© 2000 by Oxford University Press
Journal of the National Cancer Institute, Vol. 92, No. 20, 1651-1656,
October 18, 2000
© 2000 Oxford University Press
Role of Breast Cancer Resistance Protein in the Bioavailability and Fetal Penetration of Topotecan
Affiliations of authors: J. W. Jonker, J. W. Smit, R. F. Brinkhuis, M. Maliepaard, A. H. Schinkel (Division of Experimental Therapy), J. H. M. Schellens (Divisions of Experimental Therapy and Medical Oncology), The Netherlands Cancer Institute, Amsterdam; J. H. Beijnen, Department of Pharmacy and Pharmacology, Slotervaart Hospital, Amsterdam, The Netherlands.
Correspondence to: Alfred H. Schinkel, Ph.D., Division of Experimental Therapy, The Netherlands Cancer Institute, Plesmanlaan 121, 1066 CX Amsterdam, The Netherlands (e-mail: alfred{at}nki.nl).
Background and Methods: Breast cancer resistance protein (BCRP/MXR/ABCP) is a multidrug-resistance protein that is a member of the adenosine triphosphate-binding cassette family of drug transporters. BCRP can render tumor cells resistant to the anticancer drugs topotecan, mitoxantrone, doxorubicin, and daunorubicin. To investigate the physiologic role of BCRP, we used polarized mammalian cell lines to determine the direction of BCRP drug transport. We also used the BCRP inhibitor GF120918 to assess the role of BCRP in protecting mice against xenobiotic drugs. Bcrp1, the murine homologue of BCRP, was expressed in the polarized mammalian cell lines LLC-PK1 and MDCK-II, and the direction of Bcrp1-mediated transport of topotecan and mitoxantrone was determined. To avoid the confounding drug transport provided by P-glycoprotein (P-gp), the roles of Bcrp1 in the bioavailability of topotecan and the effect of GF120918 were studied in both wild-type and P-gp-deficient mice and their fetuses. Results: Bcrp1 mediated apically directed transport of drugs in polarized cell lines. When both topotecan and GF120918 were administered orally, the bioavailability (i.e., the extent to which a drug becomes available to a target tissue after administration) of topotecan in plasma was dramatically increased in P-gp-deficient mice (greater than sixfold) and wild-type mice (greater than ninefold), compared with the control (i.e., vehicle-treated) mice. Furthermore, treatment with GF120918 decreased plasma clearance and hepatobiliary excretion of topotecan and increased (re-)uptake by the small intestine. In pregnant GF120918-treated, P-gp-deficient mice, relative fetal penetration of topotecan was twofold higher than that in pregnant vehicle-treated mice, suggesting a function for BCRP in the maternal–fetal barrier of the placenta. Conclusions: Bcrp1 mediates apically directed drug transport, appears to reduce drug bioavailability, and protects fetuses against drugs. We propose that strategic application of BCRP inhibitors may thus lead to more effective oral chemotherapy with topotecan or other BCRP substrate drugs.
