Cell-based high-throughput screening for aromatase inhibitors in the Tox21 10K library

Toxicological Sciences

Volumn 147, Issue 2, 2015, Pages 446-457

  Chen, Shiuan ^a   Hsieh, Jui Hua ^b   Huang, Ruili ^c   Sakamuru, Srilatha ^c   Hsin, Li Yu ^a   Xia, Menghang ^c   Shockley, Keith R ^b   Auerbach, Scott ^b   Kanaya, Noriko ^a   Lu, Hannah ^a   Svoboda, Daniel ^b   Witt, Kristine L ^b   Merrick, B Alex ^b   Teng, Christina T ^b   Tice, Raymond R ^b  

^a CITY OF HOPE NATIONAL MEDICAL CENTER   (United States)

^b NATIONAL INSTITUTE OF ENVIRONMENTAL HEALTH SCIENCES   (United States)

^c NATIONAL INSTITUTES OF HEALTH   (United States)

Author keywords

AroER tri screen; Aromatase enzyme assay; Environmental chemicals; Quantitative high throughput screening; Tox21 10K library

Indexed keywords

AROMATASE; AROMATASE INHIBITOR; ENVIRONMENTAL CHEMICAL; ESTRADIOL; ESTROGEN RECEPTOR ALPHA; ESTROGEN RECEPTOR ANTAGONIST; FUNGICIDE; TESTOSTERONE; MOLECULAR LIBRARY;

ARTICLE; CONTROLLED STUDY; CYTOTOXICITY; ENVIRONMENTAL PROTECTION; ENZYME ASSAY; ESTROGEN RESPONSIVE ELEMENT; HIGH THROUGHPUT SCREENING; HUMAN; HUMAN CELL; MOLECULAR LIBRARY; STRUCTURE ACTIVITY RELATION; ANIMAL; DRUG EFFECTS; MCF-7 CELL LINE; PROCEDURES; TOXICITY;

ANIMALS; AROMATASE INHIBITORS; ESTRADIOL; HIGH-THROUGHPUT SCREENING ASSAYS; HUMANS; MCF-7 CELLS; SMALL MOLECULE LIBRARIES; STRUCTURE-ACTIVITY RELATIONSHIP; TESTOSTERONE;

EID: 84943756669     PISSN: 10966080     EISSN: 10960929     Source Type: Journal    
DOI: 10.1093/toxsci/kfv141     Document Type: Article

References (44)

