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Development of bombesin peptide kit for prostate cancer diagnosis and treatment using 64Cu/177Lu.

  • Kim, Mi Hyun (RI-Convergence Research, Korea Institute of Radiological and Medical Sciences) ;
  • Kim, Min Hwan (RI-Convergence Research, Korea Institute of Radiological and Medical Sciences) ;
  • Kim, Kwang Il (RI-Convergence Research, Korea Institute of Radiological and Medical Sciences) ;
  • Kim, Jung Young (RI-Convergence Research, Korea Institute of Radiological and Medical Sciences) ;
  • Lee, Tae Sup (RI-Convergence Research, Korea Institute of Radiological and Medical Sciences) ;
  • Kang, Joo Hyun (RI-Convergence Research, Korea Institute of Radiological and Medical Sciences) ;
  • Lee, Kyo Chul (RI-Convergence Research, Korea Institute of Radiological and Medical Sciences) ;
  • Lee, Yong Jin (RI-Convergence Research, Korea Institute of Radiological and Medical Sciences)
  • 투고 : 2017.11.08
  • 심사 : 2017.12.08
  • 발행 : 2017.12.30

초록

It has been reported that $^{64}Cu$ was radiolabeled with bombesin (BBN) peptide binding to the gastrin releasing peptide receptor expressed in human prostate cancer cells (PC3), confirming tumor target efficacy in mouse model. In this study, we developed the kit for the diagnosis and treatment of prostate cancer that can be used clinically using bombesin peptide available of $^{64}Cu$ and $^{177}Lu$ radioisotope labeling. The NODAGA-galacto-BBN peptide containing the NODAGA chelator and galactose was dispensed into a sterilized glass vial and lyophilized to prepare a kit. The stability of the kit after long-term storage in the $4^{\circ}C$ cold chamber and the radiolabeling efficiency after $^{64}Cu$ or $^{177}Lu$ labeling were confirmed by thin layer chromatography. When labeling with $^{64}Cu$ at the initial stage of storage, labeling efficiency of NODAGA-galacto-BBN peptide kit was over 96%, labeling efficiency was over 90% when $^{177}Lu$ was labeled. At 11 months after storage, the radiolabeling efficiency of kit against $^{64}Cu$ and $^{177}Lu$ was each over 95% and 90%. The cell viability was significantly reduced in the $^{177}Lu$-NODAGA-galacto-BBN treated group compared with the control and $^{177}Lu$ alone treated group in clonogenic assay. In conclusion, the NODAGA-galacto-BBN kit prepared by the lyophilization showed high stability over time and high yield of radioisotope labeling. Also $^{177}Lu$-NODAGA-galacto-BBN confirmed high cytotoxicity to prostate cancer cells. Therefore, the NODAGA-galacto-bombesin kit is expected to be useful for the diagnosis and treatment of prostate cancer patients.

키워드

참고문헌

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