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

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。

The Acquisition of Target Peptide 2PEG- (GEBP11) 3 and Its BiologicalActivity Evaluation for Gastric Cancer Target Therapy

Objective:To obtain gebp11 trimer. 2PEG- (GEBP11)3, in order to improve gebp11 peptide receptor binding affinityand specificity, blood circulation.Methods:by PEGylation and poly functionalized synthetic 2PEG- (GEBP11)3, by human umbilical veinendothelial cells and human gastric cancer cell line SGC7901 in vitro co cultured gastric cancer vascular endothelial cells in order toobtain the characteristics, in both of them are combined with specific test.Results:gebp11 and 2PEG- (GEBP11)3 the IC50 values were451.7 + 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 themonomer, and the affinity of the labeling process of gebp11 peptides and Co-HUVECs no obvious effect, has good biological activity.