Cellular and biochemical characterization of VX-710 as a chemosensitizer: Reversal of P-glycoprotein-mediated multidrug resistance in vitro

Anti-Cancer Drugs

Volumn 8, Issue 2, 1997, Pages 125-140

  Germann, Ursula A ^a   Shlyakhter, Dina ^a   Mason, Valerie S ^a   Zelle, Robert E ^a   Duffy, John P ^a   Galullo, Vincent ^a   Armistead, David M ^a   Saunders, Jeffrey O ^a   Boger, Joshua ^a   Harding, Matthew W ^a  

^a VERTEX PHARMACEUTICALS   (United States)

Author keywords

Chemosensitizer; Chemotherapy; FKBP12; MDR modulator; MDR1 gene product

Indexed keywords

ADENOSINE TRIPHOSPHATASE; ANTINEOPLASTIC AGENT; AZIDOPINE; BIRICODAR; CHEMOSENSITIZING AGENT; DOXORUBICIN; ETOPOSIDE; GENE PRODUCT; GLYCOPROTEIN P; IODINE 125; MULTIDRUG RESISTANCE REVERSING AGENT; PACLITAXEL; UNCLASSIFIED DRUG; VANADIC ACID; VINCRISTINE;

ANIMAL CELL; ARTICLE; CANCER CELL CULTURE; CARCINOMA CELL; CHEMOSENSITIVITY; CONCENTRATION RESPONSE; CONTROLLED STUDY; CYTOTOXICITY; DRUG UPTAKE; FIBROBLAST; GENETIC TRANSFECTION; HUMAN; HUMAN CELL; LEUKEMIA CELL; MOUSE; MULTIDRUG RESISTANCE; MYELOMA CELL; NONHUMAN; PHOTOAFFINITY LABELING; PRIORITY JOURNAL; PROTEIN BINDING;

EID: 8044235838     PISSN: 09594973     EISSN: None     Source Type: Journal    
DOI: 10.1097/00001813-199702000-00004     Document Type: Article

References (62)

