516
Views
33
CrossRef citations to date
0
Altmetric
Research Article

Human ABC transporters ABCG2 (BCRP) and ABCG4

, , , , &
Pages 863-888 | Received 27 Nov 2007, Accepted 13 Feb 2008, Published online: 22 Sep 2008

References

  • Ahmed-Belkacem A, Pozza A, Munoz-Martinez F, Bates SE, Castanys S, Gamarro F, Di Pietro A, Perez-Victoria JM. Flavonoid structure–activity studies identify 6-prenylchrysin and tectochrysin as potent and specific inhibitors of breast cancer resistance protein ABCG2. Cancer Research 2005; 65: 4852–4860
  • Allikmets R, Schriml LM, Hutchinson A, Romano-Spica V, Dean M. A human placenta-specific ATP-binding cassette gene (ABCP) on chromosome 4q22 that is involved in multidrug resistance. Cancer Research 1998; 58: 5337–5339
  • Annilo T, Tammur J, Hutchinson A, Rzhetsky A, Dean M, Allikmets R. Human and mouse orthologs of a new ATP-binding cassette gene, ABCG4. Cytogenetics and Cell Genetics 2001; 94: 196–201
  • Backstrom G, Taipalensuu J, Melhus H, Brandstrom H, Svensson AC, Artursson P, Kindmark A. Genetic variation in the ATP-binding cassette transporter gene ABCG2 (BCRP) in a Swedish population. European Journal of Pharmaceutical Science 2003; 18: 359–364
  • Bailey-Dell KJ, Hassel B, Doyle LA, Ross DD. Promoter characterization and genomic organization of the human breast cancer resistance protein (ATP-binding cassette transporter G2) gene. Biochimica et Biophysica Acta 2001; 1520: 234–241
  • Berge KE, Tian H, Graf GA, Yu L, Grishin NV, Schultz J, Kwiterovich P, Shan B, Barnes R, Hobbs HH. Accumulation of dietary cholesterol in sitosterolemia caused by mutations in adjacent ABC transporters. Science 2000; 290: 1771–1775
  • Borst P, Elferink RO. Mammalian ABC transporters in health and disease. Annual Review of Biochemistry 2002; 71: 537–592
  • Bosch TM, Kjellberg LM, Bouwers A, Koeleman BP, Schellens JH, Beijnen JH, Smits PH, Meijerman I. Detection of single nucleotide polymorphisms in the ABCG2 gene in a Dutch population. American Journal of Pharmacogenomics 2005; 5: 123–131
  • Bowers AG. Phytophotodermatitis. American Journal of Contact Dermatitis 1999; 10: 89–93
  • Breckenridge DG, Germain M, Mathai JP, Nguyen M, Shore GC. Regulation of apoptosis by endoplasmic reticulum pathways. Oncogene 2003; 22: 8608–8618
  • Brehmer D, Greff Z, Godl K, Blencke S, Kurtenbach A, Weber M, Muller S, Klebl B, Cotten M, Keri G, et al. Cellular targets of gefitinib. Cancer Research 2005; 65: 379–382
  • Chen ZS, Robey RW, Belinsky MG, Shchaveleva I, Ren XQ, Sugimoto Y, Ross DD, Bates SE, Kruh GD. Transport of methotrexate, methotrexate polyglutamates, and 17beta-estradiol 17-(beta-D-glucuronide) by ABCG2: Effects of acquired mutations at R482 on methotrexate transport. Cancer Research 2003; 63: 4048–4054
  • Cole SP, Bhardwaj G, Gerlach JH, Mackie JE, Grant CE, Almquist KC, Stewart AJ, Kurz EU, Duncan AM, Deeley RG. Overexpression of a transporter gene in a multidrug-resistant human lung cancer cell line. Science 1992; 258: 1650–1654
  • Cooray HC, Janvilisri T, Van Veen HW, Hladky SB, Barrand MA. Interaction of the breast cancer resistance protein with plant polyphenols. Biochemical and Biophysical Research Communications 2004; 317: 269–275
  • Cordon-Cardo C, O’Brien JP, Casals D, Rittman-Grauer L, Biedler JL, Melamed MR, Bertino JR. Multidrug-resistance gene (P-glycoprotein) is expressed by endothelial cells at blood–brain barrier sites. Proceedings of the National Academy of Sciences, USA 1989; 86: 695–698
