Agonist-like SERM effects on ERα-mediated repression of MMP1 promoter activity predict in vivo effects on bone and uterus

Journal of Steroid Biochemistry and Molecular Biology

Volumn 110, Issue 3-5, 2008, Pages 197-206

  Scafonas, Angela ^a   Reszka, Alfred A ^a   Kimmel, Donald B ^a   Hou, Xiaoli Shirley ^a   Su, Qin ^a   Birzin, Elizabeth T ^a   Kim, Seongkon ^a   Chen, Helen Y ^a   Tan, Qiang ^a   Roher, Susan P ^a   Dininno, Frank ^a   Hammond, Milton L ^a   Rodan, Gideon A ^a   Towler, Dwight A ^b   Schmidt, Azriel ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

^b WASHINGTON UNIVERSITY SCHOOL OF MEDICINE   (United States)

Author keywords

Estradiol receptor; MMP 1; SERM

Indexed keywords

4 HYDROXYTAMOXIFEN; BAZEDOXIFENE; CENTCHROMAN; ESTRADIOL; ESTRADIOL RECEPTOR; ESTRADIOL RECEPTOR ALPHA; FULVESTRANT; IDOXIFENE; INTERSTITIAL COLLAGENASE; LASOFOXIFENE; RALOXIFENE; TRANSCRIPTION FACTOR AP 1;

AMINO ACID SEQUENCE; ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; BINDING SITE; BREAST CANCER; CANCER CELL CULTURE; CONTROLLED STUDY; DRUG ACTIVITY; DRUG ANTAGONISM; DRUG EFFICACY; DRUG POTENCY; ENDOMETRIUM CARCINOMA; ESTROGEN ACTIVITY; FEMALE; HUMAN; HUMAN CELL; IN VITRO STUDY; IN VIVO STUDY; MUTATIONAL ANALYSIS; NONHUMAN; OSTEOSARCOMA; PROMOTER REGION; PROTEIN PROTEIN INTERACTION; RAT; TRANSCRIPTION INITIATION; UTERUS CONTRACTION;

AMINO ACID MOTIFS; ANIMALS; BONE AND BONES; DOWN-REGULATION; ESTRADIOL; ESTROGEN RECEPTOR ALPHA; FEMALE; HUMANS; MATRIX METALLOPROTEINASE 1; MUTANT PROTEINS; PROMOTER REGIONS (GENETICS); PROTEIN STRUCTURE, TERTIARY; RATS; RATS, SPRAGUE-DAWLEY; SELECTIVE ESTROGEN RECEPTOR MODULATORS; TUMOR CELLS, CULTURED; UTERUS;

MURINAE; RATTUS;

EID: 44949200993     PISSN: 09600760     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.jsbmb.2007.10.013     Document Type: Article

References (54)

