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Estrogen receptor

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https://www.readbyqxmd.com/read/28441761/e2-er-%C3%AE-enhances-calcineurin-protein-degradation-and-pi3k-akt-mdm2-signal-transduction-to-inhibit-iso-induced-myocardial-cell-apoptosis
#1
Kuan-Ho Lin, Wei-Wen Kuo, Marthandam Asokan Shibu, Cecilia-Hsuan Day, You-Liang Hsieh, Li-Chin Chung, Ray-Jade Chen, Su-Ying Wen, Vijaya Padma Viswanadha, Chih-Yang Huang
Secretion of multifunctional estrogen and its receptor has been widely considered as the reason for markedly higher frequency of heart disease in men than in women. 17β-Estradiol (E2), for instance, has been reported to prevent development of cardiac apoptosis via activation of estrogen receptors (ERs). In addition, protein phosphatase such as protein phosphatase 1 (PP1) and calcineurin (PP2B) are also involved in cardiac hypertrophy and cell apoptosis signaling. However, the mechanism by which E2/ERβ suppresses apoptosis is not fully understood, and the role of protein phosphatase in E2/ERβ action also needs further investigation...
April 24, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28441746/high-performance-prediction-of-human-estrogen-receptor-agonists-based-on-chemical-structures
#2
Yuki Asako, Yoshihiro Uesawa
Many agonists for the estrogen receptor are known to disrupt endocrine functioning. We have developed a computational model that predicts agonists for the estrogen receptor ligand-binding domain in an assay system. Our model was entered into the Tox21 Data Challenge 2014, a computational toxicology competition organized by the National Center for Advancing Translational Sciences. This competition aims to find high-performance predictive models for various adverse-outcome pathways, including the estrogen receptor...
April 23, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28440874/role-of-glycogen-synthase-kinase-3-in-ischemia-induced-blood-brain-barrier-disruption-in-aged-female-rats
#3
Han Xiao, Mingyang Deng, Binbin Yang, Jianguang Tang, Zhiping Hu
Estrogen receptors have protective effects against ischemic brain injury. However, the molecular mechanisms underlying this phenomenon have yet to be well studied. Given that inhibition of glycogen synthase kinase (GSK3) can reduce cerebral ischemia/reperfusion injury, we hypothesized that estrogen receptors-mediated protective effects against ischemia-induced blood brain barrier (BBB) disruption involve inhibition of GSK3. Thus, we evaluated GSK3 expression in the brain of ovariectomized female rats, and examined the effects of intracerebroventricular pre-treatments of SB216763, GSK3 inhibitor, on BBB permeability following middle cerebral artery occlusion (MCAO)...
April 25, 2017: Journal of Neurochemistry
https://www.readbyqxmd.com/read/28440733/morphological-and-morphometric-analysis-of-the-effects-of-intralesional-tamoxifen-on-keloids
#4
Lauro R Soares-Lopes, Ione M Soares-Lopes, Lauro Ll Filho, Airlane P Alencar, Benedito B da Silva
The aim of this study was to evaluate the effect of intralesional tamoxifen on keloids, particularly on the concentration of fibroblasts, dermal inflammatory infiltrate, and collagen degeneration. A prospective study was carried out to evaluate keloids in 13 patients of both genders pre- and post-treatment with intralesional tamoxifen. Two samples of keloid lesions were obtained by 4-mm punch biopsies during the study: the first at the time of diagnostic confirmation of keloid and the other eight weeks later at the end of intralesional tamoxifen treatment...
May 2017: Experimental Biology and Medicine
https://www.readbyqxmd.com/read/28440677/no-association-between-estrogen-receptor-gene-polymorphisms-and-premature-thelarche-in-girls
#5
Hae Sang Lee, Jong Seo Yoon, Cheol Hwan So, Kyung Hee Kim, Jin Soon Hwang
OBJECTIVE: Premature thelarche (PT) is a benign, nonprogressive condition defined as isolated breast development. While the pathophysiology of PT remains unclear, increased sensitivity to estrogen may cause PT. The aim of this study was to investigate the association between polymorphisms in the estrogen receptor alpha (ERα) gene and PT in girls. METHODS: In this case-control study, we examined 96 girls referred for early breast development (before the age of 8 years)...
