68Ga-labeled dimeric and trimeric cyclic RGD peptides as potential PET radiotracers for imaging gliomas

被引:9
作者
Zhao, Zuo-Quan [1 ,2 ]
Ji, Shundong [3 ]
Li, Xiao-Yan [4 ]
Fang, Wei [1 ,2 ]
Liu, Shuang [3 ]
机构
[1] Chinese Acad Med Sci, Natl Ctr Cardiovasc Dis, Fuwai Hosp, Dept Nucl Med, Beijing, Peoples R China
[2] Peking Union Med Coll, Beijing, Peoples R China
[3] Purdue Univ, Sch Hlth Sci, 550 Stadium Mall Dr, W Lafayette, IN 47907 USA
[4] Beijing Normal Univ, Coll Chem, Minist Educ, Key Lab Radiopharmaceut, Beijing 100875, Peoples R China
关键词
Radiotracers; Integrin alpha(v)beta(3); Ga-68-labeled cyclic RGD peptides; Glioma imaging; IMPROVING TUMOR UPTAKE; INTEGRIN ALPHA(V)BETA(3); BIOLOGICAL-PROPERTIES; EXCRETION KINETICS; F-18-ALFATIDE II; LUNG-CANCER; GLIOBLASTOMA; CILENGITIDE; EXPRESSION; LINKER;
D O I
10.1016/j.apradiso.2019.03.033
中图分类号
O61 [无机化学];
学科分类号
070301 ; 081704 ;
摘要
Ga-68-labeled cyclic RGD dimers and trimer were evaluated as PET radiotracers. It was found that the linker group had little impact on alpha(v)beta(3) binding affinity of RGD dimers, which share similar alpha(v)beta(3) binding affinity with the RGD trimer despite of their different multiplicity. Biodistribution properties of Ga-68 radiotracers depend on RGD peptides and radiometal chelates. Among the Ga-68 radiotracers evaluated, Ga-68-I2P-RGD(2) has the best tumor uptake with good tumor-to-background ratios, and is a good PET radiotracer for imaging gliomas.
引用
收藏
页码:168 / 177
页数:10
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