is the genetic material in all living organisms, ranging from single-celled bacteria to multicellular mammals. It is in the nucleus of eukaryotes and in the organelles, chloroplasts, and mitochondria. In prokaryotes,...

Nucleic Acids and Nucleotides

Nucleic Acids and Nucleotides

Nucleic acids are the most important macromolecules for the continuity of life. They carry the cell's genetic blueprint and have instructions for its functioning. The two main types of nucleic acids are deoxyribonucleic acid (DNA) and ribonucleic acid (RNA).
Deoxyribonucleic Acid (DNA)
DNA is the genetic material in all living organisms, ranging from single-celled bacteria to multicellular mammals. It is in the nucleus of eukaryotes and the organelles such as chloroplasts and mitochondria....

Ligand Binding and Linkage

Ligand Binding and Linkage

Allosteric proteins have more than one ligand binding site; the binding of a ligand to any of these sites influences the binding of ligands to the other sites. When a protein is allosteric, its binding sites are called coupled or linked. In the case of enzymes, the site that binds to the substrate is known as the active site and the other site is known as the regulatory site. When a ligand binds to the regulatory site, this leads to conformational changes in the protein that can influence...