Targeted Type 1 phototherapeutic agents using azido-peptide bioconjugates

Raghavan Rajagopalan; Samuel I. Achilefu; Hermo N. Jimenez; Elizabeth G. Webb; Michelle A. Schmidt; Joseph E. Bugaj; Richard B. Dorshow

doi:10.1117/12.432494

2 July 2001 Targeted Type 1 phototherapeutic agents using azido-peptide bioconjugates

Raghavan Rajagopalan, Samuel I. Achilefu, Hermo N. Jimenez, Elizabeth G. Webb, Michelle A. Schmidt, Joseph E. Bugaj, Richard B. Dorshow

Author Affiliations +

Proceedings Volume 4259, Biomarkers and Biological Spectral Imaging; (2001) https://doi.org/10.1117/12.432494
Event: BiOS 2001 The International Symposium on Biomedical Optics, 2001, San Jose, CA, United States

Abstract

Five peptides binding to somatostatin and bombesin receptors were conjugated to 4-azido-2,3,4,6-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 expresses somatostatin-2 (SST-2) and bombesin receptors receptively. 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.

Citation Download Citation

Raghavan Rajagopalan, Samuel I. Achilefu, Hermo N. Jimenez, Elizabeth G. Webb, Michelle A. Schmidt, Joseph E. Bugaj, and Richard B. Dorshow "Targeted Type 1 phototherapeutic agents using azido-peptide bioconjugates", Proc. SPIE 4259, Biomarkers and Biological Spectral Imaging, (2 July 2001); https://doi.org/10.1117/12.432494

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