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Proceedings Paper

Targeted Type 1 phototherapeutic agents using azido-peptide bioconjugates
Author(s): Raghavan Rajagopalan; Samuel I. Achilefu; Hermo N. Jimenez; Elizabeth G. Webb; Michelle A. Schmidt; Joseph E. Bugaj; Richard B. Dorshow
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Paper 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.

Paper Details

Date Published: 2 July 2001
PDF: 4 pages
Proc. SPIE 4259, Biomarkers and Biological Spectral Imaging, (2 July 2001); doi: 10.1117/12.432494
Show Author Affiliations
Raghavan Rajagopalan, Mallinckrodt, Inc. (United States)
Samuel I. Achilefu, Mallinckrodt, Inc. (United States)
Hermo N. Jimenez, Mallinckrodt, Inc. (United States)
Elizabeth G. Webb, Mallinckrodt, Inc. (United States)
Michelle A. Schmidt, Mallinckrodt, Inc. (United States)
Joseph E. Bugaj, Mallinckrodt, Inc. (United States)
Richard B. Dorshow, Mallinckrodt, Inc. (United States)

Published in SPIE Proceedings Vol. 4259:
Biomarkers and Biological Spectral Imaging
Gregory H. Bearman; Darryl J. Bornhop; Darryl J. Bornhop; Richard M. Levenson, Editor(s)

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