Evaluation of an estrogen receptor-β agonist in animal models of human disease

Endocrinology

Volumn 144, Issue 10, 2003, Pages 4241-4249

  Harris, Heather A ^a,b   Albert, Leo M ^a   Leathurby, Yelena ^a   Malamas, Michael S ^a   Mewshaw, Richard E ^a   Miller, Chris P ^a,c   Kharode, Yogendra P ^a   Marzolf, James ^a   Komm, Barry S ^a   Winneker, Richard C ^a   Frail, Donald E ^a   Henderson, Ruth A ^a   Zhu, Yuan ^a   Keith Jr , James C ^a  

^a PFIZER INC   (United States)

^b Women's Health Research Institute   (United States)

^c Health Law Practice Group of Cozen O'Connor   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

2 (3 FLUORO 4 HYDROXYPHENYL) 7 VINYL 5 BENZOXAZOLOL; ANTIINFLAMMATORY AGENT; ESTROGEN RECEPTOR BETA AGONIST; HORMONE RECEPTOR STIMULATING AGENT; IMMUNOMODULATING AGENT; UNCLASSIFIED DRUG;

ADJUVANT ARTHRITIS; ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ANTIINFLAMMATORY ACTIVITY; ARTICLE; ARTICULAR CARTILAGE; CHRONIC DIARRHEA; COLON; CONTROLLED STUDY; DRUG EFFICACY; DRUG SCREENING; ENTERITIS; FEMALE; HISTOPATHOLOGY; IMMUNE RESPONSE; IMMUNOMODULATION; MALE; NONHUMAN; PRIORITY JOURNAL; RAT;

ANIMALS; ANIMALS, GENETICALLY MODIFIED; ARTHRITIS, EXPERIMENTAL; BETA 2-MICROGLOBULIN; BONE DENSITY; BONE DISEASES, METABOLIC; CELL LINE; DISEASE MODELS, ANIMAL; ESTROGEN RECEPTOR BETA; FEMALE; HLA-B27 ANTIGEN; HUMANS; INFLAMMATORY BOWEL DISEASES; MAMMARY GLANDS, ANIMAL; MICE; OVARIECTOMY; OXAZOLES; RATS; RATS, INBRED LEW; RATS, SPRAGUE-DAWLEY; RECEPTORS, ESTROGEN; UTERUS; WEIGHT GAIN;

EID: 0141525429     PISSN: 00137227     EISSN: None     Source Type: Journal    
DOI: 10.1210/en.2003-0550     Document Type: Article

References (47)

