P-glycoprotein substrates and antagonists cluster into two distinct groups

Molecular Pharmacology

Volumn 51, Issue 6, 1997, Pages 1024-1033

  Scala, Stefania ^a   Akhmed, Nadia ^a   Rao, U S ^b   Paull, Ken ^a   Lan, Lu Bin ^c   Dickstein, Bruce ^a   Lee, Jong Seok ^d   Elgemeie, Galal H ^e   Stein, Wilfred D ^c   Bates, Susan E ^a  

^a NATIONAL CANCER INSTITUTE   (United States)

^b UNIVERSITY OF NORTH CAROLINA SCHOOL OF MEDICINE   (United States)

^c HEBREW UNIVERSITY OF JERUSALEM   (Israel)

^d Gyeongsang National University   (South Korea)

^e HELWAN UNIVERSITY   (Egypt)

Author keywords

[No Author keywords available]

Indexed keywords

ADENOSINE TRIPHOSPHATASE; ADENOSINE TRIPHOSPHATE; AZIDOPINE; COLCHICINE; CYCLOSPORIN A; DOXORUBICIN; GLYCOPROTEIN P; MESSENGER RNA; PACLITAXEL; RHODAMINE; RHODAMINE 123; THALICARPINE; VALSPODAR; VERAPAMIL; VINBLASTINE;

ANIMAL CELL; ARTICLE; BINDING SITE; COLON CARCINOMA; CONTROLLED STUDY; CROSS RESISTANCE; CYTOTOXICITY; DRUG ACCUMULATION; DRUG POTENCY; DRUG TRANSPORT; ENZYME ACTIVITY; FLOW CYTOMETRY; FLUORESCENCE; HUMAN; HUMAN CELL; LEPIDOPTERA; MULTIDRUG RESISTANCE; NONHUMAN; PRIORITY JOURNAL; PROTEIN INTERACTION;

EID: 0030976879     PISSN: 0026895X     EISSN: None     Source Type: Journal    
DOI: 10.1124/mol.51.6.1024     Document Type: Article

References (46)