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|
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|
|
|
|
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|
|
|
|
|
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|
|
|
|
|
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|
|
|
|
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|
|
|
|
 |
|
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|
|
|
|
|
|
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|
|
|
|
 |
|
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|
|
|
|
 |
|
 K. J. Linton Structure and Function of ABC Transporters Physiology, April 1, 2007; 22(2): 122 - 130. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
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|
|
|
|
|
|
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|
|
|
|
|
|
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|
|
|
|
|
|
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|
|
|
|
 |
|
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|
|
|
|
 |
|
 J. G. Turner, J. L. Gump, C. Zhang, J. M. Cook, D. Marchion, L. Hazlehurst, P. Munster, M. J. Schell, W. S. Dalton, and D. M. Sullivan ABCG2 expression, function, and promoter methylation in human multiple myeloma Blood, December 1, 2006; 108(12): 3881 - 3889. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 K. K. W. To, Z. Zhan, and S. E. Bates Aberrant Promoter Methylation of the ABCG2 Gene in Renal Carcinoma Mol. Cell. Biol., November 15, 2006; 26(22): 8572 - 8585. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
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|
|
|
|
 |
|
 B. Sarkadi, L. Homolya, G. Szakacs, and A. Varadi Human Multidrug Resistance ABCB and ABCG Transporters: Participation in a Chemoimmunity Defense System. Physiol Rev, October 1, 2006; 86(4): 1179 - 1236. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
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|
|
|
|
 |
|
 I. Szatmari, G. Vamosi, P. Brazda, B. L. Balint, S. Benko, L. Szeles, V. Jeney, C. Ozvegy-Laczka, A. Szanto, E. Barta, et al. Peroxisome Proliferator-activated Receptor {gamma}-regulated ABCG2 Expression Confers Cytoprotection to Human Dendritic Cells J. Biol. Chem., August 18, 2006; 281(33): 23812 - 23823. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 S. Choudhuri and C. D. Klaassen Structure, Function, Expression, Genomic Organization, and Single Nucleotide Polymorphisms of Human ABCB1 (MDR1), ABCC (MRP), and ABCG2 (BCRP) Efflux Transporters International Journal of Toxicology, July 1, 2006; 25(4): 231 - 259. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
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|
|
|
|
|
|
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|
|
|
|
 |
|
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|
|
|
|
|
|
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|
|
|
|
 |
|
 D. A. Evseenko, J. W. Paxton, and J. A. Keelan ABC drug transporter expression and functional activity in trophoblast-like cell lines and differentiating primary trophoblast Am J Physiol Regulatory Integrative Comp Physiol, May 1, 2006; 290(5): R1357 - R1365. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
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|
|
|
|
|
|
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|
|
|
|
|
|
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|
|
|
|
 |
|
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|
|
|
|
 |
|
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|
|
|
|
|
|
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|
|
|
|
 |
|
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|
|
|
|
|
|
