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KMID : 1145520160020020118
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Journal of Radiopharmaceuticals and Molecular Probes
2016 Volume.2 No. 2 p.118 ~ p.122
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Preliminary evaluation of new 68Ga-labeled cyclic RGD peptides by PET imaging
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Shin Un-Chol
Jung Ki-Hye
Lee Ji-Woong
Lee Kyo-Chul
Lee Yong-Jin
Park Ji-Ae
Kim Jung-Young
Kang Joo-Hyun
An Gwang-Il
Ryu Young-Hoon
Choi Jae-Yong
Kim Kyeong-Min
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Abstract
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Integrin αvβ3 plays an important role in the tumor metastases and angiogenesis. Arginine-glycine-aspartate (RGD) peptide motif binds to the integrin αvβ3. General 68Ga-labeled cyclic RGD peptides was rapidly eliminated from the circulatory system by renal excretion because of its hydrophilic property. The purpose of this study was to develop a novel 68Ga-labeled cyclic RGD peptides, which could acquire enhanced PET tumor images with improved pharmacokinetics by adopting biphenyl group between chelator and RGD peptides. 68Ga-DOTA2P-c(RGDyK) was demonstrated a 12% higher lipophilicity level than 68Ga-DOTA-c(RGDyK) as a reference compound. In the animal PET, 68Ga-DOTA-2P-c(RGDyK) represented relatively lower blood-clearance, and an increased signal to noise ratio compared to 68Ga-DOTA-c(RGDyK). From these perspective, 68Ga-DOTA-2Pc(RGDyK) could be a good candidate for in integrin αvβ3-expressed tumor imaging.
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KEYWORD
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Radiometals, 68Ga-DOTA-c(RGDyK), 68Ga-DOTA-2P-c(RGDyK), Cyclic RGD peptides, PET imaging
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