• 1
    Borst P, Elferink R. Mammalian ABC transporters in health and disease. Annu Rev Biochem 2002; 71: 53792.
  • 2
    Haimeur A, Conseil G, Deeley RG, Cole SP. The MRP-related and BCRP/ABCG2 multidrug resistance proteins: biology, substrate specificity and regulation. Curr Drug Metab 2004; 5: 2153.
  • 3
    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: 16504.
  • 4
    Rosenberg MF, Mao Q, Holzenburg A, Ford RC, Deeley RG, Cole SP. The structure of the multidrug resistance protein 1 (MRP1/ABCC1). crystallization and single-particle analysis. J Biol Chem 2001; 276: 1607682.
  • 5
    Doyle LA, Ross DD. Multidrug resistance mediated by the breast cancer resistance protein BCRP (ABCG2). Oncogene 2003; 22: 734058.
  • 6
    Ambudkar SV, Kimchi-Sarfaty C, Sauna ZE, Gottesman MM. P-glycoprotein: from genomics to mechanism. Oncogene 2003; 22: 746885.
  • 7
    Gottesman MM, Fojo T, Bates SE. Multidrug resistance in cancer: role of ATP-dependent transporters. Nat Rev Cancer 2002; 2: 4858.
  • 8
    Leonard GD, Fojo T, Bates SE. The role of ABC transporters in clinical practice. Oncologist 2003; 8: 41124.
  • 9
    Nakanishi T, Karp JE, Tan M, Doyle LA, Peters T, Yang W, Wei D, Ross DD. Quantitative analysis of breast cancer resistance protein and cellular resistance to flavopiridol in acute leukemia patients. Clin Cancer Res 2003; 9: 33208.
  • 10
    Niv R, Assaraf YG, Segal D, Pirak E, Reiter Y. Targeting multidrug resistant tumor cells with a recombinant single-chain FV fragment directed to P-glycoprotein. Int J Cancer 2001; 94: 86472.
  • 11
    Haus-Cohen M, Assaraf YG, Binyamin L, Benhar I, Reiter Y. Disruption of P-glycoprotein anticancer drug efflux activity by a small recombinant single-chain Fv antibody fragment targeted to an extracellular epitope. Int J Cancer 2004; 109: 7508.
  • 12
    Binyamin L, Assaraf YG, Haus-Cohen M, Stark M, Reiter Y. Targeting an extracellular epitope of the human multidrug resistance protein 1 (MRP1) in malignant cells with a novel recombinant single chain Fv antibody. Int J Cancer 2004; 110: 88290.
  • 13
    Zijlstra JG, de Vries EG, Muskiet FA, Martini IA, Timmer-Bosscha H, Mulder NH. Influence of docosahexaenoic acid in vitro on intracellular adriamycin concentration in lymphocytes and human adriamycin-sensitive and -resistant small-cell lung cancer cell lines, and on cytotoxicity in the tumor cell lines. Int J Cancer 1987; 40: 8506.
  • 14
    Assaraf YG, Slotky JI. Characterization of a lipophilic antifolate resistance provoked by treatment of mammalian cells with the antiparasitic agent pyrimethamine. J Biol Chem 1993; 268: 455666.
  • 15
    Stark M, Rothem L, Jansen G, Scheffer GL, Goldman ID, Assaraf YG. Antifolate resistance associated with loss of MRP1 expression and function in Chinese hamster ovary cells with markedly impaired export of folate and cholate. Mol Pharmacol 2003; 64: 2207.
  • 16
    Brinkmann U, Pai LH, FitzGerald DJ, Willingham M, Pastan I. B3(Fv)-PE38KDEL, a single-chain immunotoxin that causes complete regression of a human carcinoma in mice. Proc Natl Acad Sci USA 1991; 88: 861620.
  • 17
    Cohen CJ, Denkberg G, Segal D, Reiter Y. Generation of recombinant immunotoxins for specific targeting of tumor-related peptides presented by MHC molecules. Methods Mol Biol 2003; 207: 26982.
  • 18
    Buchner J, Pastan I, Brinkmann U. A method for increasing the yield of properly folded recombinant fusion proteins: single-chain immunotoxins from renaturation of bacterial inclusion bodies. Anal Biochem 1992; 205: 26370.
  • 19
    Hollo Z, Homolya L, Hegedus T, Muller M, Szakacs G, Jakab K, Antal F, Sarkadi B. Parallel functional and immunological detection of human multidrug resistance proteins, P-glycoprotein and MRP1. Anticancer Res 1998; 18: 29817.
  • 20
    Mechetner EB, Schott B, Morse BS, Stein WD, Druley T, Davis KA, Tsuruo T, Roninson IB. P-glycoprotein function involves conformational transitions detectable by differential immunoreactivity. Proc Natl Acad Sci USA 1997; 94: 1290813.
