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Subcellular Localization and Distribution of the Breast Cancer Resistance Protein Transporter in Normal Human Tissues¹

Divisions of Experimental Therapy [M. M., M. A. v. G., A. H. S., J. H. M. S.], Medical Oncology [J. H. M. S.], and Pathology [I. F. F., M. J. v. d. V.], The Netherlands Cancer Institute, 1066 CX Amsterdam; and Department of Pathology, Free University Hospital, 1081 HV Amsterdam [G. L. S., A. C. L. M. P., R. J. S.], the Netherlands

High expression of the Breast Cancer Resistance Protein (BCRP) gene has been shown to be involved in resistance to chemotherapeutic drugs. Knowledge of the localization of BCRP protein in normal tissues may help unravel the normal function of this protein. Therefore, we characterized the tissue distribution and cellular localization of BCRP in frozen sections of normal human tissues. For this purpose, we used the recently described monoclonal antibody BXP-34 and another independently developed monoclonal antibody directed against BCRP, BXP-21. Both monoclonal antibodies show specific BCRP plasma membrane staining on cytospins obtained from topotecan- or mitoxantrone-selected cell lines, as well as from BCRP-transfected cell lines. Immunoprecipitation experiments using either BXP-21 or BXP-34 yielded a clear M_r 72,000 BCRP band from BCRP-overexpressing tumor cells. In the topotecan-selected T8 and mitoxantrone-selected MX3 tumor cell lines, BCRP turned out to be differentially glycosylated. In contrast to BXP-34, BXP-21 is able to detect the M_r 72,000 BCRP protein on immunoblots and is reactive with BCRP in formalin-fixed, paraffin-embedded tissues.

Using BXP-21 and BXP-34, prominent staining of BCRP was observed in placental syncytiotrophoblasts, in the epithelium of the small intestine and colon, in the liver canalicular membrane, and in ducts and lobules of the breast. Furthermore, BCRP was present in veinous and capillary endothelium, but not in arterial endothelium in all of the tissues investigated. In the tissues studied, the mRNA levels of BCRP were assessed using reverse transcription-PCR, and these corresponded with the levels of BCRP protein estimated from immunohistochemical staining. The presence of BCRP at the placental syncytiotrophoblasts is consistent with the hypothesis of a protective role of BCRP for the fetus. The apical localization in the epithelium of the small intestine and colon indicates a possible role of BCRP in the regulation of the uptake of p.o. administered BCRP substrates by back-transport of substrate drugs entering from the gut lumen. Therefore, it may be useful to attempt to modulate the uptake of p.o. delivered BCRP substrates, e.g., topotecan or irinotecan, by using a BCRP inhibitor. Clinical trials testing this hypothesis have been initiated in our institute.

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				U. Henriksen, J. U. Fog, T. Litman, and U. Gether Identification of Intra- and Intermolecular Disulfide Bridges in the Multidrug Resistance Transporter ABCG2 J. Biol. Chem., November 4, 2005; 280(44): 36926 - 36934. [Abstract] [Full Text] [PDF]

				B. Ebert, A. Seidel, and A. Lampen Identification of BCRP as transporter of benzo[a]pyrene conjugates metabolically formed in Caco-2 cells and its induction by Ah-receptor agonists Carcinogenesis, October 1, 2005; 26(10): 1754 - 1763. [Abstract] [Full Text] [PDF]

				A. Shafran, I. Ifergan, E. Bram, G. Jansen, I. Kathmann, G. J. Peters, R. W. Robey, S. E. Bates, and Y. G. Assaraf ABCG2 Harboring the Gly482 Mutation Confers High-Level Resistance to Various Hydrophilic Antifolates Cancer Res., September 15, 2005; 65(18): 8414 - 8422. [Abstract] [Full Text] [PDF]

