【摘要】 采用2种方法修饰RGD环肽二聚体,在2个RGD模序之间引入2个PEG4分子,以及在RGD二聚体与双功能螯合剂HYNIC之间引入1个PEG4分子,比较在不同部位引入PEG4分子对99Tcm标记的RGD环肽二聚体体内外性质的影响。研究结果表明,在2个RGD模序之间引入2个PEG4分子能显著提高RGD环肽二聚体与整合素αvβ3的亲和力;PEG4的引入能够增强标记物的水溶性9。9Tcm-HYNIC-2PEG4-RGD dimer具有更好的体内外性质,作为一种潜在的肿瘤显像剂,具有进一步研究开发的价值。更多还原

【Abstract】 The cyclic RGD dimer was modified with 2 PEG4 between RGD motifs in the RGD dimer,as well as with 1 PEG4 between the RGD dimer and chelator HYNIC.The in vitro and in vivo characteristics of 99Tcm-labeled different RGD dimer were evaluated,including IC50,lg P,pharmacokinetics and biodistribution.It is demonstrated that introducing of 2 PEG4 between RGD motifs significantly enhances the binding affinity of RGD dimer and integrin αvβ3;the introducing of PEG4 improves the hydrophilicity of 99Tcm-labeled RGD dimmer.99Tcm-HYNIC-2PEG4-RGD dimer possess better properties,with the value of further development for integrin αvβ3-positive tumors imaging.更多还原