The DOI matches its Crossref record; 1 of the 1 references it cites were found in a registry or an index.
Pheophorbide a Is a Specific Probe for ABCG2 Function and Inhibition
Open accessAbstract
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 μm of the cyclin-dependent kinase inhibitor UCN-01 or 1 μm 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 μm 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.
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Citations
Cites
Multidrug resistance in cancer: role of ATP–dependent transporters
Gottesman, M. M., Fojo, T., & Bates, S. E. (2002) · Nature Reviews Cancer · doi:10.1038/nrc706 · Cited by 5,536
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Cited by
Targeting multidrug resistance in cancer
Szakács, G., Paterson, J. K., Ludwig, J. A., Booth-Genthe, C., & Gottesman, M. M. (2006) · Nature Reviews Drug Discovery · doi:10.1038/nrd1984 · Cited by 3,609
Revisiting the role of ABC transporters in multidrug-resistant cancer
Robey, R. W., Pluchino, K. M., Hall, M. D., Fojo, A. T., Bates, S. E., & Gottesman, M. M. (2018) · Nature Reviews Cancer · doi:10.1038/s41568-018-0005-8 · Cited by 1,866
Self-citationRole of breast cancer resistance protein (BCRP/ABCG2) in cancer drug resistance
Natarajan, K., Xie, Y., Baer, M. R., & Ross, D. D. (2012) · Biochemical Pharmacology · doi:10.1016/j.bcp.2012.01.002 · Cited by 405
Role of the breast cancer resistance protein (ABCG2) in drug transport
Mao, Q. (2005) · The AAPS Journal · doi:10.1208/aapsj070112 · Cited by 405
Modulation of P-glycoprotein efflux pump: induction and activation as a therapeutic strategy
Silva, R., Vilas-Boas, V., Carmo, H., Dinis-Oliveira, R. J., Carvalho, F., de Lourdes Bastos, M., & Remião, F. (2015) · Pharmacology & Therapeutics · doi:10.1016/j.pharmthera.2014.11.013 · Cited by 339
Metadata
- Authors
- Robey, R. W., Steadman, K., Polgar, O., Morisaki, K., Blayney, M., Mistry, P., & Bates, S. E.
- Venue
- Cancer Research
- Published
- 2004-02-15
- Volume
- 64
- Issue
- 4
- Pages
- 1242-1246
- ISSN
- 0008-5472 (ISSN-L)
- 1538-7445
- OpenAlex
- W2148146955
- Cited by
- 350
- References
- 1
- FWCI
- 8.23
- Type
- journal article
- Language
- en
- Open access
- bronze
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- Robey, R. W., Steadman, K., Polgar, O., Morisaki, K., Blayney, M., Mistry, P., & Bates, S. E. (2004). Pheophorbide a Is a Specific Probe for ABCG2 Function and Inhibition. Cancer Research. https://doi.org/10.1158/0008-5472.can-03-3298
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