  • Cserepes J, Szentpetery Z, Seres L, Özvegy-Laczka C, Langmann T, Schmitz G, Glavinas H, Klein I, Homolya L, Varadi A, et al. Functional expression and characterization of the human ABCG1 and ABCG4 proteins: indications for heterodimerization. Biochemical and Biophysical Research Communications 2004; 320: 860–867
  • Cui Y, Konig J, Buchholz JK, Spring H, Leier I, Keppler D. Drug resistance and ATP-dependent conjugate transport mediated by the apical multidrug resistance protein, MRP2, permanently expressed in human and canine cells. Molecular Pharmacology 1999; 55: 929–937
  • De Jong FA, Marsh S, Mathijssen RH, King C, Verweij J, Sparreboom A, McLeod HL. ABCG2 pharmacogenetics: Ethnic differences in allele frequency and assessment of influence on irinotecan disposition. Clinical Cancer Research 2004; 10: 5889–5894
  • Dean M, Rzhetsky A, Allikmets R. The human ATP-binding cassette (ABC) transporter superfamily. Genome Research 2001; 11: 1156–1166
  • Doyle LA, Yang W, Abruzzo LV, Krogmann T, Gao Y, Rishi AK, Ross DD. A multidrug resistance transporter from human MCF-7 breast cancer cells. Proceedings of the National Academy of Sciences, USA 1998; 95: 15665–15670
  • Elkind NB, Szentpetery Z, Apati A, Özvegy-Laczka C, Varady G, Ujhelly O, Szabo K, Homolya L, Varadi A, Buday L, et al. Multidrug transporter ABCG2 prevents tumor cell death induced by the epidermal growth factor receptor inhibitor Iressa (ZD1839, Gefitinib). Cancer Research 2005; 65: 1770–1777
  • Engel T, Lorkowski S, Lueken A, Rust S, Schluter B, Berger G, Cullen P, Assmann G. The human ABCG4 gene is regulated by oxysterols and retinoids in monocyte-derived macrophages. Biochemical and Biophysical Research Communications 2001; 288: 483–488
  • Gottesman MM, Fojo T, Bates SE. Multidrug resistance in cancer: role of ATP-dependent transporters. Nature Reviews Cancer 2002; 2: 48–58
  • Graf GA, Yu L, Li WP, Gerard R, Tuma PL, Cohen JC, Hobbs HH. ABCG5 and ABCG8 are obligate heterodimers for protein trafficking and biliary cholesterol excretion. Journal of Biological Chemistry 2003; 278: 48275–48282
  • Henriksen U, Fog JU, Litman T, Gether U. Identification of intra- and intermolecular disulfide bridges in the multidrug resistance transporter ABCG2. Journal of Biological Chemistry 2005; 280: 36926–36934
  • Higgins CF. ABC transporters: From microorganisms to man. Annual Review of Cell Biology 1992; 8: 67–113
  • Hirano H, Kurata A, Onishi Y, Sakurai A, Saito H, Nakagawa H, Nagakura M, Tarui S, Kanamori Y, Kitajima M, et al. High-speed screening and QSAR analysis of human ATP-binding cassette transporter ABCB11 (bile salt export pump) to predict drug-induced intrahepatic cholestasis. Molecular Pharmaceutics 2006; 3: 252–265
  • Honjo Y, Morisaki K, Huff LM, Robey RW, Hung J, Dean M, Bates SE. Single-nucleotide polymorphism (SNP) analysis in the ABC half-transporter ABCG2 (MXR/BCRP/ABCP1). Cancer Biological Therapy 2002; 1: 696–702
  • Hwang C, Sinskey AJ, Lodish HF. Oxidized redox state of glutathione in the endoplasmic reticulum. Science 1992; 257: 1496–1502
  • Iida A, Saito S, Sekine A, Mishima C, Kitamura Y, Kondo K, Harigae S, Osawa S, Nakamura Y. Catalog of 605 single-nucleotide polymorphisms (SNPs) among 13 genes encoding human ATP-binding cassette transporters: ABCA4, ABCA7, ABCA8, ABCD1, ABCD3, ABCD4, ABCE1, ABCF1, ABCG1, ABCG2, ABCG4, ABCG5, and ABCG8. Journal of Human Genetics 2002; 47: 285–310