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|
|
|
|
 |
|
 G. M. Kalabis, A. Kostaki, M. H. Andrews, S. Petropoulos, W. Gibb, and S. G. Matthews Multidrug Resistance Phosphoglycoprotein (ABCB1) in the Mouse Placenta: Fetal Protection Biol Reprod, October 1, 2005; 73(4): 591 - 597. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
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|
|
|
|
|
|
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|
|
|
|
|
|
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|
|
|
|
|
|
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|
|
|
|
|
|
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|
|
|
|
|
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|
|
|
|
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C. Q. Xia, N. Liu, D. Yang, G. Miwa, and L.-S. Gan EXPRESSION, LOCALIZATION, AND FUNCTIONAL CHARACTERISTICS OF BREAST CANCER RESISTANCE PROTEIN IN CACO-2 CELLS Drug Metab. Dispos., May 1, 2005; 33(5): 637 - 643. [Abstract] [Full Text] [PDF]
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G. Merino, J. W. Jonker, E. Wagenaar, A. E. van Herwaarden, and A. H. Schinkel The Breast Cancer Resistance Protein (BCRP/ABCG2) Affects Pharmacokinetics, Hepatobiliary Excretion, and Milk Secretion of the Antibiotic Nitrofurantoin Mol. Pharmacol., May 1, 2005; 67(5): 1758 - 1764. [Abstract] [Full Text] [PDF]
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G. Merino, A. E. van Herwaarden, E. Wagenaar, J. W. Jonker, and A. H. Schinkel Sex-Dependent Expression and Activity of the ATP-Binding Cassette Transporter Breast Cancer Resistance Protein (BCRP/ABCG2) in Liver Mol. Pharmacol., May 1, 2005; 67(5): 1765 - 1771. [Abstract] [Full Text] [PDF]
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D. Kolwankar, D. D. Glover, J. A. Ware, and T. S. Tracy EXPRESSION AND FUNCTION OF ABCB1 AND ABCG2 IN HUMAN PLACENTAL TISSUE Drug Metab. Dispos., April 1, 2005; 33(4): 524 - 529. [Abstract] [Full Text] [PDF]
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P. Breedveld, D. Pluim, G. Cipriani, P. Wielinga, O. van Tellingen, A. H. Schinkel, and J. H.M. Schellens The Effect of Bcrp1 (Abcg2) on the In vivo Pharmacokinetics and Brain Penetration of Imatinib Mesylate (Gleevec): Implications for the Use of Breast Cancer Resistance Protein and P-Glycoprotein Inhibitors to Enable the Brain Penetration of Imatinib in Patients Cancer Res., April 1, 2005; 65(7): 2577 - 2582. [Abstract] [Full Text] [PDF]
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S. Zhou, Y. Zong, P. A. Ney, G. Nair, C. F. Stewart, and B. P. Sorrentino Increased expression of the Abcg2 transporter during erythroid maturation plays a role in decreasing cellular protoporphyrin IX levels Blood, March 15, 2005; 105(6): 2571 - 2576. [Abstract] [Full Text] [PDF]
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S. Zhang, X. Wang, K. Sagawa, and M. E. Morris FLAVONOIDS CHRYSIN AND BENZOFLAVONE, POTENT BREAST CANCER RESISTANCE PROTEIN INHIBITORS, HAVE NO SIGNIFICANT EFFECT ON TOPOTECAN PHARMACOKINETICS IN RATS OR MDR1A/1B (-/-) MICE Drug Metab. Dispos., March 1, 2005; 33(3): 341 - 348. [Abstract] [Full Text] [PDF]
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Y. Adachi, H. Suzuki, A. H. Schinkel, and Y. Sugiyama Role of Breast Cancer Resistance Protein (Bcrp1/Abcg2) in the Extrusion of Glucuronide and Sulfate Conjugates from Enterocytes to Intestinal Lumen Mol. Pharmacol., March 1, 2005; 67(3): 923 - 928. [Abstract] [Full Text] [PDF]
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K. F. K. Ejendal and C. A. Hrycyna Differential Sensitivities of the Human ATP-Binding Cassette Transporters ABCG2 and P-Glycoprotein to Cyclosporin A Mol. Pharmacol., March 1, 2005; 67(3): 902 - 911. [Abstract] [Full Text] [PDF]
