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Review

Development of inhibitors of ATP-binding cassette drug transporters – present status and challenges

, PhD (Postdoctoral Fellow) , , PhD (Postdoctoral Fellow) & , PhD (Senior Investigator & Chief, Transport Biochemistry Section)
Pages 205-223 | Published online: 05 Feb 2008

Bibliography

  • Riordan JR, Rommens JM, Kerem B, et al. Identification of the cystic fibrosis gene: cloning and characterization of complementary DNA. Science 1989;245(4922):1066-73
  • Inagaki N, Tsuura Y, Namba N, et al. Cloning and functional characterization of a novel ATP-sensitive potassium channel ubiquitously expressed in rat tissues, including pancreatic islets, pituitary, skeletal muscle, and heart. J Biol Chem 1995;270(11):5691-4
  • Inagaki N, Gonoi T, Clement JP, et al. A family of sulfonylurea receptors determines the pharmacological properties of ATP-sensitive K+ channels. Neuron 1996;16(5):1011-7
  • Szakacs G, Paterson JK, Ludwig JA, Booth-Genthe C, Gottesman MM. Targeting multidrug resistance in cancer. Nat Rev Drug Discov 2006;5(3):219-34
  • Juliano RL, Ling V. A surface glycoprotein modulating drug permeability in Chinese hamster ovary cell mutants. Biochim Biophys Acta 1976;455(1):152-62
  • Schinkel AH. P-glycoprotein, a gatekeeper in the blood–brain barrier. Adv Drug Deliv Rev 1999;36(2-3):179-94
  • Sparreboom A, Van Asperen J, Mayer U, et al. Limited oral bioavailability and active epithelial excretion of paclitaxel (Taxol) caused by P-glycoprotein in the intestine. Proc Natl Acad Sci USA 1997;94(5):2031-5
  • Drach J, Gsur A, Hamilton G, et al. Involvement of P-glycoprotein in the transmembrane transport of interleukin-2 (IL-2), IL-4, and interferon-gamma in normal human T lymphocytes. Blood 1996;88(5):1747-54
  • Johnstone RW, Ruefli AA, Tainton KM, Smyth MJ. A role for P-glycoprotein in regulating cell death. Leuk Lymphoma 2000;38(1-2):1-11
  • Randolph GJ, Beaulieu S, Pope M, et al. A physiologic function for P-glycoprotein (MDR-1) during the migration of dendritic cells from skin via afferent lymphatic vessels. Proc Natl Acad Sci USA 1998;95(12):6924-9
  • Cole SP, Bhardwaj G, Gerlach JH, et al. Overexpression of a transporter gene in a multidrug-resistant human lung cancer cell line [see comments]. Science 1992;258(5088):1650-4
  • Loe DW, Almquist KC, Deeley RG, Cole SP. Multidrug resistance protein (MRP)-mediated transport of leukotriene C4 and chemotherapeutic agents in membrane vesicles. Demonstration of glutathione-dependent vincristine transport. J Biol Chem 1996;271(16):9675-82
  • Renes J, De Vries EGE, Nienhuis EF, Jansen PLM, Muller M. ATP- and glutathione-dependent transport of chemotherapeutic drugs by the multidrug resistance protein MRP1. Br J Pharmacol 1999;126(3):681-8
  • Hirrlinger J, Konig J, Keppler D, et al. The multidrug resistance protein MRP1 mediates the release of glutathione disulfide from rat astrocytes during oxidative stress. J Neurochem 2001;76(2):627-36
  • Wijnholds J, Evers R, Van Leusden MR, et al. Increased sensitivity to anticancer drugs and decreased inflammatory response in mice lacking the multidrug resistance-associated protein. Nat Med 1997;3(11):1275-9
  • Evers R, Zaman GJ, Van Deemter L, et al. Basolateral localization and export activity of the human multidrug resistance-associated protein in polarized pig kidney cells. J Clin Invest 1996;97(5):1211-8
  • Wijnholds J, Scheffer GL, Van Der Valk M, et al. Multidrug resistance protein 1 protects the oropharyngeal mucosal layer and the testicular tubules against drug-induced damage. J Exp Med 1998;188(5):797-808
  • Wijnholds J, Delange EC, Scheffer GL, et al. Multidrug resistance protein 1 protects the choroid plexus epithelium and contributes to the blood–cerebrospinal fluid barrier. J Clin Invest 2000;105(3):279-85
  • 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 Res 1998;58(23):5337-9
  • Doyle LA, Yang W, Abruzzo LV, et al. A multidrug resistance transporter from human MCF-7 breast cancer cells. Proc Natl Acad Sci USA 1998;95(26):15665-70
  • Miyake K, Mickley L, Litman T, et al. Molecular cloning of cDNAs which are highly overexpressed in mitoxantrone-resistant cells: demonstration of homology to ABC transport genes. Cancer Res 1999;59(1):8-13
  • Maliepaard M, Van Gastelen MA, Tohgo A, et al. Circumvention of breast cancer resistance protein (BCRP)-mediated resistance to camptothecins in vitro using non-substrate drugs or the BCRP inhibitor GF120918. Clin Cancer Res 2001;7(4):935-41
  • Cooray HC, Blackmore CG, Maskell L, Barrand MA. Localisation of breast cancer resistance protein in microvessel endothelium of human brain. Neuroreport 2002;13(16):2059-63
  • Mao Q, Unadkat JD. Role of the breast cancer resistance protein (ABCG2) in drug transport. AAPS J 2005;7(1):E118-33
  • Ifergan I, Shafran A, Jansen G, et al. Folate deprivation results in the loss of breast cancer resistance protein (BCRP/ABCG2) expression. A role for BCRP in cellular folate homeostasis. J Biol Chem 2004;279(24):25527-34
  • Krishnamurthy P, Ross DD, Nakanishi T, et al. The stem cell marker Bcrp/ABCG2 enhances hypoxic cell survival through interactions with heme. J Biol Chem 2004;279(23):24218-25
  • Mizuno N, Suzuki M, Kusuhara H, et al. 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 2004;32(9):898-901
  • Van Herwaarden AE, Jonker JW, Wagenaar E, et al. 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 2003;63(19):6447-52
  • Bunting KD. ABC transporters as phenotypic markers and functional regulators of stem cells. Stem Cells 2002;20(1):11-20
  • Sarkadi B, Homolya L, Szakacs G, Varadi A. Human multidrug resistance ABCB and ABCG transporters: participation in a chemoimmunity defense system. Physiol Rev 2006;86(4):1179-236