  • Imai Y, Nakane M, Kage K, Tsukahara S, Ishikawa E, Tsuruo T, Miki Y, Sugimoto Y. C421A polymorphism in the human breast cancer resistance protein gene is associated with low expression of Q141K protein and low-level drug resistance. Molecular Cancer Therapeutics 2002; 1: 611–616
  • Imai Y, Tsukahara S, Asada S, Sugimoto Y. Phytoestrogens/flavonoids reverse breast cancer resistance protein/ABCG2-mediated multidrug resistance. Cancer Research 2004; 64: 4346–4352
  • Inanami O, Yoshito A, Takahashi K, Hiraoka W, Kuwabara M. Effects of BAPTA-AM and forskolin on apoptosis and cytochrome c release in photosensitized Chinese hamster V79 cells. Photochemistry and Photobiology 1999; 70: 650–655
  • Ishikawa T. ATP/Mg2+-dependent cardiac transport system for glutathione S-conjugates. A study using rat heart sarcolemma vesicles. Journal of Biological Chemistry 1989; 264: 17343–17348
  • Ishikawa T. The ATP-dependent glutathione S-conjugate export pump. Trends in Biochemical Sciences 1992; 17: 463–468
  • Ishikawa T. Multidrug resistance: genetics of ABC transporters. Nature encyclopedia of the human genome, DN Cooper. Nature Publishing Group, London 2003; 154–160
  • Ishikawa T, Hirano H, Onishi Y, Sakurai A, Tarui S. Functional evaluation of ABCB1 (P-glycoprotein) polymorphisms: High-speed screening and structure–activity relationship analyses. Drug Metabolism and Pharmacokinetics 2004a; 19: 1–14
  • Ishikawa T, Sakurai A, Kanamori Y, Nagakura M, Hirano H, Takarada Y, Yamada K, Fukushima K, Kitajima M. High-speed screening of human ATP-binding cassette transporter function and genetic polymorphisms: New strategies in pharmacogenomics. Methods in Enzymology 2005a; 400: 485–510
  • Ishikawa T, Tamura A, Saito H, Wakabayashi K, Nakagawa H. Pharmacogenomics of the human ABC transporter ABCG2: From functional evaluation to drug molecular design. Naturwissenschaften 2005b; 92: 451–463
  • Ishikawa T, Tsuji A, Inui K, Sai Y, Anzai N, Wada M, Endou H, Sumino Y. The genetic polymorphism of drug transporters: Functional analysis approaches. Pharmacogenomics 2004b; 5: 67–99
  • Itoda M, Saito Y, Shirao K, Minami H, Ohtsu A, Yoshida T, Saijo N, Suzuki H, Sugiyama Y, Ozawa S, Sawada J. Eight novel single nucleotide polymorphisms in ABCG2/BCRP in Japanese cancer patients administered irinotacan. Drug Metabolism and Pharmacokinetics 2003; 18: 212–217
  • Jitsukawa K, Suizu R, Hidano A. Chlorella photosensitization. New phytophotodermatosis. International Journal of Dermatology 1984; 23: 263–268
  • Johnston JA, Ward CL, Kopito RR. Aggresomes: A cellular response to misfolded proteins. Journal of Cell Biology 1998; 143: 1883–1898
  • Jonker JW, Buitelaar M, Wagenaar E, Van der Valk MA, Scheffer GL, Scheper RJ, Plosch T, Kuipers F, Elferink RP, Rosing H, et al. The breast cancer resistance protein protects against a major chlorophyll-derived dietary phototoxin and protoporphyria. Proceedings of the National Academy of Sciences, USA 2002; 99: 15649–15654
  • Jonker JW, Merino G, Musters S, Van Herwaarden AE, Bolscher E, Wagenaar E, Mesman E, Dale TC, Schinkel AH. The breast cancer resistance protein BCRP (ABCG2) concentrates drugs and carcinogenic xenotoxins into milk. Nature Medicine 2005; 11: 127–129
  • Jonker JW, Smit JW, Brinkhuis RF, Maliepaard M, Beijnen JH, Schellens JH, Schinkel AH. Role of breast cancer resistance protein in the bioavailability and fetal penetration of topotecan. Journal of the National Cancer Institute 2000; 92: 1651–1656