				S. Matsushima, K. Maeda, C. Kondo, M. Hirano, M. Sasaki, H. Suzuki, and Y. Sugiyama Identification of the Hepatic Efflux Transporters of Organic Anions Using Double-Transfected Madin-Darby Canine Kidney II Cells Expressing Human Organic Anion-Transporting Polypeptide 1B1 (OATP1B1)/Multidrug Resistance-Associated Protein 2, OATP1B1/Multidrug Resistance 1, and OATP1B1/Breast Cancer Resistance Protein J. Pharmacol. Exp. Ther., September 1, 2005; 314(3): 1059 - 1067. [Abstract] [Full Text] [PDF]

				M. Hirano, K. Maeda, S. Matsushima, Y. Nozaki, H. Kusuhara, and Y. Sugiyama Involvement of BCRP (ABCG2) in the Biliary Excretion of Pitavastatin Mol. Pharmacol., September 1, 2005; 68(3): 800 - 807. [Abstract] [Full Text] [PDF]

				M. J. Zamek-Gliszczynski, K. A. Hoffmaster, X. Tian, R. Zhao, J. W. Polli, J. E. Humphreys, L. O. Webster, A. S. Bridges, J. C. Kalvass, and K. L. R. Brouwer MULTIPLE MECHANISMS ARE INVOLVED IN THE BILIARY EXCRETION OF ACETAMINOPHEN SULFATE IN THE RAT: ROLE OF MRP2 AND BCRP1 Drug Metab. Dispos., August 1, 2005; 33(8): 1158 - 1165. [Abstract] [Full Text] [PDF]

				X.-f. Zhou, X. Yang, Q. Wang, R. A. Coburn, and M. E. Morris EFFECTS OF DIHYDROPYRIDINES AND PYRIDINES ON MULTIDRUG RESISTANCE MEDIATED BY BREAST CANCER RESISTANCE PROTEIN: IN VITRO AND IN VIVO STUDIES Drug Metab. Dispos., August 1, 2005; 33(8): 1220 - 1228. [Abstract] [Full Text] [PDF]

				H. E. Meyer zu Schwabedissen, G. Jedlitschky, M. Gratz, S. Haenisch, K. Linnemann, C. Fusch, I. Cascorbi, and H. K. Kroemer VARIABLE EXPRESSION OF MRP2 (ABCC2) IN HUMAN PLACENTA: INFLUENCE OF GESTATIONAL AGE AND CELLULAR DIFFERENTIATION Drug Metab. Dispos., July 1, 2005; 33(7): 896 - 904. [Abstract] [Full Text] [PDF]

				R. R. Vethanayagam, H. Wang, A. Gupta, Y. Zhang, F. Lewis, J. D. Unadkat, and Q. Mao FUNCTIONAL ANALYSIS OF THE HUMAN VARIANTS OF BREAST CANCER RESISTANCE PROTEIN: I206L, N590Y, AND D620N Drug Metab. Dispos., June 1, 2005; 33(6): 697 - 705. [Abstract] [Full Text] [PDF]

				A. L. A. Sesink, I. C. W. Arts, V. C. J. de Boer, P. Breedveld, J. H. M. Schellens, P. C. H. Hollman, and F. G. M. Russel Breast Cancer Resistance Protein (Bcrp1/Abcg2) Limits Net Intestinal Uptake of Quercetin in Rats by Facilitating Apical Efflux of Glucuronides Mol. Pharmacol., June 1, 2005; 67(6): 1999 - 2006. [Abstract] [Full Text] [PDF]

				N. Zelcer, K. van de Wetering, M. Hillebrand, E. Sarton, A. Kuil, P. R. Wielinga, T. Tephly, A. Dahan, J. H. Beijnen, and P. Borst Mice lacking multidrug resistance protein 3 show altered morphine pharmacokinetics and morphine-6-glucuronide antinociception PNAS, May 17, 2005; 102(20): 7274 - 7279. [Abstract] [Full Text] [PDF]

				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]

				M. T. Budak, O. S. Alpdogan, M. Zhou, R. M. Lavker, M.A. M. Akinci, and J. M. Wolosin Ocular surface epithelia contain ABCG2-dependent side population cells exhibiting features associated with stem cells J. Cell Sci., April 15, 2005; 118(8): 1715 - 1724. [Abstract] [Full Text] [PDF]

				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]

