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https://www.readbyqxmd.com/read/28412809/selective-estrogen-receptor-modulator-serm-like-activities-of-diarylheptanoid-a-phytoestrogen-from-curcuma-comosa-in-breast-cancer-cells-pre-osteoblast-cells-and-rat-uterine-tissues
#1
Natthakan Thongon, Nittaya Boonmuen, Kanoknetr Suksen, Patsorn Wichit, Arthit Chairoungdua, Patoomratana Tuchinda, Apichart Suksamrarn, Wipawee Winuthayanon, Pawinee- Piyachaturawat
Diarylheptanoids from Curcuma comosa (C. comosa), Zingiberaceae family, exhibit diverse estrogenic activities. In this study we investigated the estrogenic activity of a major hydroxyl diarylheptanoid, 7-(3,4 dihydroxyphenyl)-5-hydroxy-1-phenyl-(1E)-1-heptene (compound-092) isolated from C. comosa. The compound elicited different transcriptional activities of being estrogen agonist at low concentrations (0.1-1 μM) and antagonist at higher concentrations (10-50 μM) using luciferase reporter gene assay in HEK-293T cells...
April 15, 2017: Journal of Agricultural and Food Chemistry
https://www.readbyqxmd.com/read/28401437/estrogens-regulate-life-and-death-in-mitochondria
#2
Carolyn M Klinge
Estrogens coordinate and integrate cellular metabolism and mitochondrial activities by direct and indirect mechanisms mediated by differential expression and localization of estrogen receptors (ER) in a cell-specific manner. Estrogens regulate transcription and cell signaling pathways that converge to stimulate mitochondrial function- including mitochondrial bioenergetics, mitochondrial fusion and fission, calcium homeostasis, and antioxidant defense against free radicals. Estrogens regulate nuclear gene transcription by binding and activating the classical genomic estrogen receptors α and β (ERα and ERβ) and by activating plasma membrane-associated mERα, mERβ, and G-protein coupled ER (GPER, GPER1)...
April 11, 2017: Journal of Bioenergetics and Biomembranes
https://www.readbyqxmd.com/read/28396978/a-novel-strategy-to-co-target-estrogen-receptor-and-nuclear-factor-%C3%AE%C2%BAb-pathways-with-hybrid-drugs-for-breast-cancer-therapy
#3
Irida Kastrati, Marton I Siklos, Svitlana D Brovkovych, Gregory R J Thatcher, Jonna Frasor
Nearly 75% of breast tumors express estrogen receptor (ER), and will be treated with endocrine therapy, such as selective estrogen receptor modulator (SERM), tamoxifen, or aromatase inhibitors. Despite their proven success, as many as 40-50% of ER+ tumors fail to respond to endocrine therapy and eventually recur as aggressive, metastatic cancers. Therefore, preventing and/or overcoming endocrine resistance in ER+ tumors remains a major clinical challenge. Deregulation or activation of the nuclear factor κB (NFκB) pathway has been implicated in endocrine resistance and poor patient outcome in ER+ tumors...
April 10, 2017: Hormones & Cancer
https://www.readbyqxmd.com/read/28396216/assessment-of-the-potential-activity-of-major-dietary-compounds-as-selective-estrogen-receptor-modulators-in-two-distinct-cell-models-for-proliferation-and-differentiation
#4
Sylvain Lecomte, Marie Lelong, Gaëlle Bourgine, Theo Efstathiou, Christian Saligaut, Farzad Pakdel
Estrogen receptors (ERs) α and β are distributed in most tissues of women and men. ERs are bound by estradiol (E2), a natural hormone, and mediate the pleiotropic and tissue-specific effects of E2, such as proliferation of breast epithelial cells or protection and differentiation of neuronal cells. Numerous environmental molecules, called endocrine disrupting compounds, also interact with ERs. Phytoestrogens belong to this large family and are considered potent therapeutic molecules that act through their selective estrogen receptor modulator (SERM) activity...
