Receptors, Estrogen

Publication Title: 
The Journal of Biological Chemistry

Estrogen receptors (ER alpha/ER beta) are expressed in neuronal cells and exhibit a variety of activities in the central nervous system. ER activity is regulated in a ligand-dependent manner and by co-regulatory factors. Caveolin-1 is a recently identified co-activator of ER alpha mediating the ligand-independent activation of this steroid receptor. Here the influence of ERs on caveolin expression in human neuroblastoma SK-N-MC cells as well as in rodent brain was investigated.

Author(s): 
Zschocke, J¸rgen
Manthey, Dieter
Bayatti, Nadhim
van der Burg, Bart
Goodenough, Sharon
Behl, Christian
Publication Title: 
Chemical & Pharmaceutical Bulletin

Extensive chromatographic screening of extracts of the fruits of the Indian Ayurvedic plant, Dendrophthoe falcata, resulted in the isolation of three new triterpenes, 3beta-acetoxy-1beta-(2-hydroxy-2-propoxy)-11alpha-hydroxy-olean-12-ene (1), 3beta-acetoxy-11alpha-ethoxy-1beta-hydroxy-olean-12-ene (2) and 3beta-acetoxy-1beta-hydroxy-11alpha-methoxy-olean-12-ene (3) along with nine known compounds, 3beta-acetoxy-1beta,11alpha-dihydroxy-olean-12-ene (4), 3beta-acetoxy-1beta,11alpha-dihydroxy-urs-12-ene (5), 3beta-acetoxy-urs-12-ene-11-one (6), 3beta-acetoxy-lup-20(29)-ene (7), 30-nor-lup-3bet

Author(s): 
Mallavadhani, Uppuluri Venkata
Narasimhan, Kilambi
Sudhakar, Akella Venkata Subrahmanya
Mahapatra, Anita
Li, Wenkui
van Breemen, Richard Bruce
Publication Title: 
Chemical & Pharmaceutical Bulletin

Extensive chromatographic screening of extracts of the fruits of the Indian Ayurvedic plant, Dendrophthoe falcata, resulted in the isolation of three new triterpenes, 3beta-acetoxy-1beta-(2-hydroxy-2-propoxy)-11alpha-hydroxy-olean-12-ene (1), 3beta-acetoxy-11alpha-ethoxy-1beta-hydroxy-olean-12-ene (2) and 3beta-acetoxy-1beta-hydroxy-11alpha-methoxy-olean-12-ene (3) along with nine known compounds, 3beta-acetoxy-1beta,11alpha-dihydroxy-olean-12-ene (4), 3beta-acetoxy-1beta,11alpha-dihydroxy-urs-12-ene (5), 3beta-acetoxy-urs-12-ene-11-one (6), 3beta-acetoxy-lup-20(29)-ene (7), 30-nor-lup-3bet

Author(s): 
Mallavadhani, Uppuluri Venkata
Narasimhan, Kilambi
Sudhakar, Akella Venkata Subrahmanya
Mahapatra, Anita
Li, Wenkui
van Breemen, Richard Bruce
Publication Title: 
Journal of the American Society for Mass Spectrometry

Although hormone replacement therapy (HRT) is used by post-menopausal women for the relief of menopausal symptoms and the potential reduction of osteoporosis, HRT also increases their risk of Alzheimer's disease, stroke, breast cancer, and endometrial cancer. Since the majority of these effects are associated primarily with estrogen binding to only one of the estrogen receptors (ER), new assays are needed that can more efficiently evaluate ER-binding and identify ligands selective for ER-alpha and ER-beta.

Author(s): 
Sun, Yongkai
Gu, Chungang
Liu, Xuemei
Liang, Wenzhong
Yao, Ping
Bolton, Judy L.
van Breemen, Richard B.
Publication Title: 
American Journal of Physiology. Heart and Circulatory Physiology

The antiatherogenic effects of soy isoflavone consumption have been demonstrated in a variety of studies. However, the mechanisms involved remain poorly defined. Adhesion of monocytes to vascular endothelial cells is a key step within the inflammatory cascade that leads to atherogenesis. Many factors, including the physical forces associated with blood flow, regulate this process.

Author(s): 
Chacko, Balu K.
Chandler, Robert T.
Mundhekar, Ameya
Khoo, Nicholas
Pruitt, Heather M.
Kucik, Dennis F.
Parks, Dale A.
Kevil, Christopher G.
Barnes, Stephen
Patel, Rakesh P.
Publication Title: 
Cancer Research

1,25-Dihydroxyvitamin D3 [1,25(OH)2D3], the active metabolite of vitamin D3, inhibits the proliferation of prostate cancer cells. However, the molecular mechanisms by which 1,25(OH)2D3 inhibits the proliferation of these cells remain to be fully elucidated. In this study, we used microarray technology to identify target genes of 1,25(OH)2D3 in androgen-responsive prostate cancer LNCaP cells. 1,25(OH)2D3 up-regulated CCAAT/enhancer-binding protein delta (C/EBPdelta) by approximately 5-fold in these cells.

Author(s): 
Ikezoe, Takayuki
Gery, Sigal
Yin, Dong
O'Kelly, James
Binderup, Lise
Lemp, Nathan
Taguchi, Hirokuni
Koeffler, H. Phillip
Publication Title: 
Cancer Research

Soy isoflavones are promising dietary agents for prevention of breast cancer. Isoflavones bind estrogen receptors (ER) and may variably act as either estrogen agonists or antagonists depending on the estrogen environment. In this study, we used a postmenopausal primate model to evaluate interactive effects of dietary soy isoflavones and estrogen on risk markers for breast cancer.

Author(s): 
Wood, Charles E.
Register, Thomas C.
Franke, Adrian A.
Anthony, Mary S.
Cline, J. Mark
Publication Title: 
Veterinary Pathology

Macaques provide an important animal model for the study of hormonal agents and their effects on risk biomarkers for breast cancer. A common criticism of this model is that spontaneous breast cancer has rarely been described in these animals. In this report, we characterize 35 mammary gland lesions ranging from ductal hyperplasia to carcinoma in situ and invasive ductal carcinoma in cynomolgus and rhesus macaques. Based on a retrospective analysis, we estimated the lifetime incidence of mammary gland neoplasia in aged female macaques to be about 6%.

Author(s): 
Wood, C. E.
Usborne, A. L.
Starost, M. F.
Tarara, R. P.
Hill, L. R.
Wilkinson, L. M.
Geisinger, K. R.
Feiste, E. A.
Cline, J. M.
Publication Title: 
Carcinogenesis

Endogenous estrogens are important determinants of breast cancer risk in postmenopausal women. In this study we evaluated the effects of dietary soy isoflavonoids on endogenous estrogen metabolism in a postmenopausal primate model.

Author(s): 
Wood, Charles E.
Register, Thomas C.
Cline, J. Mark
Publication Title: 
Molecular Carcinogenesis

Although tamoxifen (TAM) is used for the front-line treatment and prevention of estrogen receptor-positive (ER+) breast tumors, nearly 40% of estrogen-dependent breast tumors do not respond to TAM treatment. Moreover, the positive response is usually of short duration, and most tumors eventually develop TAM-resistance. Overexpression of HER2 gene is associated with TAM-resistance of breast tumor, and suppression of HER2 expression enhances the TAM activity. Soy isoflavone genistein has been shown to have anti-cancer activities and suppress expression of HER2 and ERalpha.

Author(s): 
Mai, Zhiming
Blackburn, George L.
Zhou, Jin-Rong

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