				U. Henriksen, U. Gether, and T. Litman Effect of Walker A mutation (K86M) on oligomerization and surface targeting of the multidrug resistance transporter ABCG2 J. Cell Sci., April 1, 2005; 118(7): 1417 - 1426. [Abstract] [Full Text] [PDF]

				I. Ifergan, G. Jansen, and Y. G. Assaraf Cytoplasmic Confinement of Breast Cancer Resistance Protein (BCRP/ABCG2) as a Novel Mechanism of Adaptation to Short-Term Folate Deprivation Mol. Pharmacol., April 1, 2005; 67(4): 1349 - 1359. [Abstract] [Full Text] [PDF]

				M. H.G.P. Raaijmakers, E. P.L.M. de Grouw, L. H.H. Heuver, B. A. van der Reijden, J. H. Jansen, R. J. Scheper, G. L. Scheffer, T. J.M. de Witte, and R. A.P. Raymakers Breast Cancer Resistance Protein in Drug Resistance of Primitive CD34+38- Cells in Acute Myeloid Leukemia Clin. Cancer Res., March 15, 2005; 11(6): 2436 - 2444. [Abstract] [Full Text] [PDF]

				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]

				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]

				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]

				Y. Nakamura, M. Oka, H. Soda, K. Shiozawa, M. Yoshikawa, A. Itoh, Y. Ikegami, J. Tsurutani, K. Nakatomi, T. Kitazaki, et al. Gefitinib ("Iressa", ZD1839), an Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor, Reverses Breast Cancer Resistance Protein/ABCG2-Mediated Drug Resistance Cancer Res., February 15, 2005; 65(4): 1541 - 1546. [Abstract] [Full Text] [PDF]

				C. Ozvegy-Laczka, G. Varady, G. Koblos, O. Ujhelly, J. Cervenak, J. D. Schuetz, B. P. Sorrentino, G.-J. Koomen, A. Varadi, K. Nemet, et al. Function-dependent Conformational Changes of the ABCG2 Multidrug Transporter Modify Its Interaction with a Monoclonal Antibody on the Cell Surface J. Biol. Chem., February 11, 2005; 280(6): 4219 - 4227. [Abstract] [Full Text] [PDF]

				Y. Imai, E. Ishikawa, S. Asada, and Y. Sugimoto Estrogen-Mediated Post transcriptional Down-regulation of Breast Cancer Resistance Protein/ABCG2 Cancer Res., January 15, 2005; 65(2): 596 - 604. [Abstract] [Full Text] [PDF]

				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]

				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]

				H. E.U. Meyer zu Schwabedissen, M. Grube, B. Heydrich, K. Linnemann, C. Fusch, H. K. Kroemer, and G. Jedlitschky Expression, Localization, and Function of MRP5 (ABCC5), a Transporter for Cyclic Nucleotides, in Human Placenta and Cultured Human Trophoblasts: Effects of Gestational Age and Cellular Differentiation Am. J. Pathol., January 1, 2005; 166(1): 39 - 48. [Abstract] [Full Text] [PDF]

				P.L. R. Ee, X. He, D. D. Ross, and W. T. Beck Modulation of breast cancer resistance protein (BCRP/ABCG2) gene expression using RNA interference Mol. Cancer Ther., December 1, 2004; 3(12): 1577 - 1584. [Abstract] [Full Text] [PDF]

				F. Loganzo, M. Hari, T. Annable, X. Tan, D. B. Morilla, S. Musto, A. Zask, J. Kaplan, A. A. Minnick Jr., M. K. May, et al. Cells resistant to HTI-286 do not overexpress P-glycoprotein but have reduced drug accumulation and a point mutation in {alpha}-tubulin Mol. Cancer Ther., October 1, 2004; 3(10): 1319 - 1327. [Abstract] [Full Text] [PDF]

				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]

				K. Yanase, S. Tsukahara, S. Asada, E. Ishikawa, Y. Imai, and Y. Sugimoto Gefitinib reverses breast cancer resistance protein-mediated drug resistance Mol. Cancer Ther., September 1, 2004; 3(9): 1119 - 1125. [Abstract] [Full Text] [PDF]

				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]

				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]