PET study on mice bearing human colon adenocarcinoma cells using [ 11C]GF120918, a dual radioligand for P-glycoprotein and breast cancer resistance protein

Nuclear Medicine Communications

Volumn 31, Issue 11, 2010, Pages 985-993

  Yamasaki, Tomoteru ^a   Kawamura, Kazunori ^a   Hatori, Akiko ^a   Yui, Joji ^a   Yanamoto, Kazuhiko ^a   Yoshida, Yuichiro ^a,b   Ogawa, Masanao ^a   Nengaki, Nobuki ^a,b   Wakisaka, Hidekatsu ^a   Fukumura, Toshimitsu ^a   Zhang, Ming Rong ^a  

^a NATIONAL INSTITUTE OF RADIOLOGICAL SCIENCES   (Japan)

^b Japan   (Japan)

Author keywords

breast cancer resistance protein; carbon 11; GF120918 (elacridar); human colon adenocarcinoma; multidrug resistance; P glycoprotein; positron emission tomography

Indexed keywords

BREAST CANCER RESISTANCE PROTEIN; CYCLOSPORIN A; DRUG METABOLITE; ELACRIDAR; ELACRIDAR CARBON 11; GLYCOPROTEIN P; RADIOLIGAND; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; AREA UNDER THE CURVE; ARTICLE; CANCER MODEL; CELL STRAIN CACO 2; COLON ADENOCARCINOMA; CONTROLLED STUDY; DRUG DISTRIBUTION; DRUG POTENTIATION; DRUG STRUCTURE; DRUG SYNTHESIS; DRUG UPTAKE; HUMAN; HUMAN CELL; IN VITRO STUDY; KIDNEY CELL; MALE; MOUSE; NONHUMAN; POSITRON EMISSION TOMOGRAPHY; PROTEIN EXPRESSION; PROTEIN FUNCTION; RADIOACTIVITY;

ACRIDINES; ADENOCARCINOMA; ANIMALS; ATP-BINDING CASSETTE TRANSPORTERS; BIOLOGICAL TRANSPORT; BLOTTING, WESTERN; CACO-2 CELLS; CARBON RADIOISOTOPES; COLONIC NEOPLASMS; DOGS; HUMANS; LIGANDS; MALE; MICE; NEOPLASM PROTEINS; P-GLYCOPROTEIN; POSITRON-EMISSION TOMOGRAPHY; TETRAHYDROISOQUINOLINES; TOMOGRAPHY, EMISSION-COMPUTED, SINGLE-PHOTON;

EID: 77957996931     PISSN: 01433636     EISSN: None     Source Type: Journal    
DOI: 10.1097/MNM.0b013e32833fbf87     Document Type: Article

References (40)

