Article ID Journal Published Year Pages File Type
2154813 Nuclear Medicine and Biology 2006 10 Pages PDF
Abstract

We have described the synthesis of tridentate pyrazolyl ligand frameworks for coordination to the fac-[*M(CO)3]+ metal fragment (*M=186/188Re or 99mTc). These ligands impart a degree of kinetic inertness on the metal center, warranting their study in biological systems. We herein report in vitro/in vivo radiolabeling investigations of a new series of pyrazolyl bombesin (BBN) conjugates radiolabeled via the Isolink kit. These new conjugates are based on the general structure [99mTc-pyrazolyl-X-BBN[7–14]NH2], where X=β-alanine, serylserylserine or glycylglycylglycine. The pyrazolyl ligand is a tridentate ligand framework that coordinates the metal center through nitrogen donor atoms. The results of these investigations demonstrate the ability of these new conjugates to specifically target the gastrin-releasing peptide receptor subtype 2, which is overexpressed on human prostate PC-3 cancerous tissues. Therefore, these studies suggest the tridentate pyrazolyl ligand framework to be an ideal candidate for the design and development of low-valent 99mTc-based diagnostic radiopharmaceuticals based on BBN or other targeting vectors.

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