| 冉浩男 王燕 李佳蔚 邢宝继 刘金峰.胃癌靶向治疗中靶向肽2PEG-(GEBP11)3的获取及其生物学活性评价[J].,2015,15(33):6455-6457 |
| 胃癌靶向治疗中靶向肽2PEG-(GEBP11)3的获取及其生物学活性评价 |
| The Acquisition of Target Peptide 2PEG- (GEBP11) 3 and Its BiologicalActivity Evaluation for Gastric Cancer Target Therapy |
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| DOI： |
| 中文关键词: 胃癌细胞 靶向治疗 靶向肽 |
| 英文关键词: Gastric cancer cells Target therapy Target peptide |
| 基金项目: |
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| 中文摘要: |
| 目的：获取GEBP11（肿瘤血管靶向肽）三聚体，即2PEG-(GEBP11)3，以期提高GEBP11 短肽的受体亲和力及特异性、血液循
环。方法：通过PEGylation 和多聚化修饰合成2PEG-(GEBP11)3，通过人脐静脉内皮细胞与胃癌细胞SGC7901 体外共培养以获的
胃癌血管内皮细胞的部分特性，在对两者进行结合特异性的检验。结果：成功获取2PEG-(GEBP11)3；GEBP11 和2PEG-(GEBP11)3
的IC50值分别为451.7± 3.8，52.6± 3.4 nmol/L (n=3)，三聚体GEBP11 短肽的受体结合活性几乎是单体的10 倍。结论：细胞竞争性
结合实验和放射自显影提示2PEG-(GEBP11)3与Co-HUVECs 的亲和力高于单体，且标记过程对GEBP11 短肽与Co-HUVECs的
亲和力无明显影响，具有良好的生物学活性。 |
| 英文摘要: |
| Objective:To obtain gebp11 trimer. 2PEG- (GEBP11)3, in order to improve gebp11 peptide receptor binding affinity
and specificity, blood circulation.Methods:by PEGylation and poly functionalized synthetic 2PEG- (GEBP11)3, by human umbilical vein
endothelial cells and human gastric cancer cell line SGC7901 in vitro co cultured gastric cancer vascular endothelial cells in order to
obtain the characteristics, in both of them are combined with specific test.Results:gebp11 and 2PEG- (GEBP11)3 the IC50 values were
451.7 + 3.8, 52.6 + 3.4 nmol / L (n = 3), trimer of gebp11 peptide receptor binding activity is almost 10 times that of monomer.Conclusion:Cell competition binding experiments and autoradiography prompt 2PEG- (of GEBP11)3 and Co-HUVECs affinity than the
monomer, and the affinity of the labeling process of gebp11 peptides and Co-HUVECs no obvious effect, has good biological activity. |
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