1. Gottesman, M. M., and I. Pastan. Biochemistry of multidrug resistance mediated by the multidrug transporter. Annu. Rev. Biochem. 62:385-427 (1993).
2. Fojo, A. T., K. Ueda, D. J. Slamon, D. G. Poplack, M. M. Gottesman, and I. Pastan. Expression of a multidrug resistance gene in human tumors and tissues. Proc. Natl. Acad. Sci. USA 84:265-269 (1987).
3. Eytan, G., R. Borgnia, R. Regev, and Y. Assaraf. Transport of polypeptide ionophores into proteoliposomes reconstituted with rat liver P-glycoprotein. J. Biol. Chem. 269:26058-26065 (1994).
4. Raymond, M., P. Gros, M. Whiteway, and D. Thomas. Functional complementation of yeast ste6 by a mammalian multidrug resistance mdr gene. Science (Washington D. C.) 232-234 (1992).
5. Deverson, E., I. Gow, W. Coadwell, J. Monaco, G. Butcher, and J. Howard. MHC class II region encoding proteins related to the multidrug resistance family of transmembrane transporters. Nature (Lond.) 348:738-741 (1990).
6. Masci, A., S. Scala, L. Racioppi, and S. Zappacosta. Cell surface expression of Major Histocompatibility class I antigens is modulated by the P-glycoprotein transporter. Hum. Immunol. 42:245-253 (1995).
7. Sharom, G., G. Diodato, X. Yu, and K. Ashbourne. Interactions of the P-glycoprotein multidrug transporter with peptides and ionophores. J. Biol. Chem. 270:10334-10341 (1995).
8. Hait, W., and D. Aftab. Rational design and pre-clinical pharmacology of drugs for reversing multidrug resistance. Biochem. Pharmacol. 43:103-107 (1992).
9. Ford, J., and W. Hait. Pharmacologic circumvention of multidrug resistance. Cytotech. 12:171-212 (1993).
10. Cardarelli, C., I. Aksentijevich, I. Pastan, and M. Gottesman. Differential effects of P-glycoprotein inhibitors on NIH3T3 cells transfected with wild type (G185) or mutant (V185) multidrug transporter. Cancer Res. 55: 1086-1091 (1995).
11. Rao, U. Mutation of glycine 185 to valine alters the ATPase function of the human P-glycoprotein expressed in Sf9 cells. J. Biol. Chem. 270:6686-6690 (1995).
12. 939/941 position in predicted transmembrane domain 11 of P-glycoproteins. Biochemistry 32: 9492-9497 (1993).
13. Loo, T. W., and D. M. Clarke. Functional consequences of phenylalanine mutations in the predicted transmembrane domain of P-glycoprotein. J. Biol. Chem. 268:19965-19972 (1993).
14. Loo, T. W., and D. M. Clarke. Functional consequences of proline mutations in the predicted transmembrane domain of P-glycoprotein. J. Biol. Chem. 268:3143-3149 (1993).
15. Loo, T. W., and D. M. Clarke. Mutations to amino acids located in predicted transmembrane segment 6 (TM6) modulate the activity and substrate specificity of human P-glycoprotein. Biochemistry 33:14049-14057 (1994).
16. 939/941. Biochemistry 33:5041-5048 (1994).
17. Tamai, I., and A. R. Safa. Azidopine noncompetitively interacts with vinblastine and cyclosporin A binding to P-glycoprotein in multidrug resistant cells. J. Biol. Chem. 266:16796-16800 (1991).
18. Tamai, I., and A. Safa. Competitive interaction of cyclosporins with the vinca alkaloid-binding site of P-glycoprotein in multidrug resistant cells. J. Biol. Chem. 27:16509-16513 (1990).
19. Saeki, T., K. Ueda, Y. Tanigawara, R. Hori, and T. Komano. P-glycoprotein mediated transcellular transport of MDR-reversing agents. FEBS Lett. 324:99-102 (1993).
20. Bates, S. E., J. S. Lee, B. Dickstein, M. Spolyar, and A. T. Fojo. Differential modulation of P-glycoprotein transport by protein kinase inhibition. Biochemistry 32:9156-9164 (1993).
21. Barnes, K. M., B. Dickstein, Jr., G. B. Cutler, T. Fojo, and S. E. Bates. Steroid transport, accumulation, and antagonism of P-glycoprotein in multidrug-resistant cells. Biochemistry 35:4820-4827 (1996).
22. Paull, K. D., R. H. Shoemaker, L. Hodes, A. Monks, D. A. Scudiero, L. Rubinstein, J. Plowman, and M. R. Boyd. Display and analysis of patterns of differential activity of drugs against human tumor cell lines: development of mean graph and COMPARE algorithm. J. Natl. Cancer Inst. 81:1088-1092 (1989).
23. Lee, J. S., K. Paull, M. Alvarez, C. Hose, A. Monks, M. Grever, A. T. Fojo, and S. E. Bates. Rhodamine efflux patterns predict P-glycoprotein substrates in the National Cancer Institute Drug Screen. Mol. Pharmacol. 46:627-638 (1994).
24. Alvarez, M., K. Paull, A. Monks, C. Hose, J. S. Lee, J. Weinstein, M. Grever, S. Bates, and T. Fojo. Generation of a drug resistance profile by quantitation of mdr-1/P-glycoprotein in the cell lines of the National Cancer Institute Anticancer Drug Screen. J. Clin. Invest. 95:2205-2214 (1995).
