1. 68Ga-labeled dimeric and trimeric cyclic RGD peptides as potential PET radiotracers for imaging gliomas.
- Author
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Zhao, Zuo-Quan, Ji, Shundong, Li, Xiao-Yan, Fang, Wei, and Liu, Shuang
- Subjects
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RADIOACTIVE tracers , *CYCLIC peptides , *DIMERS - Abstract
68Ga-labeled cyclic RGD dimers and trimer were evaluated as PET radiotracers. It was found that the linker group had little impact on α v β 3 binding affinity of RGD dimers, which share similar α v β 3 binding affinity with the RGD trimer despite of their different multiplicity. Biodistribution properties of 68Ga radiotracers depend on RGD peptides and radiometal chelates. Among the 68Ga radiotracers evaluated, 68Ga-I2P-RGD 2 has the best tumor uptake with good tumor-to-background ratios, and is a good PET radiotracer for imaging gliomas. • Three new 68Ga radiotracers were prepared and evaluated as radiotracers for glioma imaging. • NOTA-Galacto-RGD 2 , NOTA-I2P-RGD 2 and NOTA-4P-RGD 3 share similar α v β 3 binding affinity. • 68Ga-I2P-RGD 2 has higher tumor uptake than 68Ga-Galacto-RGD 2 and 68Ga-4P-RGD 3. • The blocking experiment shows that the tumor uptake of 68Ga radiotracers is α v β 3 –specific. [ABSTRACT FROM AUTHOR]
- Published
- 2019
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