1. Kuiper GGJM, Enmark E, Pelto Huikko M, Nilsson S, Gustafsson JA 1996 Cloning of a novel estrogen receptor expressed in rat prostate and ovary. Proc Natl Acad Sci USA 93:5925-5930
2. Green S, Walter P, Kumar V, Krust A, Bornert JM, Argos P, Chambon P 1986 Human oestrogen receptor cDNA: sequence, expression and homology to v-erb-A. Nature 320:134-139
3. Lubahn D, Moyer J, Golding T, Couse J, Korach K, Smithies O 1993 Alteration of reproductive function but not prenatal sexual development after insertional disruption of the mouse estrogen receptor gene. Proc Natl Acad Sci USA 90:11162-11166
4. Mueller SO, Korach KS 2001 Estrogen receptors and endocrine diseases: lessons from estrogen receptor knockout mice. Curr Opin Pharmacol 1:613-619
5. Curtis HS, Couse JF, Korach KS 2000 Estrogen receptor transcription and transactivation: estrogen receptor knockout mice: what their phenotypes reveal about mechanisms of estrogen action. Breast Cancer Res 2:345-352
6. Couse JF, Korach KS 1999 Reproductive phenotypes in the estrogen receptor-α knockout mouse. Ann Endocrinol (Paris) 60:143-148
7. Couse JF, Curtis SW, Washburn TF, Lindzey J, Golding TS, Lubahn DB, Smithies O, Korach KS 1995 Analysis of transcription and estrogen insensitivity in the female mouse after targeted disruption of the estrogen receptor gene. Mol Endocrinol 9:1441-1454
8. Pare G, Krust A, Karas RH, Dupont S, Aronovitz M, Chambon P, Mendelsohn ME 2002 Estrogen receptor-α mediates the protective effects of estrogen against vascular injury. Circ Res 90:1087-1092
9. Kuiper GGJM, Carlsson B, Grandian K, Enmark E, Haggblad J, Nilsson S, Gustafsson JA 1997 Comparison of the ligand binding specificity and transcript tissue distribution of estrogen receptor α and β. Endocrinology 138:863-870
10. Nilsson S, Kuiper G, Gustafsson JA 1998 ERβ: a novel estrogen receptor offers the potential for new drug development. Trends Endocrinol Metab 9:387-395
11. Dupont S, Krust A, Gansmuller A, Dierich A, Chambon P, Mark M 2000 Effect of single and compound knockouts of estrogen receptors α (ERα) and β (ERβ) on mouse reproductive phenotypes. Development 127:4277-4291
12. Harris HA, Bapat AR, Gonder DS, Frail DE 2002 The ligand binding profiles of estrogen receptors α and β are species dependent. Steroids 67:379-384
13. Jefferson W, N., Padilla-Banks E, Clark G, Newbold Retha R 2002 Assessing estrogenic activity of phytochemicals using transcriptional activation and immature mouse uterotrophic responses. J Chromatogr B 777:179-189
14. Harris HA, Katzenellenbogen JA, Katzenellenbogen BS 2002 Characterization of the biological roles of the estrogen receptors, ERα and ERβ, in estrogen target tissues in vivo through the use of an ERα-selective ligand. Endocrinology 143:4172-4177
15. Meyers M, J., Sun J, Carlson Kathryn E, Marriner Gwendolyn A, Katzenellenbogen Benita S, Katzenellenbogen John A 2001 Estrogen receptor-β potency-selective ligands: structure-activity relationship studies of diarylpropionitriles and their acetylene and polar analogues. J Med Chem 44:4230-4251
16. Henke BR, Consler TG, Go N, Hale RL, Hohman DR, Jones SA, Lu AT, Moore LB, Moore JT, Orband-Miller LA, Robinett RG, Shearin J, Spearing PK, Stewart EL, Turnbull PS, Weaver SL, Williams SP, Wisely GB, Lambert MH 2002 A new series of estrogen receptor modulators that display selectivity for estrogen receptor β. J Med Chem 45:5492-5505
17. Schopfer U, Schoeffter P, Bischoff SF, Nozulak J, Feuerbach D, Floersheim P 2002 Toward selective ERβ agonists for central nervous system disorders: synthesis and characterization of aryl benzthiophenes. J Med Chem 45:1399-1401
18. Harris HA, Henderson RA, Bhat RA, Komm BS 2001 Regulation of metallothionein II messenger ribonucleic acid measures exogenous estrogen receptor-β activity in SAOS-2 and LNCaPLN3 cells. Endocrinology 142:645-652
19. Lundeen SG, Zhang Z, Zhu Y, Carver JM, Winneker RC 2001 Rat uterine complement C3 expression as a model for progesterone receptor modulators: characterization of the new progestin trimegestone. J Steroid Biochem Mol Biol 78:137-143
20. Boughton-Smith N, Wallace J, Morris G, Whittle B 1988 The effect of anti-inflammatory drugs on eicosanoid formation in a chronic model of inflammatory bowel disease in the rat. Br J Pharmacol 94:65-72
21. Greenwood-Van Meerveld B, Tyler K, Keith Jr JC 2000 Recombinant human interleukin-11 modulates mucosal ion transport in the small intestine and colon of normal and HLA-B27 rats in vitro. Lab Invest 80:1269-1280
22. Greenwood-Van Meerveld B, Venkova K, Keith Jr JC 2001 Recombinant human interleukin-11 restores smooth muscle function in the jejunum and colon of human leukocyte antigen-B27 rats with intestinal inflammation. J Pharmacol Exp Ther 299:58-66
23. Peterson RL, Wang L, Albert L, Keith Jr JC, Dorner AJ 1998 Molecular effects of recombinant human interleukin-11 in the HLA-B27 rat model of inflammatory bowel disease. Lab Invest 78:1503-1512