1. WHI Writing Group, Writing Group for the Women's Health Initiative Investigators, Risks and benefits of estrogen plus progestin in healthy postmenopausal women: principal results from the Women's Health Initiative randomized controlled trial, JAMA 288 (2002) 321-333.
2. Smith E.P., Boyd J., Frank G.R., Takahashi H., Cohen R.M., Specker B., Williams T.C., Lubahn D.B., and Korach K.S. Estrogen resistance caused by a mutation in the estrogen-receptor gene in a man. N. Engl. J. Med. 331 (1994) 1056-1061
3. Korach K. Estrogen receptor knock-out mice: molecular and endocrine phenotypes. J. Soc. Gynecol. Investig. 7 (2000) S16-S17
4. Jilka R.L. Cytokines, bone remodeling, and estrogen deficiency: a 1998 update. Bone 23 (1998) 75-81
5. Kassem M., Harris S.A., Spelsberg T.C., and Riggs B.L. Estrogen inhibits interleukin-6 production and gene expression in a human osteoblastic cell line with high levels of estrogen receptors. J. Bone Miner. Res. 11 (1996) 193-199
6. Pacifici R. Estrogen, cytokines, and pathogenesis of postmenopausal osteoporosis. J. Bone Miner. Res. 11 (1996) 1043-1051
7. Cenci S., Weitzmann M.N., Roggia C., Namba N., Novack D., Woodring J., and Pacifici R. Estrogen deficiency induces bone loss by enhancing T-cell production of TNF-alpha. J. Clin. Invest. 106 (2000) 1229-1237
8. Khosla S., Atkinson E.J., Dunstan C.R., and O'Fallon W.M. Effect of estrogen versus testosterone on circulating osteoprotegerin and other cytokine levels in normal elderly men. J. Clin. Endocrinol. Metab. 87 (2002) 1550-1554
9. Shevde N.K., Bendixen A.C., Dienger K.M., and Pike J.W. Estrogens suppress RANK ligand-induced osteoclast differentiation via a stromal cell independent mechanism involving c-Jun repression. Proc. Natl. Acad. Sci. U.S.A. 97 (2000) 7829-7834
10. Srivastava S., Toraldo G., Weitzmann M.N., Cenci S., Ross F.P., and Pacifici R. Estrogen decreases osteoclast formation by down-regulating receptor activator of NF-kappa B ligand (RANKL)-induced JNK activation. J. Biol. Chem. 276 (2001) 8836-8840
11. Chang J., Powles T.J., Ashley S.E., Gregory R.K., Tidy V.A., Treleaven J.G., and Singh R. The effect of tamoxifen and hormone replacement therapy on serum cholesterol, bone mineral density and coagulation factors in healthy postmenopausal women participating in a randomized, controlled tamoxifen prevention study. Ann. Oncol. 7 (1996) 671-675
12. Powles T.J., Hickish T., Kanis J.A., Tidy A., and Ashley S. Effect of tamoxifen on bone mineral density measured by dual-energy X-ray absorptiometry in healthy premenopausal and postmenopausal women. J. Clin. Oncol. 14 (1996) 78-84
13. Barrett-Connor E., Cauley J.A., Kulkarni P.M., Sashegyi A., Cox D.A., and Geiger M.J. Risk-benefit profile for raloxifene: 4-year data from the Multiple Outcomes Of Raloxifene Evaluation (MORE) randomized trial. J. Bone Miner. Res. 19 (2004) 1270-1275
14. Barrett-Connor E., Grady D., Sashegyi A., Anderson P.W., Cox D.A., Hoszowski K., Rautaharju P., and Harper K.D. Raloxifene and cardiovascular events in osteoporotic postmenopausal women: four-year results from the MORE (Multiple Outcomes Of Raloxifene Evaluation) randomized trial. JAMA 287 (2002) 847-857
15. Martino S., Costantino J., McNabb M., Mershon J., Bryant K., Powles T., and Secrest R.J. The role of selective estrogen receptor modulators in the prevention of breast cancer: comparison of the clinical trials. Oncologist 9 (2004) 116-125
16. Delmas P.D., Ensrud K.E., Adachi J.D., Harper K.D., Sarkar S., Gennari C., Reginster J.Y., Pols H.A., Recker R.R., Harris S.T., Wu W., Genant H.K., Black D.M., and Eastell R. Efficacy of raloxifene on vertebral fracture risk reduction in postmenopausal women with osteoporosis: four-year results from a randomized clinical trial. J. Clin. Endocrinol. Metab. 87 (2002) 3609-3617
17. Scott J.A., Da Camara C.C., and Early J.E. Raloxifene: a selective estrogen receptor modulator. Am. Fam. Physician 60 (1999) 1131-1139
18. Sibonga J.D., Dobnig H., Harden R.M., and Turner R.T. Effect of the high-affinity estrogen receptor ligand ICI 182,780 on the rat tibia. Endocrinology 139 (1998) 3736-3742