April 7, 2017: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/28374135/oxabicycloheptene-sulfonate-protects-against-%C3%AE-amyloid-induced-toxicity-by-activation-of-pi3k-akt-and-erk-signaling-pathways-via-gper1-in-c6-cells
#5
Li-Juan Deng, Chen Cheng, Jun Wu, Cai-Hua Wang, Hai-Bing Zhou, Jian Huang
Oxabicycloheptene sulfonate (OBHS) is a novel bicyclic core selective estrogen receptor modulator (SERM) with estrogen receptor (ER) antagonistic-activity and anti-inflammatory activity. However, little is known about protective action of OBHS on neurodegenerative disorders. In the present study, OBHS demonstrated a remarkably protective effect against amyloid beta (Aβ) induced cytotoxicity via G-protein-coupled estrogen receptor 1 (GPER1) in rat astroglial cell line (C6). The C6 cell death induced by Aβ was decreased by OBHS (1 μM) treatment for 45 min...
April 4, 2017: Neurochemical Research
https://www.readbyqxmd.com/read/28372959/-cherchez-la-femme-modulation-of-estrogen-receptor-function-with-selective-modulators-clinical-implications-in-the-field-of-urology
#6
REVIEW
Sevann Helo, Blake Wynia, Andrew McCullough
INTRODUCTION: Selective estrogen receptor modulators (SERMs) have been used off-label in men for more than 50 years. SERMs exert their action on the estrogen receptor agonistically or antagonistically. A fundamental knowledge of the complex molecular action and physiology of SERMs is important in understanding their use and future directions of study in men. AIM: To review the basic science and mechanism of the action of estrogens, the estrogen receptor, and SERMs, and the existing clinical publications on the use of SERMs in men for infertility and hypogonadism with their strengths and weaknesses and to identify the need for future studies...
March 31, 2017: Sexual Medicine Reviews
https://www.readbyqxmd.com/read/28364860/regulatory-effects-of-estetrol-on-the-endothelial-plasminogen-pathway-and-endothelial-cell-migration
#7
Maria Magdalena Montt-Guevara, Giulia Palla, Stefania Spina, Guja Bernacchi, Elena Cecchi, Adrian Esteban Campelo, Jorge Eduardo Shortrede, Alessio Canu, Tommaso Simoncini
BACKGROUND: Estetrol (E4) is a natural estrogen produced solely during human pregnancy. E4 is suitable for clinical use since it acts as a selective estrogen receptor modulator. In clinical trials E4 has been seen to have little or no effect on coagulation. Hence, it is interesting to investigate whether E4 alters endothelial-dependent fibrinolysis. OBJECTIVES: We studied the effects of E4 on the fibrinolytic system and whether this could influence the ability of endothelial cells to migrate...
May 2017: Maturitas
https://www.readbyqxmd.com/read/28349511/risk-of-endometrial-cancer-in-women-treated-with-ovary-stimulating-drugs-for-subfertility
#8
REVIEW
Alkistis Skalkidou, Theodoros N Sergentanis, Spyros P Gialamas, Marios K Georgakis, Theodora Psaltopoulou, Marialena Trivella, Charalampos S Siristatidis, Evangelos Evangelou, Eleni Petridou
BACKGROUND: Medical treatment for subfertility principally involves the use of ovary-stimulating agents, including selective oestrogen receptor modulators (SERMs), such as clomiphene citrate, gonadotropins, gonadotropin-releasing hormone (GnRH) agonists and antagonists, as well as human chorionic gonadotropin. Ovary-stimulating drugs may act directly or indirectly upon the endometrium (lining of the womb). Nulliparity and some causes of subfertility are recognized as risk factors for endometrial cancer...
March 25, 2017: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/28319725/antiestrogen-use-in-breast-cancer-patients-reduces-the-risk-of-subsequent-lung-cancer-a-population-based-study
#9
Sung-Chao Chu, Chia-Jung Hsieh, Tso-Fu Wang, Mun-Kun Hong, Tang-Yuan Chu
BACKGROUND: There is accumulating epidemiological and preclinical evidence that estrogen might be a driver of lung cancer. Breast cancer survivors can offer a unique patient cohort to examine the effect of antiestrogen therapy on lung cancer carcinogenesis because many of these women would have received long-term selective estrogen receptor modulators (SERMs) and/or aromatase inhibitors (AIs) as adjuvant treatment. Our hypothesis is that estrogens play a role in lung cancer development, and that antiestrogen therapy would affect the incidence of subsequent lung cancer among breast cancer survivors...
