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 language | English |
|---|---|
| Pages (from-to) | 317-326 |
| Number of pages | 10 |
| Journal | Cancer Biotherapy and Radiopharmaceuticals |
| Volume | 17 |
| Issue number | 3 |
| Publication status | Published - 2002 |
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ASJC Scopus subject areas
- Cancer Research
- Pharmacology
- Oncology
Cite this
Synthesis, chemical, radiochemical and radiobiological evaluation of a new 99mTc-labelled bombesin-like peptide. / 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.
In: Cancer Biotherapy and Radiopharmaceuticals, Vol. 17, No. 3, 2002, p. 317-326.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - Synthesis, chemical, radiochemical and radiobiological evaluation of a new 99mTc-labelled bombesin-like peptide
AU - Varvarigou, A. D.
AU - Leonti, A.
AU - Xanthopoulos, S.
AU - Delle Fave, G.
AU - Archimandritis, S. C.
AU - Scopinaro, F.
AU - Leondiadis, L.
AU - Corleto, V.
AU - Schillaci, O.
AU - De Vincentis, G.
AU - Sourlingas, T. G.
AU - Sekeri-Pataryas, K. E.
AU - Evangelatos, G. P.
PY - 2002
Y1 - 2002
N2 - 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.
AB - 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.
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UR - http://www.scopus.com/inward/citedby.url?scp=0036062011&partnerID=8YFLogxK
M3 - Article
VL - 17
SP - 317
EP - 326
JO - Cancer Biotherapy and Radiopharmaceuticals
JF - Cancer Biotherapy and Radiopharmaceuticals
SN - 1084-9785
IS - 3
ER -