The P-glycoprotein multidrug transporter

Essays in Biochemistry

Volumn 50, Issue 1, 2011, Pages 161-178

  Sharom, Frances J ^a  

^a UNIVERSITY OF GUELPH   (Canada)

Author keywords

[No Author keywords available]

Indexed keywords

ADENOSINE TRIPHOSPHATE; GLYCOPROTEIN P;

BLOOD BRAIN BARRIER; HUMAN; METABOLISM; PHARMACOKINETICS; REVIEW; TISSUE DISTRIBUTION; X RAY CRYSTALLOGRAPHY;

ADENOSINE TRIPHOSPHATE; BLOOD-BRAIN BARRIER; CRYSTALLOGRAPHY, X-RAY; HUMANS; P-GLYCOPROTEINS; PHARMACOKINETICS; TISSUE DISTRIBUTION;

EID: 84856271899     PISSN: 00711365     EISSN: None     Source Type: Journal    
DOI: 10.1042/BSE0500161     Document Type: Article

References (55)

1. Juliano, R.L. and Ling, V. (1976) A surface glycoprotein modulating drug permeability in Chinese hamster ovary cell mutants. Biochim. Biophys. Acta 455, 152-162
2. Alvarez, M., Paull, K., Monks, A., Hose, C., Lee, J.S., Weinstein, J., Grever, M., Bates, S. and Fojo, T. (1995) 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
3. Thiebaut, F., Tsuruo, T., Hamada, H., Gottesman, M.M., Pastan, I. and Willingham, M.C. (1987) Cellular localization of the multidrug-resistance gene product P-glycoprotein in normal human tissues. Proc. Natl. Acad. Sci. U.S.A. 84, 7735-7738
4. Schinkel, A.H. (1999) P-glycoprotein, a gatekeeper in the blood-brain barrier. Adv. Drug Delivery Rev. 36, 179-194
5. Schinkel, A.H., Smit, J.J., van Tellingen, O., Beijnen, J.H., Wagenaar, E., van Deemter, L., Mol, C.A., van der Valk, M.A., Robanus-Maandag, E.C. and te Riele, H.P. (1994) Disruption of the mouse mdr1a P-glycoprotein gene leads to a deficiency in the blood-brain barrier and to increased sensitivity to drugs. Cell 77, 491-502
6. Eckford, P.D. and Sharom, F.J. (2009) ABC efflux pump-based resistance to chemotherapy drugs. Chem. Rev. 109, 2989-3011
7. Ruetz, S. and Gros, P. (1994) Phosphatidylcholine translocase: a physiological role for the mdr2 gene. Cell 77, 1071-1081
8. Smit, J.J., Schinkel, A.H., Oude Elferink, R.P., Groen, A.K., Wagenaar, E., van Deemter, L., Mol, C.A., Ottenhoff, R., van der Lugt, N.M. and van Roon, M.A. (1993) Homozygous disruption of the murine mdr2 P-glycoprotein gene leads to a complete absence of phospholipid from bile and to liver disease. Cell 75, 451-462
9. Oude Elferink, R.P. and Paulusma, C.C. (2007) Function and pathophysiological importance of ABCB4 (MDR3 P-glycoprotein). Pflügers Arch. 453, 601-610
10. Stieger, B., Meier, Y. and Meier, P.J. (2007) The bile salt export pump. Pflügers Arch. 453, 611-620
11. Robert, J. and Jarry, C. (2003) Multidrug resistance reversal agents. J. Med. Chem. 46, 4805-4817
12. Saeki, T., Ueda, K., Tanigawara, Y., Hori, R. and Komano, T. (1993) Human P-glycoprotein transports cyclosporin A and FK506. J. Biol. Chem. 268, 6077-6080
13. Dantzig, A.H., Law, K.L., Cao, J. and Starling, J.J. (2001) Reversal of multidrug resistance by the P-glycoprotein modulator, LY335979, from the bench to the clinic. Curr. Med. Chem. 8, 39-50
14. Loo, T.W. and Clarke, D.M. (2000) Blockage of drug resistance in vitro by disulfiram, a drug used to treat alcoholism. J. Natl. Cancer Inst. 92, 898-902
15. Woodcock, D.M., Linsenmeyer, M.E., Chojnowski, G., Kriegler, A.B., Nink, V., Webster, L.K. and Sawyer, W.H. (1992) Reversal of multidrug resistance by surfactants. Br. J. Cancer 66, 62-68
16. Breedveld, P., Beijnen, J.H. and Schellens, J.H. (2006) Use of P-glycoprotein and BCRP inhibitors to improve oral bioavailability and CNS penetration of anticancer drugs. Trends Pharmacol. Sci. 27, 17-24