March 17, 2017: Cancer Epidemiology
https://www.readbyqxmd.com/read/28283546/functional-association-of-oestrogen-receptors-with-hpv-infection-in-cervical-carcinogenesis
#10
REVIEW
Balaji Ramachandran
Repeated parity and usage of oral contraceptives have demonstrated an increased risk of cervical cancer (CC) in HPV-infected women. These lifestyle observations raise the likelihood that oestrogens and HPV infection might act synergistically to affect cancers of the cervix. In vivo studies have indicated the requirement of oestrogens and ERα in the development of atypical squamous metaplasia followed by cervical intraepithelial neoplasia (CIN) I, II and III. CIN II and III are precancerous cervical lesions that can progress over time to CC as an invasive carcinoma...
April 2017: Endocrine-related Cancer
https://www.readbyqxmd.com/read/28281842/opportunities-and-challenges-of-long-term-anti-estrogenic-adjuvant-therapy-treatment-forever-or-intermittently
#11
Poulomi Bhattacharya, Balkees Abderrahman, V Craig Jordan
Extended adjuvant (5-10 years) therapy targeted to the estrogen receptor (ER) has significantly decreased mortality from breast cancer (BC). Areas covered: Translational research advanced clinical testing of extended adjuvant therapy with tamoxifen or aromatase inhibitors (AIs). Short term therapy or non-compliance increase recurrence, but surprisingly recurrence and death does not increase dramatically after 5 years of adjuvant therapy stops. Expert commentary: Compliance ensures optimal benefit from extended antihormone adjuvant therapy...
April 2017: Expert Review of Anticancer Therapy
https://www.readbyqxmd.com/read/28261281/induction-of-mitochondrial-apoptotic-pathway-by-raloxifene-and-estrogen-in-human-endometrial-stromal-thesc-cell-line
#12
Ivana Nikolic, Marija Andjelkovic, Milan Zaric, Ivanka Zelen, Petar Canovic, Zoran Milosavljevic, Marina Mitrovic
INTRODUCTION: Endometrial hyperplasia is a condition that occurs as a result of hormonal imbalance between estrogen and progesterone. Morphological disturbance of endometrial cells occurs consequently leading towards endometrial cancer. In therapy of endometrial hyperplasia SERMs are used to supress effects of locally high estrogen level in uterus. There is strong evidence suggesting that estrogen could be involved in cell death - apoptosis. There are no experimental data demstrating the direct apoptotic effect of both raloxifene and estrogen on the ThESC cell line...
March 1, 2017: Archives of Medical Science: AMS
https://www.readbyqxmd.com/read/28252426/adjuvant-hormonal-therapy-as-a-cause-of-bone-loss-in-patients-with-breast-cancer-review-of-literature
#13
REVIEW
N Khachidze, E Giorgadze, M Tsagareli
Adjuvant (hormonal) therapy is the main method of treatment after surgery in hormone (estrogen and/or progesterone) positive breast cancer patients. The goal of above mentioned treatment is to reduce or block the level of estrogen and progesterone. ultiple clinical trials have revealed that hormonal therapy in breast cancer patients affect bone mineral density (BMD). Authors have analyzed data obtained from several clinical trials conducted in several countries (including Georgia). The final conclusion is that selective estrogen receptor modulators (SERMs) have negative effect on BMD in pre-menopausal women and aromatase inhibitors (anastrozole, letrozole, exemestane) are associated with significant bone loss in post-menopausal women...
January 2017: Georgian Medical News
https://www.readbyqxmd.com/read/28246081/the-4ps-of-breast-cancer-chemoprevention-putting-proven-principles-into-practice
#14
EDITORIAL
V Craig Jordan
The pioneering Royal Marsden Tamoxifen Prevention Trial recruited 2,471 eligible high-risk women to be randomized to either placebo or tamoxifen (20 mg daily) for 8 years. Breast cancer incidence was evaluated at a median of 18.4 years from the start of the study. There was a 32% reduction in estrogen/progesterone receptor (ER/PR)-positive breast cancers after tamoxifen treatment finished. Translational research, to study "the good, the bad, and the ugly of tamoxifen" in the 1980s, subsequently ensured women's safety from possible increases in osteoperosis, coronary heart disease, and endometrial cancer...
April 2017: Cancer Prevention Research
https://www.readbyqxmd.com/read/28228354/effect-of-tamoxifen-on-spermatogenesis-and-testicular-steroidogenesis
#15
Rachna Verma, Amitabh Krishna
The aim of this study was to evaluate the effects of in vivo and in vitro treatments with selective estrogen receptor modulator (SERM), tamoxifen on testicular functions. The testis treated with tamoxifen, in vivo or in vitro, showed dose-dependent regressive changes in spermatogenesis. This study showed that the decreased estrogenic effect due to tamoxifen may be directly responsible for decreased testicular expression of aromatase, which in turn may be responsible for decreased synthesis of estradiol in the testis...
