Source:http://linkedlifedata.com/resource/pubmed/id/20608940
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
10
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pubmed:dateCreated |
2010-9-23
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pubmed:abstractText |
Tumor cell targeting of drug carriers is a promising strategy and uses the attachment of various ligands to enhance the therapeutic potential of chemotherapy agents. Folic acid is a high-affinity ligand for folate receptor, which is a functional tumor-specific receptor. The transforming growth factor (TGF)-? type I receptor (T?R-I) inhibitor A-83-01 was expected to enhance the accumulation of nanocarriers in tumors by changing the microvascular environment. To enhance the therapeutic effect of folate-linked liposomal doxorubicin (F-SL), we co-administrated F-SL with A-83-01. Intraperitoneally injected A-83-01-induced alterations in the cancer-associated neovasculature were examined by magnetic resonance imaging (MRI) and histological analysis. The targeting efficacy of single intravenous injections of F-SL combined with A-83-01 was evaluated by measurement of the biodistribution and the antitumor effect in mice bearing murine lung carcinoma M109. A-83-01 temporarily changed the tumor vasculature around 3 h post injection. A-83-01 induced 1.7-fold higher drug accumulation of F-SL in the tumor than liposome alone at 24 h post injection. Moreover F-SL co-administrated with A-83-01 showed significantly greater antitumor activity than F-SL alone. This study shows that co-administration of T?R-I inhibitor will open a new strategy for the use of FR-targeting nanocarriers for cancer treatment.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/A-83-01,
http://linkedlifedata.com/resource/pubmed/chemical/Doxorubicin,
http://linkedlifedata.com/resource/pubmed/chemical/Folic Acid,
http://linkedlifedata.com/resource/pubmed/chemical/Protein-Serine-Threonine Kinases,
http://linkedlifedata.com/resource/pubmed/chemical/Pyrazoles,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Transforming Growth...,
http://linkedlifedata.com/resource/pubmed/chemical/TGF-beta type I receptor,
http://linkedlifedata.com/resource/pubmed/chemical/Thiocarbamates
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pubmed:status |
MEDLINE
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pubmed:month |
Oct
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pubmed:issn |
1349-7006
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pubmed:author | |
pubmed:copyrightInfo |
© 2010 Japanese Cancer Association.
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pubmed:issnType |
Electronic
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pubmed:volume |
101
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
2207-13
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pubmed:meshHeading |
pubmed-meshheading:20608940-Animals,
pubmed-meshheading:20608940-Doxorubicin,
pubmed-meshheading:20608940-Drug Synergism,
pubmed-meshheading:20608940-Female,
pubmed-meshheading:20608940-Folic Acid,
pubmed-meshheading:20608940-Magnetic Resonance Imaging,
pubmed-meshheading:20608940-Mice,
pubmed-meshheading:20608940-Mice, Inbred BALB C,
pubmed-meshheading:20608940-Neoplasms, Experimental,
pubmed-meshheading:20608940-Protein-Serine-Threonine Kinases,
pubmed-meshheading:20608940-Pyrazoles,
pubmed-meshheading:20608940-Receptors, Transforming Growth Factor beta,
pubmed-meshheading:20608940-Thiocarbamates,
pubmed-meshheading:20608940-Tissue Distribution
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pubmed:year |
2010
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pubmed:articleTitle |
Enhanced antitumor efficacy of folate-linked liposomal doxorubicin with TGF-? type I receptor inhibitor.
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pubmed:affiliation |
Institute of Medicinal Chemistry, Hoshi University, Tokyo, Japan.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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