17. Rosenberg, M.F., Callaghan, R., Modok, S., Higgins, C.F. and Ford, R.C. (2005) Three-dimensional structure of P-glycoprotein: the transmembrane regions adopt an asymmetric configuration in the nucleotide-bound state. J. Biol. Chem. 280, 2857-2862
18. Aller, S.G., Yu, J., Ward, A., Weng, Y., Chittaboina, S., Zhuo, R., Harrell, P.M., Trinh, Y.T., Zhang, Q., Urbatsch, I.L. and Chang, G. (2009) Structure of P-glycoprotein reveals a molecular basis for poly-specific drug binding. Science 323, 1718-1722
19. Dawson, R.J. and Locher, K.P. (2006) Structure of a bacterial multidrug ABC transporter. Nature 443, 180-185
20. Ward, A., Reyes, C.L., Yu, J., Roth, C.B. and Chang, G. (2007) Flexibility in the ABC transporter MsbA: alternating access with a twist. Proc. Natl. Acad. Sci. U.S.A. 104, 19005-19010
21. Loo, T.W. and Clarke, D.M. (2005) Do drug substrates enter the common drug-binding pocket of P-glycoprotein through "gates"? Biochem. Biophys. Res. Commun. 329, 419-422
22. Sharom, F.J. (2007) Multidrug resistance protein: P-glycoprotein. In Drug Transporters: Molecular Characterization and Role in Drug Disposition (You, G. and Morris, M.E., eds), pp. 223-262, John Wiley & Sons, Hoboken
23. Scala, S., Akhmed, N., Rao, U.S., Paull, K., Lan, L.B., Dickstein, B., Lee, J.S., Elgemeie, G.H., Stein, W.D. and Bates, S.E. (1997) P-glycoprotein substrates and antagonists cluster into two distinct groups. Mol. Pharmacol. 51, 1024-1033
24. Doige, C.A. and Sharom, F.J. (1992) Transport properties of P-glycoprotein in plasma membrane vesicles from multidrug-resistant Chinese hamster ovary cells. Biochim. Biophys. Acta 1109, 161-171
25. Sharom, F.J., Yu, X. and Doige, C.A. (1993) Functional reconstitution of drug transport and ATPase activity in proteoliposomes containing partially purified P-glycoprotein. J. Biol. Chem. 268, 24197-24202
26. Lu, P., Liu, R. and Sharom, F.J. (2001) Drug transport by reconstituted P-glycoprotein in proteoliposomes: effect of substrates and modulators, and dependence on bilayer phase state. Eur. J. Biochem. 268, 1687-1697
27. Shapiro, A.B. and Ling, V. (1997) Positively cooperative sites for drug transport by P-glycoprotein with distinct drug specificities. Eur. J. Biochem. 250, 130-137
28. Higgins, C.F. and Gottesman, M.M. (1992) Is the multidrug transporter a flippase? Trends Biochem. Sci. 17, 18-21
29. Eckford, P.D. and Sharom, F.J. (2006) P-glycoprotein (ABCB1) interacts directly with lipid-based anti-cancer drugs and platelet-activating factors. Biochem. Cell Biol. 84, 1022-1033
30. Raggers, R.J., Vogels, I. and van Meer, G. (2001) Multidrug-resistance P-glycoprotein (MDR1) secretes platelet-activating factor. Biochem. J. 357, 859-865
31. Romsicki, Y. and Sharom, F.J. (2001) Phospholipid flippase activity of the reconstituted P-glycoprotein multidrug transporter. Biochemistry 40, 6937-6947
32. Oswald, C., Holland, I.B. and Schmitt, L. (2006) The motor domains of ABC-transporters: what can structures tell us? Naunyn Schmiedeberg's Arch. Pharmacol. 372, 385-399
33. Smith, P.C., Karpowich, N., Millen, L., Moody, J.E., Rosen, J., Thomas, P.J. and Hunt, J.F. (2002) ATP binding to the motor domain from an ABC transporter drives formation of a nucleotide sandwich dimer. Mol. Cell 10, 139-149
34. Jones, P.M. and George, A.M. (1999) Subunit interactions in ABC transporters: towards a functional architecture. FEMS Microbiol. Lett. 179, 187-202
35. Loo, T.W., Bartlett, M.C. and Clarke, D.M. (2002) The "LSGGQ" motif in each nucleotide-binding domain of human P-glycoprotein is adjacent to the opposing Walker A sequence. J. Biol. Chem. 277, 41303-41306
36. Callaghan, R., Ford, R.C. and Kerr, I.D. (2006) The translocation mechanism of P-glycoprotein. FEBS Lett. 580, 1056-1063
