Cellular uptake of covalent conjugates of oligonucleotide with membrane-modifying peptide, peptaibol.
Cellular uptake of covalent conjugates of oligonucleotide with membrane-modifying peptide, peptaibol.
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细胞摄取寡核苷酸与膜修饰肽 peptaibol 的共价缀合物。
DOI：
10.1016/j.bmc.2012.03.054
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发表时间：
2012
影响因子：
3.5
通讯作者：
H. Urata
中科院分区：
文献类型：
--
作者：
S. Wada;Yasunari Hitora;Saori Yokoe;O. Nakagawa;H. Urata
利用从真菌木霉（Trichoderma viride）中分离出的11个残余肽——trichorovin-XIIa (TV-XIIa)，我们与TV-XIIa合成了20聚寡核苷酸的共价偶联物，以研究TV-XIIa在细胞传递中的潜在应用。结果表明，结合物被人肺癌A549细胞逐渐吸收。接下来，我们检测了这些偶联物对p53蛋白表达的反义作用。在偶联物存在的情况下，用浓度为5μM的转染液处理后，p53的表达显著降低约20-50%。
Using the membrane-modifying peptide, trichorovin-XIIa (TV-XIIa), which is an 11-residual peptaibol isolated from the fungus Trichoderma viride, we synthesized covalent conjugates of 20-mer oligonucleotide with TV-XIIa to examine the potential use of TV-XIIa in cellular delivery. The results indicated that the conjugates were progressively taken up by human lung carcinoma A549 cells. Next, the antisense effects of the conjugates on p53 protein expression were examined. The p53 expression was significantly decreased by ca. 20–50% in the presence of the conjugates upon treatment with the transfection solution at the concentration of 5μM.