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肽核酸(PNA)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。为了优化肽核酸的性质,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。
Peptide nucleic acid (PNA), as an antisense nucleic acid compound, is a DNA mimic that binds DNA and RNA in a sequence-specific manner and has its unique advantages and gene-therapy at the molecular level Application prospects. In order to optimize the properties of peptide nucleic acids, many PNA analogs have also been synthesized to improve PNA performance and broaden DNA applications. After modification of long-chain PNA molecules with specific gene-targeted affinity, labeling with radionuclides can achieve the goal of targeting clear and minimal damage to non-target tissues in the treatment of radioactive tumors. For gene therapy of tumors at gene level It has very important significance in applied research. In this paper, the basic synthetic ideas and main synthetic routes of PNAs and their analogs are reviewed. At the same time, the related studies of radionuclide labeled PNAs are reviewed and discussed.