1. Anderson, I. M. (2001). Meta-analytical studies on new antidepressants. Br. Med. Bull. 57, 161-178.
2. Andrade, R. J., and Tulkens, P. M. (2011). Hepatic safety of antibiotics used in primary care. J. Antimicrob. Chemother. 66, 1431-1446.
3. Bourke, C. H., Stowe, Z. N., and Owens, M. J. (2014). Prenatal antidepressant exposure: Clinical and preclinical findings. Pharmacol. Rev. 66, 435-465.
4. Braunstein, G. D. (1999). Aromatase and gynecomastia. Endocr. Relat. Cancer 6, 315-324.
5. Charlier, T. D., Cornil, C. A., Ball, G. F., and Balthazart, J. (2010). Diversity of mechanisms involved in aromatase regulation and estrogen action in the brain. Biochim. Biophys. Acta 1800, 1094-1105.
6. Chen, S. (1998). Aromatase and breast cancer. Front. Biosci. 3, d922-d933.
7. Chen, S., Zhou, D., Hsin, L. Y., Kanaya, N., Wong, C., Yip, R., Sakamuru, S., Xia, M., Yuan, Y. C., Witt, K., et al. (2014). AroER tri-screen is a biologically relevant assay for endocrine disrupting chemicals modulating the activity of aromatase and/or the estrogen receptor. Toxicol. Sci. 139, 198-209.
8. Chen, Z., Wang, O., Nie, M., Elison, K., Zhou, D., Li, M., Jiang, Y., Xia, W., Meng, X., Chen, S., et al. (2015). Aromatase deficiency in a Chinese adult man caused by novel compound heterozygous CYP19A1 mutations: effects of estrogen replacement therapy on the bone, lipid, liver and glucose metabolism. Mol. Cell. Endocrinol. 399, 32-42.
9. Cheshenko, K., Pakdel, F., Segner, H., Kah, O., and Eggen, R. I. (2008). Interference of endocrine disrupting chemicals with aromatase CYP19 expression or activity, and consequences for reproduction of teleost fish. Gen. Comp. Endocrinol. 155, 31-62.
10. Eliassen, A. H., Colditz, G. A., Rosner, B., Willett, W. C., and Hankinson, S. E. (2006). Adult weight change and risk of postmenopausal breast cancer. JAMA 296, 193-201.
11. Fowler, P. A., Bellingham, M., Sinclair, K. D., Evans, N. P., Pocar, P., Fischer, B., Schaedlich, K., Schmidt, J. S., Amezaga, M. R., Bhattacharya, S., et al. (2012). Impact of endocrine-disrupting compounds (EDCs) on female reproductive health. Mol. Cell. Endocrinol. 355, 231-239.
12. Grube, B. J., Eng, E. T., Kao, Y. C., Kwon, A., and Chen, S. (2001). White button mushroom phytochemicals inhibit aromatase activity and breast cancer cell proliferation. J. Nutr. 131, 3288-3293.
13. Hsieh, J.-H., Sedykh A., Huang, R., Xia, M., and Tice, R. R. (2015). A data analysis pipeline accounting for artifacts in Tox21 quantitative high throughput screening assays. J. Biomol. Screen. 2015 Apr 22, 2015, pii: 1087057115581317 [Epub ahead of print]
14. Huang, R., Sakamuru, S., Martin, M. T., Reif, D. M., Judson, R. S., Houck, K. A., Casey, W., Hsieh, J. H., Shockley, K. R., Ceger, P., et al. (2014). Profiling of the Tox21 10K compound library for agonists and antagonists of the estrogen receptor alpha signaling pathway. Sci. Rep. 4, 5664.
15. Huang, R., Southall, N., Wang, Y., Yasgar, A., Shinn, P., Jadhav, A., Nguyen, D. T., and Austin, C. P. (2011a). The NCGC pharmaceutical collection: a comprehensive resource of clinically approved drugs enabling repurposing and chemical genomics. Sci. Transl. Med. 3, 80ps16.
16. Huang, R., Xia, M., Cho, M. H., Sakamuru, S., Shinn, P., Houck, K. A., Dix, D. J., Judson, R. S., Witt, K. L., Kavlock, R. J., et al. (2011b). Chemical genomics profiling of environmental chemical modulation of human nuclear receptors. Environ. Health Perspect. 119, 1142-1148.
17. Huang, R. L., Southall, N., Xia, M. G., Cho, M. H., Jadhav, A., Nguyen, D. T., Inglese, J., Tice, R. R., and Austin, C. P. (2009). Weighted feature significance: A simple, interpretable model of compound toxicity based on the statistical enrichment of structural features. Toxicol. Sci. 112, 385-393.
18. Inglese, J., Auld, D. S., Jadhav, A., Johnson, R. L., Simeonov, A., Yasgar, A., Zheng, W., and Austin, C. P. (2006). Quantitative high-throughput screening: A titration-based approach that efficiently identifies biological activities in large chemical libraries. Proc. Natl. Acad. Sci. U.S.A. 103, 11473-11478.
19. Jones, M. E., Boon, W. C., McInnes, K., Maffei, L., Carani, C., and Simpson, E. R. (2007). Recognizing rare disorders: Aromatase deficiency. Nat. Clin. Pract. Endocrinol. Metab. 3, 414-421.
20. Kravetz de Srulijes, L., Israeli, E., and Barzilai, D. (1975). RNA:DNA ratios in a developing fibrosarcoma and its lung metastases in C3H mice. J. Natl. Cancer Inst. 55, 659-663.
21. Morris, P. G., Hudis, C. A., Giri, D., Morrow, M., Falcone, D. J., Zhou, X. K., Du, B., Brogi, E., Crawford, C. B., Kopelovich, L., et al. (2011). Inflammation and increased aromatase expression occur in the breast tissue of obese women with breast cancer. Cancer Prevent. Res. 4, 1021-1029.
22. Murakami, M., Kinukawa, M., Kanazawa, T., Maruyama, K., Miyagi, M., Miyata, H., and Ujiie, A. (1996). Effects of the new class I antiarrhythmic agent Ro 22-9194, (2R)-2-amino-N- (2,6-dimethylphenyl)-N-[3-(3-pyridyl)propyl]propionamide D-tartrate, on ischemia- and reperfusion-induced arrhythmias in dogs: involvement of thromboxane A2 synthase inhibitory activity. J. Pharmacol. Exp. Ther. 279, 877-883.
