Abstract |
Recently, a disulfide-based cyclic RGD peptide called iRGD, that is, c(CRGDKGPDC), has been reported to interact with both integrin and neuropilin-1 receptors for cellular and deep tissue penetration to improve the imaging sensitivity and therapeutic efficacy. In this study, two new near-infrared fluorescent iRGD conjugates, that is, Ac-Cys(IRDye®800CW)-iRGD (1), and its dual labeling analog DOTA-Cys(IRDye®800CW)-iRGD (2) were synthesized via the specific mercapto- maleimide reaction for tumor imaging. Both 1 and 2 showed significant tumor localization in optical imaging of MDA-MB-435 tumor-bearing mice. The potential of such iRGD compounds in tumor-targeted imaging and drug delivery deserves further exploration.
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Authors | Yunpeng Ye, Lei Zhu, Ying Ma, Gang Niu, Xiaoyuan Chen |
Journal | Bioorganic & medicinal chemistry letters
(Bioorg Med Chem Lett)
Vol. 21
Issue 4
Pg. 1146-50
(Feb 15 2011)
ISSN: 1464-3405 [Electronic] England |
PMID | 21251820
(Publication Type: Journal Article, Research Support, N.I.H., Intramural)
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Copyright | Published by Elsevier Ltd. |
Chemical References |
- Fluorescent Dyes
- Heterocyclic Compounds, 1-Ring
- Integrin alphaVbeta3
- Oligopeptides
- Peptides, Cyclic
- 1,4,7,10-tetraazacyclododecane- 1,4,7,10-tetraacetic acid
- arginyl-glycyl-aspartic acid
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Topics |
- Amino Acid Sequence
- Animals
- Fluorescent Dyes
(chemistry)
- Heterocyclic Compounds, 1-Ring
(chemistry)
- Integrin alphaVbeta3
(chemistry, metabolism)
- Mice
- Mice, Nude
- Neoplasms
(diagnosis)
- Oligopeptides
(chemistry)
- Peptides, Cyclic
(chemical synthesis, chemistry)
- Positron-Emission Tomography
- Transplantation, Heterologous
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