Synthesis, chemical, radiochemical and radiobiological evaluation of a new 99mTc-labelled bombesin-like peptide

A. D. Varvarigou, A. Leonti, S. Xanthopoulos, G. Delle Fave, S. C. Archimandritis, F. Scopinaro, L. Leondiadis, V. Corleto, O. Schillaci, G. De Vincentis, T. G. Sourlingas, K. E. Sekeri-Pataryas, G. P. Evangelatos

Research output: Contribution to journalArticle

Abstract

A new pentadecapeptide bombesin analogue was prepared by Fmoc synthesis, purified by HPLC and identified by electron ionization mass spectrometry. The biological activity of the new peptide was tested on isolated human colonic muscle cells and compared to native bombesin. Labelling of the new biomolecule with Tc-99m yielded a single radioactive species which remained stable at room temperature for eight hours. In a binding assay, the radiolabelled peptide showed high affinity for oat-cell carcinoma (Kd = 9.8 nM) and colorectal adenocarcinoma (Kd = 27.2 nM). Biodistribution studies, performed in normal rodents, indicated uptake by organs that normally express bombesin receptors, such as liver, intestines and kidneys. Scintigraphic studies, performed in nude mice transplanted with small cell lung carcinoma and colon cancer cells, showed significant tumor uptake two hours p.i. The new synthetic pentadecapeptide appears to have promise for several malignancies, including oat-cell lung carcinoma, colorectal cancer and gastroenteropancreatic (GEP) tumors.

Original languageEnglish
Pages (from-to)317-326
Number of pages10
JournalCancer Biotherapy and Radiopharmaceuticals
Volume17
Issue number3
Publication statusPublished - 2002

ASJC Scopus subject areas

  • Cancer Research
  • Pharmacology
  • Oncology

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    Varvarigou, A. D., Leonti, A., Xanthopoulos, S., Delle Fave, G., Archimandritis, S. C., Scopinaro, F., Leondiadis, L., Corleto, V., Schillaci, O., De Vincentis, G., Sourlingas, T. G., Sekeri-Pataryas, K. E., & Evangelatos, G. P. (2002). Synthesis, chemical, radiochemical and radiobiological evaluation of a new 99mTc-labelled bombesin-like peptide. Cancer Biotherapy and Radiopharmaceuticals, 17(3), 317-326.