PNA conjugated to high-molecular weight poly(ethylene glycol): Synthesis and properties
PNA conjugated to high-molecular weight poly(ethylene glycol): Synthesis and properties
复制标题
DOI：
10.1080/15257770701490548
复制
发表时间：
2007-01-01
影响因子：
1.3
通讯作者：
Xodo, Luigi
中科院分区：
文献类型：
--
作者：
Bonora, Gian Maria;Drioli, Sara;Xodo, Luigi
肽核酸（PNAs）能够识别并结合特定的DNA或RNA链，具有高亲和力和选择性，优于类似的寡核苷酸序列。这些衍生物具有很高的化学稳定性，它们对核酸酶和蛋白酶的抗性使它们成为分子生物学中治疗药物、诊断工具和探针的良好候选者。然而，一个实际的限制是它们的低水溶性和高自聚集倾向。此外，仍然需要一种方便和有用的递送系统，并且已经提出了几种方法来改善它们的细胞摄取，如肽，（[2]）阳离子脂质体，（[3]）和亲脂配体。（b[4]）在这方面，PNAs与两亲性、毒性和大部分可溶性聚乙二醇（peg）的结合可以评估，以增加其在水介质中的溶解度，以及改善其细胞膜通透性和抗酶降解能力，使用与先前描述的寡核苷酸相同的方法。([5])
Peptide nucleic acids (PNAs) are able to recognize and bind to a specific DNA or RNA strand with high affinity and selectivity, superior to analogous oligonucleotide sequences. These derivatives have high chemical stability, and their resistance to nucleases and proteases make them good candidates as therapeutic agents, diagnostic tools, and probes in molecular biology.([1]) However, a practical limitation is their low water solubility and high tendency toward self-aggregation. Moreover, a facile and useful system of delivery is still demanded and several methods have been proposed to improve their cellular uptake, as peptides,([2]) cationic liposomes,([3]) and lipophilic ligands.([4]) In this regard, the conjugation of PNAs with the amphiphilic, atoxic, and largely soluble poly(ethylene glycol)s (PEGs) can be evaluated to increase their solubility in aqueous media, as well as to improve their cell membrane permeability and resistance to enzymatic degradation, using the same approach previously described for oligonucleotides.([5])