  • Kage K, Fujita T, Sugimoto Y. Role of Cys-603 in dimer/oligomer formation of the breast cancer resistance protein BCRP/ABCG2. Cancer Science 2005; 96: 866–872
  • Kage K, Tsukahara S, Sugiyama T, Asada S, Ishikawa E, Tsuruo T, Sugimoto Y. Dominant-negative inhibition of breast cancer resistance protein as drug efflux pump through the inhibition of S-S dependent homodimerization. International Journal of Cancer 2002; 97: 626–630
  • Kalow E, Meyer U, Tyndale RF. Pharmacogenomics. Marcel Dekker, New York, NY 2001
  • Kato H, Furukawa K, Sato M, Okunaka T, Kusunoki Y, Kawahara M, Fukuoka M, Miyazawa T, Yana T, Matsui K, et al. Phase II clinical study of photodynamic therapy using mono-L-aspartyl chlorin e6 and diode laser for early superficial squamous cell carcinoma of the lung. Lung Cancer 2003; 42: 103–111
  • Kim WS, Rahmanto AS, Kamili A, Rye KA, Guillemin GJ, Gelissen IC, Jessup W, Hill AF, Garner B. Role of ABCG1 and ABCA1 in regulation of neuronal cholesterol efflux to apolipoprotein E discs and suppression of amyloid-beta peptide generation. Journal of Biological Chemistry 2007; 282: 2851–2861
  • Kirov G, Lowry CA, Stephens M, Oldfield S, O’Donovan MC, Lightman SL, Owen MJ. Screening ABCG1, the human homologue of the Drosophila white gene, for polymorphisms and association with bipolar affective disorder. Molecular Psychiatry 2001; 6: 671–677
  • Klein I, Sarkadi B, Varadi A. An inventory of the human ABC proteins. Biochimica et Biophysica Acta 1999; 1461: 237–262
  • Klucken J, Buchler C, Orso E, Kaminski WE, Porsch-Ozcurumez M, Liebisch G, Kapinsky M, Diederich W, Drobnik W, Dean M, et al. ABCG1 (ABC8), the human homolog of the Drosophila white gene, is a regulator of macrophage cholesterol and phospholipid transport. Proceedings of the National Academy of Sciences, USA 2000; 97: 817–822
  • Kobayashi D, Ieiri I, Hirota T, Takane H, Maegawa S, Kigawa J, Suzuki H, Nanba E, Oshimura M, Terakawa N, et al. Functional assessment of ABCG2 (BCRP) gene polymorphisms to protein expression in human placenta. Drug Metabolism and Disposition 2005; 33: 94–101
  • Kool M, De Haas M, Scheffer GL, Scheper RJ, Van Eijk MJ, Juijn JA, Baas F, Borst P. Analysis of expression of cMOAT (MRP2), MRP3, MRP4, and MRP5, homologues of the multidrug resistance-associated protein gene (MRP1), in human cancer cell lines. Cancer Research 1997; 57: 3537–3547
  • Koshiba S, Ito T, Shiota A, Wakabayashi K, Ueda M, Ichinose H, Ishikawa T. Development of polyclonal antibodies specific to ATP-binding cassette transporters human ABCG4 and mouse Abcg4: site-specific expression of mouse Abcg4 in brain. Journal of Experimental Therapeutics and Oncology 2007; 6: 321–333
  • Krasnovsky Jr AA, Neverov KV, Egorov S, Roeder B, Levald T. Photophysical studies of pheophorbide a and pheophytin a. Phosphorescence and photosensitized singlet oxygen luminescence. Journal of Photochemistry and Photobiology B 1990; 5: 245–254
  • Krishnamurthy P, Ross DD, Nakanishi T, Bailey-Dell K, Zhou S, Mercer KE, Sarkadi B, Sorrentino BP, Schuetz JD. The stem cell marker Bcrp/ABCG2 enhances hypoxic cell survival through interactions with heme. Journal of Biological Chemistry 2004; 279: 24218–24225
  • Kyte J, Doolittle RF. A simple method for displaying the hydropathic character of a protein. Journal of Molecular Biology 1982; 157: 105–132
