Source:http://linkedlifedata.com/resource/pubmed/id/19397852
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
2
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pubmed:dateCreated |
2009-4-28
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pubmed:abstractText |
Cyclic arginine-glycine-aspartate (RGD) peptides and their derivatives have been intensively studied as tumor targeting probes. One major drawback, however, is their short blood circulation half-lives, which greatly compromises their targeting efficacy. To address this issue, a cyclic peptide, c(RGDyK), and an organic dye (IRDye800 or Cy5.5) were covalently conjugated onto human serum albumin (HSA). The conjugates were subjected to in vitro cell staining, in vivo near-infrared fluorescence (NIRF) imaging, ex vivo NIRF imaging, and histologic studies to evaluate their feasibility as tumor imaging probes. As a control, RAD peptide was also coupled with HSA and labeled with IRDye800 for in vivo imaging. The HSA-RGD-IRDye800 exhibited integrin alpha(v)beta(3)-specific binding in cell staining experiment. In vivo NIRF imaging showed higher tumor accumulation and tumor to background contrast of HSA-RGD-IRDye800 over RGD-IRDye800. The integrin specificity of HSA-RGD-IRDye800 is confirmed by both successful inhibition of tumor uptake in the presence of c(RGDyK) and the inability to accumulate in integrin-positive tumors by RAD-HSA-IRDye800. Histologic examination revealed initial tumor vascular binding and eventually both tumor vasculature and tumor cell integrin binding in vivo. In summary, we successfully developed an RGD-based protein conjugate with prolonged circulation half-life for NIRF imaging of tumor integrin alpha(v)beta(3) expression. The success of this study may be generalizable for other peptide-based probes to be conjugated with HSA for prolonged tumor contrast and improved pharmacokinetics.
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pubmed:grant | |
pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/CY5.5 cyanine dye,
http://linkedlifedata.com/resource/pubmed/chemical/Carbocyanines,
http://linkedlifedata.com/resource/pubmed/chemical/IRDye800,
http://linkedlifedata.com/resource/pubmed/chemical/Indoles,
http://linkedlifedata.com/resource/pubmed/chemical/Integrin alphaVbeta3,
http://linkedlifedata.com/resource/pubmed/chemical/Peptides, Cyclic,
http://linkedlifedata.com/resource/pubmed/chemical/Serum Albumin,
http://linkedlifedata.com/resource/pubmed/chemical/cyclic arginine-glycine-aspartic...
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pubmed:status |
MEDLINE
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pubmed:issn |
1535-3508
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
8
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
65-73
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pubmed:dateRevised |
2011-4-7
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pubmed:meshHeading |
pubmed-meshheading:19397852-Animals,
pubmed-meshheading:19397852-Carbocyanines,
pubmed-meshheading:19397852-Cell Line, Tumor,
pubmed-meshheading:19397852-Disease Models, Animal,
pubmed-meshheading:19397852-Half-Life,
pubmed-meshheading:19397852-Histocytochemistry,
pubmed-meshheading:19397852-Humans,
pubmed-meshheading:19397852-Indoles,
pubmed-meshheading:19397852-Integrin alphaVbeta3,
pubmed-meshheading:19397852-Mice,
pubmed-meshheading:19397852-Mice, Nude,
pubmed-meshheading:19397852-Molecular Probe Techniques,
pubmed-meshheading:19397852-Neoplasm Transplantation,
pubmed-meshheading:19397852-Neoplasms, Experimental,
pubmed-meshheading:19397852-Peptides, Cyclic,
pubmed-meshheading:19397852-Protein Binding,
pubmed-meshheading:19397852-Serum Albumin,
pubmed-meshheading:19397852-Spectroscopy, Near-Infrared,
pubmed-meshheading:19397852-Tissue Distribution
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pubmed:articleTitle |
RGD-human serum albumin conjugates as efficient tumor targeting probes.
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pubmed:affiliation |
Molecular Imaging Program at Stanford, Department of Radiology and Bio-X Program, Stanford University School of Medicine, Standford, CA 94305-5484, USA.
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pubmed:publicationType |
Journal Article,
Research Support, N.I.H., Extramural
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