April 25, 2017: Gynecological Endocrinology
https://www.readbyqxmd.com/read/28440514/silibinin-downregulates-mmp2-expression-via-jak2-stat3-pathway-and-inhibits-the-migration-and-invasive-potential-in-mda-mb-231-cells
#6
Hyo Joo Byun, Pramod Darvin, Dong Young Kang, Nipin Sp, Youn Hee Joung, Jong Hwan Park, Sun Jin Kim, Young Mok Yang
Worldwide, breast cancer (BCa) is the most common cancer in women. Among its subtypes, triple-negative breast cancer (TNBC) is an aggressive form associated with diminished survival. TNBCs are characterized by their absence, or minimal expression, of the estrogen and progesterone receptors, as well as the human epidermal growth factor receptor 2 (i.e. ER-/-, PR-/-, Her2-/Low). Consequently, treatment for this subtype of BCa remains problematic. Silibinin, a derivative of the flavonoid silymarin, is reported to have anticancer activities against hepatic and non-small cell lung cancers...
April 19, 2017: Oncology Reports
https://www.readbyqxmd.com/read/28440460/triple-negative-breast-cancer-new-therapeutic-options-via-signalling-transduction-cascades
#7
Ulrich Andergassen, Alexandra C Kölbl, Jan-Niclas Mumm, Sven Mahner, Udo Jeschke
Triple-negative breast cancer is a highly aggressive type of mammalian carcinoma. It is defined by a rather weak expression of estrogen-, progesterone- and Her2-receptor, and is thus difficult to treat, resulting in low disease-free and overall survival rates of the affected patients. Hence it is important to find new therapeutic options. To this aim we analysed the incidence of some molecules from different signal transduction cascades by immunohistochemistry, which are known to correlate with triple-negative breast cancer, and correlated the expression of these molecules to different tumour traits, such as size, grading, menopausal stage, histology, lymph node affection, remote metastasis formation, and to the incidence of local and lymph node recurrence and metastasis by statistical analysis...
May 2017: Oncology Reports
https://www.readbyqxmd.com/read/28440394/g-protein-coupled-receptor-30-mediates-the-effects-of-estrogen-on-endothelial-cell-tube-formation-in%C3%A2-vitro
#8
Liyuan Zhou, Hong Chen, Xun Mao, Hongbo Qi, Philip N Baker, Hua Zhang
The placenta is the exchange organ between the mother and the fetus. The inadequate function of this organ is associated with a number of pregnancy disorders. Hypoxia and oxidative stress during placental development may induce endothelial dysfunction, resulting in the reduction in the perfusion of the placenta. During pregnancy, the levels of estrogen are increased. Decreased estrogen levels have been reported in women with preeclampsia. However, whether estrogen is involved in placental angiogenesis remains unclear...
April 20, 2017: International Journal of Molecular Medicine
https://www.readbyqxmd.com/read/28439683/genistein-modulation-of-seizure-involvement-of-estrogen-and-serotonin-receptors
#9
Saeed Amiri Gheshlaghi, Razieh Mohammad Jafari, Mohammad Algazo, Nastaran Rahimi, Hussein Alshaib, Ahmad Reza Dehpour
Genistein, a major source of phytoestrogen exposure for humans and animals, has been shown to mediate neuroprotection in Alzheimer's disease and status epilepticus. In the present study, we investigated the effect of genistein on pentylenetetrazole-induced seizures in ovariectomized mice and the possible involvement of estrogenic and serotonergic pathways in the probable effects of genistein. Intraperitoneal (i.p.) administration of genistein (10 mg/kg) significantly increased the seizure threshold 30 min prior to induction of seizures 14 days after ovariectomy surgery...
April 24, 2017: Journal of Natural Medicines
https://www.readbyqxmd.com/read/28439061/-calcium-and-bone-metabolism-across-women-s-life-stages-bone-quality-and-treatment-of-osteoporosis-by-serm
#10
Mitsuru Saito, Keishi Marumo
Estrogen deficiency induces bone resorption and bone collagen crosslink abnormalities such as reductions in enzymatic cross-links and accumulation of Advanced glycation end products(AGEs). In this review, we described that the mechanism of poor bone quality in estrogen deficiency and how selective estrogen receptor modulators such as raloxifene and bazedoxifene improve bone structural and material properties.
2017: Clinical Calcium
https://www.readbyqxmd.com/read/28439055/-calcium-and-bone-metabolism-across-women-s-life-stages-bone-metabolism-and-estrogen-androgen-balance-in-women
#11
Toshiyuki Yasui, Miwa Fukuoka
Androgen as well as estrogen has physical, psychological and sexual roles in women. The action of androgen on bone health in women is important. The androgen receptor is expressed in osteoblasts and osteocytes but the mechanism has not been clarified in women. It has been reported that endogenous testosterone level was positively correlated with bone mineral density and higher testosterone level might be associated with decrease in bone fractures. Also, it has been reported that bone mineral density in women who received testosterone with estrogen was higher than that in women who received estrogen alone...