  • Loe DW, Deeley RG, Cole SP. Biology of the multidrug resistance-associated protein, MRP. Eur J Cancer 1996;32A(6):945-57
  • Hipfner DR, Deeley RG, Cole SP. Structural, mechanistic and clinical aspects of MRP1. Biochim Biophys Acta 1999;1461(2):359-76
  • Allen JD, Brinkhuis RF, Van Deemter L, Wijnholds J, Schinkel AH. Extensive contribution of the multidrug transporters P-glycoprotein and Mrp1 to basal drug resistance. Cancer Res 2000;60(20):5761-6
  • Johnson DR, Finch RA, Lin ZP, Zeiss CJ, Sartorelli AC. The pharmacological phenotype of combined multidrug-resistance mdr1a/1b- and mrp1-deficient mice. Cancer Res 2001;61(4):1469-76
  • Loe DW, Deeley RG, Cole SP. Characterization of vincristine transport by the M(r) 190,000 multidrug resistance protein (MRP): evidence for cotransport with reduced glutathione. Cancer Res 1998;58(22):5130-6
  • Doyle LA, Yang W, Abruzzo LV, et al. A multidrug resistance transporter from human MCF-7 breast cancer cells. Proc Natl Acad Sci USA 1998;95(26):15665-70
  • Krishnamurthy P, Schuetz JD. Role of ABCG2/BCRP in biology and medicine. Ann Rev Pharmacol Toxicol 2006;46:381-410
  • Jonker JW, Merino G, Musters S, et al. The breast cancer resistance protein BCRP (ABCG2) concentrates drugs and carcinogenic xenotoxins into milk. Nat Med 2005;11(2):127-9
  • Van Herwaarden AE, Wagenaar E, Merino G, et al. Multidrug transporter ABCG2/breast cancer resistance protein secretes riboflavin (vitamin B2) into milk. Mol Cell Biol 2007;27(4):1247-53
  • Takara K, Sakaeda T, Okumura K. An update on overcoming MDR1-mediated multidrug resistance in cancer chemotherapy. Curr Pharm Des 2006;12(3):273-86
  • Tsuruo T, Iida H, Tsukagoshi S, Sakurai Y. Overcoming of vincristine resistance in P388 leukemia in vivo and in vitro through enhanced cytotoxicity of vincristine and vinblastine by verapamil. Cancer Res 1981;41(5):1967-72
  • Slater L, Sweet P, Wetzel M, Stupecky M, Osann K. Comparison of cyclosporin A, verapamil, PSC-833 and cremophor EL as enhancing agents of VP-16 in murine lymphoid leukemias. Leuk Res 1995;19(8):543-8
  • Twentyman PR, Fox NE, White DJ. Cyclosporin A and its analogues as modifiers of adriamycin and vincristine resistance in a multi-drug resistant human lung cancer cell line. Br J Cancer 1987;56:55-7
  • Pawarode A, Shukla S, Minderman H, et al. Differential effects of the immunosuppressive agents cyclosporin A, tacrolimus and sirolimus on drug transport by multidrug resistance proteins. Cancer Chemother Pharmacol 2007;60(2):179-88
  • Gupta A, Dai Y, Vethanayagam RR, et al. Cyclosporin A, tacrolimus and sirolimus are potent inhibitors of the human breast cancer resistance protein (ABCG2) and reverse resistance to mitoxantrone and topotecan. Cancer Chemother Pharmacol 2006;58(3):374-83
  • Boesch D, Gaveriaux C, Jachez B, et al. In vivo circumvention of P-glycoprotein-mediated multidrug resistance of tumor cells with SDZ PSC 833. Cancer Res 1991;51(16):4226-33
  • Gekeler V, Ise W, Sanders KH, Ulrich WR, Beck J. The leukotriene LTD4 receptor antagonist MK571 specifically modulates MRP associated multidrug resistance. Biochem Biophys Res Commun 1995;208:345-52
  • Wu CP, Klokouzas A, Hladky SB, Ambudkar SV, Barrand MA. Interactions of mefloquine with ABC proteins, MRP1 (ABCC1) and MRP4 (ABCC4) that are present in human red cell membranes. Biochem Pharmacol 2005;70(4):500-10
  • Bakos E, Evers R, Sinko E, et al. Interactions of the human multidrug resistance proteins MRP1 and MRP2 with organic anions. Mol Pharmacol 2000;57(4):760-8
  • Rabindran SK, Ross DD, Doyle LA, Yang W, Greenberger LM. Fumitremorgin C reverses multidrug resistance in cells transfected with the breast cancer resistance protein. Cancer Res. (2000) 60(1):47-50
  • Allen JD, Van Loevezijn A, Lakhai JM, et al. Potent and specific inhibition of the breast cancer resistance protein multidrug transporter in vitro and in mouse intestine by a novel analogue of fumitremorgin C. Mol Cancer Ther 2002;1(6):417-25
  • Chearwae W, Anuchapreeda S, Nandigama K, Ambudkar SV, Limtrakul P. Biochemical mechanism of modulation of human P-glycoprotein (ABCB1) by curcumin I, II, and III purified from turmeric powder. Biochem Pharmacol 2004;68(10):2043-52
  • Chearwae W, Shukla S, Limtrakul P, Ambudkar SV. Modulation of the function of the multidrug resistance-linked ATP-binding cassette transporter ABCG2 by the cancer chemopreventive agent curcumin. Mol Cancer Ther 2006;5(8):1995-2006
  • Chearwae W, Wu C-P, Chu H, et al. Curcuminoids purified from turmeric powder modulate the function of human multidrug resistance protein 1 (ABCC1). Cancer Chemother Pharmacol 2006;57(3):376-88
  • Limtrakul P, Chearwae W, Shukla S, Phisalphong C, Ambudkar SV. Modulation of function of three ABC drug transporters, P-glycoprotein (ABCB1), mitoxantrone resistance protein (ABCG2) and multidrug resistance protein 1 (ABCC1) by tetrahydrocurcumin, a major metabolite of curcumin. Mol Cell Biochem 2007:296(1-2):85-95
  • Li L, Ahmed B, Mehta K, Kurzrock R. Liposomal curcumin with and without oxaliplatin: effects on cell growth, apoptosis, and angiogenesis in colorectal cancer. Mol Cancer Ther 2007;6(4):1276-82
  • Lan Li, Braiteh KS, Kurzrock R. Liposome-encapsulated curcumin. Cancer 2005;104(6):1322-31
  • Aggarwal BB, Kumar A, Bharti AC. Anticancer potential of curcumin: preclinical and clinical studies. Anticancer Res 2003;23(1A):363-98
  • Friedenberg WR, Rue M, Blood EA, et al. Phase III study of PSC-833 (valspodar) in combination with vincristine, doxorubicin, and dexamethasone (valspodar/VAD) versus VAD alone in patients with recurring or refractory multiple myeloma (E1A95): a trial of the Eastern Cooperative Oncology Group. Cancer 2006;106(4):830-8
