Source:http://linkedlifedata.com/resource/pubmed/id/15653145
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
1
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pubmed:dateCreated |
2005-1-17
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pubmed:abstractText |
Sites of neovascular angiogenesis are important chemotherapy targets. In this study, the synthesis, characterization, in-vivo imaging and biodistribution of a technetium-99m labeled, water-soluble, N-(2-hydroxypropyl) methacrylamide (HPMA) copolymer carrying doubly cyclized Arg-Gly-Asp motifs (HPMA copolymer-RGD4C conjugate) are reported. In vitro endothelial cell adhesion assays indicated that HPMA copolymer-RGD4C conjugates inhibited alphaVbeta3-mediated endothelial cell adhesion while HPMA copolymer Arg-Gly-Glu control conjugates (HPMA copolymer-RGE4C conjugate) and hydrolyzed HPMA copolymer precursor (HPMA copolymer) showed no activity. The scintigraphic images of prostate tumor bearing SCID mice obtained 24 h post-i.v. injection indicated greater tumor localization of HPMA copolymer-RGD4C conjugate than the control, HPMA copolymer-RGE4C conjugate. The 24-h necropsy radioactivity data showed that HPMA copolymer-RGD4C conjugate had significantly higher (p<0.001) tumor localization compared to HPMA copolymer-RGE4C conjugate and HPMA copolymer. Also, HPMA copolymer-RGD4C conjugates had sustained tumor retention over 72 h and reasonably efficient clearance from the background organs. These results suggest that specific tumor angiogenesis targeting is possible with HPMA copolymer-RGD4C conjugates. This construct provides a foundation that should support targeted delivery of radionuclides and drugs to solid tumors for diagnostic and therapeutic applications.
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pubmed:grant | |
pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Jan
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pubmed:issn |
0168-3659
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:day |
20
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pubmed:volume |
102
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
191-201
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pubmed:dateRevised |
2007-11-14
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pubmed:meshHeading |
pubmed-meshheading:15653145-Animals,
pubmed-meshheading:15653145-Cell Line, Tumor,
pubmed-meshheading:15653145-Cells, Cultured,
pubmed-meshheading:15653145-Dose-Response Relationship, Drug,
pubmed-meshheading:15653145-Drug Delivery Systems,
pubmed-meshheading:15653145-Humans,
pubmed-meshheading:15653145-Male,
pubmed-meshheading:15653145-Mice,
pubmed-meshheading:15653145-Mice, SCID,
pubmed-meshheading:15653145-Neovascularization, Pathologic,
pubmed-meshheading:15653145-Oligopeptides,
pubmed-meshheading:15653145-Polymers,
pubmed-meshheading:15653145-Prostatic Neoplasms,
pubmed-meshheading:15653145-Xenograft Model Antitumor Assays
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pubmed:year |
2005
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pubmed:articleTitle |
Targeting tumor angiogenic vasculature using polymer-RGD conjugates.
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pubmed:affiliation |
Department of Pharmaceutical Sciences, University of Maryland, Baltimore, MD 21201, USA.
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pubmed:publicationType |
Journal Article,
Comparative Study,
Research Support, U.S. Gov't, P.H.S.
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