24. Poole AR, Coombs RR 1977 Rheumatoid-like joint lesions in rabbits injected intravenously with bovine serum. Int Arch Allergy Appl Immunol 54:97-113
25. Mankin HJ, Dorfman H, Lippiello L, Zarins A 1971 Biochemical and metabolic abnormalities in articular cartilage from osteo-arthritic human hips. II. Correlation of morphology with biochemical and metabolic data. J Bone Joint Surg 53:523-537
26. Rudnick K, Zhu Y, Winneker R, Lundeen S, Identification of progestin regulated genes in the rat mammary gland. Program of the 83rd Annual Meeting of The Endocrine Society, Denver, CO, 2001 (Abstract P3-611), p 578
27. Miller CP, Collini MD, Tran BD, Harris HA, Kharode YP, Marzolf JT, Moran RA, Henderson RA, Bender RH, Unwalla RJ, Greenberger LM, Yardley JP, Abou-Gharbia MA, Lyttle CR, Komm BS 2001 Design, synthesis, and preclinical characterization of novel, highly selective indole estrogens. J Med Chem 44:1654-1657
28. Shughrue PJ, Askew GR, Dellovade TL, Merchenthaler I 2002 Estrogen-binding sites and their functional capacity in estrogen receptor double knockout mouse brain. Endocrinology 143:1643-1650
29. Pike ACW, Brzozowski AM, Hubbard RE, Bonn T, Thorsell AG, Engstrom O, Ljunggren J, Gustafsson JK, Carlquist M 1999 Structure of the ligand-binding domain of oestrogen receptor β in the presence of a partial agonist and a full antagonist. EMBO J 18:4608-4618
30. Yanagisawa H, Richardson JA, Taurog JD, Hammer RE 1995 Characterization of psoriasiform and alopecic skin lesions in HLA-B27 transgenic rats. Am J Pathol 147:955-964
31. Taurog JD, Maika SD, Satumtira N, Dorris ML, McLean IL, Yanagisawa H, Sayad A, Stagg AJ, Fox GM, Le O'Brien A, Rehman M, Zhou M, Weiner AL, Splawski JB, Richardson JA, Hammer RE 1999 Inflammatory disease in HLA-B27 transgenic rats. Immunol Rev 169:209-223
32. Kim YS, Son M, Ko JI, Cho H, Yoo M, Kim WB, Song IS, Kim CY 1999 Effect of DA-6034, a derivative of flavonoid, on experimental animal models of inflammatory bowel disease. Arch Pharmacol Res 22:354-360
33. Gehm BD, McAndrews JM, Jordan VC, Jameson JL 2000 EGF activates highly selective estrogen-responsive reporter plasmids by an ER-independent pathway. Mol Cell Endocrinol 159:53-62
34. Wardley AM, Howell A, Osborne CK, Morris C, Wakeling AE, Gehm BD, McAndrews JM, Jordan VC, Jameson JL 2002 Fulvestrant: a review of its development, pre-clinical and clinical data. Int J Clin Pract 56:305-309
35. Howell A, Osborne CK, Morris C, Wakeling AE, Gehm BD, McAndrews JM, Jordan VC, Jameson JL 2000 ICI 182, 780 (Faslodex (TM)): development of a novel, "pure" antiestrogen. Cancer 89:817-825
36. Perretti M, Duncan GS, Flower RJ, Peers SH 1993 Serum corticosterone, interleukin-1 and tumour necrosis factor in rat experimental endotoxaemia: comparison between Lewis and Wistar strains. Br J Pharmacol 110:868-874
37. Oitzl MS, van Haarst AD, Sutanto W, de Kloet ER 1995 Corticosterone, brain mineralocorticoid receptors (MRs) and the activity of the hypothalamic-pituitary-adrenal (HPA) axis: the Lewis rat as an example of increased central MR capacity and a hyporesponsive HPA axis. Psychoneuroendocrinology 20:655-675
38. Foley EF, Jazaeri AA, Shupnik MA, Jazaeri O, Rice LW 2000 Selective loss of estrogen receptor β in malignant human colon. Cancer Res 60:245-248
39. Ushiyama T, Ueyama H, Inoue K, Ohkubo I, Hukuda S 1999 Expression of genes for estrogen receptors α and β in human articular chondrocytes. Osteoarthritis Cartilage 7:560-566
40. Campbell-Thompson M, Lynch IJ, Bhardwaj B 2001 Expression of estrogen receptor (ER) subtypes and ERβ isoforms in colon cancer. Cancer Res 61:632-640
41. Juma S, Munson ME, Malayer J, Svanborg A, Khalil DA, Arjmandi BH 1999 Evidence for the presence of estrogen receptor β but not α in human articular and meniscus cartilage. J Bone Miner Res (Suppl 1):S452
42. Cutolo M, Sulli A, Seriolo B, Accardo S, Masi AT 1995 Estrogens, the immune response and autoimmunity. Clin Exp Rheumatol 13:217-226
43. McMurray RW 2001 Estrogen, prolactin, and autoimmunity: actions and interactions. Int Immunopharmacol 1:995-1008
44. Jansson L, Holmdahl R 1998 Estrogen-mediated immunosuppression in autoimmune diseases. Inflamm Res 47:290-301
45. Evans MJ, Eckert A, Lai K, Adelman SJ, Harnish DC 2001 Reciprocal antagonism between estrogen receptor and NF-κB activity in vivo. Circ Res 89:823-830
46. Bhat RA, Harnish DC, Stevis PE, Lyttle CR, Komm BS 1998 A novel human estrogen receptor β: identification and functional analysis of additional N-terminal amino acids. J Steroid Biochem Mol Biol 67:233-240
47. Quaedackers ME, Van den Brink CE, Wissink S, Schreurs R, Gustafsson JA, Van der Saag PT, Van der Burg B 2001 4-Hydroxytamoxifen trans-represses nuclear factor-κB activity in human osteoblastic U2-OS cells through estrogen receptor (ER)α, and not through ERβ. Endocrinology 142:1156-1166