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

doi:10.1117/12.432494

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 journal › Conference article › peer-review

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 language	English
Pages (from-to)	129-132
Number of pages	4
Journal	Proceedings of SPIE - The International Society for Optical Engineering
Volume	4259
DOIs	https://doi.org/10.1117/12.432494
State	Published - 2001
Event	Biomarkers and Biological Spectral Imaging - San Jose, CA, United States Duration: Jan 23 2001 → …

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title = "Targeted Type 1 phototherapeutic agents using azido-peptide bioconjugates",

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.",

author = "R. Rajagopalan and Achilefu, {S. A.} and Jimenez, {H. N.} and Webb, {E. G.} and Schmidt, {M. A.} and Bugaj, {J. E.} and Dorshow, {R. B.}",

year = "2001",

doi = "10.1117/12.432494",

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T1 - Targeted Type 1 phototherapeutic agents using azido-peptide bioconjugates

AU - Rajagopalan, R.

AU - Achilefu, S. A.

AU - Jimenez, H. N.

AU - Webb, E. G.

AU - Schmidt, M. A.

AU - Bugaj, J. E.

AU - Dorshow, R. B.

PY - 2001

Y1 - 2001

N2 - 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.

AB - 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.

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DO - 10.1117/12.432494

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AN - SCOPUS:0034860140

SN - 0277-786X

VL - 4259

SP - 129

EP - 132

JO - Proceedings of SPIE - The International Society for Optical Engineering

JF - Proceedings of SPIE - The International Society for Optical Engineering

T2 - Biomarkers and Biological Spectral Imaging

Y2 - 23 January 2001

ER -

Targeted Type 1 phototherapeutic agents using azido-peptide bioconjugates

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