2017: Clinical Calcium
https://www.readbyqxmd.com/read/28439051/-calcium-and-bone-metabolism-across-women-s-life-stages-molecular-mechanisms-underlying-bone-metabolism-by-estrogen
#12
Yuuki Imai
Osteoporosis, which patients are estimated as more than 13 million in Japan, is mainly caused by postmenopausal osteoporosis. Estrogen deficiency induced by menopause can disturb endocrine feedback and homeostasis, followed by bone loss by increased bone resorption with high bone turnover. Recent studies using systemic or conditional Estrogen Receptor α(ERα)gene knockout mice have unveiled molecular mechanisms underlying bone metabolism. In this review, it will be discussed that direct and indirect effects of estrogen and its metabolites for bone metabolism...
2017: Clinical Calcium
https://www.readbyqxmd.com/read/28439009/estrogen-receptor-%C3%AE-a-regulator-of-androgen-receptor-signaling-in-the-mouse-ventral-prostate
#13
Wan-Fu Wu, Laure Maneix, Jose Insunza, Ivan Nalvarte, Per Antonson, Juha Kere, Nancy Yiu-Lin Yu, Virpi Tohonen, Shintaro Katayama, Elisabet Einarsdottir, Kaarel Krjutskov, Yu-Bing Dai, Bo Huang, Wen Su, Margaret Warner, Jan-Åke Gustafsson
As estrogen receptor β(-/-) (ERβ(-/-)) mice age, the ventral prostate (VP) develops increased numbers of hyperplastic, fibroplastic lesions and inflammatory cells. To identify genes involved in these changes, we used RNA sequencing and immunohistochemistry to compare gene expression profiles in the VP of young (2-mo-old) and aging (18-mo-old) ERβ(-/-) mice and their WT littermates. We also treated young and old WT mice with an ERβ-selective agonist and evaluated protein expression. The most significant findings were that ERβ down-regulates androgen receptor (AR) signaling and up-regulates the tumor suppressor phosphatase and tensin homolog (PTEN)...
April 24, 2017: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/28438785/nuclear-receptor-research-in-zebrafish
#14
Marcel J M Schaaf
Nuclear receptors (NRs) form a superfamily of transcription factors that can be activated by ligands and are involved in a wide range of physiological processes. NRs are well conserved between vertebrate species. The zebrafish, an increasingly popular animal model system, contains a total of 73 NR genes, and orthologues of almost all human NRs are present. In this review article, an overview is presented of NR research in which the zebrafish has been used as a model. Research is described on the three most studied zebrafish NRs: the Estrogen Receptors (ERs), Retinoic Acid Receptors (RARs) and Peroxisome Proliferator-Activated Receptors (PPARs)...
April 24, 2017: Journal of Molecular Endocrinology
https://www.readbyqxmd.com/read/28438614/the-expression-of-growth-hormone-releasing-hormone-ghrh-and-its-receptors-in-breast-carcinomas-with-apocrine-differentiation-further-evidence-of-the-presence-of-a-ghrh-pathway-in-these-tumors
#15
Bence Kővári, Semir Vranic, Caterina Marchio, Anna Sapino, Gábor Cserni
Apocrine breast carcinomas were evaluated for the expression of components of the growth hormone-releasing hormone (GHRH) autocrine/paracrine pathway: GHRH and its receptors (GHRH-R), as mammary apocrine carcinomas and epithelium seemed to be uniformly positive for GHRH-R in a pilot study. The apocrine phenotype was determined on the basis of hematoxylin-eosin morphology and a congruent immunohistochemical profile (estrogen receptor negativity, androgen receptor and gross cystic disease fluid protein-15 positivity)...
April 21, 2017: Human Pathology
https://www.readbyqxmd.com/read/28438385/small-molecules-inhibit-stat3-activation-autophagy-and-cancer-cell-anchorage-independent-growth
#16
Donghui Zhou, Maya Z Springer, David Xu, Degang Liu, Andy Hudmon, Kay F Macleod, Samy O Meroueh
Triple-negative breast cancers (TNBCs) lack the signature targets of other breast tumors, such as HER2, estrogen receptor, and progesterone receptor. These aggressive basal-like tumors are driven by a complex array of signaling pathways that are activated by multiple driver mutations. Here we report the discovery of 6 (KIN-281), a small molecule that inhibits multiple kinases including maternal leucine zipper kinase (MELK) and the non-receptor tyrosine kinase bone marrow X-linked (BMX) with single-digit micromolar IC50s...