April 22, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28185712/the-effect-of-selective-estrogen-receptor-modulators-on-type-2-diabetes-onset-in-women-basic-and-clinical-insights
#16
REVIEW
Beibei Xu, Dragana Lovre, Franck Mauvais-Jarvis
Selective estrogen receptor modulators (SERMs) are a class of compounds that interact with estrogen receptors (ERs) and exert agonist or antagonist effects on ERs in a tissue-specific manner. Tamoxifen, a first generation SERM, is used for treatment of ER positive breast cancer. Raloxifene, a second generation SERM, was used to prevent postmenopausal osteoporosis. The third-generation SERM bazedoxifene (BZA) effectively prevents osteoporosis while preventing estrogenic stimulation of breast and uterus. Notably, BZA combined with conjugated estrogens (CE) is a new menopausal treatment...
April 2017: Journal of Diabetes and its Complications
https://www.readbyqxmd.com/read/28163101/identification-of-mirnas-as-biomarkers-for-acquired-endocrine-resistance-in-breast-cancer
#17
Penn Muluhngwi, Carolyn M Klinge
Therapies targeting estrogen receptor α (ERα) including tamoxifen, a selective estrogen receptor modulator (SERM) and aromatase inhibitors (AI), e.g., letrozole, have proven successful in reducing the death rate for breast cancer patients whose initial tumors express ERα. However, about 40% of patients develop acquired resistance to these endocrine treatments. There is a critical need to develop sensitive circulating biomarkers that accurately identify signaling pathways altered in breast cancer patients resistant to endocrine therapies...
February 2, 2017: Molecular and Cellular Endocrinology
https://www.readbyqxmd.com/read/28140792/determination-and-confirmation-of-selective-estrogen-receptor-modulators-serms-anti-estrogens-and-aromatase-inhibitors-in-bovine-and-porcine-urine-using-uhplc-ms-ms
#18
Thijs Meijer, Martien L Essers, George Kaklamanos, Saskia S Sterk, Leendert A van Ginkel
Selective estrogen receptor modulators (SERMs), anti-estrogens and aromatase inhibitors are prohibited in human sports doping. However, they also present a risk of being used illegally in animal husbandry for fattening purposes. A method was developed and validated using UHPLC-MS/MS for the determination and confirmation of SERMs, anti-estrogens and aromatase inhibiters in bovine and porcine urine. This method was used in a survey of more than 200 bovine and porcine urine samples from Dutch farms. In 18 out of 103 porcine urine samples (17%) and two out of 114 bovine samples (2%) formestane, an aromatase inhibitor, was detected...
April 2017: Food Additives & Contaminants. Part A, Chemistry, Analysis, Control, Exposure & Risk Assessment
https://www.readbyqxmd.com/read/28131133/combined-pharmacologic-therapy-in-postmenopausal-osteoporosis
#19
REVIEW
Yang Shen, Dona L Gray, Dorothy S Martinez
Antiresorptive agents for treating postmenopausal osteoporosis include selective estrogen receptor modulator (SERM), bisphosphonates and denoumab. Teriparatide is the only Food and Drug Administration-approved anabolic agent. Synergistic effects of combining teriparatide with an antiresorptive agent have been proposed and studied. This article reviews the trial designs and the outcomes of combination therapies. Results of the combination therapy for teriparatide and bisphosphonates were mixed; while small increases of bone density were observed in the combination therapy of teriparatide and estrogen/SERM and that of teriparatide and denosumab...
March 2017: Endocrinology and Metabolism Clinics of North America
https://www.readbyqxmd.com/read/28123120/-drug-selection-and-treatment-goal-in-osteoporosis-therapy
#20
Mika Yamauchi, Toshitsugu Sugimoto
The goal of treatment for osteoporosis is to reduce the risk of fracture. Achieving effective reductions in the risk of fracture requires evidence-based drug selection and careful consideration of patient background, including concomitant diseases and drug adherence. Selective estrogen receptor modulators(SERM)and active vitamin D3 such as eldecalcitol are well indicated in early menopausal women with no history of fragility fractures. Moreover, elderly individuals with a history of fragility fractures are at high risk of vertebral and hip fractures, so bisphosphonates, denosumab and teriparatide are well indicated in these patients...
2017: Clinical Calcium
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