氨酸-氨酸二聚体:一种全碳水化合物支架,对富含AT的DNA复合体具有很高的亲和力
Sunil Kumar1, Liang Xue, Dev P Arya
1Laboratory of Medicinal Chemistry, Department of Chemistry, Clemson University, Clemson, South Carolina 29634, USA.
Journal of the American Chemical Society
|April 29, 2011
概括
一种新型的二次性尼奥米辛结合物选择性地与富含AT的DNA序列结合. 生物物理研究揭示了它对连续AT通道的高度亲和力,这表明在准特定DNA结构方面有潜在的应用.
科学领域:
- 药用化学 医学化学
- 分子生物学分子生物学
- 生物物理学的生物物理.
背景情况:
- 尼奥米是一种氨基糖化物抗生素,已知能结合核酸.
- 开发选择性DNA结合剂对于治疗应用至关重要.
- 双体合物提供了增强结合亲和力和选择性的潜力.
研究的目的:
- 合成和表征一个二次性尼奥米辛结合物 (3).
- 调查结合物3对具有不同基组成和构造的DNA的结合选择性和亲和力.
- 为了阐明与DNA结合3的结合模式和固态度.
主要方法:
- 二次性尼奥米辛结合物的合成和表征 3.
- 生物物理技术包括异热定位热量计 (ITC),循环二元化 (CD),光间位移 (FID) 和紫外线热变质.
- 用各种合成DNA双重体,三重体和发针结构进行研究.
主要成果:
- 结合物3对富含AT的DNA序列表现出强烈的偏好,而不是富含GC的DNA序列.
- 与DNA三重体相比,它对DNA双重体的亲和力更高,并且稳定了多重体,同时破坏了多重体的稳定.
- 连续的AT通道的结合亲和力明显高于交替的AT基对,结合部位大小为10-12个基对,分子内双重体的1:1石基度.
结论:
- 立米胺结合物3选择性地与富含AT的DNA结合,特别是连续的AT通道.
- 绑定模式可能涉及主要槽,并稳定双重组和破坏三重组的稳定性.
- 结合物3显示出高度的亲和力和选择性,具有针对特定DNA结构的潜力.
相关概念视频
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 has a double-helix structure. The...
DNA Structure
DNA has a double-helix structure. The...
Single-Strand DNA Binding Proteins
For successful DNA replication, the unwinding of double-stranded DNA must be accompanied by stabilization and protection of the separated single strands of the DNA. This crucial task is performed by single-strand DNA-binding (SSB) proteins. They bind to the DNA in a sequence-independent manner, which means that the nitrogenous bases of the DNA need not be present in a specific order for binding of SSB proteins to it. The binding of SSB proteins straightens single-stranded DNA (ssDNA) and makes...


