14973080

Source:http://linkedlifedata.com/resource/pubmed/id/14973080

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Predicate	Object
rdf:type	pubmed:Citation
lifeskim:mentions	umls-concept:C0021467, umls-concept:C0021469, umls-concept:C0070716, umls-concept:C0182400, umls-concept:C0205369, umls-concept:C0542341, umls-concept:C1332002
pubmed:issue	4
pubmed:dateCreated	2004-2-19
pubmed:abstractText	Pheophorbide a (PhA), a chlorophyll catabolite, was shown to be an ABCG2 substrate based on Abcg2(-/-) knockout mouse studies (J. W. Jonker et al., Proc. Natl. Acad. Sci. USA, 99: 15649-15654, 2002). We developed a functional assay for ABCG2 using PhA and the ABCG2 inhibitor fumitremorgin C. In selected cell lines expressing high levels of P-glycoprotein, multidrug resistance-associated protein 1, or ABCG2, PhA transport was observed only in cells expressing ABCG2. Fumitremorgin C-inhibitable PhA transport was found to correlate with cell surface ABCG2 expression as measured by the anti-ABCG2 antibody 5D3. We found that 100 micro M of the cyclin-dependent kinase inhibitor UCN-01 or 1 micro M of the P-glycoprotein inhibitor tariquidar inhibited ABCG2-mediated PhA transport. In 4-day cytotoxicity assays, ABCG2-mediated resistance to SN-38 and topotecan was abrogated in ABCG2-transfected HEK-293 cells treated with 1 micro M tariquidar, and ABCG2-transfected cells were 6-7-fold resistant to UCN-01. PhA is an ABCG2-specific substrate with potential value in measuring ABCG2 function and expression in clinical samples.
pubmed:language	eng
pubmed:journal	http://linkedlifedata.com/resource/pubmed/journal/2984705R
pubmed:citationSubset	IM
pubmed:chemical	http://linkedlifedata.com/resource/pubmed/chemical/7-hydroxystaurosporine, http://linkedlifedata.com/resource/pubmed/chemical/ABCG2 protein, human, http://linkedlifedata.com/resource/pubmed/chemical/ATP-Binding Cassette Transporters, http://linkedlifedata.com/resource/pubmed/chemical/Camptothecin, http://linkedlifedata.com/resource/pubmed/chemical/Chlorophyll, http://linkedlifedata.com/resource/pubmed/chemical/Neoplasm Proteins, http://linkedlifedata.com/resource/pubmed/chemical/Quinolines, http://linkedlifedata.com/resource/pubmed/chemical/Staurosporine, http://linkedlifedata.com/resource/pubmed/chemical/Topotecan, http://linkedlifedata.com/resource/pubmed/chemical/irinotecan, http://linkedlifedata.com/resource/pubmed/chemical/pheophorbide a, http://linkedlifedata.com/resource/pubmed/chemical/tariquidar
pubmed:status	MEDLINE
pubmed:month	Feb
pubmed:issn	0008-5472
pubmed:author	pubmed-author:BatesSusan ESE, pubmed-author:BlayneyMargaretM, pubmed-author:MistryPrakashP, pubmed-author:MorisakiKuniakiK, pubmed-author:PolgarOrsolyaO, pubmed-author:RobeyRobert WRW, pubmed-author:SteadmanKennethK
pubmed:issnType	Print
pubmed:day	15
pubmed:volume	64
pubmed:owner	NLM
pubmed:authorsComplete	Y
pubmed:pagination	1242-6
pubmed:dateRevised	2007-9-25
pubmed:meshHeading	pubmed-meshheading:14973080-ATP-Binding Cassette Transporters, pubmed-meshheading:14973080-Breast Neoplasms, pubmed-meshheading:14973080-Camptothecin, pubmed-meshheading:14973080-Chlorophyll, pubmed-meshheading:14973080-Drug Resistance, Neoplasm, pubmed-meshheading:14973080-Humans, pubmed-meshheading:14973080-Neoplasm Proteins, pubmed-meshheading:14973080-Quinolines, pubmed-meshheading:14973080-Staurosporine, pubmed-meshheading:14973080-Topotecan
pubmed:year	2004
pubmed:articleTitle	Pheophorbide a is a specific probe for ABCG2 function and inhibition.
pubmed:affiliation	Cancer Therapeutics Branch, Center for Cancer Research, National Cancer Institute, National Institutes of Health, Building 10, Rm. 12C203, 9000 Rockville Pike, Bethesda, MD 20892, USA. robeyr@mail.nih.gov
pubmed:publicationType	Journal Article, Research Support, U.S. Gov't, P.H.S.