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Stability evaluation of Tc-99m radiolabeled GRPr antagonist with amino acid chelators

  • Zhengkun Zhong
  • Wentao Kan
  • Wei Liao
Article
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Abstract

In order to select a chelator with excellent stability, easier radiolabeling process and low cost, GRPr antagonist RM26 with the amino acid based chelator was radiolabeled with technetium-99m. The stability of the radiolabeled peptides in PBS, serum as well as in the presence of excess cysteine was compared.

Keywords

Technetium-99m Radiopeptide RM26 KGC N3S 
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Notes

Acknowledgements

This research is financially supported by Science and Technology Development of Foundation of China Academy of Engineering Physics (2014A0301011) and China National Natural Science Foundation (21571164).

References

  1. 1.
    Schroeder RPJ (2009) Peptide receptor imaging of prostate cancer with radiolabeled bombesin analogues. Methods 48:200–204CrossRefPubMedGoogle Scholar
  2. 2.
    Mansi R (2013) Targeting GRPR in urological cancers-from basic research to clinical application. Nat Rev Urol 10:235–244CrossRefPubMedGoogle Scholar
  3. 3.
    Carsten K (2013) Hybrid bombesin analogues: combining an agonist and an antagonist in defined distances for optimized tumor targeting. J Am Chem Soc 135:16793–16796CrossRefGoogle Scholar
  4. 4.
    Mansi R (2011) Evaluation of a 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid-conjugated bombesin-based radioantagonist for the labeling with single-photon emission computed tomography, positron emission tomography, and therapeutic radionuclides. Clin Cancer Res 15:5240–5249CrossRefGoogle Scholar
  5. 5.
    Ginj M (2006) Radiolabeled somatostatin receptor antagonists are preferable to agonists for in vivo peptide receptor targeting of tumors. Proc Natl Acad Sci USA 103:16436–16441CrossRefPubMedGoogle Scholar
  6. 6.
    Ginj M (2006) Radiolabeled somatostatin receptor antagonists are preferable to agonists for in vivo peptide receptor targeting of tumors. PNAS 103:16436–16441CrossRefPubMedGoogle Scholar
  7. 7.
    Kristell LSC (2014) Preclinical comparison of Al18F and 68Ga labeled gastrin-releasing peptide receptor antagonists for PET imaging of prostate cancer. J Nucl Med 12:2050–2056Google Scholar
  8. 8.
    Mansi R (2016) Bombesin-targeted PET of prostate cancer. J Nucl Med 10:67S–72SCrossRefGoogle Scholar
  9. 9.
    Shirmardi SP (2011) Synthesis and evaluation of a new bombesin analog labeled with 99mTc as a GRP receptor imaging agent. J Radioanal Nucl Chem 288:327–335CrossRefGoogle Scholar
  10. 10.
    Monroy-Guzman F (2003) Effect of Zr: Mo ratio on 99mTc generator performance based on zirconium molybdate gels. Appl Radiat Isot 59:27–34CrossRefPubMedGoogle Scholar
  11. 11.
    Monroy-Guzman F (2012) Production optimization of 99Mo/99mTc zirconium molybate gel generators at semi-automatic device: DISIGEG. Appl Radiat Isot 70:103–111CrossRefPubMedGoogle Scholar
  12. 12.
    Abram U (2006) Technetium and rhenium—coordination chemistry and nuclear medical applications. J Braz Chem Soc 17:1486–1500CrossRefGoogle Scholar
  13. 13.
    Lei K (1996) Technetium-99m antibodies labeled with MAG3 and SHNH: an in vitro and animal in vivo comparison. Nucl Med Biol 23:917–922CrossRefPubMedGoogle Scholar
  14. 14.
    Zhang Y (2000) Influence of different chelators (HYNIC, MAG3 and DTPA) on tumor cell accumulation and mouse biodistribution of technetium-99m labeled to antisense DNA. Eur J Nucl Med 27:1700–1707CrossRefPubMedGoogle Scholar
  15. 15.
    Vanderheyden JL (2006) Evaluation of 99mTc-MAG3-annexin V: influence of the chelate on in vitro and in vivo properties in mice. Nucl Med Biol 33:135–144CrossRefPubMedGoogle Scholar
  16. 16.
    Hjelstuen OK (1998) 3′-99mTc labeling and biodistribution of a CAPL antisense oligodeoxynucleotide. Nucl Med Biol 25:651–657CrossRefPubMedGoogle Scholar
  17. 17.
    Verduyckt T (2003) Identity confirmation of 99mTc-MAG3, 99mTc-Sestamibi and 99mTc-ECD using radio-LC-MS. J Pharmaceut Biomed. 32:669–678CrossRefGoogle Scholar
  18. 18.
    Kan W (2016) Coordination investigation of rhenium with MAG3 using LC-MS and UV spectrometer and the simple radiolabelling process. J Radioanal Nucl Chem 310:695–702CrossRefGoogle Scholar

Copyright information

© Akadémiai Kiadó, Budapest, Hungary 2018

Authors and Affiliations

  1. 1.Institute of Nuclear Physics and ChemistryChina Academy of Engineering PhysicsMianyangChina

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