23. Nordkap, L., Joensen, U. N., Blomberg Jensen, M., and Jorgensen, N. (2012). Regional differences and temporal trends in male reproductive health disorders: Semen quality may be a sensitive marker of environmental exposures. Mol. Cell. Endocrinol. 355, 221-230.
24. Ohlsson, A., Cedergreen, N., Oskarsson, A., and Ulleras, E. (2010). Mixture effects of imidazole fungicides on cortisol and aldosterone secretion in human adrenocortical H295R cells. Toxicology 275(1-3), 21-28.
25. Olvera-Hernandez, S., Chavira, R., and Fernandez-Guasti, A. (2015). Prenatal letrozole produces a subpopulation of male rats with same-sex preference and arousal as well as female sexual behavior. Physiol. Behav. 139, 403-411.
26. Pfeiler, G., Konigsberg, R., Fesl, C., Mlineritsch, B., Stoeger, H., Singer, C. F., Postlberger, S., Steger, G. G., Seifert, M., Dubsky, P., et al. (2011). Impact of body mass index on the efficacy of endocrine therapy in premenopausal patients with breast cancer: An analysis of the prospective ABCSG-12 trial. J. Clin. Oncol. 29, 2653-2659.
27. Quignot, N., Desmots, S., Barouki, R., and Lemazurier, E. (2012). A comparison of two human cell lines and two rat gonadal cell primary cultures as in vitro screening tools for aromatase modulation. Toxicol. in vitro 26, 107-118.
28. Roberts, D. L., Dive, C., and Renehan, A. G. (2010). Biological mechanisms linking obesity and cancer risk: New perspectives. Annu. Rev. Med. 61, 301-316.
29. Saad, F., and Gooren, L. J. (2011). The role of testosterone in the etiology and treatment of obesity, the metabolic syndrome, and diabetes mellitus type 2. J. Obes., 2011, 471584, doi:10.1155/2011/471584.
30. Sanderson, J. T. (2006). The steroid hormone biosynthesis pathway as a target for endocrine-disrupting chemicals. Toxicol. Sci. 94, 3-21.
31. Sanderson, J. T., Boerma, J., Lansbergen, G. W., and van den Berg, M. (2002). Induction and inhibition of aromatase (CYP19) activity by various classes of pesticides in H295R human adrenocortical carcinoma cells. Toxicol. Appl. Pharmacol. 182, 44-54.
32. Sedykh, A., Zhu, H., Tang, H., Zhang, L., Richard, A., Rusyn, I., and Tropsha, A. (2011). Use of in vitro HTS-derived concentration- response data as biological descriptors improves the accuracy of QSAR models of in vivo toxicity. Environ. Health Perspect. 119, 364-370.
33. Shockley, K. R. (2012). A three-stage algorithm to make toxicologically relevant activity calls from quantitative high throughput screening data. Environ. Health Perspect. 120, 1107-1115.
34. Sisman, T., and Turkez, H. (2010). Toxicologic evaluation of imazalil with particular reference to genotoxic and teratogenic potentials. Toxicol. Ind. Health 26, 641-648.
35. Sparano, J. A., Wang, M., Zhao, F., Stearns, V., Martino, S., Ligibel, J. A., Perez, E. A., Saphner, T., Wolff, A. C., Sledge, G. W., Jr, et al. (2010). Obesity at diagnosis is associated with inferior outcomes in hormone receptor-positive operable breast cancer. Cancer 118, 5937-5946.
36. Tanaka, T., Ogata, A., Inomata, A., and Nakae, D. (2013). Effects of maternal exposure to imazalil on behavioral development in F(1)-generation mice. Birth Defects Res. B Dev. Reprod. Toxicol. 98, 334-342.
37. Tice, R. R., Austin, C. P., Kavlock, R. J., and Bucher, J. R. (2013). Improving the human hazard characterization of chemicals: A tox21 update. Environ. Health Perspect. 121, 756-765.
38. Turkez, H., and Aydin, E. (2012). The protective role of ascorbic acid on imazalil-induced genetic damage assessed by the cytogenetic tests. Toxicol. Ind. Health 28, 648-654.
39. Valerio, L. G., Yang, C., Arvidson, K. B., and Kruhlak, N. L. (2010). A structural feature-based computational approach for toxicology predictions. Expert Opin. Drug Metabol. Toxicol. 6, 505-518.
40. Veith, H., Southall, N., Huang, R., James, T., Fayne, D., Artemenko, N., Shen, M., Inglese, J., Austin, C. P., Lloyd, D. G., et al. (2009). Comprehensive characterization of cytochrome P450 isozyme selectivity across chemical libraries. Nat. Biotechnol. 27, 1050-1055.
41. Vinggaard, A. M., Hnida, C., Breinholt, V., and Larsen, J. C. (2000). Screening of selected pesticides for inhibition of CYP19 aromatase activity in vitro. Toxicol. in vitro 14, 227-234.
42. Wang, J. G., Yan, P., and Jeffers, B. W. (2014). Effects of amlodipine and other classes of antihypertensive drugs on long-term blood pressure variability: Evidence from randomized controlled trials. J. Am. Soc. Hypertens., 8, 340-349.
43. Wang, X., and Chen, S. (2006). Aromatase destabilizer: novel action of exemestane, a food and drug administrationapproved aromatase inhibitor. Cancer Res. 66, 10281-10286.
44. Yewale, C., Baradia, D., Vhora, I., Patil, S., and Misra, A. (2013). Epidermal growth factor receptor targeting in cancer: A review of trends and strategies. Biomaterials 34, 8690-8707.