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D. Kobayashi, I. Ieiri, T. Hirota, H. Takane, S. Maegawa, J. Kigawa, H. Suzuki, E. Nanba, M. Oshimura, N. Terakawa, et al. FUNCTIONAL ASSESSMENT OF ABCG2 (BCRP) GENE POLYMORPHISMS TO PROTEIN EXPRESSION IN HUMAN PLACENTA Drug Metab. Dispos., January 1, 2005; 33(1): 94 - 101. [Abstract] [Full Text] [PDF]
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Y.-J. Lee, H. Kusuhara, J. W. Jonker, A. H. Schinkel, and Y. Sugiyama Investigation of Efflux Transport of Dehydroepiandrosterone Sulfate and Mitoxantrone at the Mouse Blood-Brain Barrier: A Minor Role of Breast Cancer Resistance Protein J. Pharmacol. Exp. Ther., January 1, 2005; 312(1): 44 - 52. [Abstract] [Full Text] [PDF]
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P. Pavek, G. Merino, E. Wagenaar, E. Bolscher, M. Novotna, J. W. Jonker, and A. H. Schinkel Human Breast Cancer Resistance Protein: Interactions with Steroid Drugs, Hormones, the Dietary Carcinogen 2-Amino-1-methyl-6-phenylimidazo(4,5-b)pyridine, and Transport of Cimetidine J. Pharmacol. Exp. Ther., January 1, 2005; 312(1): 144 - 152. [Abstract] [Full Text] [PDF]
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C. F. Stewart, M. Leggas, J. D. Schuetz, J. C. Panetta, P. J. Cheshire, J. Peterson, N. Daw, J. J. Jenkins III, R. Gilbertson, G. S. Germain, et al. Gefitinib Enhances the Antitumor Activity and Oral Bioavailability of Irinotecan in Mice Cancer Res., October 15, 2004; 64(20): 7491 - 7499. [Abstract] [Full Text] [PDF]
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N. Mizuno, M. Suzuki, H. Kusuhara, H. Suzuki, K. Takeuchi, T. Niwa, J. W. Jonker, and Y. Sugiyama IMPAIRED RENAL EXCRETION OF 6-HYDROXY-5,7-DIMETHYL-2-METHYLAMINO-4-(3-PYRIDYLMETHYL) BENZOTHIAZOLE (E3040) SULFATE IN BREAST CANCER RESISTANCE PROTEIN (BCRP1/ABCG2) KNOCKOUT MICE Drug Metab. Dispos., September 1, 2004; 32(9): 898 - 901. [Abstract] [Full Text] [PDF]
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F. A. de Jong, S. Marsh, R. H. J. Mathijssen, C. King, J. Verweij, A. Sparreboom, and H. L. McLeod ABCG2 Pharmacogenetics: Ethnic Differences in Allele Frequency and Assessment of Influence on Irinotecan Disposition Clin. Cancer Res., September 1, 2004; 10(17): 5889 - 5894. [Abstract] [Full Text] [PDF]
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P. Breedveld, N. Zelcer, D. Pluim, O. Sonmezer, M. M. Tibben, J. H. Beijnen, A. H. Schinkel, O. van Tellingen, P. Borst, and J. H. M. Schellens Mechanism of the Pharmacokinetic Interaction between Methotrexate and Benzimidazoles: Potential Role for Breast Cancer Resistance Protein in Clinical Drug-Drug Interactions Cancer Res., August 15, 2004; 64(16): 5804 - 5811. [Abstract] [Full Text] [PDF]
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K. W. Ward and L. M. Azzarano Preclinical Pharmacokinetic Properties of the P-Glycoprotein Inhibitor GF120918A (HCl salt of GF120918, 9,10-Dihydro-5-methoxy-9-oxo-N-[4-[2-(1,2,3,4-tetrahydro-6,7-dimethoxy-2-isoquinolinyl)ethyl]phenyl]-4-acridine-carboxamide) in the Mouse, Rat, Dog, and Monkey J. Pharmacol. Exp. Ther., August 1, 2004; 310(2): 703 - 709. [Abstract] [Full Text] [PDF]
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S. E. Bates, W. Y. Medina-Perez, G. Kohlhagen, S. Antony, T. Nadjem, R. W. Robey, and Y. Pommier ABCG2 Mediates Differential Resistance to SN-38 (7-Ethyl-10-hydroxycamptothecin) and Homocamptothecins J. Pharmacol. Exp. Ther., August 1, 2004; 310(2): 836 - 842. [Abstract] [Full Text] [PDF]