1. Lehnert M. Clinical multidrug resistance in cancer - a multifactorial problem. Eur J Cancer 1996; 32A: 912-20.
2. Gottesman MM, Pastan I. Biochemistry of multidrug resistance mediated by the multidrug transporter. Annu Rev Biochem 1993; 62: 385-427.
3. Germann UA. P-glycoprotein - a mediator of multidrug resistance in tumour cells. Eur J Cancer 1996; 32A: 927-44.
4. Marie J-P, Zhou D-C, Gurbuxani S, Legrand O, Zittoun R. MDR1/P-glycoprotein in haematological neoplasms. Eur J Cancer 1996; 32A: 1034-8.
5. Goldstein LJ. MDR1 gene expression in solid tumours. Eur J Cancer 1996; 32A: 1039-50.
6. Cole SPC, Bhardwaj G, Gerlach JH, et al. Overexpression of a transporter gene in a multidrug-resistant human lung cancer cell line. Science 1992; 258: 1650-4.
7. Scheffer GL, Wijngaard PIJ, Flens MJ, et al. The drug resistance-related protein LRP is the human major vault protein. Nature Medicine 1995; 1: 578-82.
8. O'Brien ML, Tew KD. Glutathione and related enzymes in multidrug resistance. Eur J Cancer 1996; 32A: 967-78.
9. Nitiss JL, Beck WT. Antitopoisomerase drug action and resistance. Eur J Cancer 1996; 32A: 958-66.
10. Sarkadi B, Price EM, Boucher RC, Germann UA, Scarborough GA. Expression of the human multidrug resistance cDNA in insect cells generates a high activity drug-stimulated membrane ATPase. J Biol Chem 1992; 267: 4854-8.
11. Homolya L, Hollo Z, Germann UA, et al. Fluorescent cellular indicators are extruded by the multidrug resistance protein. J Biol Chem 1993; 268: 21493-6.
12. Sarkadi B, Müller M, Homoloya L, et al. Interaction of bioactive hydrophobic peptides with the human multidrug transporter. FASEB J 1994; 8: 766-70.
13. Al-Shawi MK, Senior AE. Characterization of the adenosine triphosphatase activity of Chinese hamster P-glycoprotein. J Biol Chem 1993; 268: 4197-206.
14. Rao US, Scarborough GA. Direct demonstration of high affinity interactions of immunosuppressant drugs with the drug binding site of the human P-glycoprotein. Mol Pharmacol 1994; 45: 773-6
15. Sharom FJ, DiDiodato G, Yu X, Ashbourne KJD. Interaction of the P-glycoprotein multidrug transporter with peptides and ionophores. J Biol Chem 1995; 270: 10334-41.
16. Shapiro AB, Ling V. ATPase activity of purified and reconstituted P-glycoprotein from Chinese hamster ovary cells. J Biol Chem 1994; 269: 3745-54.
17. Sharom F. Characterization and functional reconstitution of the multidrug transporter. J Bioenerget Biomem 1995; 27: 15-22.
18. Ambudkar SV. Purification and reconstitution of functional human P-glycoprotein. J Bioenerget Biomemb 1995; 27: 23-9.
19. Shapiro AB, Ling V. Reconstitution of drug transport by purified P-glycoprotein. J Biol Chem 1995; 270: 16167-75.
20. Shapiro AB, Ling V. Using purified P-glycoprotein to understand multidrug resistance. J Bioenerget Biomem 1995; 27: 7-13.
21. Bellamy WT, Dalton WS. Multidrug resistance in the laboratory and clinic. Adv Clin Chem 1994; 31: 1-61.
22. Ford JM. Experimental reversal of P-glycoprotein-mediated multidrug resistance by pharmacological chemosensitizers. Eur J Cancer 1996; 32A: 991-1001.
23. Yusa K, Tsuruo T. Reversal mechanism of multidrug resistance by verapamil. Cancer Res 1989; 49: 5002-6.
24. 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 Nat Cancer Inst 1993; 85: 311-6.
25. Saeki T, Ueda K, Tanigawara Y, Hori R, Komano T. Human P-glycoprotein transports cyclosporin A and FK506. J Biol Chem 1993; 268: 6077-80.
26. Raderer M, Scheithauer W. Clinical trials of agents that reverse multidrug resistance. Cancer 1993; 72: 3553-63.
27. Fisher GA, Sikic BI. Clinical studies with modulators of multidrug resistance. Hematol Oncol Clin Am 1995; 9: 363-82.
28. Boesch D, Muller K, Pourtier-Manzanedo A, Loor E Restoration of daunomycin retention in multidrug-resistant P388 cells by submicromolar concentrations of SDZ PSC 833, an nonimmunosuppressive cyclosporin derivative. Exp Cell Res 1991; 196: 26-32.
29. Hyafil F, Vergely C, Duvignaud P, Grandperret T. In vitro and in vivo reversal of multidrug resistance by GF120918, an acridonecarboxamide derivative. Cancer Res 1993; 53: 4595-602.
30. Sato W, Fukuzawa N, Nakanishi O, et al. Reversal of multidrug resistance by a novel quinoline derivative, MS-209. Cancer Chemother Pharmacol 1995; 35: 271-7.
31. Hofmann J, Gekeler V, Ise W, et al. Mechanism of action of dexniguldipine-HCI (B8509-035), a new potent modulator of multidrug resistance. Biochem Pharmacol 1995; 49: 603-9.
32. Shudo N, Mizoguchi T, Kiyosue T, et al. Two pyridine analogues with more effective ability to reverse multidrug resistance and with lower calcium channel blocking activity than their dihydropyridine counterparts. Cancer Res 1990; 50: 3055-61.
33. Slate DL, Bruno NA, Casey SM, et al. RS-33295-198: a novel potent modulator of P-glycoprotein-mediated multidrug resistance. Anticancer Res 1995; 15: 811-4.
34. Arceci RJ, Stieglitz K, Bierer BE. Immunosuppressants FK506 and rapamycin function as reversal agents of the multidrug resistance phenotype. Blood 1992; 80: 1528-36.
35. Harding MW, Galat A, Uehling DE, Schreiber SL. A receptor for the immunorepressant FK506 is a cistrans peptidyl-prolyl isomerase. Nature 1989; 341: 758-60.