  • Litman T, Jensen U, Hansen A, Covitz KM, Zhan Z, Fetsch P, Abati A, Hansen PR, Horn T, Skovsgaard T, et al. Use of peptide antibodies to probe for the mitoxantrone resistance-associated protein MXR/BCRP/ABCP/ABCG2. Biochimica et Biophysica Acta 2002; 1565: 6–16
  • Loscher W, Potschka H. Role of drug efflux transporters in the brain for drug disposition and treatment of brain diseases. Progress in Neurobiology 2005; 76: 22–76
  • Ma Y, Hendershot LM. ER chaperone functions during normal and stress conditions. Journal of Chemical Neuroanatomy 2004; 28: 51–65
  • Mayer U, Wagenaar E, Beijnen JH, Smit JW, Meijer DK, Van Asperen J, Borst P, Schinkel AH. Substantial excretion of digoxin via the intestinal mucosa and prevention of long-term digoxin accumulation in the brain by the mdr 1a P-glycoprotein. British Journal of Pharmacology 1996; 119: 1038–1044
  • Meister A, Anderson ME. Glutathione. Annual Review of Biochemistry 1983; 52: 711–760
  • Millard TP, Hawk JL. Photosensitivity disorders: Cause, effect and management. American Journal of Clinical Dermatology 2002; 3: 239–246
  • Millard TP, Kirk A, Ratnavel R. Cutaneous hyperpigmentation during therapy with hydroxychloroquine. Clinical and Experimental Dermatology 2004; 29: 92–93
  • Mitomo H, Kato R, Ito A, Kasamatsu S, Ikegami Y, Kii I, Kudo A, Kobatake E, Sumino Y, Ishikawa T. A functional study on polymorphism of the ATP-binding cassette transporter ABCG2: Critical role of arginine-482 in methotrexate transport. Biochemical Journal 2003; 373: 767–774
  • Miyake K, Mickley L, Litman T, Zhan Z, Robey R, Cristensen B, Brangi M, Greenberger L, Dean M, Fojo T, et al. Molecular cloning of cDNAs which are highly overexpressed in mitoxantrone-resistant cells: demonstration of homology to ABC transport genes. Cancer Research 1999; 59: 8–13
  • Molteni SN, Fassio A, Ciriolo MR, Filomeni G, Pasqualetto E, Fagioli C, Sitia R. Glutathione limits Ero1-dependent oxidation in the endoplasmic reticulum. Journal of Biological Chemistry 2004; 279: 32667–32673
  • Mori K. Tripartite management of unfolded proteins in the endoplasmic reticulum. Cell 2000; 101: 451–454
  • Mottino AD, Hoffman T, Jennes L, Vore M. Expression and localization of multidrug resistant protein mrp2 in rat small intestine. Journal of Pharmacology and Experimental Therapeutics 2000; 293: 717–723
  • Nakagawa H, Tamura A, Wakabayashi K, Hoshijima K, Komada M, Yoshida T, Kometani S, Matsubara T, Mikuriya K, Ishikawa T. Ubiquitin-mediated proteasomal degradation of non-synonymous SNP variants of human ABC transporter ABCG2. Biochemical Journal 2008; 411: 623–631
  • Nakatomi K, Yoshikawa M, Oka M, Ikegami Y, Hayasaka S, Sano K, Shiozawa K, Kawabata S, Soda H, Ishikawa T, et al. Transport of 7-ethyl-10-hydroxycamptothecin (SN-38) by breast cancer resistance protein ABCG2 in human lung cancer cells. Biochemical and Biophysical Research Communications 2001; 288: 827–832
  • Noble ME, Endicott JA, Johnson LN. Protein kinase inhibitors: insights into drug design from structure. Science 2004; 303: 1800–1805
  • O’Gorman S, Fox DT, Wahl GM. Recombinase-mediated gene activation and site-specific integration in mammalian cells. Science 1991; 251: 1351–1355
  • Okura I. Charactarization of porphyrins and phthalocyanines. Photosensitization of porphyrins and phthalocyanines, I Okura. Kodansha/Gordon & Breach, Tokyo 2000; 45–62
  • Özvegy-Laczka C, Hegedus T, Varady G, Ujhelly O, Schuetz JD, Varadi A, Keri G, Orfi L, Nemet K, Sarkadi B. High-affinity interaction of tyrosine kinase inhibitors with the ABCG2 multidrug transporter. Molecular Pharmacology 2004; 65: 1485–1495
