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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
1
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pubmed:dateCreated |
2006-10-30
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pubmed:abstractText |
Trabectedin (ET-743, Yondelis) is a novel anticancer drug currently undergoing phase II and III investigations. There are various and conflicting reports whether trabectedin is a substrate for P-glycoprotein (P-gp), an important factor in drug disposition and multi-drug resistance (MDR). We have now unambiguously shown that trabectedin is a P-gp substrate by investigating vectorial transport over monolayers of LLC-PK1 pig kidney and Madine-Darby Canine kidney (MDCK) cells and the mdr1a and/or MDR1 transfected subclones. We further characterized the cytotoxic effects and cellular accumulation of trabectedin in these cell lines as well as in a panel of other cell lines with high or moderate expression levels of P-gp. Trabectedin displayed the typical MDR phenotype only in highly P-gp expressing cell lines, but not in cell lines with expression levels more closely conforming to clinical samples, suggesting that P-gp will not confer resistance to trabectedin in cancer patients.
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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 |
http://linkedlifedata.com/resource/pubmed/chemical/Antineoplastic Agents, Alkylating,
http://linkedlifedata.com/resource/pubmed/chemical/Carbon Radioisotopes,
http://linkedlifedata.com/resource/pubmed/chemical/Dibenzocycloheptenes,
http://linkedlifedata.com/resource/pubmed/chemical/Dioxoles,
http://linkedlifedata.com/resource/pubmed/chemical/Membrane Transport Proteins,
http://linkedlifedata.com/resource/pubmed/chemical/P-Glycoprotein,
http://linkedlifedata.com/resource/pubmed/chemical/Paclitaxel,
http://linkedlifedata.com/resource/pubmed/chemical/Quinolines,
http://linkedlifedata.com/resource/pubmed/chemical/Tetrahydroisoquinolines,
http://linkedlifedata.com/resource/pubmed/chemical/trabectedin,
http://linkedlifedata.com/resource/pubmed/chemical/zosuquidar trihydrochloride
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pubmed:status |
MEDLINE
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pubmed:month |
Feb
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pubmed:issn |
0167-6997
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:volume |
25
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1-7
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pubmed:dateRevised |
2008-11-29
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pubmed:meshHeading |
pubmed-meshheading:16633714-Animals,
pubmed-meshheading:16633714-Antineoplastic Agents, Alkylating,
pubmed-meshheading:16633714-Biological Transport,
pubmed-meshheading:16633714-Carbon Radioisotopes,
pubmed-meshheading:16633714-Cell Line,
pubmed-meshheading:16633714-Cell Membrane Permeability,
pubmed-meshheading:16633714-Cell Survival,
pubmed-meshheading:16633714-Dibenzocycloheptenes,
pubmed-meshheading:16633714-Dioxoles,
pubmed-meshheading:16633714-Drug Resistance, Multiple,
pubmed-meshheading:16633714-Drug Resistance, Neoplasm,
pubmed-meshheading:16633714-Humans,
pubmed-meshheading:16633714-Inhibitory Concentration 50,
pubmed-meshheading:16633714-Intracellular Fluid,
pubmed-meshheading:16633714-LLC-PK1 Cells,
pubmed-meshheading:16633714-Membrane Transport Proteins,
pubmed-meshheading:16633714-Mice,
pubmed-meshheading:16633714-P-Glycoprotein,
pubmed-meshheading:16633714-Paclitaxel,
pubmed-meshheading:16633714-Quinolines,
pubmed-meshheading:16633714-Swine,
pubmed-meshheading:16633714-Tetrahydroisoquinolines,
pubmed-meshheading:16633714-Transfection
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pubmed:year |
2007
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pubmed:articleTitle |
Trabectedin (ET-743, Yondelis) is a substrate for P-glycoprotein, but only high expression of P-glycoprotein confers the multidrug resistance phenotype.
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pubmed:affiliation |
Department of Pharmacy and Pharmacology, The Netherlands Cancer Institute/Slotervaart Hospital, Amsterdam, The Netherlands.
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pubmed:publicationType |
Journal Article
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