19. Shang Y., and Brown M. Molecular determinants for the tissue specificity of SERMs. Science 295 (2002) 2465-2468
20. Stein B., and Yang M.X. Repression of the interleukin-6 promoter by estrogen receptor is mediated by NF-kappa B and C/EBP beta. Mol. Cell Biol. 15 (1995) 4971-4979
21. Jakacka M., Ito M., Weiss J., Chien P.Y., Gehm B.D., and Jameson J.L. Estrogen receptor binding to DNA is not required for its activity through the nonclassical AP1 pathway. J. Biol. Chem. 276 (2001) 13615-13621
22. Paech K., Webb P., Kuiper G.G., Nilsson S., Gustafsson J., Kushner P.J., and Scanlan T.S. Differential ligand activation of estrogen receptors ERalpha and ERbeta at AP1 sites. Science 277 (1997) 1508-1510
23. Webb P., Lopez G.N., Uht R.M., and Kushner P.J. Tamoxifen activation of the estrogen receptor/AP-1 pathway: potential origin for the cell-specific estrogen-like effects of antiestrogens. Mol. Endocrinol. 9 (1995) 443-456
24. Yang N.N., Venugopalan M., Hardikar S., and Glasebrook A. Identification of an estrogen response element activated by metabolites of 17beta-estradiol and raloxifene. Science 273 (1996) 1222-1225
25. Montano M.M., Ekena K., Krueger K.D., Keller A.L., and Katzenellenbogen B.S. Human estrogen receptor ligand activity inversion mutants: receptors that interpret antiestrogens as estrogens and estrogens as antiestrogens and discriminate among different antiestrogens. Mol. Endocrinol. 10 (1996) 230-242
26. Montano M.M., Jaiswal A.K., and Katzenellenbogen B.S. Transcriptional regulation of the human quinone reductase gene by antiestrogen-liganded estrogen receptor-alpha and estrogen receptor-beta. J. Biol. Chem. 273 (1998) 25443-25449
27. Green S., and Chambon P. A superfamily of potentially oncogenic hormone receptors. Nature 324 (1986) 615-617
28. Greene G.L., Gilna P., Waterfield M., Baker A., Hort Y., and Shine J. Sequence and expression of human estrogen receptor complementary DNA. Science 231 (1986) 1150-1154
29. Walter P., Green S., Greene G., Krust A., Bornert J.M., Jeltsch J.M., Staub A., Jensen E., Scrace G., Waterfield M., et al. Cloning of the human estrogen receptor cDNA. Proc. Natl. Acad. Sci. U.S.A. 82 (1985) 7889-7893
30. Ettinger B., Black D.M., Mitlak B.H., Knickerbocker R.K., Nickelsen T., Genant H.K., Christiansen C., Delmas P.D., Zanchetta J.R., Stakkestad J., Gluer C.C., Krueger K., Cohen F.J., Eckert S., Ensrud K.E., Avioli L.V., Lips P., and Cummings S.R. Reduction of vertebral fracture risk in postmenopausal women with osteoporosis treated with raloxifene: results from a 3-year randomized clinical trial. Multiple Outcomes of Raloxifene Evaluation (MORE) investigators. JAMA 282 (1999) 637-645
31. Sambrook P.N., Geusens P., Ribot C., Solimano J.A., Ferrer-Barriendos J., Gaines K., Verbruggen N., and Melton M.E. Alendronate produces greater effects than raloxifene on bone density and bone turnover in postmenopausal women with low bone density: results of EFFECT (Efficacy of FOSAMAX versus EVISTA Comparison Trial) International. J. Intern. Med. 255 (2004) 503-511
32. Goldstein S.R., and Nanavati N. Adverse events that are associated with the selective estrogen receptor modulator levormeloxifene in an aborted phase III osteoporosis treatment study. Am. J. Obstet. Gynecol. 187 (2002) 521-527
33. Hendrix S.L., and McNeeley S.G. Effect of selective estrogen receptor modulators on reproductive tissues other than endometrium. Ann. NY Acad. Sci. 949 (2001) 243-250
34. Newberry E.P., Willis D., Latifi T., Boudreaux J.M., and Towler D.A. Fibroblast growth factor receptor signaling activates the human interstitial collagenase promoter via the bipartite Ets-AP1 element. Mol. Endocrinol. 11 (1997) 1129-1144
35. Frantz B., Nordby E.C., Bren G., Steffan N., Paya C.V., Kincaid R.L., Tocci M.J., O'Keefe S.J., and O'Neill E.A. Calcineurin acts in synergy with PMA to inactivate I kappa B/MAD3, an inhibitor of NF-kappa B. EMBO J. 13 (1994) 861-870
36. Ernst M., Parker M.G., and Rodan G.A. Functional estrogen receptors in osteoblastic cells demonstrated by transfection with a reporter gene containing an estrogen response element. Mol. Endocrinol. 5 (1991) 1597-1606