  • Pirmohamed M. Pharmacogenetics and pharmacogenomics. British Journal of Clinical Pharmacology 2001; 52: 345–347
  • Puglielli L, Tanzi RE, Kovacs DM. Alzheimer's disease: The cholesterol connection. Nature Neuroscience 2003; 6: 345–351
  • Rao RV, Ellerby HM, Bredesen DE. Coupling endoplasmic reticulum stress to the cell death program. Cell Death and Differentiation 2004; 11: 372–380
  • Rao VV, Dahlheimer JL, Bardgett ME, Snyder AZ, Finch RA, Sartorelli AC, Piwnica-Worms D. Choroid plexus epithelial expression of MDR1 P glycoprotein and multidrug resistance-associated protein contribute to the blood–cerebrospinal-fluid drug-permeability barrier. Proceedings of the National Academy of Sciences, USA 1999; 96: 3900–3905
  • Reed DJ. Glutathione: Toxicological implications. Annual Review of Pharmacology and Toxicology 1990; 30: 603–631
  • Robey RW, Steadman K, Polgar O, Bates SE. ABCG2-mediated transport of photosensitizers: potential impact on photodynamic therapy. Cancer Biological Therapy 2005; 4: 187–194
  • Saito H, Hirano H, Nakagawa H, Fukami T, Oosumi K, Murakami K, Kimura H, Kouchi T, Konomi M, Tao E, et al. A new strategy of high-speed screening and quantitative structure–activity relationship analysis to evaluate human ATP-binding cassette transporter ABCG2–drug interactions. Journal of Pharmacology and Experimental Therapeutics 2006; 317: 1114–1124
  • Sakurai A, Onishi Y, Hirano H, Seigneuret M, Obanayama K, Kim G, Liew EL, Sakaeda T, Yoshiura K, Niikawa N, et al. Quantitative structure–activity relationship analysis and molecular dynamics simulation to functionally validate nonsynonymous polymorphisms of human ABC transporter ABCB1 (P-glycoprotein/MDR1). Biochemistry 2007; 46: 7678–7693
  • Sakurai A, Tamura A, Onishi Y, Ishikawa T. Genetic polymorphisms of ATP-binding cassette transporters ABCB1 and ABCG2: therapeutic implications. Expert Opinion on Pharmacotherapy 2005; 6: 2455–2473
  • Sarkadi B, Özvegy-Laczka C, Nemet K, Varadi A. ABCG2–a transporter for all seasons. FEBS Letters 2004; 567: 116–120
  • Sauer B. Site-specific recombination: Developments and applications. Current Opinion in Biotechnology 1994; 5: 521–527
  • Schinkel AH, Jonker JW. Mammalian drug efflux transporters of the ATP binding cassette (ABC) family: An overview. Advanced Drug Delivery Reviews 2003; 55: 3–29
  • Schinkel AH, Smit JJ, Van Tellingen O, Beijnen JH, Wagenaar E, Van Deemter L, Molecular CA, Van der Valk MA, Robanus-Maandag EC, Te Riele HP, et al. Disruption of the mouse mdr1a P-glycoprotein gene leads to a deficiency in the blood–brain barrier and to increased sensitivity to drugs. Cell 1994; 77: 491–502
  • Schinkel AH, Wagenaar E, Molecular CA, Van Deemter L. P-glycoprotein in the blood–brain barrier of mice influences the brain penetration and pharmacological activity of many drugs. Journal of Clinical Investigation 1996; 97: 2517–2524
  • Schroder M, Kaufman RJ. ER stress and the unfolded protein response. Mutation Research 2005; 569: 29–63
  • Sesink AL, Arts IC, De Boer VC, Breedveld P, Schellens JH, Hollman PC, Russel FG. Breast cancer resistance protein (Bcrp1/Abcg2) limits net intestinal uptake of quercetin in rats by facilitating apical efflux of glucuronides. Molecular Pharmacology 2005; 67: 1999–2006
  • Shen X, Zhang K, Kaufman RJ. The unfolded protein response–a stress signaling pathway of the endoplasmic reticulum. Journal of Chemical Neuroanatomy 2004; 28: 79–92