1. Benderra Z, Faussat AM, Sayada L, Perrot JY, Chaouri D, Marie JP, et al. Breast cancer resistance protein and P-glycoprotein in 149 adult acute myeloid leukemias. Clin Cancer Res 2004; 10:7896-7902.
2. Sarkadai B, Homolya L, Szakacs G, Varadi A. Human multidrug resistance ABCB and ABCG transporters: participation in a chemoimmunity defense system. Physiol Rev 2006; 86:1179-1236.
3. Sweet P, Chan PK, Slater LM. Cyclosporin A and verapamil enhancement of daunorubicin-produced nucleolar protein B23 translocation in daunorubicinresistant and -sensitive human and murine tumor cells. Cancer Res 1989; 49:677-680.
4. Watanabe T, Tsuge H, Oh-Hara T, Naito M, Tsuruo T. Comparative study on reversal efficacy of SDZ PSC 833, cyclosporin A and verapamil on multidrug resistance in vitro and in vivo. Acta Oncol 1995; 34:235-241.
5. Yusa K, Tsuruo T. Reversal mechanism of multidrug resistance by verapamil: direct binding of verapamil to P-glycoprotein on specific sites and transport of verapamil outward across the plasma membrane of K562/ADM cells. Cancer Res 1989; 15:5002-5006.
6. Rabindran SK, Ross DD, Doyle LA, Yang W, Greenberger LM. Fumitremorgan C reverses multidrug resistance in cells transfected with the breast cancer resistance protein. Cancer Res 2000; 60:47-50.
7. Enokizono J, Kusuhara H, Ose A, Schinkel AH, Sugiyama Y. Quantitative investigation of the role of breast cancer resistance protein (Bcrp/Abcg2) in limiting brain and testis penetration of xenobiotic compounds. Drug Metab Dispos 2008; 36:995-1002.
8. Boesch D, Gaveriaux C, Jachez B, Pourtier-Manzanedo A, Bollinger P, Loor F. In vivo circumvention of P-glycoprotein-mediated multidrug resistance of tumor cells with SDZ PSC 833. Cancer Res 1991; 51:4226-4233.
9. Allen JD, Van Loevezin A, Lakhai JM, Van der Valk M, Van Tellingen O, Reid G, 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; 1:417-425.
10. Francois H, Catherine V, Pierre DV, Thierry GP. In vitro and in vivo reversal of multidrug resistance by GF120918, an acridonecarboxamide derivative. Cancer Res 1993; 53:4595-4602.
11. Maliepaard M, Van Gastelen MA, Tohgo A, Hausheer FH, Van Waardenburg RC, De Jong LA, 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; 7:935-941.
12. De Bruin M, Miyake K, Litman T, Robey R, Bates SE. Reversal of resistance by GF120918 in cell lines expressing the half-transporter, MXR. Cancer Lett 1999; 146:117-126.
13. Dale IL, Tuffley W, Callaghan R, Holmes JA, Martin K, Luscombe M, et al. Reversal of P-glycoprotein-mediated multidrug resistance by XR9051, a novel diketopiperazine derivative. Br J Cancer 1998; 78:885-892.
14. Di Nicolantonio F, Knight LA, Glaysher S, Whitehouse PA, Mercer SJ, Sharma S, et al. Ex vivo reversal of chemoresistance by tariquidar (XR9576). Anticancer Drugs 2004; 15:861-869.
15. Fox E, Bates SE. Tariquidar (XR9576): a P-glycoprotein drug efflux pump inhibitor. Expert Rev Anticancer Ther 2007; 7:447-459.
16. Luo FR, Paranjpe PV, Guo A, Rubin E, Sinko P. Intestinal transport of irinotecan in Caco-2 cells and MDCK II cells overexpressing efflux transporters Pgp, cMOAT, and MRP1. Drug Metab Dispos 2002; 30:763-770.
17. Zhang Y, Benet LZ. Characterization of P-glycoprotein mediated transport of K02, a novel vinylsulfone peptidomimetic cysteine protease inhibitor, across MDR1-MDCK and Caco-2 cell monolayers. Pharm Res 1998; 15:1520-1524.
18. Szakacs G, Paterson JK, Ludwig JA, Booth-Genthe C, Gottesman MM. Targeting multidrug resistance in cancer. Nat Rev Drug Discov 2006; 5:219-234.
19. Kruijtzer CM, Beijnen JH, Rosing H, Ten Bokkel Huinink WW, Schot M, Jewell RC, et al. Increased oral bioavailability of topotecan in combination with the breast cancer resistance protein and P-glycoprotein inhibitor GF120918. J Clin Oncol 2002; 20:2943-2950.
20. Malingre MM, Beijnen JH, Rosing H, Koopman FJ, Jewell RC, Paul EM, et al. Co-administration of GF120918 significantly increases the systemic exposure to oral paclitaxel in cancer patients. Br J Cancer 2001; 84:42-47.
21. Doner B, Kuntner C, Bankstahl JP, Bankstahl M, Stanek J, Wanek T, et al. Synthesis and small-animal positron emission tomography evaluation of [11C]-elacridar as a radiotracer to assess the distribution of P-glycoprotein at the blood-brain barrier. J Med Chem 2009; 52:6073-6082.