25. Lai, G.-M., Y.-N. Chen, L. A. Mickley, A. T. Fojo, and S. E. Bates. P-glycoprotein expression and schedule dependence of Adriamycin cytotoxicity in human colon carcinoma cell lines. Int. J. Cancer 49:696-703 (1991).
26. Paull, K. D., C. M. Lin, L. Malspeis, and E. Hamel. Identification of novel antimitotic agents acting at the tubulin level by computer-assisted evaluation of differential cytotoxicity data. Cancer Res. 52:3892-3900 (1992).
27. Skehan, P., R. Storeng, D. Scudiero, A. Monks, J. McMahon, D. Vistica, J. T. Warren, H. Bokesch, S. Kenney, and M. R. Boyd. New colorimetric cytotoxicity assay for anticancer-drug screening. J. Natl. Cancer Inst. 82:1107-1112 (1990).
28. Bruggemann, E. P., U. A. Germann, M. M. Gottesman, and I. Pastan. Two different regions of phosphoglycoprotein are photoaffinity labeled by azidopine. J. Biol. Chem. 264:15483-15488 (1989).
29. Fojo, A., S. Akiyama, M. M. Gottesman, and I. Pastan. Reduced drug accumulation in multiply drug-resistant human KB carcinoma cell lines. Cancer Res. 45:3002-3007 (1985).
30. Sarkadi, B., E. Price, R. Boucher, U. Germann, and G. Scarborough. Expression of the human multidrug resistance cDNA in insect cells generates a high activity drug-stimulated ATPase. J. Biol. Chem. 267:4854-4858 (1992).
31. Lan, L.-B., S. Ayesh, E. Lyubimov, I. Pashinsky, and W. D. Stein. Kinetic parameters for reversal of the multidrug resistant pump as measured for drug accumulation and cell killing. Cancer Chemother. Pharmacol. 38: 181-190 (1966).
32. Ayesh, S., Y. Shao, and W. D. Stein. Cooperative, competitive, and non-competitive interactions between modulators of the multidrug resistance pump. Biochim. Biophys. Acta 1316:8-18 (1996).
33. Ludescher, C., J. Thaler, D. Drach, J. Drach, M. Spitaler, C. Gattringer, H. Huber, and J. Hofmann. Detection of activity of P-glycoprotein in human tumour samples using rhodamine 123. Br. J. Haematol. 82:161-168 (1992).
34. Chaudhary, P. M., and I. B. Roninson. Expression and activity of P-glycoprotein, a multidrug efflux pump, in human hematopoietic stem cells. Cell 66:85-94 (1991).
35. Lampidis, T. J., S. D. Bernal, I. C. Summerhayes, and L. B. Chen. Selective toxicity of rhodamine 123 in carcinoma cells in vitro. Cancer Res. 43:716-720 (1983).
36. Chen, G., and D. J. Waxman. Complete reversal by thaliblastine of 490-fold adriamycin resistance in multidrug-resistant (MDR) human breast cancer cells: evidence that multiple biochemical changes in MDR cells need not correspond to multiple functional determinants for drug resistance. J. Pharmacol. Exp. Ther. 274:1271-1277 (1995).
37. Safa, A. R. Photoaffinity labeling of the multidrug-resistance-related P-glycoprotein with photoactive analogs of verapamil. Proc. Natl. Acad. Sci. USA 85:7187-7191 (1988).
38. Safa, A. R., C. J. Glover, J. L. Sewell, M. Meyers, J. Biedler, and R. Felsted. Identification of the multidrug resistance-related membrane glycoprotein as an acceptor for calcium channel blockers. J. Biol. Chem. 262:7884-7888 (1987).
39. Safa, A. Photoaffinity labeling of P-glycoprotein in multidrug resistant cells. Cancer Invest. 10:295-305 (1992).
40. Urbatsch, I., M. K. Al-Shawi, and A. E. Senior. Characterization of the ATPase activity of the purified Chinese hamster P-glycoprotein. Biochemistry 33:7069-7076 (1994).
41. Choi, K., C. J. Chen, M. Kriegler, and I. B. Roninson. An altered pattern of cross-resistance in multidrug resistant human cells results from spontaneous mutations in the mdr-1 (P-glycoprotein) gene. Cell 53:519-529 (1988).
42. Zhang, X., K. I. Collins, and L. M. Greenberger. Functional evidence that transmembrane 12 and the loop between transmembrane 11 and 12 form part of the drug binding domain in P-glycoprotein encoded by MDR1. J. Biol. Chem. 270:5441-5448 (1995).
43. Loo, T. W., and D. M. Clarke. Functional consequences of glycine mutations in the predicted cytoplasmic loops of P-glycoprotein. J. Biol. Chem. 269:7243-7248 (1994).
44. Archinal-Mattheis, A., R. W. Rzepka, T. Watanabe, N. Kokubu, Y. Itoh, N. J. Combates, K. W. Bair, and D. Cohen. Analysis of the interaction of SDZ PSC 833 ([3′-keto-Bmt1]-Val2-cyclosporin), a multidrug resistance modulator, with P-glycoprotein. Oncol. Res. 7:603-610 (1995).
45. Al-Shawi, M. K., I. L. Urbatsch, and A. E. Senior. Covalent inhibitors of P-glycoprotein ATPase activity. J. Biol. Chem. 269:8986-8992 (1994).
46. Sharom, F., X. Yu, and C. Doige. Functional reconstitution of drug transport and ATPase activity in proteoliposomes containing partially purified P-glycoprotein. J. Biol. Chem. 268:24197-24202 (1993).