基因靶向肤核酸的合成及放射性核素.PDF

CNIC-01992 CAEP-0255 基因靶向肤核酸的合成及放射性核素 标记研究进展 宋宏涛张华明高晖 (中国工程物理研究院核物理与化学研究所，绵阳，621900) 摘要 肤核酸CPNA) 作为一种反义核酸类化合物，是 DNA 模拟物，能 与 DNA 和 RNA 以序列特异性方式结合，在分子水平的基因研究和 基因治疗方面有其独特的优越性和广泛的应用前景o 为了优化肤核 酸的性质，许多 PNA 类似物也被合成出来，以改良 PNA 性能、拓宽 DNA 应用。对具有特异基因靶向亲和性的长链 PNA 分子进行修饰 后，用放射性核素标记，可达到在放射性肿瘤治疗上靶向明确和对非 靶组织最小损伤的目的，对于基因水平的肿瘤治疗具有十分重要的 应用研究意义。文章综述了 PNA 及其类化合物的基本合成思路和 主要合成路线，同时对放射性核素标记 PNA 类物质的相关研究进行 了评述和展望o 关键词:肤核酸单体核昔酸基因靶向 210 Summarization on the Synthesis and Radionuclide-labeling of Peptide Nucleic Acid for An Oligonucleotide Analogue (In Chinese) SONG Hongtao ZHANG Huaming GAO Hui Clnstitute of Nuclear Physics and Chemistry , CAEP , Mianyang , 621900) ABSTRACT Peptide nucleic acid CPNA) , which is one kind of antisense nucleic acid compounds and an oligonucleotide analogue that binds strongly to DNA and RNA in a sequence specific manner , has its unique advantages in the field of molecular diagnostics and treatment of diseases. Now , people gradually attach more importance to PNA. To optimize the application of PNA in genetic re- search and therapy , a great number of backbone modifications on the newly- type structures of PNA were synthesized to improve its physicochemical proper- ties , such as hybridization speciality , solubility in biofluid , or cell permeability. The modified PNA labeled with radionuclides , which can obtain the aim at spe- cific target and minimal non-target trauma , has important role in research and application of tumorous genitherapy. Here a review on the basic synthesis idea and