C - Chemistry – Metallurgy – 07 – K
Patent
C - Chemistry, Metallurgy
07
K
C07K 1/13 (2006.01) A61K 51/08 (2006.01) C07K 7/06 (2006.01) C07K 7/08 (2006.01) A61K 38/00 (2006.01)
Patent
CA 2225326
In an effort to develop better methods for preparing 99m Tc-labelled peptides for radioimaging and radiodiagnostic applications, we have developed a simple solid phase synthetic approach that allows the mercaptoacetyltriglycine (MAG3) technetium chelate to be attached directly onto the growing peptide chain using conventional solid phase peptide chemistry. This novel approach permits the facile, high yield preparation of precisely labelled and very pure (>95%) peptide-chelator conjugates. We believe this method has a number of significant advantages over other widely used protocols. In particular, it reduces the number of purification steps, eliminates the need for solution-phase conjugation and avoids the problems of non-specific chelator conjugation. Tests involving two different MAG3-bombesin conjugates, prepared using this technique, show that the peptide-conjugates can be efficiently labelled with 99mTc (92%), are highly resistant to cysteine challenge, are very stable in plasma and can bind to the desired cellular targets. This suggests that the protocols described here should be generally applicable in the preparation of other 99mTc labelled peptides.
Okarvi Subhani M.
Suresh Mavanur R.
Van Domeselaar Gary
Wishart David
Biotools Inc.
Field Atkinson Perraton
Immunocreations Inc.
Okarvi Subhani M.
Suresh Mavanur R.
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