  • Saeki T, Nomizu T, Toi M, et al. Dofequidar fumarate (MS-209) in combination with cyclophosphamide, doxorubicin, and fluorouracil for patients with advanced or recurrent breast cancer. J Clin Oncol 2007;25(4):411-7
  • Peck RA, Hewett J, Harding MW, et al. Phase I and pharmacokinetic study of the novel MDR1 and MRP1 inhibitor biricodar administered alone and in combination with doxorubicin. J Clin Oncol 2001;19(12):3130-41
  • Von Pawel J, Schiller JH, Shepherd FA, et al. Topotecan versus cyclophosphamide, doxorubicin, and vincristine for the treatment of recurrent small-cell lung cancer. J Clin Oncol 1999;17(2):658-67
  • Gandhi L, Harding MW, Neubauer M, et al. A Phase II study of the safety and efficacy of the multidrug resistance inhibitor VX-710 combined with doxorubicin and vincristine in patients with recurrent small cell lung cancer. Cancer 2007;109(5):924-32
  • Jonker JW, Smit JW, Brinkhuis RF, et al. Role of breast cancer resistance protein in the bioavailability and fetal penetration of topotecan. J Natl Cancer Inst 2000;92(20):1651-6
  • Kruijtzer CM, Beijnen JH, Rosing H, et al. Increased oral bioavailability of topotecan in combination with the breast cancer resistance protein and P-glycoprotein inhibitor GF120918. J Clin Oncol 2002;20(13):2943-50
  • Kuppens IELM, Witteveen EO, Jewell RC, et al. A Phase I, randomized, open-label, parallel-cohort, dose-finding study of elacridar (GF120918) and oral topotecan in cancer patients. Clin Cancer Res 2007;13(11):3276-85
  • Dantzig AH, Law KL, Cao J, Starling JJ. Reversal of multidrug resistance by the P-glycoprotein modulator, LY335979, from the bench to the clinic. Curr Med Chem 2001;8(1):39-50
  • Kemper EM, Cleypool C, Boogerd W, Beijnen J, Tellingen O. The influence of the P-glycoprotein inhibitor zosuquidar trihydrochloride (LY335979) on the brain penetration of paclitaxel in mice. Cancer Chemother Pharmacol 2004;53(2):173-8
  • Rubin EH, De Alwis DP, Pouliquen I, et al. A Phase I trial of a potent p-glycoprotein inhibitor, zosuquidar.3HCl trihydrochloride (LY335979), administered orally in combination with doxorubicin in patients with advanced malignancies. Clin Cancer Res 2002;8(12):3710-7
  • Gerrard G, Payne E, Baker RJ, et al. Clinical effects and P-glycoprotein inhibition in patients with acute myeloid leukemia treated with zosuquidar trihydrochloride, daunorubicin and cytarabine. Haematologica 2004;89(7):782-90
  • Morschhauser F, Zinzani PL, Burgess M, et al. Phase I/II trial of a P-glycoprotein inhibitor, Zosuquidar.3HCl trihydrochloride (LY335979), given orally in combination with the CHOP regimen in patients with non-Hodgkin's lymphoma. Leuk Lymphoma 2007;48(4):708-15
  • Martin C, Berridge G, Mistry P, et al. The molecular interaction of the high affinity reversal agent XR9576 with P-glycoprotein. Br J Pharmacol 1999;128(2):403-11
  • Mistry P, Stewart AJ, Dangerfield W, et al. In vitro and in vivo reversal of P-glycoprotein-mediated multidrug resistance by a novel potent modulator, XR9576. Cancer Res 2001;61(2):749-58
  • Robey RW, Steadman K, Polgar O, et al. Pheophorbide a is a specific probe for ABCG2 function and inhibition. Cancer Res 2004;64(4):1242-6
  • Abraham J, Edgerly M, Wilson R, et al. A Phase I study of the novel P-glycoprotein (Pgp) antagonist, XR9576 in combination with vinorelbine. Proc Am Soc Clin Oncol 2001;20:Abstract 287
  • Pusztai L, Wagner N, Ibrahim N, et al. Phase II study of tariquidar, a selective P-glycoprotein inhibitor, in patients with chemotherapy-resistant, advanced breast carcinoma. Cancer 2005;104(4):682-91
  • Nobili S, Landini I, Giglioni B, Mini E. Pharmacological strategies for overcoming multidrug resistance. Curr Drug Targets 2006;7:861-79
  • Van Zuylen L, Sparreboom A, Van Der Gaast A, et al. The orally administered P-glycoprotein inhibitor R101933 does not alter the plasma pharmacokinetics of docetaxel. Clin Cancer Res 2000;6:1365-71
  • Van Zuylen L, Sparreboom A, Van Der Gaast A, et al. Disposition of docetaxel in the presence of P-glycoprotein inhibition by intravenous administration of R101933. Eur J Cancer 2002;38(8):1090-9
  • Rapoport BL, Fumoleau P, Piccart-Gebhart MJ. R101933 combined with chemotherapy in treating patients with metastatic breast cancer that has not responded to previous chemotherapy. Available at: URL: www.clinicaltrials.gov/ct/show/NCT00028873. [Accessed on December 31, 2007]
  • Vincent M. Tesmilifene may enhance breast cancer chemotherapy by killing a clone of aggressive, multi-drug resistant cells through its action on the p-glycoprotein pump. Med Hypotheses 2006;66(4):715-31
  • Khoo K, Brandes L, Reyno L, et al. Phase II trial of N,N-diethyl-2-[4-(phenylmethyl)phenoxy]ethanamine.HCl and doxorubicin chemotherapy in metastatic breast cancer: a National Cancer Institute of Canada clinical trials group study. J Clin Oncol 1999;17(11):3431-7
  • Reyno L, Seymour L, Tu D, et al. Phase III study of N,N-diethyl-2-[4-(phenylmethyl) phenoxy]ethanamine (BMS-217380-01) combined with doxorubicin versus doxorubicin alone in metastatic/recurrent breast cancer: National Cancer Institute of Canada clinical trials group study MA.19. J Clin Oncol 2004;22(2):269-76
  • YM BioSciences Inc. homepage. Available at: URL: www.ymbiosciences.com/. [Accessed on December 31, 2007]
  • Oldham RK, Reid WK, Preisler HD, Barnett D. A Phase I and pharmacokinetic study of CBT-1 as a multidrug resistance modulator in the treatment of patients with advanced cancer. Cancer Biother Radiopharm 1998;13(2):71-80
  • Oldham RK, Reid WK, Barnett D. Phase I study of CBT-1 and Taxol in patients with Taxol resistant cancers. Cancer Biother Radiopharm 2000;15(2):153-9