  • 21
    Goda K, Nagy H, Mechetner E, Cianfriglia M, Szabo GJr. Effects of ATP depletion and phosphate analogues on P-glycoprotein conformation in live cells. Eur J Biochem 2002; 269: 26727.
  • 22
    Drori S, Eytan GD, Assaraf YG. Potentiation of anticancer-drug cytotoxicity by multidrug-resistance chemosensitizers involves alterations in membrane fluidity leading to increased membrane permeability. Eur J Biochem 1995; 228: 10209.
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  • 23
    Bakos E, Hegedus T, Hollo Z, Welker E, Tusnady GE, Zaman GJ, Flens MJ, Varadi A, Sarkadi B. Altered drug-stimulated ATPase activity in mutants of the human multidrug resistance protein. J Biol Chem 1996; 271: 123226.
  • 24
    Hipfner DR, Almquist KC, Leslie EM, Gerlach JH, Grant CE, Deeley RG, Cole SP. Membrane topology of the multidrug resistance protein (MRP): a study of glycosylation-site mutants reveals an extracytosolic NH2 terminus. J Biol Chem 1997; 272: 2362330.
  • 25
    Kast C, Gros P. Topology mapping of the amino-terminal half of multidrug resistance-associated protein by epitope insertion and immunofluorescence. J Biol Chem 1997; 272: 2647987.
  • 26
    Muller M, Yong M, Peng XH, Petre B, Arora S, Ambudkar SV. Evidence for the role of glycosylation in accessibility of the extracellular domains of human MRP1 (ABCC1). Biochemistry 2002; 41: 1012332.
  • 27
    Chen Q, Yang YY, Liu Y, Han BG, Zhang JT. Cytoplasmic retraction of the amino terminus of human multidrug resistance protein 1. Biochemistry 2002; 41: 905262.
  • 28
    Jain RK. Delivery of molecular medicine to solid tumors. Science 1996; 271: 107980.
  • 29
    Adams GP, Shaller CC, Chappell LL, Wu C, Horak EM, Simmons HH, Litwin S, Marks JD, Weiner LM, Brechbiel MW. Delivery of the alpha-emitting radioisotope bismuth-213 to solid tumors via single-chain Fv and diabody molecules. Nucl Med Biol 2000; 27: 33946.
  • 30
    Adams GP, Schier R, McCall AM, Simmons HH, Horak EM, Alpaugh RK, Marks JD, Weiner LM. High affinity restricts the localization and tumor penetration of single-chain fv antibody molecules. Cancer Res 2001; 61: 47505.
  • 31
    Adams GP, Weiner LM. Radioimmunotherapy of solid tumors: from fairytale to reality. Cancer Biother Radiopharm 2001; 16: 911.
  • 32
    Manciu L, Chang XB, Riordan JR, Ruysschaert JM. Multidrug resistance protein MRP1 reconstituted into lipid vesicles: secondary structure and nucleotide-induced tertiary structure changes. Biochemistry 2000; 39: 1302633.
  • 33
    Manciu L, Chang XB, Buyse F, Hou YX, Gustot A, Riordan JR, Ruysschaert JM. Intermediate structural states involved in MRP1-mediated drug transport. Role of glutathione. J Biol Chem 2003; 278: 334756.
  • 34
    Kern A, Szentpetery Z, Liliom K, Bakos E, Sarkadi B, Varadi A. Nucleotides and transported substrates modulate different steps of the ATPase catalytic cycle of MRP1 multidrug transporter. Biochem J 2004; 380: 54960.
  • 35
    Mechetner EB, Roninson IB. Efficient inhibition of P-glycoprotein-mediated multidrug resistance with a monoclonal antibody. Proc Natl Acad Sci USA 1992; 89: 58248.
  • 36
    Druley TE, Stein WD, Roninson IB. Analysis of MDR1 P-glycoprotein conformational changes in permeabilized cells using differential immunoreactivity. Biochemistry 2001; 40: 431222.
  • 37
    Borgnia MJ, Eytan GD, Assaraf YG. Competition of hydrophobic peptides, cytotoxic drugs, and chemosensitizers on a common P-glycoprotein pharmacophore as revealed by its ATPase activity. J Biol Chem 1996; 271: 316371.
  • 38
    Altenberg GA. Structure of multidrug-resistance proteins of the ATP-binding cassette (ABC) superfamily. Curr Med Chem Anti-Cancer Agents 2004; 4: 5362.
  • 39
    Regev R, Assaraf YG, Eytan GD. Membrane fluidization by ether, other anesthetics, and certain agents abolishes P-glycoprotein ATPase activity and modulates efflux from multidrug-resistant cells. Eur J Biochem 1999; 259: 1824.