New inhibitors of ABCG2 identified by high-throughput screening

Molecular Cancer Therapeutics

Volumn 6, Issue 12, 2007, Pages 3271-3278

  Henrich, Curtis J ^a,b   Robey, Robert W ^c   Bokesch, Heidi R ^a,b   Bates, Susan E ^c   Shukla, Suneet ^c   Ambudkar, Suresh V ^c   Dean, Michael ^b   McMahon, James B ^b  

^a SAIC FREDERICK INC   (United States)

^b NATIONAL CANCER INSTITUTE   (United States)

^c NATIONAL CANCER INSTITUTE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

BREAST CANCER RESISTANCE PROTEIN; BREAST CANCER RESISTANCE PROTEIN INHIBITOR; CALCEIN; FLAVONOID; GLYCOPROTEIN P; MITOXANTRONE; MULTIDRUG RESISTANCE PROTEIN 1; NSC 11668; NSC 120688; NSC 168201; NSC 19139; NSC 375985; PHEOPHORBIDE; PRAZOSIN; PROTEIN INHIBITOR; RHODAMINE 123; UNCLASSIFIED DRUG;

ARTICLE; CELL STRAIN HEK293; CONTROLLED STUDY; DRUG PROTEIN BINDING; DRUG STRUCTURE; EMBRYO; HIGH THROUGHPUT SCREENING; HUMAN; HUMAN CELL; PRIORITY JOURNAL; PROTEIN FUNCTION; PROTEIN INTERACTION; PROTEIN TRANSPORT;

ATP-BINDING CASSETTE TRANSPORTERS; CELL LINE, TUMOR; FLOW CYTOMETRY; HUMANS; MULTIDRUG RESISTANCE-ASSOCIATED PROTEINS; NEOPLASM PROTEINS; P-GLYCOPROTEIN; PHOTOAFFINITY LABELS;

EID: 37549012993     PISSN: 15357163     EISSN: None     Source Type: Journal    
DOI: 10.1158/1535-7163.MCT-07-0352     Document Type: Article

References (35)