37. Urbatsch, I.L., Sankaran, B., Weber, J. and Senior, A.E. (1995) P-glycoprotein is stably inhibited by vanadate-induced trapping of nucleotide at a single catalytic site. J. Biol. Chem. 270, 19383-19390
38. Senior, A.E., al-Shawi, M.K. and Urbatsch, I.L. (1995) The catalytic cycle of P-glycoprotein. FEBS Lett. 377, 285-289
39. Tombline, G. and Senior, A.E. (2005) The occluded nucleotide conformation of P-glycoprotein. J. Bioenerg. Biomembr. 37, 497-500
40. Siarheyeva, A., Liu, R. and Sharom, F.J. (2010) Characterization of an asymmetric occluded state of P-glycoprotein with two bound nucleotides: implications for catalysis. J. Biol. Chem. 285, 7575-7586
41. Sauna, Z.E., Kim, I.W., Nandigama, K., Kopp, S., Chiba, P. and Ambudkar, S.V. (2007) Catalytic cycle of ATP hydrolysis by P-glycoprotein: evidence for formation of the E.S reaction intermediate with ATPγS, a nonhydrolyzable analogue of ATP. Biochemistry 46, 13787-13799
42. Higgins, C.F. and Linton, K.J. (2004) The ATP switch model for ABC transporters. Nat. Struct. Mol. Biol. 11, 918-926
43. Janas, E., Hofacker, M., Chen, M., Gompf, S., Van der Does, C. and Tampe, R. (2003) The ATP hydrolysis cycle of the nucleotide-binding domain of the mitochondrial ATP-binding cassette transporter Mdl1p. J. Biol. Chem. 278, 26862-26869
44. Sharom, F.J. (2008) ABC multidrug transporters: structure, function and role in chemoresistance. Pharmacogenomics 9, 105-127
45. Zhou, S.F. (2008) Structure, function and regulation of P-glycoprotein and its clinical relevance in drug disposition. Xenobiotica 38, 802-832
46. Staud, F., Ceckova, M., Micuda, S. and Pavek, P. (2010) Expression and function of p-glycoprotein in normal tissues: effect on pharmacokinetics. Methods Mol. Biol. 596, 199-222
47. Borrelli, F. and Izzo, A.A. (2009) Herb-drug interactions with St John's wort (Hypericum perforatum): an update on clinical observations. AAPS J. 11, 710-727
48. Giacomini, K.M., Huang, S.M., Tweedie, D.J., Benet, L.Z., Brouwer, K.L., Chu, X., Dahlin, A., Evers, R., Fischer, V., Hillgren, K.M. et al. (2010) Membrane transporters in drug development. Nat. Rev. Drug Discovery 9, 215-236
49. Choudhuri, S. and Klaassen, C.D. (2006) Structure, function, expression, genomic organization, and single nucleotide polymorphisms of human ABCB1 (MDR1), ABCC (MRP), and ABCG2 (BCRP) efflux transporters. Int. J. Toxicol. 25, 231-259
50. Sharom, F.J. and Siarheyeva, A. (2008) Functional assays for identification of compounds that interact with P-gp. In Multidrug Resistance: Biological and Pharmaceutical Advances in Antitumour Treatment (Colabufo, N.A., ed.), pp. 261-290, Research Signpost, Trivandrum
51. Polgar, O. and Bates, S.E. (2005) ABC transporters in the balance: is there a role in multidrug resistance? Biochem. Soc. Trans. 33, 241-245
52. Steinbach, D. and Legrand, O. (2007) ABC transporters and drug resistance in leukemia: was P-gp nothing but the first head of the Hydra? Leukemia 21, 1172-1176
53. Szakacs, G., Paterson, J.K., Ludwig, J.A., Booth-Genthe, C. and Gottesman, M.M. (2006) Targeting multidrug resistance in cancer. Nat. Rev. Drug Discovery 5, 219-234
54. Coley, H.M. (2010) Overcoming multidrug resistance in cancer: clinical studies of P-glycoprotein inhibitors. Methods Mol. Biol. 596, 341-358
55. Chan, H.S., DeBoer, G., Thiessen, J.J., Budning, A., Kingston, J.E., O'Brien, J.M., Koren, G., Giesbrecht, E., Haddad, G., Verjee, Z. et al. (1996) Combining cyclosporin with chemotherapy controls intraocular retinoblastoma without requiring radiation. Clin. Cancer Res. 2, 1499-1508