Exploring the Potential of 99mTc(CO)3-Labeled Triazolyl Peptides for Tumor Diagnosis

Raghuvir H. Gaonkar, Soumya Ganguly, Rinku Baishya, Saikat Dewanjee, Samarendu Sinha, Amit Gupta, Shantanu Ganguly, Mita C. Debnath

Research output: Contribution to journalArticlepeer-review

6 Scopus citations

Abstract

In recent years the authors have reported on 99mTc(CO)3-labeled peptides that serve as carriers for biomolecules or radiopharmaceuticals to the tumors. In continuation of that work they report the synthesis of a pentapeptide (Met-Phe-Phe-Gly-His; pep-1), a hexapeptide (Met-Phe-Phe-Asp-Gly-His; pep-2), and a tetrapeptide (Asp-Gly-Arg-His; pep-3) and the attachment of 3-amino-1,2,4-triazole to the β carboxylic function of the aspartic acid unit of pep-2 and pep-3. The pharmacophores were radiolabeled in high yields with [99mTc(CO)3(H2O)3]+ metal aqua ion, characterized for their stability in serum and saline, as well as in His solution, and found to be substantially stable. B16F10 cell line binding studies showed favorable uptake and internalization. In vivo behavior of the radiolabeled triazolyl peptides was assessed in mice bearing induced tumor. The 99mTc(CO)3-triazolyl pep-3 demonstrated rapid urinary clearance and comparatively better tumor uptake. Imaging studies showed visualization of the tumor using 99mTc(CO)3-triazolyl pep-3, but due to high abdominal background, low delineation occurred. Based on the results further experiments will be carried out for targeting tumor with triazolyl peptides.

Original languageEnglish
Pages (from-to)110-117
Number of pages8
JournalCancer Biotherapy and Radiopharmaceuticals
Volume31
Issue number3
DOIs
StatePublished - 1 Apr 2016
Externally publishedYes

Keywords

  • fac-[Tc(CO)(HO)]+ core
  • internalization
  • triazolyl peptide synthesis
  • tumor imaging

ASJC Scopus subject areas

  • Oncology
  • Radiology Nuclear Medicine and imaging
  • Pharmacology
  • Cancer Research

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