Targeted Type 1 phototherapeutic agents using azido-peptide bioconjugates

R. Rajagopalan, S. A. Achilefu, H. N. Jimenez, E. G. Webb, M. A. Schmidt, J. E. Bugaj, R. B. Dorshow

Research output: Contribution to journalConference article

1 Scopus citations

Abstract

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.

Original languageEnglish
Pages (from-to)129-132
Number of pages4
JournalProceedings of SPIE - The International Society for Optical Engineering
Volume4259
DOIs
StatePublished - Jan 1 2001
Externally publishedYes
EventBiomarkers and Biological Spectral Imaging - San Jose, CA, United States
Duration: Jan 23 2001 → …

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