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J. W. Polli, T. M. Baughman, J. E. Humphreys, K. H. Jordan, A. L. Mote, L. O. Webster, R. J. Barnaby, G. Vitulli, L. Bertolotti, K. D. Read, et al. THE SYSTEMIC EXPOSURE OF AN N-METHYL-D-ASPARTATE RECEPTOR ANTAGONIST IS LIMITED IN MICE BY THE P-GLYCOPROTEIN AND BREAST CANCER RESISTANCE PROTEIN EFFLUX TRANSPORTERS Drug Metab. Dispos., July 1, 2004; 32(7): 722 - 726. [Abstract] [Full Text] [PDF]
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A. Gupta, Y. Zhang, J. D. Unadkat, and Q. Mao HIV Protease Inhibitors Are Inhibitors but Not Substrates of the Human Breast Cancer Resistance Protein (BCRP/ABCG2) J. Pharmacol. Exp. Ther., July 1, 2004; 310(1): 334 - 341. [Abstract] [Full Text] [PDF]
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C. Ozvegy-Laczka, T. Heged""s, G. Varady, O. Ujhelly, J. D. Schuetz, A. Varadi, G. Keri, L. Orfi, K. Nemet, and B. Sarkadi High-Affinity Interaction of Tyrosine Kinase Inhibitors with the ABCG2 Multidrug Transporter Mol. Pharmacol., June 1, 2004; 65(6): 1485 - 1495. [Abstract] [Full Text] [PDF]
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S. Zhang, X. Yang, and M. E. Morris Flavonoids Are Inhibitors of Breast Cancer Resistance Protein (ABCG2)-Mediated Transport Mol. Pharmacol., May 1, 2004; 65(5): 1208 - 1216. [Abstract] [Full Text]
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S. U. C. Sankatsing, J. H. Beijnen, A. H. Schinkel, J. M. A. Lange, and J. M. Prins P Glycoprotein in Human Immunodeficiency Virus Type 1 Infection and Therapy Antimicrob. Agents Chemother., April 1, 2004; 48(4): 1073 - 1081. [Full Text] [PDF]
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P. L. R. Ee, S. Kamalakaran, D. Tonetti, X. He, D. D. Ross, and W. T. Beck Identification of a Novel Estrogen Response Element in the Breast Cancer Resistance Protein (ABCG2) Gene Cancer Res., February 15, 2004; 64(4): 1247 - 1251. [Abstract] [Full Text] [PDF]
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K. S. Pang MODELING OF INTESTINAL DRUG ABSORPTION: ROLES OF TRANSPORTERS AND METABOLIC ENZYMES (FOR THE GILLETTE REVIEW SERIES) Drug Metab. Dispos., December 1, 2003; 31(12): 1507 - 1519. [Full Text] [PDF]
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 C G Dietrich, A Geier, and R P J Oude Elferink ABC of oral bioavailability: transporters as gatekeepers in the gut Gut, December 1, 2003; 52(12): 1788 - 1795. [Full Text] [PDF]
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T. Nakanishi, L. A. Doyle, B. Hassel, Y. Wei, K. S. Bauer, S. Wu, D. W. Pumplin, H.-B. Fang, and D. D. Ross Functional Characterization of Human Breast Cancer Resistance Protein (BCRP, ABCG2) Expressed in the Oocytes of Xenopus laevis Mol. Pharmacol., December 1, 2003; 64(6): 1452 - 1462. [Abstract] [Full Text] [PDF]
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A. E. van Herwaarden, J. W. Jonker, E. Wagenaar, R. F. Brinkhuis, J. H. M. Schellens, J. H. Beijnen, and A. H. Schinkel The Breast Cancer Resistance Protein (Bcrp1/Abcg2) Restricts Exposure to the Dietary Carcinogen 2-Amino-1-methyl-6-phenylimidazo[4,5-b]pyridine Cancer Res., October 1, 2003; 63(19): 6447 - 6452. [Abstract] [Full Text] [PDF]
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Y. Imai, S. Asada, S. Tsukahara, E. Ishikawa, T. Tsuruo, and Y. Sugimoto Breast Cancer Resistance Protein Exports Sulfated Estrogens but Not Free Estrogens Mol. Pharmacol., September 1, 2003; 64(3): 610 - 618. [Abstract] [Full Text] [PDF]
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 N. Mizuno, T. Niwa, Y. Yotsumoto, and Y. Sugiyama Impact of Drug Transporter Studies on Drug Discovery and Development Pharmacol. Rev., September 1, 2003; 55(3): 425 - 461. [Abstract] [Full Text] [PDF]
