10-23 DNA 酶中腺苷的 2’- 功能基团促进催化活性。
2'-Functional group of adenosine in 10-23 DNAzyme promotes catalytic activity.
机构信息
College of Chemical Engineering and Materials, Hebei Key Laboratory of Heterocyclic Compounds, Handan University, Handan 056005, China; State Key Laboratory of Toxicology and Medical Countermeasures, Beijing Institute of Pharmacology & Toxicology, Beijing 100850, China.
School of Life Science and Engineering, Handan University, Handan 056005, China; State Key Laboratory of Toxicology and Medical Countermeasures, Beijing Institute of Pharmacology & Toxicology, Beijing 100850, China.
出版信息
Bioorg Med Chem Lett. 2020 Feb 15;30(4):126961. doi: 10.1016/j.bmcl.2020.126961. Epub 2020 Jan 8.
10-23 DNAzyme is an artificially selected catalytic DNA molecule. Its great potential as genetic therapeutics promoted chemical modifications for more efficient DNAzymes. Here, 10-23 DNAzyme was modified on its six deoxyadenosine residues (A5, A9, A11, A12, A15 in the catalytic domain and A0 of the recognition arm next to the cleavage site) with compound 1, an adenosine analogue with 2'-O-[N-(aminoethyl)carbamoyl]methyl group. A positive effect of compound 1 at A15 was observed (HJDS-05, k = 0.0111 min). Compared to the effect of 2'-H and 2'-OMe at A15, this result provided an approach for more efficient DNAzyme by combining 2'-substituted amino group of adenosine with A15 as the lead structure.
10-23DNA 酶是一种人工选择的催化 DNA 分子。它作为基因治疗的巨大潜力促进了化学修饰以获得更有效的 DNA 酶。在这里，在 10-23DNA 酶的六个脱氧腺苷残基（催化结构域中的 A5、A9、A11、A12、A15 和靠近切割位点的识别臂中的 A0）上用化合物 1 进行了修饰，化合物 1 是一种具有 2'-O-[N-(氨乙基)氨基甲酰基]甲基取代基的腺嘌呤类似物。在 A15 处观察到化合物 1 的积极作用（HJDS-05，k=0.0111min）。与 2'-H 和 2'-OMe 在 A15 处的作用相比，这一结果为通过将腺嘌呤的 2'-取代氨基与 A15 结合作为先导结构来获得更有效的 DNA 酶提供了一种方法。
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