The solid phase synthesis and NMR spectroscopy of a Tc-99 chelate-bombesinderived peptide conjugate

A bombesin derived peptide-(TC)-T-99 chelate conjugate was prepared using a solid phase synthetic methodology. The reported approach involved linking a prefabricated bifunctional N2N'S technetium chelate complex to a resin bo und peptide sequence derived from bombesin, which has been shown to bind to the gastrin-releasing peptide (GRP) receptor. The technetium chelate-pepti de conjugate was subsequently isolated from the solid support and character ized 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 tech niques for the development of receptor selective technetium radiopharmaceut icals, Furthermore, the NMR studies of the reported radiometal-peptide conj ugate provide an important reference for the characterization of future bom besin-based radiopharmaceuticals. (C) 2001 Elsevier Science B.V. All rights reserved.