37. Tzukerman M.T., Esty A., Santiso-Mere D., Danielian P., Parker M.G., Stein R.B., Pike J.W., and McDonnell D.P. Human estrogen receptor transactivational capacity is determined by both cellular and promoter context and mediated by two functionally distinct intramolecular regions. Mol. Endocrinol. 8 (1994) 21-30
38. Higuchi R., Krummel B., and Saiki R.K. A general method of in vitro preparation and specific mutagenesis of DNA fragments: study of protein and DNA interactions. Nucleic Acids Res. 16 (1988) 7351-7367
39. Diascro Jr. D.D., Vogel R.L., Johnson T.E., Witherup K.M., Pitzenberger S.M., Rutledge S.J., Prescott D.J., Rodan G.A., and Schmidt A. High fatty acid content in rabbit serum is responsible for the differentiation of osteoblasts into adipocyte-like cells. J. Bone Miner. Res. 13 (1998) 96-106
40. Kim S., Wu J.Y., Birzin E.T., Frisch K., Chan W., Pai L.Y., Yang Y.T., Mosley R.T., Fitzgerald P.M., Sharma N., Dahllund J., Thorsell A.G., DiNinno F., Rohrer S.P., Schaeffer J.M., and Hammond M.L. Estrogen receptor ligands. II. Discovery of benzoxathiins as potent, selective estrogen receptor alpha modulators. J. Med. Chem. 47 (2004) 2171-2175
41. Lipfert L., Fisher J.E., Wei N., Scafonas A., Su Q., Yudkovitz J., Chen F., Warrier S., Birzin E.T., Kim S., Chen H.Y., Tan Q., Schmidt A., Dininno F., Rohrer S.P., Hammond M.L., Rodan G.A., Freedman L.P., and Reszka A.A. Antagonist-induced, AF-2 independent estrogen receptor {alpha} phosphorylation. Mol. Endocrinol. 20 (2006) 516-533
42. Nantermet P.V., Masarachia P., Gentile M.A., Pennypacker B., Xu J., Holder D., Gerhold D., Towler D., Schmidt A., Kimmel D.B., Freedman L.P., Harada S.I., and Ray W.J. Androgenic induction of growth and differentiation in the rodent uterus involves the modulation of estrogen-regulated genetic pathways. Endocrinology 146 (2004) 564-578
43. Yamamoto M., Fisher J.E., Gentile M., Seedor J.G., Leu C.T., Rodan S.B., and Rodan G.A. The integrin ligand echistatin prevents bone loss in ovariectomized mice and rats. Endocrinology 139 (1998) 1411-1419
44. Yamamoto M., Markatos A., Seedor J.G., Masarachia P., Gentile M., Rodan G.A., and Balena R. The effects of the aminobisphosphonate alendronate on thyroid hormone-induced osteopenia in rats. Calcif. Tissue Int. 53 (1993) 278-282
45. Kato S., Endoh H., Masuhiro Y., Kitamoto T., Uchiyama S., Sasaki H., Masushige S., Gotoh Y., Nishida E., Kawashima H., Metzger D., and Chambon P. Activation of the estrogen receptor through phosphorylation by mitogen-activated protein kinase. Science 270 (1995) 1491-1494
46. Acevedo M.L., Lee K.C., Stender J.D., Katzenellenbogen B.S., and Kraus W.L. Selective recognition of distinct classes of coactivators by a ligand-inducible activation domain. Mol. Cell 13 (2004) 725-738
47. McClung M.R., Siris E., Cummings S., Bolognese M., Ettinger M., Moffett A., Emkey R., Day W., Somayaji V., and Lee A. Prevention of bone loss in postmenopausal women treated with lasofoxifene compared with raloxifene. Menopause 13 (2006) 377-386
48. McDonnell D.P., Clemm D.L., Hermann T., Goldman M.E., and Pike J.W. Analysis of estrogen receptor function in vitro reveals three distinct classes of antiestrogens. Mol. Endocrinol. 9 (1995) 659-669
49. Kedar R.P., Bourne T.H., Powles T.J., Collins W.P., Ashley S.E., Cosgrove D.O., and Campbell S. Effects of tamoxifen on uterus and ovaries of postmenopausal women in a randomised breast cancer prevention trial. Lancet 343 (1994) 1318-1321
50. Lahti E., Blanco G., Kauppila A., Apaja-Sarkkinen M., Taskinen P.J., and Laatikainen T. Endometrial changes in postmenopausal breast cancer patients receiving tamoxifen. Obstet. Gynecol. 81 (1993) 660-664
51. B.R. Macdonald, Clinical assessment of the risk-to-benefit profile of idoxifene, NIH Workshop on SERMS, 2000, p. 143
52. Gennari L. Lasofoxifene (Pfizer). Curr. Opin. Investig. Drugs 6 (2005) 1067-1078
53. Gruber C., and Gurber D. Bazedoxifene. Curr. Opin. Investig. Drugs 5 (2004) 1086-1093
54. Ronkin S., Northington R., Baracat E., Nunes M.G., Archer D.F., Constantine G., and Pickar J.H. Endometrial effects of bazedoxifene acetate, a novel selective estrogen receptor modulator, in postmenopausal women. Obstet. Gynecol. 105 (2005) 1397-1404