  • Sies H, Menck CF. Singlet oxygen induced DNA damage. Mutation Research 1992; 275: 367–375
  • Sparreboom A, Van Asperen J, Mayer U, Schinkel AH, Smit JW, Meijer DK, Borst P, Nooijen WJ, Beijnen JH, Van Tellingen O. Limited oral bioavailability and active epithelial excretion of paclitaxel (Taxol) caused by P-glycoprotein in the intestine. Proceedings of the National Academy of Sciences, USA 1997; 94: 2031–2035
  • Stewart CF, Leggas M, Schuetz JD, Panetta JC, Cheshire PJ, Peterson J, Daw N, Jenkins JJ, III, Gilbertson R, Germain GS, et al. Gefitinib enhances the antitumor activity and oral bioavailability of irinotecan in mice. Cancer Research 2004; 64: 7491–7499
  • Tachikawa M, Watanabe M, Hori S, Fukaya M, Ohtsuki S, Asashima T, Terasaki T. Distinct spatio-temporal expression of ABCA and ABCG transporters in the developing and adult mouse brain. Journal of Neurochemistry 2005; 95: 294–304
  • Tamura A, Onishi Y, An R, Koshiba S, Wakabayashi K, Hoshijima K, Priebe W, Yoshida T, Kometani S, Matsubara T, et al. In vitro evaluation of photosensitivity risk related to genetic polymorphisms of human ABC transporter ABCG2 and inhibition by drugs. Drug Metabolism and Pharmacokinetics 2007; 22: 428–440
  • Tamura A, Watanabe M, Saito H, Nakagawa H, Kamachi T, Okura I, Ishikawa T. Functional validation of the genetic polymorphisms of human ATP-binding cassette (ABC) transporter ABCG2: Identification of alleles that are defective in porphyrin transport. Molecular Pharmacology 2006; 70: 287–296
  • Tansley GH, Burgess BL, Bryan MT, Su Y, Hirsch-Reinshagen V, Pearce J, Chan JY, Wilkinson A, Evans J, Naus KE, et al. The cholesterol transporter ABCG1 modulates the subcellular distribution and proteolytic processing of beta-amyloid precursor protein. Journal of Lipid Research 2007; 48: 1022–1034
  • Tarr PT, Edwards PA. ABCG1 and ABCG4 are coexpressed in neurons and astrocytes of the CNS and regulate cholesterol homeostasis through SREBP-2. Journal of Lipid Research 2008; 49: 169–182
  • Taylor JG, Choi EH, Foster CB, Chanock SJ. Using genetic variation to study human disease. Trends in Molecular Medicine 2001; 7: 507–512
  • Thiebaut F, Tsuruo T, Hamada H, Gottesman MM, Pastan I, Willingham MC. Cellular localization of the multidrug-resistance gene product P-glycoprotein in normal human tissues. Proceedings of the National Academy of Sciences, USA 1987; 84: 7735–7738
  • Tu BP, Weissman JS. Oxidative protein folding in eukaryotes: Mechanisms and consequences. Journal of Cell Biology 2004; 164: 341–346
  • Van Herwaarden AE, Schinkel AH. The function of breast cancer resistance protein in epithelial barriers, stem cells and milk secretion of drugs and xenotoxins. Trends in Pharmacological Sciences 2006; 27: 10–16
  • Vance JE, Hayashi H, Karten B. Cholesterol homeostasis in neurons and glial cells. Seminars in Cell and Developmental Biology 2005; 16: 193–212
  • Varadi A, Tusnady GE, Sarkadi B. Membrane topology the human ABC transporter proteins. ABC proteins: From bacteria to man, IB Holland, SPC Cole, K Kuchler, CF Higgins. Academic Press, London 2003; 37–46
  • Volk EL, Schneider E. Wild-type breast cancer resistance protein (BCRP/ABCG2) is a methotrexate polyglutamate transporter. Cancer Research 2003; 63: 5538–5543