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Z.-S. Chen, R. W. Robey, M. G. Belinsky, I. Shchaveleva, X.-Q. Ren, Y. Sugimoto, D. D. Ross, S. E. Bates, and G. D. Kruh Transport of Methotrexate, Methotrexate Polyglutamates, and 17{beta}-Estradiol 17-({beta}-D-glucuronide) by ABCG2: Effects of Acquired Mutations at R482 on Methotrexate Transport Cancer Res., July 15, 2003; 63(14): 4048 - 4054. [Abstract] [Full Text] [PDF]
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 K. Shimano, M. Satake, A. Okaya, J. Kitanaka, N. Kitanaka, M. Takemura, M. Sakagami, N. Terada, and T. Tsujimura Hepatic Oval Cells Have the Side Population Phenotype Defined by Expression of ATP-Binding Cassette Transporter ABCG2/BCRP1 Am. J. Pathol., July 1, 2003; 163(1): 3 - 9. [Abstract] [Full Text] [PDF]
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M. Suzuki, H. Suzuki, Y. Sugimoto, and Y. Sugiyama ABCG2 Transports Sulfated Conjugates of Steroids and Xenobiotics J. Biol. Chem., June 13, 2003; 278(25): 22644 - 22649. [Abstract] [Full Text] [PDF]
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R O. Elferink Cholestasis Gut, May 1, 2003; 52(90002): ii42 - 48. [Abstract] [Full Text]
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J. D. Allen, S. C. van Dort, M. Buitelaar, O. van Tellingen, and A. H. Schinkel Mouse Breast Cancer Resistance Protein (Bcrp1/Abcg2) Mediates Etoposide Resistance and Transport, but Etoposide Oral Availability Is Limited Primarily by P-glycoprotein Cancer Res., March 15, 2003; 63(6): 1339 - 1344. [Abstract] [Full Text] [PDF]
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R. H. Stephens, J. Tanianis-Hughes, N. B. Higgs, M. Humphrey, and G. Warhurst Region-Dependent Modulation of Intestinal Permeability by Drug Efflux Transporters: In Vitro Studies in mdr1a(-/-) Mouse Intestine J. Pharmacol. Exp. Ther., December 1, 2002; 303(3): 1095 - 1101. [Abstract] [Full Text] [PDF]
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 C.M.F. Kruijtzer, J.H. Beijnen, and J.H.M. Schellens Improvement of Oral Drug Treatment by Temporary Inhibition of Drug Transporters and/or Cytochrome P450 in the Gastrointestinal Tract and Liver: An Overview Oncologist, December 1, 2002; 7(6): 516 - 530. [Abstract] [Full Text] [PDF]
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 J. W. Jonker, M. Buitelaar, E. Wagenaar, M. A. van der Valk, G. L. Scheffer, R. J. Scheper, T. Plosch, F. Kuipers, R. P. J. O. Elferink, H. Rosing, et al. The breast cancer resistance protein protects against a major chlorophyll-derived dietary phototoxin and protoporphyria PNAS, November 26, 2002; 99(24): 15649 - 15654. [Abstract] [Full Text] [PDF]
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S. Zhou, J. J. Morris, Y. Barnes, L. Lan, J. D. Schuetz, and B. P. Sorrentino Bcrp1 gene expression is required for normal numbers of side population stem cells in mice, and confers relative protection to mitoxantrone in hematopoietic cells in vivo PNAS, September 17, 2002; 99(19): 12339 - 12344. [Abstract] [Full Text] [PDF]
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 G. Hudes Boosting Bioavailability of Topotecan: What Do We Gain? J. Clin. Oncol., July 1, 2002; 20(13): 2918 - 2919. [Full Text] [PDF]
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C. M.F. Kruijtzer, J. H. Beijnen, H. Rosing, W. W. ten Bokkel Huinink, M. Schot, R. C. Jewell, E. M. Paul, and J. H.M. Schellens Increased Oral Bioavailability of Topotecan in Combination With the Breast Cancer Resistance Protein and P-Glycoprotein Inhibitor GF120918 J. Clin. Oncol., July 1, 2002; 20(13): 2943 - 2950. [Abstract] [Full Text] [PDF]
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