  • Mamot C, Drummond DC, Hong K, Kirpotin DB, Park JW. Liposome-based approaches to overcome anticancer drug resistance. Drug Resist Updates 2003;6(5):271-9
  • Lee K-D, Hong K, Papahadjopoulos D. Recognition of liposomes by cells: in vitro binding and endocytosis mediated by specific lipid headgroups and surface charge density. Biochim Biophys Acta Biomembr 1992;1103(2):185-97
  • Krishna R, Mayer LD. Liposomal doxorubicin circumvents PSC 833-free drug interactions, resulting in effective therapy of multidrug-resistant solid tumors. Cancer Res 1997;57(23):5246-53
  • Tsuruo T, Hamada H, Sato S, Heike Y. Inhibition of multidrug-resistant human tumor growth in athymic mice by anti-P-glycoprotein monoclonal antibodies. Jpn J Cancer Res 1989;80(7):627-31
  • Pearson JW, Fogler WE, Volker K, et al. Reversal of drug resistance in a human colon cancer xenograft expressing MDR1 complementary DNA by in vivo administration of MRK-16 monoclonal antibody. J Natl Cancer Inst 1991;83(19):1386-91
  • Mickisch GH, Pai LH, Gottesman MM, Pastan I. Monoclonal antibody MRK16 reverses the multidrug resistance of multidrug-resistant transgenic mice. Cancer Res 1992;52(16):4427-32
  • Iwahashi T, Okochi E, Ariyoshi K, et al. Specific targeting and killing activities of anti-P-glycoprotein monoclonal antibody MRK16 directed against intrinsically multidrug-resistant human colorectal carcinoma cell lines in the nude mouse model. Cancer Res 1993;53(22):5475-82
  • Watanabe T, Naito M, Kokubu N, Tsuruo T. Regression of established tumors expressing P-glycoprotein by combinations of adriamycin, cyclosporin derivatives, and MRK-16 antibodies. J Natl Cancer Inst 1997;89(7):512-8
  • Naito M, Tsuge H, Kuroko C, et al. Enhancement of cellular accumulation of cyclosporine by anti-P-glycoprotein monoclonal antibody MRK-16 and synergistic modulation of multidrug resistance. J Natl Cancer Inst 1993;85(4):311-6
  • Goda K, Fenyvesi F, Bacso Z, et al. Complete Inhibition of P-glycoprotein by simultaneous treatment with a distinct class of modulators and the UIC2 monoclonal antibody. J Pharmacol Exp Ther 2007;320(1):81-8
  • Fitzgerald DJ, Willingham MC, Cardarelli CO, et al. A monoclonal antibody – Pseudomonas toxin conjugate that specifically kills multidrug-resistant cells. Proc Natl Acad Sci USA 1987;84(12):4288-92
  • Efferth T, Volm M. Modulation of P-glycoprotein-mediated multidrug resistance by monoclonal antibodies, immunotoxins or antisense oligodeoxynucleotides in kidney carcinoma and normal kidney cells. Oncology 1993;50(4):303-8
  • Masuda Y, Kobayashi H, Holland JF, Ohnuma T. Reversal of multidrug resistance by a liposome–MDR1 ribozyme complex. Cancer Chemother Pharmacol 1998;42(1):9-16
  • Kobayashi H, Takemura Y, Wang FS, Oka T, Ohnuma T. Retrovirus-mediated transfer of anti-MDR1 hammerhead ribozymes into multidrug-resistant human leukemia cells: screening for effective target sites. Int J Cancer 1999;81(6):944-50
  • Nagata J, Kijima H, Hatanaka H, et al. Reversal of drug resistance using hammerhead ribozymes against multidrug resistance-associated protein and multidrug resistance 1 gene. Int J Oncol 2002;21(5):1021-6
  • Crooke ST. Therapeutic applications of oligonucleotides. Ann Rev Pharmacol Toxicol 1992;32(1):329-76
  • Hannon GJ. RNA interference. Nature 2002;418(6894):244-51
  • Nieth C, Priebsch A, Stege A, Lage H. Modulation of the classical multidrug resistance (MDR) phenotype by RNA interference (RNAi). FEBS Lett 2003;545(2-3):144-50
  • Wu H, Hait WN, Yang J-M. Small interfering RNA-induced suppression of MDR1 (P-glycoprotein) restores sensitivity to multidrug-resistant cancer cells. Cancer Res 2003;63(7):1515-9
  • Priebsch A, Rompe F, Tonnies H, et al. Complete reversal of ABCG2-depending atypical multidrug resistance by RNA interference in human carcinoma cells. Oligonucleotides 2006;16(3):263-74
  • Ee PLR, He X, Ross DD, Beck WT. Modulation of breast cancer resistance protein (BCRP/ABCG2) gene expression using RNA interference. Mol Cancer Ther 2004;3(12):1577-84
  • Li L, Xu J, Min T, Huang W. Reversal of MDR1 gene-dependent multidrug resistance using low concentration of endonuclease-prepared small interference RNA. Eur J Pharmacol 2006;536(1-2):93-7
  • Kanzaki A, Takebayashi Y, Ren X-Q, et al. Overcoming multidrug drug resistance in P-glycoprotein/MDR1-overexpressing cell lines by ecteinascidin 743. Mol Cancer Ther 2002;1(14):1327-34
  • Choi CH, Sun KH, An CS, et al. Reversal of P-glycoprotein-mediated multidrug resistance by 5,6,7,3′,4′-pentamethoxyflavone (Sinensetin). Biochem Biophys Res Commun 2002;295:832-40
  • Mei Y, Qian F, Wei D, Liu J. Reversal of cancer multidrug resistance by green tea polyphenols. J Pharm Pharmacol 2004;56(10):1307-14
  • Nakanishi T, Shiozawa K, Hassel BA, Ross DD. Complex interaction of BCRP/ABCG2 and imatinib in BCR-ABL-expressing cells: BCRP-mediated resistance to imatinib is attenuated by imatinib-induced reduction of BCRP expression. Blood 2006;108(2):678-84
  • Sims-Mourtada J, Izzo JG, Ajani J, Chao KSC. Sonic Hedgehog promotes multiple drug resistance by regulation of drug transport. Oncogene 2007;26(38):5674-9
  • Hu XF, Li J, Yang E, Vandervalk S, Xing PX. Anti-cripto Mab inhibit tumour growth and overcome MDR in a human leukaemia MDR cell line by inhibition of Akt and activation of JNK/SAPK and bad death pathways. Br J Cancer 2007;96(6):918-27
  • Ludwig JA, Szakacs G, Martin SE, et al. Selective toxicity of NSC73306 in MDR1-positive cells as a new strategy to circumvent multidrug resistance in cancer. Cancer Res 2006;66(9):4808-15
  • Szakacs G, Annereau J-P, Lababidi S, et al. Predicting drug sensitivity and resistance: profiling ABC transporter genes in cancer cells. Cancer Cell 2004;6(2):129-37
