^(99)Tc^m标记的PEG_4/2PEG_4修饰的环状RGD二聚体体内外性质的对比  

Comparison of in Vitro and in Vivo Characteristics of ^(99)Tc^m-Labeled Cyclic RGD Dimers With PEG_4/2PEG_4 Linkers

作　　者：靳存敬[1] 史继云[1] 刘妍[1] 靳晓娜[2] 黄金铭[1] 赵慧云[1] 李方[2] 王凡[1] 

机构地区：[1]北京大学医学同位素研究中心,北京100191 [2]北京协和医院核医学科,北京100730

出　　处：《核化学与放射化学》2010年第5期287-292,共6页Journal of Nuclear and Radiochemistry

基　　金：国家自然科学基金资助项目(30780728)

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。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.

关 键 词：RGD环肽二聚体 整合素ΑVΒ3 PEG4 99Tcm标记 

分 类 号：O615.4[理学—无机化学]