【摘要】 目的 发展一种针对表皮生长因子过量表达的肿瘤细胞的基因转移系统。方法 人工合成了一种N端含多个赖氨酸残基，C端为人表皮生长因子(EGF)的受体结合域的33肽，此合成肽(K9E肽)既具有DNA结合活性，又能为细胞表面EGF受体所识别并内在化。K9E肽与萤火虫荧光素酶表达质粒pEBluc按一定比例结合形成核酸复合物，以此为基础，利用受体介导的基因转移技术，组建了外源基因转移系统。结果 核酸复合物直接加入于类上皮癌细胞A431的培养液中，48小时后可从细胞裂解液中测出荧光素酶的显著表达。结论 该系统可特异性地将外源 基因导入EGF受体过量表达的肿瘤细胞。

Abstract A polypeptide with 33 amino acid residues was designed and synthesized. Its C terminal was composed of multiple lysine residues, which played as a DNA condensing agent, whereas the N terminal was the receptor binding domain of Epidermal Growth Factor(N₃₂ ～K₄₈ ). Through a spontaneous self-assembly process with electrostatic interaction, the synthetic peptide combined with a luciferase expression vector, pEBluc, to form an EGF receptor targeting nucleic acid complex. Significant luciferase activity was detected 48 hours after adding this complex directly to the culture medium of the A431 cells. This synthetic peptide could be used to construct a gene transfer system mediated by the endocytosis via EGF receptor. It promoted a very possibility of the gene therapy for the cancers such as glioma, melanoma and squamous carcinoma which are known of epidermal growth factor receptor overexpresssion.

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