  • Van Vlerken LE, Duan Z, Seiden MV, Amiji MM. Modulation of intracellular ceramide using polymeric nanoparticles to overcome multidrug resistance in cancer. Cancer Res 2007;67(10):4843-50
  • Devalapally H, Duan Z, Seiden MV, Amiji MM. Paclitaxel and ceramide co-administration in biodegradable polymeric nanoparticulate delivery system to overcome drug resistance in ovarian cancer. Int J Cancer 2007;121(8):1830-8
  • Ambudkar SV, Kimchi-Sarfaty C, Sauna ZE, Gottesman MM. P-glycoprotein: from genomics to mechanism. Oncogene 2003;22(47):7468-85
  • Cascorbi I. Role of pharmacogenetics of ATP-binding cassette transporters in the pharmacokinetics of drugs. Pharmacol Ther 2006;112(2):457-73
  • Kimchi-Sarfaty C, Oh JM, Kim IW, et al. A “silent” polymorphism in the MDR1 gene changes substrate specificity. Science 2007;315(5811):525-8
  • Kawase M, Shah A, Gaveriya H, et al. 3,5-Dibenzoyl-1,4-dihydropyridines: synthesis and MDR reversal in tumor cells. Bioorg Med Chem 2002;10:1051-5
  • Ganeshaguru K, Wickremasinghe RG, Jones DT, et al. Actions of the selective protein kinase C inhibitor PKC412 on B-chronic lymphocytic leukemia cells in vitro. Haematologica 2002;87:167-76
  • Qi J, Yang CZ, Wang CY, et al. Function and mechanism of pyronaridine: a new inhibitor of P-glycoprotein-mediated multidrug resistance. Acta Pharmacol Sin 2002;23:544-50
  • Tanaka J, Trianto A, Musman M, et al. New polyoxygenated steroids exhibiting reversal of multidrug resistance from the gorgonian Isis hippuris. Tetrahedron 2002;58(32):6259-66
  • Ramachandran C, Rabi T, Fonseca HB, Melnick SJ, Escalon EA. Novel plant triterpenoid drug amooranin overcomes multidrug resistance in human leukemia and colon carcinoma cell lines. Int J Cancer 2003;105(6):784-9
  • Mitsuo M, Noguchi T, Nakajima Y, et al. Binding site(s) on P-glycoprotein for a newly synthesized photoaffinity analog of agosterol A. Oncol Res 2003;14(1):39-48
  • Zhang S, Morris ME. Effects of the flavonoids biochanin A, morin, phloretin, and silymarin on P-glycoprotein-mediated transport. J Pharmacol Exp Ther 2003;304(3):1258-67
  • Kim SW, Kwon HY, Chi DW, et al. Reversal of P-glycoprotein-mediated multidrug resistance by ginsenoside Rg(3). Biochem Pharmacol 2003;65:75-82
  • Hohmann J, Redei D, Forgo P, et al. Jatrophane diterpenoids from Euphorbia mongolica as modulators of the multidrug resistance of L5128 mouse lymphoma cells. J Nat Prod 2003;66(7):976-9
  • Lee BH, Lee CO, Kwon MJ, et al. Differential effects of the optical isomers of KR30031 on cardiotoxicity and on multidrug resistance reversal activity. Anticancer Drugs 2003;14:175-81
  • Soenen DR, Hwang I, Hedrick MP, Boger DL. Multidrug resistance reversal activity of key ningalin analogues. Bioorg Med Chem Lett 2003;13(10):1777-81
  • Tao H, Hwang I, Boger DL. Multidrug resistance reversal activity of permethyl ningalin B amide derivatives. Bioorg Med Chem Lett 2004;14(24):5979-81
  • Ketabi-Kiyanvash N, Weiss J, Haefeli WE, Mikus G. P-glycoprotein modulation by the designer drugs methylenedioxymethamphetamine, methylenedioxyethylamphetamine and paramethoxyamphetamine. Addict Biol 2003;8:413-8
  • Choi CH, Kang G, Min YD. Reversal of P-glycoprotein-mediated multidrug resistance by protopanaxatriol ginsenosides from Korean red ginseng. Planta Med 2003;69:235-40
  • Wu JY, Fong WF, Zhang JX, et al. Reversal of multidrug resistance in cancer cells by pyranocoumarins isolated from Radix Peucedani. Eur J Pharmacol 2003;473(1):9-17
  • Dupuis ML, Tombesi M, Sabatini M, Cianfriglia M. Differential effect of HIV-1 protease inhibitors on P-glycoprotein function in multidrug-resistant variants of the human CD4+ T lymphoblastoid CEM cell line. Chemotherapy 2003;49:8-16
  • Woehlecke H, Osada H, Herrmann A, Lage H. Reversal of breast cancer resistance protein-mediated drug resistance by tryprostatin A. Int J Cancer 2003;107(5):721-8
  • Madureira AM, Molnar A, Abreu PM, Molnar J, Ferreira MJ. A new sesquiterpene-coumarin ether and a new abietane diterpene and their effects as inhibitors of P-glycoprotein. Planta Med 2004;70(9):828-33
  • Wang C, Zhang JX, Shen XL, et al. Reversal of P-glycoprotein-mediated multidrug resistance by Alisol B 23-acetate. Biochem Pharmacol 2004;68(5):843-55
  • Lee Y, Yeo H, Liu SH, et al. Increased anti-P-glycoprotein activity of baicalein by alkylation on the A ring. J Med Chem 2004;47(22):5555-66
  • Ke Hu MEM. Effects of benzyl-, phenethyl-, and ?-naphthyl isothiocyanates on P-glycoprotein- and MRP1-mediated transport. J Pharm Sci 2004;93(7):1901-11
  • Limtrakul P, Khantamat O, Pintha K. Inhibition of P-glycoprotein activity and reversal of cancer multidrug resistance by Momordica charantia extract. Cancer Chemother Pharmacol 2004;54(6):525-30
  • Kitagawa S, Nabekura T, Kamiyama S. Inhibition of P-glycoprotein function by tea catechins in KB-C2 cells. J Pharm Pharmacol 2004;56(8):1001-5
  • Madureira AM, Spengler G, Molnar A, et al. Effect of cycloartanes on reversal of multidrug resistance and apoptosis induction on mouse lymphoma cells. Anticancer Res 2004;24(2B):859-64
  • Lee BD, Li Z, French KJ, et al. Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein. J Med Chem 2004;47(6):1413-22
  • Sauna ZE, Peng XH, Nandigama K, Tekle S, Ambudkar SV. The molecular basis of the action of disulfiram as a modulator of the multidrug resistance-linked ATP binding cassette transporters MDR1 (ABCB1) and MRP1 (ABCC1). Mol Pharmacol 2004;65(3):675-84
  • Palomo C, Oiarbide M, Garcia JM, et al. A practical total synthesis of hapalosin, a 12-membered cyclic depsipeptide with multidrug resistance-reversing activity, by employing improved segment coupling and macrolactonization. J Org Chem 2004;69(12):4126-34
