Journal of Radiopharmaceuticals and Molecular Probes (대한방사성의약품학회지)

Korean Society of Radiopharmaceuticals and Molecular Probes (대한방사성의약품학회)
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Preliminary evaluation of new 68Ga-labeled cyclic RGD peptides by PET imaging

  • Shin, Un Chol (Division of RI convergence research, Korea Institute of Radiological and Medical Sciences) ;
  • Jung, Ki-Hye (Division of RI convergence research, Korea Institute of Radiological and Medical Sciences) ;
  • Lee, Ji Woong (Division of RI convergence research, Korea Institute of Radiological and Medical Sciences) ;
  • Lee, Kyo Chul (Division of RI convergence research, Korea Institute of Radiological and Medical Sciences) ;
  • Lee, Yong Jin (Division of RI convergence research, Korea Institute of Radiological and Medical Sciences) ;
  • Park, Ji-Ae (Division of RI convergence research, Korea Institute of Radiological and Medical Sciences) ;
  • Kim, Jung Young (Division of RI convergence research, Korea Institute of Radiological and Medical Sciences) ;
  • Kang, Joo Hyun (Division of RI convergence research, Korea Institute of Radiological and Medical Sciences) ;
  • An, Gwang Il (Division of RI convergence research, Korea Institute of Radiological and Medical Sciences) ;
  • Ryu, Young Hoon (Department of Nuclear Medicine, Gangnam Severance Hospital, Yonsei University College of Medicine) ;
  • Choi, Jae Yong (Department of Nuclear Medicine, Gangnam Severance Hospital, Yonsei University College of Medicine) ;
  • Kim, Kyeong Min (Division of Medical Radiation Equipment, Korea Institute Radiological and Medical Sciences)
  • Received : 2016.11.23
  • Accepted : 2016.12.13
  • Published : 2016.12.30
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Abstract

Integrin ${\alpha}_v{\beta}_3$ plays an important role in the tumor metastases and angiogenesis. Arginine-glycine-aspartate (RGD) peptide motif binds to the integrin ${\alpha}_v{\beta}_3$. General $^{68}Ga$-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 $^{68}Ga$-labeled cyclic RGD peptides, which could acquire enhanced PET tumor images with improved pharmacokinetics by adopting biphenyl group between chelator and RGD peptides. $^{68}Ga$-DOTA-2P-c(RGDyK) was demonstrated a 12% higher lipophilicity level than $^{68}Ga$-DOTA-c(RGDyK) as a reference compound. In the animal PET, $^{68}Ga$-DOTA-2P-c(RGDyK) represented relatively lower blood-clearance, and an increased signal to noise ratio compared to $^{68}Ga$-DOTA-c(RGDyK). From these perspective, $^{68}Ga$-DOTA-2P-c(RGDyK) could be a good candidate for in integrin ${\alpha}_v{\beta}_3$-expressed tumor imaging.

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References

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