The solid phase synthesis and NMR spectroscopy of a 99Tc chelate–bombesin derived peptide conjugate

A bombesin derived peptide– 99Tc chelate conjugate was prepared using a solid phase synthetic methodology. The reported approach involved linking a prefabricated bifunctional N 2N′S technetium chelate complex to a resin bound peptide sequence derived from bombesin, which has been shown to bind to th...

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Bibliographic Details
Published in:Inorganica Chimica Acta 2001-12, Vol.325 (1), p.155-163
Main Authors: Valliant, John F, Riddoch, R.William, Hughes, Donald W, Roe, David G, Fauconnier, Theresa K, Thornback, John R
Format: Article
Language:English
Subjects:
NMR
Peptides
Radiopharmaceuticals
Solid-phase synthesis
Technetium
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Summary:A bombesin derived peptide– 99Tc chelate conjugate was prepared using a solid phase synthetic methodology. The reported approach involved linking a prefabricated bifunctional N 2N′S technetium chelate complex to a resin bound peptide sequence derived from bombesin, which has been shown to bind to the gastrin-releasing peptide (GRP) receptor. The technetium chelate–peptide conjugate was subsequently isolated from the solid support and characterized by electrospray mass spectrometry, HPLC and NMR spectroscopy. The goal of the approach was to develop a versatile solid phase synthetic procedure that would facilitate the future application of modern drug discovery techniques for the development of receptor selective technetium radiopharmaceuticals. Furthermore, the NMR studies of the reported radiometal–peptide conjugate provide an important reference for the characterization of future bombesin-based radiopharmaceuticals. A bombesin derived peptide– 99Tc chelate conjugate was prepared using a solid phase synthetic methodology. The reported approach involved linking a prefabricated bifunctional N 2N′S technetium chelate complex to a resin bound peptide sequence derived from bombesin. The technetium chelate–peptide conjugate was subsequently isolated from the solid support and characterized by ESMS, HPLC and NMR spectroscopy. The goal of the approach was to develop a versatile solid phase synthetic procedure that would facilitate the future application of modern drug discovery techniques for the development of receptor selective technetium radiopharmaceuticals.
ISSN:0020-1693
1873-3255
DOI:10.1016/S0020-1693(01)00637-5