March 23, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28438091/analytic-response-curves-of-clinical-breast-cancer-ihc-tests
#17
Kodela Vani, Seshi R Sompuram, Anika K Schaedle, Anuradha Balasubramanian, Steven A Bogen
An important limitation in the field of immunohistochemistry (IHC) is the inability to correlate stain intensity with specific analyte concentrations. Clinical immunohistochemical tests are not described in terms of analytic response curves, namely, the analyte concentrations in a tissue sample at which an immunohistochemical stain (1) is first visible, (2) increases in proportion to the analyte concentration, and (3) ultimately approaches a maximum color intensity. Using a new immunostaining tool ( IHControls), we measured the analytic response curves of the major clinical immunohistochemical tests for human epidermal growth factor receptor type II (HER-2), estrogen receptor (ER), and progesterone receptor (PR)...
May 2017: Journal of Histochemistry and Cytochemistry: Official Journal of the Histochemistry Society
https://www.readbyqxmd.com/read/28438054/evaluation-of-active-hexose-correlated-compound-ahcc-in-combination-with-anticancer-hormones-in-orthotopic-breast-cancer-models
#18
Lata Mathew, Anjali Gaikwad, Anneliese Gonzalez, Elizabeth K Nugent, Judith A Smith
OBJECTIVE: To determine the impact on antitumor activity when active hexose correlated compound (AHCC) in combination with anticancer hormonal agents in orthotopic mouse models of human estrogen receptor positive breast cancer and evaluate impact of AHCC on aromatase activity. METHODS: The study consisted of 7 treatment arms (n=10) conducted in 2 breast cancer mouse models: MCF-7 and ZR-75. Treatment groups included untreated, vehicle, AHCC 50 mg/kg, AHCC 50 mg/kg + tamoxifen 10 mg/kg, tamoxifen 10 mg/kg, AHCC 50 mg/kg + letrozole 10 µg/mouse, or letrozole 10 µg/mouse...
April 1, 2017: Integrative Cancer Therapies
https://www.readbyqxmd.com/read/28437394/selective-degradation-of-splicing-factor-caper%C3%AE-by-anticancer-sulfonamides
#19
Taisuke Uehara, Yukinori Minoshima, Koji Sagane, Naoko Hata Sugi, Kaoru Ogawa Mitsuhashi, Noboru Yamamoto, Hiroshi Kamiyama, Kentaro Takahashi, Yoshihiko Kotake, Mai Uesugi, Akira Yokoi, Atsushi Inoue, Taku Yoshida, Miyuki Mabuchi, Akito Tanaka, Takashi Owa
Target-protein degradation is an emerging field in drug discovery and development. In particular, the substrate-receptor proteins of the cullin-ubiquitin ligase system play a key role in selective protein degradation, which is an essential component of the anti-myeloma activity of immunomodulatory drugs (IMiDs), such as lenalidomide. Here, we demonstrate that a series of anticancer sulfonamides NSC 719239 (E7820), indisulam, and NSC 339004 (chloroquinoxaline sulfonamide, CQS) induce proteasomal degradation of the U2AF-related splicing factor coactivator of activating protein-1 and estrogen receptors (CAPERα) via CRL4(DCAF15) mediated ubiquitination in human cancer cell lines...
April 24, 2017: Nature Chemical Biology
https://www.readbyqxmd.com/read/28436411/benign-mixed-epithelial-and-stromal-tumor-of-the-kidney-with-inferior-vena-cava-tumor-thrombus-a-rare-case-report-and-review-of%C3%A2-literature
#20
Chi Zhang, Xiaofei Li, Chengqiang Mo, Zhenpeng Peng, Ruilin Yang, Yiming Tang, Yuanyuan Zhang, Rongpei Wu
Mixed epithelial and stromal tumor of the kidney (MESTK) is a rare renal tumor composed of epithelial and stromal cells. In this study, we report a rare case of MESTK, which was pathologically benign but complicated with renal vein and inferior vena cava tumor thrombus. The 50-year-old female patient was admitted to hospital for a mass on the left kidney. Computed tomography showed a 32 mm×18 mm mass with slight delayed enhancement in the left renal sinus, and neoplastic thrombus was detected in left renal vein and inferior vena cava...
April 18, 2017: Journal of X-ray Science and Technology
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