Domain exchangeability between the multidrug transporter (MDR1) and phosphatidylcholine flippase (MDR2)

Molecular Pharmacology

Volumn 56, Issue 5, 1999, Pages 997-1004

  Zhou, Yi ^a   Gottesman, Michael M ^a   Pastan, Ira ^a  

^a NATIONAL CANCER INSTITUTE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

GLYCOPROTEIN P;

AMINO TERMINAL SEQUENCE; ARTICLE; CONTROLLED STUDY; DRUG RECEPTOR BINDING; ENZYME ANALYSIS; MULTIDRUG RESISTANCE; PHOTOAFFINITY LABELING; PRIORITY JOURNAL; PROTEIN BINDING; PROTEIN DOMAIN; SITE DIRECTED MUTAGENESIS;

EID: 0032731917     PISSN: 0026895X     EISSN: None     Source Type: Journal    
DOI: 10.1124/mol.56.5.997     Document Type: Article

References (36)

1. Bosch I, Dunussi-Joannopouloa K, Wu RL, Furlong ST and Croop J (1997) Phosphatidylcholine and phosphatidylethanolamine behave as substrates of the human MDR1 P-glycoprotein. Biochemistry 36:5685-5694.
2. Bruggemann EP, Currier SJ, Gottesman MM and Pastan I (1992) Characterization of the azidopine and vinblastine binding site of P-glycoprotein. J Biol Chem 267:21020-21026.
3. Bruggemann EP, Germann UA, Gottesman MM and Pastan I (1989) Two different regions of P-glycoprotein are photoaffinity labeled by azidopine. J Biol Chem 264:15483-15488.
4. Buschman E and Gros P (1991) Functional analysis of chimeric genes obtained by exchanging homologous domains of the mouse mdr1 and mdr2 genes. Mol Cell Biol 11:595-603.
5. Buschman E and Gros P (1994) The inability of the mouse mdr2 gene to confer multidrug resistance is linked to reduced drug binding to the protein. Cancer Res 54:4892-4898.
6. Chen C-J, Chin JE, Ueda K, Clark D, Pastan I, Gottesman MM and Roninson IB (1986) Internal duplication and homology with bacterial transport proteins in the mdr1 (P-glycoprotein) gene from multidrug-resistant human cells. Cell 47:381-389.
7. Currier SJ, Kane SE, Willingham MC, Cardarelli CO, Pastan I and Gottesman MM (1992) Identification of residues in the first cytoplasmic loop of P-glycoprotein involved in the function of chimeric human MDR1-MDR2 transporters. J Biol Chem 267:25153-25159.
8. Elroy-Stein O, Fuerst TR and Moss B (1989) Cap-independent translation of mRNA conferred by encephalomyocarditis virus 5′ sequence improves the performance of the vaccinia virus/bacteriophage T7 hybrid expression system. Proc Natl Acad Sci USA 86:6126-6130.
9. Fuerst TR, Niles EG, Studier FW and Moss B (1986) Eukaryotic transient-expression system based on recombinant vaccinia virus that synthesizes bacteriophage T7 RNA polymerase. Proc Natl Acad Sci USA 83:8122-8126.
10. Gottesman MM, Hrycyna CA, Schoenlein PV, Germann UA and Pastan I (1995) Genetic analysis of the multidrug transporter. Annu Rev Genet 29:607-649.
11. Greenberger LM (1993) 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 268:11417-11425.
12. Greenberger LM, Lisanti CJ, Silva JT and Horwitz SB (1991) Domain mapping of the photoaffinity drug-binding sites in P-glycoprotein encoded by mouse mdr1b. J Biol Chem 266:20744-20751.
13. Hefkemeyer P, Dey S, Ambudkar SV, Hrycyna CA, Pastan I and Gottesman MM (1998) Contribution to substrate specificity and transport of nonconserved residues in transmembrane domain 12 of human P-glycoprotein, Biochemistry 37: 16400-16409.
14. Hrycyna CA, Ramachandra M, Ambudkar SV, Ko YH, Pedersen PL, Pastan I and Gottesman MM (1998) Mechanism of action of human P-glycoprotein ATPase activity. Photochemical cleavage during a catalytic transition state using orthovanadate reveals cross-talk between the two ATP sites. J Biol Chem 273: 16631-16634.
15. Kino K, Taguchi Y, Yamada K, Komano T and Ueda K (1996) Aureobasidin A, an antifungal cyclic depsipeptide antibiotic, is a substrate for both human MDR1 and MDR2/P-glycoproteins. FEBS Lett 399:29-32.
16. Loo TW and Clarke DM (1994a) Reconstitution of drug-stimulated ATPase activity following co-expression of each half of human P-glycoprotein as separate polypeptides. J Biol Chem 269:7750-7755.