1. Robey RW, Polgar O, Deeken J, To KW, Bates SE. ABCG2: determining its relevance in clinical drug resistance. Cancer Metastasis Rev 2007;26:39-57.
2. Sarkadi B, Homolya L, Szakacs G, Varadi A. Human multidrug resistance ABCB and ABCG transporters: participation in a chemoimmunity defense system. Physiol Rev 2006;86:1179-236.
3. Krishnamurthy P, Schuetz JD. Role of ABCG2/BCRP in biology and medicine. Annu Rev Pharmacol Toxicol 2006;46:381-410.
4. Szakacs G, Paterson JK, Ludwig JA, Booth-Genthe C, Gottesman MM. Targeting multidrug resistance in cancer. Nat Rev Drug Discov 2006;5:219-34.
5. Xu J, Peng H, Zhang J-T. Human multidrug transporter ABCG2, a target for sensitizing drug resistance in cancer chemotherapy. Curr Med Chem 2007;14:689-701.
6. Diestra JE, Scheffer GL, Catala I, et al. Frequent expression of the multi-drug resistance-associated protein BCRP/MXR/ABCP/ABCG2 in human tumours detected by the BXP-21 monoclonal antibody in paraffin-embedded material. J Pathol 2002;198:213-9.
7. Yoh K, Ishii G, Yokose T, et al. Breast cancer resistance protein impacts clinical outcome in platinum-based chemotherapy for advanced non-small cell lung cancer. Clin Cancer Res 2004;10:1691-7.
8. Uggla B, Stahl E, Wagsater D, et al. BCRP mRNA expression v. clinical outcome in 40 adult AML patients. Leuk Res 2005;29:141-6.
9. Baderra Z, Faussat AM, Sayada L, et al. MRP3, BCRP, and P-glycoprotein activities are prognostic factors in adult acute myeloid leukemia. Clin Cancer Res 2005;11:7764-72.
10. Damiani D, Tiribelli M, Calistri E, et al. The prognostic value of P-glycoprotein (ABCB) and breast cancer resistance protein (ABCG2) in adults with de novo acute myeloid leukemia with normal karyotype. Haematologica 2006;91:825-8.
11. Wilson CS, Davidson GS, Martin SB, et al. Gene expression profiling of adult acute myeloid leukemia identifies novel biologic clusters for risk classification and outcome prediction. Blood 2006;108:685-96.
12. Dean M, Fojo T, Bates S. Tumour stem cells and drug resistance. Nat Rev Cancer 2005;5:275-84.
13. Jonker JW, Smit JW, Binkhuis RF, et al. Role of breast cancer resistance protein in the bioavailability and fetal penetration of topotecan. J Natl Cancer Inst 2000;92:1651-6.
14. Stewart CF, Leggas M, Schuetz JD, et al. Gefitinib enhances the antitumor activity and bioavailability of irinotecan in mice. Cancer Res 2004;64:7491-9.
15. Breedveld P, Pluim D, Cipriani G, et al. The effect of Bcrp1 (Abcg2) on the in vivo pharmacokinetics and brain penetration of imatinib mesylate (Gleevec): implications for the use of breast cancer resistance protein and P-glycoprotein inhibitors to enable the brain penetration of imatinib in patients. Cancer Res 2005;65:2577-82.
16. de Vries NA, Zhao J, Kroon E, Buckle T, Beijnen JH, van Tellingen O. P-glycoprotein and breast cancer resistance protein: two dominant transporters working together in limiting the brain penetration of topotecan. Clin Cancer Res 2007;13:6440-9.
17. Rabindran SK, He H, Singh M, et al. Reversal of a novel multidrug resistance mechanism in human colon carcinoma cells by fumitremorgin C. Cancer Res 1998;58:5850-8.
18. Henrich CJ, Bokesch HR, Dean M, et al. A high-throughput cell-based assay for inhibitors of ABCG2 activity. J Biomol Screen 2006;11:176-83.
19. Holbeck SL. Update on NCI in vitro drug screen utilities. Eur J Cancer 2004;40:785-93.
20. Shoemaker RH. The NCI60 human tumour cell line anticancer drug screen. Nat Rev Cancer 2006;6:813-23.
21. Robey RW, Honjo Y, van de Laar A, et al. A functional assay for detection of the mitoxantrone resistance protein MXR (ABCG2). Biochim Biophys Acta 2001;1512:171-82.
22. Robey RW, Honjo Y, Morisaki K, et al. Mutations at amino acid 482 in the ABCG2 gene affect substrate and antagonist specificity. Br J Cancer 2003;89:1971-8.
23. Robey RW, Medina-Perez WY, Nishiyama K, et al. Overexpression of the ATP-binding cassette half-transporter, ABCG2 (Mxr/BCrp/ABCP1), in flavopiridol-resistant human breast cancer cells. Clin Cancer Res 2001;7:145-52.
24. Jonker JW, Buitelaar M, Wagenaar E, et al. The breast cancer resistance protein protects against a major chlorophyll-derived dietary phototoxin and protoporphyria. Proc Natl Acad Sci U S A 2002;99:15649-54.
25. Robey RW, Steadman K, Polgar O, et al. Pheophorbide a is a specific probe for ABCG2 function and inhibition. Cancer Res 2004;64:1242-6.
26. Scudiero DA, Shoemaker RH, Paull KD, et al. Evaluation of a soluble tetrazolium/formazan assay for cell growth and drug sensitivity in culture using human and other tumor cell lines. Cancer Res 1988;48:4827-33.
27. Alvarez M, Robey R, Sandor V, et al. Using the National Cancer Institute anticancer drug screen to assess the effect of MRP expression on drug sensitivity profiles. Mol Pharmacol 1998;54:802-14.
28. Ozvegy-Laczka C, Varady G, Koblos G, et al. Function-dependent conformational changes of the ABCG2 multidrug transporter modify its interaction with a monoclonal antibody on the cell surface. J Biol Chem 2005;280:4219-27.
29. Shukla S, Robey RW, Bates SE, Ambudkar SV. The calcium channel blockers, 1,4-dihydropyridines, are substrates of the multidrug resistance-linked ABC drug transporter, ABCG2. Biochemistry 2006;45:8940-51.
30. Ahmed-Belkacem A, Pozza A, Munoz-Martinez F, et al. Flavonoid structure-activity studies identify 6-prenylchrysin and tectochrysin as potent and specific inhibitors of breast cancer resistance protein ABCG2. Cancer Res 2005;65:4852-60.
31. Zhang S, Yang X, Morris ME. Flavonoids are inhibitors of breast cancer resistance protein (ABCG2)-mediated transport. Mol Pharmacol 2004;65:1208-16.
32. Plasschaert SLA, van der Klolk D, de Bont EVSJM, Vellenga E, Kamps WA, de Vries GE. Breast cancer resistance protein (BCRP) in acute leukemia. Leuk Lymphoma 2004;45:649-54.
33. Takano M, Yumoto R, Murakami T. Expression and function of efflux drug transporters in the intestine. Pharmacol Ther 2006;109:137-61.
34. Kruijtzer CM, Beijnen JH, Rosing H, et al. Increased oral bioavailability of topotecan in combination with the breast cancer resistance protein and P-glycoprotein inhibitor GF120918. J Clin Oncol 2002;20:2943-50.
35. Allen JD, van Loevezijn A, Lakhal JM, 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;1:417-25.