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KMID : 1145520160020020108
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Journal of Radiopharmaceuticals and Molecular Probes
2016 Volume.2 No. 2 p.108 ~ p.112
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Kinetic analysis of 64Cu-NODAGA-gluco-E[c(RGDfK)]2 for a tumor angiogenesis PET tracer
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Choi Jae-Yong
Park Ji-Ae
Kim Jung-Young
Lee Ji-Woong
Lee Min-Kyung
Shin Un-Chol
Kang Joo-Hyun
An Gwang-Il
Lee Kyo-Chul
Ryu Young-Hoon
Kim Kyeong-Min
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Abstract
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Molecular imaging with the radiolabeled RGD peptides for αvβ3 integrin has been an increasing interest for tumor diagnosis and the treatment monitoring. Recently, 64Cu-NODAGA-gluco-E[c(RGDfK)]2 was developed for quantification of αvβ3 integrin and its biological properties was elucidated. To better understand the molecular process in vivo, we performed the kinetic analysis for the 64Cu-NODAGA-gluco-E[c(RGDfK)]2. After preparation of a radiotracer, dynamic PET images were obtained in the U87MG xenograft mice for 60 min (n = 6). Binding potential values were estimated from the 3-tissue compartment model, reference Logan andsimplified reference tissue model. In the early time frame (0-20 min), the liver, kidney, intestine, urinary bladder and tumor were visualized but these uptakes were diminished as time went by. The tumors showed a good contrast at 40 min after administration. 64Cu-NODAGA-E[c(RGDfK)]2 showed the 2-fold uptake in the tumor compared with that in the muscle. The parametric maps for binding values also provide the higher tumor-tobackground contrast than the static images. A binding value obtained from the 3-tissue compartment model was comparable to other modeling methods. From these results, we conclude that 64Cu-NODAGA-glucoE[c(RGDfK)]2 may be a promising PET radiotracer for the evaluation of angiogenesis.
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KEYWORD
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Integrin αvβ3, Angiogenesis, NODAGA, 64Cu, Bifunctional chelator, RGD
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