36. Bierer BE, Mattila PS, Standaert RF, et al. Two distinct signal transmission pathways in T lymphocytes are inhibited by complexes formed between an immunophilin and either FK506 or rapamycin. Proc Natl Acad Sci USA 1990; 87: 9231-5.
37. Armistead DM, Badia MC, Deininger DD, et al. Design, synthesis and structure of non-macrocyclic inhibitors of FKBP12, the major binding protein for the immunosuppressant FK506. Acta Crystallogr 1995; D51: 522-8.
38. Park ST, Aldape RA, Futer O, DeCenzo MT, Livingston DJ. PPlase catalysis by human FK506-binding protein proceeds through a conformational twist mechanism. J Biol Chem 1992; 267: 3316-24.
39. Calvo V, Crews CM, Vik TA, Bierer BE. Interleukin 2 stimulation of p70 S6 kinase activity is inhibited by the immunosuppressant rapamycin. Proc Natl Acad Sci USA 1992; 89: 7571-5.
40. Fruman DA, Klee C, Bierer BE, Burakoff SJ. Calcineurin phosphatase activity in T lymphocytes is inhibited by FK506 and calcineurin A. Proc Natl Acad Sci USA 1992; 89: 3686-90.
41. Wilson KP, Yamshita MM, Sintchak MD, et al. Immune system applications of structure-aided drug design. Acta Crystallogr 1995; D51: 511-21.
42. Dalton WS, Grogan TM, Meltzer PS, et al. Drug resistance in multiple myeloma and non-Hodgkin's Iymphoma: detection of P-glycoprotein and potential circumvention by addition of verapamil to chemotherapy. J Clin Oncol 1989; 7: 415-24
43. Shen DW, Cardarelli C, Hwang J, et al. Multiple drug-resistant human KB carcinoma cells independently selected for high-level resistance to colchicine, adriamycin, or vinblastine show changes in expression of specific proteins. J Biol Chem 1986; 261: 7762-70.
44. Hait WN, Aftab DT. Rational design and pre-clinical pharmacology of drugs for reversing multidrug resistance. Biochem Pharmacol 1992; 43: 103-7.
45. Germann UA, Chambers TC, Ambudkar SV, et al. Characterization of phosphorylation-defective mutants of human P-glycoprotein expressed in mammalian cells. J Biol Chem 1996; 271: 1708-16.
46. Lemontt JF, Azzaria M, Gros P. Increased mdr gene expression and decreased drug accumulation in multidrug resistant human melanoma cells. Cancer Res 1988; 48: 6348-53.
47. Slater LM, Murray SL, Wetzel MW, Sweet P, Stupecky M. Verapamil potentiation of VP-16-213 in acute lymphatic leukemia and reversal of pleiotropic drug resistance. Cancer Chemotber Pharmacol 1986; 16: 50-4.
48. Slater LM, Cho J, Wetzel M. Cyclosporin A potentiation of VP-16: production of long-term survival in murine acute lymphatic leukemia. Cancer Chemother Pharmacol 1992; 1992: 53-6.
49. Roehm NW, Rodgers GH, Hatfield SM, Glasebrook AL. An improved colorimetric assay for cell proliferation and viability utilizing the tetrazolium salt XTT. J Immunol Methods 1991; 142: 257-65.
50. 3H]vinblastine from Chinese hamster ovary cells transfected with a full-length complimentary DNA clone for the mdr1 gene. Cancer Res 1989; 49: 3867-71.
51. Bruggemann EP, Germann UA, Gottesman MM, Pastan I. Two different regions of P-glycoprotein are photoaffinity labeled by azidopine. J Biol Chem 1989; 264: 15483-8.
52. Dalton WS, Grogan TM, Rybski JA, et al. Immunohistochemical detection and quantitation of P-glycoprotein in multiple drug-resistant human myeloma cells: association with level of drug resistance and drug accumulation. Blood 1989; 73: 747-52.
53. Feller N, Kuiper CM, Lankelma J, et al. Functional detection of MDR1/P170 and MRP/P190 mediated multidrug resistance in tumour cells by flow cytometry. Br J Cancer 1995; 72: 543-9.
54. Piwnica-Worms D, Chiu ML, Budding M, et al. Functional imaging of multidrug-resistant P-glycoprotein with an organotechnetium complex. Cancer Res 1993; 53: 977-84.
55. Safa AR. Photoaffinity labeling of P-glycoprotein in multidrug-resistant cells. Cancer Invest 1993; 11: 46-56.
56. Greenberger LM. Major photoaffinity drug labeling sites for iodoaryl azidoprazosin in P-glycoprotein are within, or immediately C-terminal to, transmembrane domains 6 and 12. J Biol Chem 1993; 268: 11411-25.
57. Germann UA, Ford PJ, Shlyakhter D, Mason VS and Harding MW. Chemosensitization and drug accumulation effects of VX-710, verapamil, cyclosporin A, MS-209 and GF120918 in multidrug resistant HL60/ADR cells expressing the multidrug resistance-associated protein MPR. Anti-Cancer Drugs 1997; 8: 141-55.
58. Naito M, Tsuge H, Kuroko C, Tomida A, Tsuruo T. Enhancement of reversing effect of Cyclosporin-A on vincristine resistance by anti-P-glycoprotein monoclonal antibody MRK-16. Jpn J Cancer Res 1993; 84: 489-492.
59. Hauske JR, Kajiji S, Dorff P, et al. Investigation of the effects of synthetic, non-cytotoxic immunophilin inhibitors on mdr. Bioorg Med Chem 1994; 4: 2097-101.
60. Marsh W, Sichert D, Center MS. Isolation and characterization of adriamycin-resistant HL-60 cells which are not defective in the initial intracellular accumulation of drug. Cancer Res 1986; 46: 4053-7.
61. Chaturvedi P, Decker C, Harding MW, Schmalbach T. Evaluation of pharmacokinetic interactions of VX-710 with doxorubicin and paclitaxel in beagle dogs. Proc Am Ass Cancer Res 1996; 37: 373.
62. Peck RA, Marshall J, Ziessman H, et al. A phase I trial of doxorubicin and VX-710. Proc Am Ass Cancer Res 1996; 37: 165.