  • Wang EJ, Barecki-Roach M, Johnson WW. Quantitative characterization of direct P-glycoprotein inhibition by St John's wort constituents hypericin and hyperforin. J Pharm Pharmacol 2004;56(1):123-8
  • Aoki S, Cao L, Matsui K, et al. Kendarimide A, a novel peptide reversing P-glycoprotein-mediated multidrug resistance in tumor cells, from a marine sponge of Haliclona sp. Tetrahedron 2004;60(33):7053-9
  • Munoz-Martinez F, Lu P, Cortes-Selva F, et al. Celastraceae sesquiterpenes as a new class of modulators that bind specifically to human P-glycoprotein and reverse cellular multidrug resistance. Cancer Res 2004;64(19):7130-8
  • Brooks TA, Kennedy DR, Gruol DJ, et al. Structure–activity analysis of taxane-based broad-spectrum multidrug resistance modulators. Anticancer Res 2004;24(2A):409-15
  • Zhao X, Gu J, Yin D, Chen X. Synthesis and biological evaluation of taxinine analogues as orally active multidrug resistance reversal agents in cancer. Bioorg Med Chem Lett 2004;14(18):4767-70
  • Fu L, Liang Y, Deng L, et al. Characterization of tetrandrine, a potent inhibitor of P-glycoprotein-mediated multidrug resistance. Cancer Chemother Pharmacol 2004;53(4):349-56
  • Jin J, Wang FP, Wei H, Liu G. Reversal of multidrug resistance of cancer through inhibition of P-glycoprotein by 5-bromotetrandrine. Cancer Chemother Pharmacol 2005;55(2):179-88
  • Ferreira MJ GN, Madureira AM, Molnár J. Inhibition of P-glycoprotein transport activity in a resistant mouse lymphoma cell line by diterpenic lactones. Anticancer Res 2005;25(5):3259-62
  • Weiss J, Sauer A, Frank A, Unger M. Extracts and kavalactones of Piper methysticum G. Forst (kava-kava) inhibit P-glycoprotein in vitro. Drug Metab Dispos 2005;33(11):1580-3
  • Walter RB, Pirga JL, Cronk MR, et al. PK11195, a peripheral benzodiazepine receptor (pBR) ligand, broadly blocks drug efflux to chemosensitize leukemia and myeloma cells by a pBR-independent, direct transporter-modulating mechanism. Blood 2005;106(10):3584-93
  • Raad I, Terreux R, Richomme P, et al. Structure–activity relationship of natural and synthetic coumarins inhibiting the multidrug transporter P-glycoprotein. Bioorg Med Chem 2006;14(20):6979-87
  • Iwaki K, Sakaeda T, Kakumoto M, et al. Haloperidol is an inhibitor but not substrate for MDR1/P-glycoprotein. J Pharm Pharmacol 2006;58:1617-22
  • Galski H, Sivan H, Lazarovici P, Nagler A. In vitro and in vivo reversal of MDR1-mediated multidrug resistance by KT-5720: implications on hematological malignancies. Leuk Res 2006;30(9):1151-8
  • Jekerle V, Klinkhammer W, Scollard DA, et al. In vitro and in vivo evaluation of WK-X-34, a novel inhibitor of P-glycoprotein and BCRP, using radio imaging techniques. Int J Cancer 2006;119(2):414-22
  • Teodori E, Martelli C, Salerno M, et al. Isomeric N,N-bis(cyclohexanol)amine aryl esters: the discovery of a new class of highly potent P-glycoprotein (Pgp)-dependent multidrug resistance (MDR) inhibitors. J Med Chem 2007;50(4):599-602
  • Limtrakul P, Siwanon S, Yodkeeree S, Duangrat C. Effect of Stemona curtisii root extract on P-glycoprotein and MRP-1 function in multidrug-resistant cancer cells. Phytomedicine 2007;14(6):381-9
  • Yoo HH, Lee M, Lee MW, et al. Effects of Schisandra lignans on P-glycoprotein-mediated drug efflux in human intestinal Caco-2. Planta Med 2007;73(5):444-50
  • Paek IB, Kim SY, Kim MS, et al. Characterization of human liver cytochrome P-450 enzymes involved in the O-demethylation of a new P-glycoprotein inhibitor HM-30181. J Toxicol Environmental Health A 2007;70(15):1356-64
  • Patanasethanont D, Nagai J, Yumoto R, et al. Effects of Kaempferia parviflora extracts and their flavone constituents on P-glycoprotein function. J Pharm Sci 2007;96(1):223-33
  • Fong W-F, Wan C-K, Zhu G-Y, et al. Schisandrol A from Schisandra chinensis reverses P-glycoprotein-mediated multidrug resistance by affecting Pgp-substrate complexes. Planta Med 2007;(3):212-20
  • Yu S-T, Chen T-M, Tseng S-Y, Chen Y-H. Tryptanthrin inhibits MDR1 and reverses doxorubicin resistance in breast cancer cells. Biochem Biophys Res Commun 2007;358(1):79-84
  • Medeiros BC, Landau HJ, Morrow M, et al. The farnesyl transferase inhibitor, tipifarnib, is a potent inhibitor of the MDR1 gene product, P-glycoprotein, and demonstrates significant cytotoxic synergism against human leukemia cell lines. Leukemia 2007;21(4):739-46
  • Collnot EM, Baldes C, Wempe MF, et al. Mechanism of inhibition of P-glycoprotein mediated efflux by vitamin E TPGS: influence on ATPase activity and membrane fluidity. Mol Pharma 2007;4(3):465-74
  • Burg D, Wielinga P, Zelcer N, et al. Inhibition of the multidrug resistance protein 1 (MRP1) by peptidomimetic glutathione-conjugate analogs. Mol Pharmacol 2002;62(5):1160-6
  • Vergote J, Moretti JL, Kouyoumdjian JC, Garnier-Suillerot A. MRP1 modulation by PAK-104P: detection with technetium-99m-MIBI in cultured lung tumor cells. Anticancer Res 2002;22(1A):251-6
  • Wang S, Ryder H, Pretswell I, et al. Studies on quinazolinones as dual inhibitors of Pgp and MRP1 in multidrug resistance. Bioorg Med Chem Lett 2002;12(4):571-4
  • Hegedus T, Orfi L, Seprodi A, et al. Interaction of tyrosine kinase inhibitors with the human multidrug transporter proteins, MDR1 and MRP1. Biochim Biophys Acta 2002;1587(2-3):318-25
  • Norman BH, Gruber JM, Hollinshead SP, et al. Tricyclic isoxazoles are novel inhibitors of the multidrug resistance protein (MRP1). Bioorg Med Chem Lett 2002;12(6):883-6
  • Reid G, Wielinga P, Zelcer N, et al. The human multidrug resistance protein MRP4 functions as a prostaglandin efflux transporter and is inhibited by nonsteroidal antiinflammatory drugs. Proc Natl Acad Sci USA 2003;100(16):9244-9
