Five peptides binding to somatostatin and bombesin receptors were conjugated to 4-azido-2,3,5,6-tetrafluorophenylbenzoic acid, a Type 1 photosensitizer, at the N-terminal position. The receptor affinities were determined by competition binding assay using two different pancreatic tumor cell lines, CA20948 and AR42-J, that express somatostatin-2 (SST-2) and bombesin receptors respectively All compounds exhibited high receptor specificity, i.e., the IC50 values ranged between 1.0 to 64.0 nM. These conjugates may be useful for targeted Type 1 phototherapy via the generation of nitrenes at the cell surfaces expressing these receptors.
|Number of pages||4|
|Journal||Proceedings of SPIE - The International Society for Optical Engineering|
|State||Published - Jan 1 2001|
|Event||Biomarkers and Biological Spectral Imaging - San Jose, CA, United States|
Duration: Jan 23 2001 → …