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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
7
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pubmed:dateCreated |
2011-3-14
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pubmed:abstractText |
We synthesized disulfide-based cyclic RGD pentapeptides bearing a near-infrared fluorescent dye (cypate), represented by cypate-c(CRGDC) (1) for integrin-targeted optical imaging. These compounds were compared with the traditional lactam-based cyclic RGD counterpart, cypate-c(RGDfK) (2). Molecular modeling suggests that the binding affinity of 2 to integrin ?(v)?(3) is an order of magnitude higher than that of 1. This was confirmed experimentally, which further showed that substitution of Gly with Pro, Val and Tyr in 1 remarkably hampered the ?(v)?(3) binding. Interestingly, cell microscopy with A549 cells showed that 1 exhibited higher cellular staining than 2. These results indicate that factors other than receptor binding affinity to ?(v)?(3) dimeric proteins mediate cellular uptake. Consequently, 1 and its analogs may serve as valuable molecular probes for investigating the selectivity and specificity of integrin targeting by optical imaging.
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pubmed:grant |
http://linkedlifedata.com/resource/pubmed/grant/R01 CA109754-01,
http://linkedlifedata.com/resource/pubmed/grant/R01 CA109754-02,
http://linkedlifedata.com/resource/pubmed/grant/R01 CA109754-03,
http://linkedlifedata.com/resource/pubmed/grant/R01 CA109754-04,
http://linkedlifedata.com/resource/pubmed/grant/R01 CA109754-05,
http://linkedlifedata.com/resource/pubmed/grant/R01 EB007276,
http://linkedlifedata.com/resource/pubmed/grant/R01 EB007276-02,
http://linkedlifedata.com/resource/pubmed/grant/R01 EB007276-02S1,
http://linkedlifedata.com/resource/pubmed/grant/R01 EB007276-03,
http://linkedlifedata.com/resource/pubmed/grant/R01 EB007276-04,
http://linkedlifedata.com/resource/pubmed/grant/R01 EB008111-01A2,
http://linkedlifedata.com/resource/pubmed/grant/R01 EB008111-02,
http://linkedlifedata.com/resource/pubmed/grant/R01 EB008111-03,
http://linkedlifedata.com/resource/pubmed/grant/R01CA109754,
http://linkedlifedata.com/resource/pubmed/grant/R01EB00811,
http://linkedlifedata.com/resource/pubmed/grant/R13 EB007477-01,
http://linkedlifedata.com/resource/pubmed/grant/R33 CA123537,
http://linkedlifedata.com/resource/pubmed/grant/R33 CA123537-02,
http://linkedlifedata.com/resource/pubmed/grant/R33 CA123537-03,
http://linkedlifedata.com/resource/pubmed/grant/R33 CA123537-04
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Apr
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pubmed:issn |
1464-3405
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pubmed:author |
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pubmed:copyrightInfo |
Copyright © 2011 Elsevier Ltd. All rights reserved.
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pubmed:issnType |
Electronic
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pubmed:day |
1
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pubmed:volume |
21
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
2116-20
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pubmed:meshHeading |
pubmed-meshheading:21349709-Chromatography, High Pressure Liquid,
pubmed-meshheading:21349709-Cyclization,
pubmed-meshheading:21349709-Disulfides,
pubmed-meshheading:21349709-Fluorescent Dyes,
pubmed-meshheading:21349709-Integrins,
pubmed-meshheading:21349709-Oligopeptides,
pubmed-meshheading:21349709-Spectrometry, Mass, Electrospray Ionization,
pubmed-meshheading:21349709-Spectroscopy, Near-Infrared
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pubmed:year |
2011
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pubmed:articleTitle |
Exploring new near-infrared fluorescent disulfide-based cyclic RGD peptide analogs for potential integrin-targeted optical imaging.
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pubmed:affiliation |
Department of Radiology, Washington University School of Medicine, 4525 Scott Avenue, St Louis, MO 63110, USA.
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pubmed:publicationType |
Journal Article,
Research Support, N.I.H., Extramural
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