22. Wang RB, Kuo CL, Lien LL, Lien EJ. Structure-activity relationship: analyses of P-glycoprotein substrates and inhibitors. J Clin Pharm Ther 2003; 28:203-228.
23. Luurtsema G, Schuit RC, Klok RP, Verbeek J, Leysen JE, Lammertsma AA, et al. Evaluation of [11C]laniquidar as a tracer of P-glycoprotein: radiosynthesis and biodistribution in rats. Nucl Med Biol 2009; 36:643-649.
24. Kawamura K, Yamasaki T, Konno F, Yui J, Hatori A, Yanamoto K, et al. Evaluation of limiting brain penetration related to P-glycoprotein and breast cancer resistance protein using [11C]GF120918 by PET in mice. Mol Imaging Biol. doi: 10.1007/s11307-010-0313-1.
25. Peters WH, Roelofs HM. Biochemical characterization of resistance to mitoxantrone and adriamycin in Caco-2 human colon adenocarcinoma cells: a possible role for glutathione S-transferases. Cancer Res 1992; 52:1886-1890.
26. Ebert A, Seidel A, Lampen A. Identification of BCRP as transporter of benzopyrene conjugates metabolically formed in Caco-2 cells and its induction by Ah-receptor agonists. Carcinogenesis 2005; 26:1754-1763.
27. Taipalensuu J, Tornblom H, Lindberg G, Einarsson C, Sjoqvist F, Melhus H, et al. Correlation of gene expression of ten drug efflux proteins of the ATP-binding cassette transporter family in normal human jejunum and in human intestinal epithelial Caco-2 cell monolayers. J Pharmacol Exp Ther 2001; 299:164-170.
28. Liu Y, Shu XZ, Prestwich GD. Tumor engineering: orthotopic cancer models in mice using cell-loaded, injectable, cross-linked hyaluronan-derived hydrogels. Tissue Eng 2007; 13:1091-1101.
29. Yamasaki T, Kumata K, Yanamoto K, Hatori A, Takei M, Nakamura Y, et al. Imaging of peripheral-type benzodiazepine receptor in tumor: in vitro binding and in vivo biodistribution of N-benzyl-N-[11C]methyl-2-(7-methyl- 8-oxo-2-phenyl-7,8-dihydro-9H-purin-9-yl)acetamide. Nucl Med Biol 2009; 36:801-809.
30. Kawamura K, Yamasaki T, Yui J, Hatori A, Konno F, Kumata K, et al. In vivo evaluation of P-glycoprotein and breast cancer resistance protein modulation in the brain using [11C]gefitinib. Nucl Med Biol 2009; 36:239-246.
31. Takei M, Kida T, Suzuki K. Sensitive measurement of positron emitters eluted from HPLC. Appl Radiat Isot 2001; 55:229-234.
32. Luurtsema G, Molthoff CF, Schuit RC, Windhorst AD, Lammertsma AA, Franssen EJ, et al. Evaluation of (R)-[11C]verapamil as PET tracer of P-glycoprotein function in the blood-brain barrier: kinetics and metabolism in the rat. Nucl Med Biol 2005; 32:87-93.
33. Kannan P, John C, Zoghbi SS, Halldin C, Gottesman MM, Innis RB, et al. Imaging the function of P-glycoprotein with radiotracers: pharmacokinetics and in vivo applications. Clin Pharmacol Ther 2009; 86:368-377.
34. Hendrikse NH, De Vries EG, Eriks-Fluks L, Van der Graaf WT, Hospers GA, Willemsen AT, et al. A new in vivo method to P-glycoprotein transport in tumors and the blood-brain barrier. Cancer Res 1999; 59:2411-2416.
35. Levchenko A, Mehta BM, Lee JB, Humm JL, Augensen F, Squire O, et al. Evaluation of 11C-colchicine for PET imaging of multiple drug resistance. J Nucl Med 2000; 41:493-501.
36. Ambudkar SV, Dey S, Hrycyna CA, Ramachandra M, Pastan I, Gottesman MM. Biochemical, cellular, and pharmacological aspects of the multidrug transporter. Annu Rev Pharmacol Toxicol 1999; 39:361-398.
37. Langer O, Bauer M, Hammers A, Karch R, Pataraia E, Koepp MJ, et al. Pharmacoresistance in epilepsy: a pilot PET study with the P-glycoprotein substrate R-[11C]verapamil. Epilepsia 2007; 48:1774-1784.
38. Hendrikse NH, Schinkel AH, De Vries EG, Fluks E, Van der Graaf WT, Willemsen AT, et al. Complete in vivo reversal of P-glycoprotein pump function in the blood-brain barrier visualized with positron emission tomography. Br J Pharmacol 1998; 124:1413-1418.
39. Deeken JF, Loscher W. The blood-brain barrier and cancer: transporters, treatment, and Trojan horses. Clin Cancer Res 2007; 13:1663-1674.
40. Horio M, Chin KV, Currier SJ, Goldenberg S, Williams C, Pastan I, et al. Transepithelial transport of drugs by the multidrug transporter in cultured Madin-Darby canine kidney cell epithelia. J Biol Chem 1989; 264:14880-14884.