  • Batrakova EV, Li S, Alakhov VY, et al. Sensitization of cells overexpressing multidrug-resistant proteins by pluronic P85. Pharma Res 2003;20(10):1581-90
  • Brooks TA, Minderman H, O'Loughlin KL, et al. Taxane-based reversal agents modulate drug resistance mediated by P-glycoprotein, multidrug resistance protein, and breast cancer resistance protein. Mol Cancer Ther 2003;2(11):1195-205
  • Wang S, Folkes A, Chuckowree I, et al. Studies on pyrrolopyrimidines as selective inhibitors of multidrug-resistance-associated protein in multidrug resistance. J Med Chem 2004;47(6):1329-38
  • Xiao-Fei Zhou RACMEM. Effects of new 4-aryl-1,4-dihydropyridines and 4-arylpyridines on drug efflux mediated by multidrug resistance-associated protein 1. J Pharm Sci 2005;94(10):2256-65
  • Wu C-P, Calcagno AM, Hladky SB, Ambudkar SV, Barrand MA. Modulatory effects of plant phenols on human multidrug-resistance proteins 1, 4 and 5 (ABCC1, 4 and 5). FEBS J 2005;272(18):4725-40
  • Van Zanden JJ, De Mul A, Wortelboer HM, et al. Reversal of in vitro cellular MRP1 and MRP2 mediated vincristine resistance by the flavonoid myricetin. Biochem Pharmacol 2005;69(11):1657-65
  • Lespine A, Dupuy J, Orlowski S, et al. Interaction of ivermectin with multidrug resistance proteins (MRP1, 2 and 3). Chem Biol Interact 2006;159(3):169-79
  • Abdul-Ghani R, Serra V, Gyorffy B, et al. The PI3K inhibitor LY294002 blocks drug export from resistant colon carcinoma cells overexpressing MRP1. Oncogene 2005;25(12):1743-52
  • Van Zanden JJ, Van Der Woude H, Vaessen J, et al. The effect of quercetin Phase II metabolism on its MRP1 and MRP2 inhibiting potential. Biochem Pharmacol 2007;74(2):345-51
  • El-Sheikh AAK, Van Den Heuvel JJMW, Koenderink JB, Russel FGM. Interaction of nonsteroidal anti-inflammatory drugs with multidrug resistance protein (MRP) 2/ABCC2- and MRP4/ABCC4-mediated methotrexate transport. J Pharmacol Exp Ther 2007;320(1):229-35
  • Weiss J, Theile D, Ketabi-Kiyanvash N, Lindenmaier H, Haefeli WE. Inhibition of MRP1/ABCC1, MRP2/ABCC2, and MRP3/ABCC3 by nucleoside, nucleotide, and non-nucleoside reverse transcriptase inhibitors. Drug Metab Dispos 2007;35(3):340-4
  • Li L, Pan Q, Sun M, Lu Q, Hu X. Dibenzocyclooctadiene lignans – a class of novel inhibitors of multidrug resistance-associated protein 1. Life Sci 2007;80(8):741-8
  • Mansilla S, Rojas M, Bataller M, Priebe W, Portugal J. Circumvention of the multidrug-resistance protein (MRP-1) by an antitumor drug through specific inhibition of gene transcription in breast tumor cells. Biochem Pharmacol 2007;73(7):934-42
  • Patanasethanont D, Nagai J, Matsuura C, et al. Modulation of function of multidrug resistance associated-proteins by Kaempferia parviflora extracts and their components. Eur J Pharmacol 2007;566(1-3):67-74
  • Imai Y, Tsukahara S, Ishikawa E, Tsuruo T, Sugimoto Y. Estrone and 17beta-estradiol reverse breast cancer resistance protein-mediated multidrug resistance. Jpn J Cancer Res 2002;93(3):231-5
  • Sugimoto Y, Tsukahara S, Imai Y, Ueda K, Tsuruo T. Reversal of breast cancer resistance protein-mediated drug resistance by estrogen antagonists and agonists. Mol Cancer Ther 2003;2(1):105-12
  • Shiozawa K, Oka M, Soda H, et al. Reversal of breast cancer resistance protein (BCRP/ABCG2)-mediated drug resistance by novobiocin, a coumermycin antibiotic. Int J Cancer 2004;108(1):146-51
  • Imai Y, Tsukahara S, Asada S, Sugimoto Y. Phytoestrogens/flavonoids reverse breast cancer resistance protein/ABCG2-mediated multidrug resistance. Cancer Res 2004;64(12):4346-52
  • Zhang S, Yang X, Morris ME. Flavonoids are inhibitors of breast cancer resistance protein (ABCG2)-mediated transport. Mol Pharmacol 2004;65(5):1208-16
  • Cooray HC, Janvilisri T, Van Veen HW, Hladky SB, Barrand MA. Interaction of the breast cancer resistance protein with plant polyphenols. Biochem Biophys Res Commun 2004;317(1):269-75
  • Ozvegy-Laczka C, Hegedus T, Varady G, et al. High-affinity interaction of tyrosine kinase inhibitors with the ABCG2 multidrug transporter. Mol Pharmacol 2004;65(6):1485-95
  • Houghton PJ, Germain GS, Harwood FC, et al. Imatinib mesylate is a potent inhibitor of the ABCG2 (BCRP) transporter and reverses resistance to topotecan and SN-38 in vitro. Cancer Res 2004;64(7):2333-7
  • Breedveld P, Zelcer N, Pluim D, et al. Mechanism of the pharmacokinetic interaction between methotrexate and benzimidazoles: potential role for breast cancer resistance protein in clinical drug-drug interactions. Cancer Res 2004;64(16):5804-11
  • Minderman H, Brooks TA, O'Loughlin KL, et al. Broad-spectrum modulation of ATP-binding cassette transport proteins by the taxane derivatives ortataxel (IDN-5109, BAY 59-8862) and tRA96023. Cancer Chemother Pharmacol 2004;53(5):363-9
  • Gupta A, Zhang Y, Unadkat JD, Mao Q. HIV protease inhibitors are inhibitors but not substrates of the human breast cancer resistance protein (BCRP/ABCG2). J Pharmacol Exp Ther 2004;310(1):334-41
  • Minderman H, O'Loughlin KL, Pendyala L, Baer MR. VX-710 (biricodar) increases drug retention and enhances chemosensitivity in resistant cells overexpressing P-glycoprotein, multidrug resistance protein, and breast cancer resistance protein. Clin Cancer Res 2004;10(5):1826-34
  • Pavek P, Merino G, Wagenaar E, et al. 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 2005;312(1):144-52
  • Ahmed-Belkacem A, Pozza A, Munoz-Martinez F, et al. Flavonoid structure–activity studies identify 6-prenylchrysin and tectochrysin as potent and specific inhibitors of breast cancer resistance protein ABCG2. Cancer Res 2005;65(11):4852-60
