Synthesis and evaluation of a radioiodinated bladder cancer specific peptide

Yeong Su Ha, Hwa Young Lee, Gwang Il An, Jonghee Kim, Wonjung Kwak, Eun Ju Lee, Seung Min Lee, Byung Heon Lee, In San Kim, Takele Belay, Woonghee Lee, Byeong Cheol Ahn, Jaetae Lee, Jeongsoo Yoo

Research output: Contribution to journalArticle

5 Citations (Scopus)

Abstract

Bladder cancer is the second most common cancer of the urinary tract, however the invasive cystoscopy is still the standard technique for diagnosis and surveillance of bladder cancer. Herein, we radiolabel bladder cancer specific peptide with radioactive iodine ( 131/124I) and evaluate its potential as a new radiopharmaceutical for the non-invasive diagnosis of bladder cancer. A 9-mer bladder cancer specific peptide (BP) was conjugated with tyrosine and cyclized by disulfide bond formation to give Y-BP, which was further radioiodinated to give [ 131/124I]Y-BP in good radiochemical yield. The biodistribution data showed the high selectivity of [ 124I]Y-BP in HT1376 human bladder cancer xenograft models with a tumor-to-muscle ratio of 6.2. This tumor targeting was not observed in control B16F10 melanoma tumor models. In microPET studies, while the control scrambled peptide, [ 124I]Y-sBP, did not accumulate in either the bladder cancer or melanoma, [ 124I]Y-BP showed high tumor uptake only in animals with HT1376 bladder cancer cells. Furthermore, [ 124I]Y-BP showed superior bladder cancer uptake even compared to most commonly used cancer imaging tracer, [ 18F]FDG. The experimental results suggest the potential of [ 124I]Y-BP as a new radiopharmaceutical for the non-invasive diagnosis of bladder cancer with high binding affinity and selectivity.

Original languageEnglish
Pages (from-to)4330-4335
Number of pages6
JournalBioorganic and Medicinal Chemistry
Volume20
Issue number14
DOIs
Publication statusPublished - 2012 Jul 15

Keywords

  • Bladder cancer
  • Disease-specific peptide
  • PET
  • Radioiodination
  • Radiopharmaceuticals

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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  • Cite this

    Ha, Y. S., Lee, H. Y., An, G. I., Kim, J., Kwak, W., Lee, E. J., Lee, S. M., Lee, B. H., Kim, I. S., Belay, T., Lee, W., Ahn, B. C., Lee, J., & Yoo, J. (2012). Synthesis and evaluation of a radioiodinated bladder cancer specific peptide. Bioorganic and Medicinal Chemistry, 20(14), 4330-4335. https://doi.org/10.1016/j.bmc.2012.05.049