  • Wakabayashi K, Nakagawa H, Adachi T, Kii I, Kobatake E, Kudo A, Ishikawa T. Identification of cysteine residues critically involved in homodimer formation and protein expression of human ATP-binding cassette transporter ABCG2: A new approach using the flp recombinase system. Journal of Experimental Therapeutics and Oncology 2006; 5: 205–222
  • Wakabayashi K, Nakagawa H, Tamura A, Koshiba S, Hoshijima K, Komada M, Ishikawa T. Intramolecular disulfide bond is a critical check point determining degradative fates of ATP-binding cassette (ABC) transporter ABCG2 protein. Journal of Biological Chemistry 2007; 282: 27841–27846
  • Wang N, Lan D, Chen W, Matsuura F, Tall AR. ATP-binding cassette transporters G1 and G4 mediate cellular cholesterol efflux to high-density lipoproteins. Proceedings of the National Academy of Sciences, USA 2004; 101: 9774–9779
  • Wirth D, Hauser H. Flp-mediated integration of expression cassettes into FRT-tagged chromosomal loci in mammalian cells. Methods in Molecular Biology 2004; 267: 467–476
  • Xu C, Bailly-Maitre B, Reed JC. Endoplasmic reticulum stress: cell life and death decisions. Journal of Clinical Investigation 2005; 115: 2656–2664
  • Yanase K, Tsukahara S, Asada S, Ishikawa E, Imai Y, Sugimoto Y. Gefitinib reverses breast cancer resistance protein-mediated drug resistance. Molecular Cancer Therapeutics 2004; 3: 1119–1125
  • Ye Y, Shibata Y, Kikkert M, Van Voorden S, Wiertz E, Rapoport TA. Inaugural Article: Recruitment of the p97 ATPase and ubiquitin ligases to the site of retrotranslocation at the endoplasmic reticulum membrane. Proceedings of the National Academy of Sciences, USA 2005; 102: 14132–14138
  • Yoshikawa M, Ikegami Y, Hayasaka S, Ishii K, Ito A, Sano K, Suzuki T, Togawa T, Yoshida H, Soda H, et al. Novel camptothecin analogues that circumvent ABCG2-associated drug resistance in human tumor cells. International Journal of Cancer 2004a; 110: 921–927
  • Yoshikawa M, Ikegami Y, Sano K, Yoshida H, Mitomo H, Sawada S, Ishikawa T. Transport of SN-38 by the wild-type of human ABC transporter ABCG2 and its inhibition by quercetin, a natural flavonoid. Journal of Experimental Therapeutics and Oncology 2004b; 4: 25–35
  • Yoshikawa M, Yabuuchi H, Kuroiwa A, Ikegami Y, Sai Y, Tamai I, Tsuji A, Matsuda Y, Yoshida H, Ishikawa T. Molecular and cytogenetic characterization of the mouse ATP-binding cassette transporter Abcg4. Gene 2002; 293: 67–75
  • Zamber CP, Lamba JK, Yasuda K, Farnum J, Thummel K, Schuetz JD, Schuetz EG. Natural allelic variants of breast cancer resistance protein (BCRP) and their relationship to BCRP expression in human intestine. Pharmacogenetics 2003; 13: 19–28
  • Zhang S, Yang X, Morris ME. Combined effects of multiple flavonoids on breast cancer resistance protein (ABCG2)-mediated transport. Pharmaceutical Research 2004; 21: 1263–1273
  • Zhou S, Morris JJ, Barnes Y, Lan L, Schuetz JD, Sorrentino BP. 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. Proceedings of the National Academy of Sciences, USA 2002; 99: 12339–12344
  • Zhou S, Schuetz JD, Bunting KD, Colapietro AM, Sampath J, Morris JJ, Lagutina I, Grosveld GC, Osawa M, Nakauchi H, et al. The ABC transporter Bcrp1/ABCG2 is expressed in a wide variety of stem cells and is a molecular determinant of the side-population phenotype. Nature Medicine 2001; 7: 1028–1034
  • Zhou S, Zong Y, Ney PA, Nair G, Stewart CF, Sorrentino BP. Increased expression of the Abcg2 transporter during erythroid maturation plays a role in decreasing cellular protoporphyrin IX levels. Blood 2005; 105: 2571–2576

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.