  • Zhang Y, Gupta A, Wang H, et al. BCRP transports dipyridamole and is inhibited by calcium channel blockers. Pharm Res 2005;22(12):2023-34
  • Zhou XF, Yang X, Wang Q, Coburn RA, Morris ME. Effects of dihydropyridines and pyridines on multidrug resistance mediated by breast cancer resistance protein: in vitro and in vivo studies. Drug Metab Dispos 2005;33(8):1220-8
  • Shukla S, Robey RW, Bates SE, Ambudkar SV. The calcium channel blockers, 1,4-dihydropyridines, are substrates of the multidrug resistance-linked ABC drug transporter, ABCG2. Biochemistry 2006;45(29):8940-51
  • Merino G, Jonker JW, Wagenaar E, et al. Transport of anthelmintic benzimidazole drugs by breast cancer resistance protein (bcrp/abcg2). Drug Metab Dispos 2005;33(5):614-8
  • Boumendjel A, Nicolle E, Moraux T, et al. Piperazinobenzopyranones and phenalkylaminobenzopyranones: potent inhibitors of breast cancer resistance protein (ABCG2). J Med Chem 2005;48(23):7275-81
  • Morita H, Koyama K, Sugimoto Y, Kobayashi J. Antimitotic activity and reversal of breast cancer resistance protein-mediated drug resistance by stilbenoids from Bletilla striata. Bioorg Med Chem Lett 2005;15(4):1051-4
  • Pawarode A, Shukla S, Minderman H, et al. Differential effects of the immunosuppressive agents cyclosporin A, tacrolimus and sirolimus on drug transport by multidrug resistance proteins. Cancer Chemother Pharmacol 2007;60(2):179-88
  • Henrich CJ, Bokesch HR, Dean M, et al. A high-throughput cell-based assay for inhibitors of ABCG2 activity. J Biomol Screen 2006;11(2):176-83
  • Jin J, Shahi S, Kang HK, Van Veen HW, Fan TP. Metabolites of ginsenosides as novel BCRP inhibitors. Biochem Biophys Res Commun 2006;345(4):1308-14
  • Petrangolini G, Supino R, Pratesi G, et al. Effect of a novel vacuolar-H+-ATPase inhibitor on cell and tumor response to camptothecins. J Pharmacol Exp Ther 2006;318(3):939-46
  • Katayama K, Masuyama K, Yoshioka S, et al. Flavonoids inhibit breast cancer resistance protein-mediated drug resistance: transporter specificity and structure–activity relationship. Cancer Chemother Pharmacol 2007;60(6):789-97
  • Boumendjel A, Macalou S, Ahmed-Belkacem A, Blanc M, Di Pietro A. Acridone derivatives: design, synthesis, and inhibition of breast cancer resistance protein ABCG2. Bioorg Med Chem 2007;15(8):2892-7
  • Robey RW, Shukla S, Steadman K, et al. Inhibition of ABCG2-mediated transport by protein kinase inhibitors with a bisindolylmaleimide or indolocarbazole structure. Mol Cancer Ther 2007;6(6):1877-85
  • Gupta A, Unadkat JD, Mao Q. Interactions of azole antifungal agents with the human breast cancer resistance protein (BCRP). J Pharm Sci 2007;96(12):3226-35
  • Brendel C, Scharenberg C, Dohse M, et al. Imatinib mesylate and nilotinib (AMN107) exhibit high-affinity interaction with ABCG2 on primitive hematopoietic stem cells. Leukemia 2007;21(6):1267-75
  • Ahmed-Belkacem A, Macalou S, Borrelli F, et al. Nonprenylated rotenoids, a new class of potent breast cancer resistance protein inhibitors. J Med Chem 2007;50(8):1933-8
  • Jekerle V, Klinkhammer W, Reilly RM, Piquette-Miller M, Wiese M. Novel tetrahydroisoquinolin-ethyl-phenylamine based multidrug resistance inhibitors with broad-spectrum modulating properties. Cancer Chemother Pharmacol 2007;59(1):61-9
  • Tranchand B, Catimel G, Lucas C, et al. Phase I clinical and pharmacokinetic study of S9788, a new multidrug-resistance reversal agent given alone and in combination with doxorubicin to patients with advanced solid tumors. Cancer Chemother Pharmacol 1998;41(4):281-91
  • O'Leary M, O'Connor R, Roy S, et al. Phase I trial of the multi-drug resistance (MDR) protein-1 (MRP-1) modulating agent sulindac (S) plus epirubicin (E) in patients (pts) with advanced cancer. J Clin Oncol (Meeting Abstracts) 2004;22(14 Suppl):2129
  • O'Connor R, O'Leary M, Ballot J, et al. A Phase I clinical and pharmacokinetic study of the multi-drug resistance protein-1 (MRP-1) inhibitor sulindac, in combination with epirubicin in patients with advanced cancer. Cancer Chemother Pharmacol 2007;59(1):79-87
  • Agrawal M, Abraham J, Balis FM, et al. Increased 99mTc-sestamibi accumulation in normal liver and drug-resistant tumors after the administration of the glycoprotein inhibitor, XR9576. Clin Cancer Res 2003;9(2):650-6
  • Fox E, Bates SE. Tariquidar (XR9576): a P-glycoprotein drug efflux pump inhibitor. Expert Rev Anticancer Ther 2007;7(4):447-59
  • Morschhauser F, Zinzani PL, Burgess M, et al. Phase I/II trial of a P-glycoprotein inhibitor, Zosuquidar.3HCl trihydrochloride (LY335979), given orally in combination with the CHOP regimen in patients with non-Hodgkin's lymphoma. Leuk Lymphoma 2007;48(4):708-15
  • Rowinsky EK, Smith L, Wang YM, et al. Phase I and pharmacokinetic study of paclitaxel in combination with biricodar, a novel agent that reverses multidrug resistance conferred by overexpression of both MDR1 and MRP. J Clin Oncol 1998;16(9):2964-76
  • Berruti A, Terzolo M, Sperone P, et al. Etoposide, doxorubicin and cisplatin plus mitotane in the treatment of advanced adrenocortical carcinoma: a large prospective Phase II trial. Endocr Relat Cancer 2005;12(3):657-66
  • Andreeff MGF, Kornblau S, Konopleva M, et al. Phase I study of annamycin, a novel liposomal anthracycline, in patients with relapsed/refractory acute myeloid and lymphoid leukemias. Proc Am Soc Clin Oncol 2001;20:Abstract 1211
  • Mistry PP, Folkes AA. ONT-093 (Ontogen). Curr Opin Investig Drugs 2002;3(11):1666-71
  • Oldham R. Safety and efficacy study of CBT-1 and paclitaxel with carboplatin in patients with advanced inoperable non-small cell lung cancer. Available at: URL:clinicaltrial.gov 2007 [Accessed on December 31, 2007]

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