17. Loo TW and Clarke DM (1994b) 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.
18. Loo TW and Clarke DM (1996) Inhibition of oxidative cross-linking between engineered cysteine residues at positions 332 in predicted transmembrane segments (TM) 6 and 975 in predicted TM12 of human P-glycoprotein by drug substrates. J Biol Chem 271:27482-27487.
19. Loo TW and Clarke DM (1997a) Drug-stimulated ATPase activity of human P-glycoprotein requires movement between transmembrane segments 6 and 12. J Biol Chem 272:20986-20989.
20. Loo TW and Clarke DM (1997b) Identification of residues in the drug-binding site of human P-glycoprotein using a thiol-reactive substrate. J Biol Chem 272:31945-31948.
21. Mechetner EB, Schott B, Morse B, Sten WD, Druley T, Davis KA, Tsuruo T and Roninson IB (1997) P-glycoprotein function involves conformational transitions detectable by differential immunoreactivity. Proc Natl Acad Sci USA 94:12908-12913.
22. Morris DI, Greenberger LM, Bruggemann EP, Cardarelli C, Gottesman MM, Pastan I and Seamon KB (1994) Localization of the forskolin labeling sites to both halves of P-glycoprotein: Similarity of the sites labeled by forskolin and prazosin. Mol Pharmacol 46:329-337.
23. Moss B (1991) Vaccinia virus: A tool for research and vaccine development. Science (Wash DC) 252:1662-1667.
24. Ramachandra M, Ambudkar SV, Chen D, Hrycyna CA, Dey S, Gottesman MM and Pastan I (1998) Human P-glycoprotein exhibits reduced affinity for substrates during a catalytic transition state. Biochemistry 37:5010-5019.
25. Ramachandra M, Ambudkar S, Gottesman MM, Pastan I and Hrycyna CA (1996) Functional characterization of a glycine 185 to valine substitution in human P-glycoprotein using a vaccinia based transient expression system. Mol Biol Cell 7:1485-1498.
26. Raviv Y, Pollard HB, Bruggemann EP, Pastan I and Gottesman MM (1990) Photosensitized labeling of a functional multidrug transporter in living drug-resistant tumor cells. J Biol Chem 268:3975-3980.
27. Ruetz S and Gros P (1994) Phosphatidylcholine translocase: A physiological role for the mdr2 gene. Cell 77:1071-1081.
28. Schinkel AH, Roelofs MEM and Borst P (1991) Characterization of the human MDR3 P-glycoprotein and its recognition by P-glycoprotein-specific monoclonal antibodies. Cancer Res 51:2628-2635.
29. Smit JJ, Schinkel AH, Elferink RP, Groen AK, Wagenaar E, van Deemter L, Mol CA, Ottenhoff R, van der Lugt NM, van Roon MA, van Andervalk MA, Offerhaus GJ, Berns AJ and Borst P (1993) Homozygous disruption of the murine mdr2 P-glycoprotein gene leads to a complete absence of phospholipid from bile and to liver disease. Cell 78:451-462.
30. Tamai I and Safa AR (1991) Azidopine noncompetitively interacts with vinblastine and cyclosporin A binding to P-glycoprotein in multidrug resistant cells. J Biol Chem 266:16796-16800.
31. van der Bliek AM, Kooiman PM, Schneider C and Borst P (1988) Sequence of mdr3 cDNA encoding a human P-glycoprotein. Gene 71:401-411.
32. van Helvoort A, Smith AJ, Sprang H, Fritzsche I, Schinkel AH, Borst P and van Meer G (1996) MDR1 P-glycoprotein is a lipid translocase of broad specificity, while MDR3 P-glycoprotein specifically translocates phosphatidylcholine. Cell 87:507-517.
33. Wang G, Pincheira R, Zhang A and Zhang J (1997) Conformational changes of P-glycoprotein by nucleotide binding. Biochemistry 328:897-904.
34. Zhang X, Collins KI and Greenberger LM (1995) 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.
35. Zhou Y, Gottesman MM and Pastan I (1999a) Studies of human MDR1/MDR2 chimeras demonstrate the functional exchangeability of a major transmembrane segment of the multidrug transporter and the phosphatidylcholine flippase. Mol Cell Biol 19:1450-1459.
36. Zhou Y, Gottesman MM and Pastan I (1999b) The extracellular loop between TM5 and TM6 of P-glycoprotein is required for reactivity with monoclonal antibody U1C2. Arch Biochem Biophys 367:74-80.