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https://www.readbyqxmd.com/read/29906493/the-tamoxifen-derivative-ridaifen-b-is-a-high-affinity-selective-cb-2-receptor-inverse-agonist-exhibiting-anti-inflammatory-and-anti-osteoclastogenic-effects
#1
Lirit N Franks, Benjamin M Ford, Toshifumi Fujiwara, Haibo Zhao, Paul L Prather
Selective estrogen receptor modulators (SERMs) target estrogen receptors (ERs) to treat breast cancer and osteoporosis. Several SERMs exhibit anti-cancer activity not related to ERs. To discover novel anti-cancer drugs acting via ER-independent mechanisms, derivatives of the SERM tamoxifen, known as the "ridaifen" compounds, have been developed that exhibit reduced or no ER affinity, while maintaining cytotoxicity. Tamoxifen and other SERMs bind to cannabinoid receptors with moderate affinity. Therefore, ER-independent effects of SERMs might be mediated via cannabinoid receptors...
June 12, 2018: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/29901634/high-dose-fulvestrant-as-third-line-endocrine-therapy-for-breast-cancer-metastasis-to-the-left-kidney-a-case-report-and-literature-review
#2
Dandan Xia, Huiyu Wang, Runjie Wang, Chaoying Liu, Junying Xu
RATIONALE: Endocrine therapy plays an important role in the treatment of patients with hormone receptor-positive breast cancer. Renal metastasis of breast cancer is rare in clinical practice. PATIENT CONCERNS: We present here a 54-year-old woman with breast cancer after first line chemotherapy and second line endocrinotherapy (i.e., toremifene & exemestane) failure. DIAGNOSES: The patient was rarely diagnosed breast cancer metastasis to the kidney and a positive hormone status (ER and PR) but was negative for human epidermal factor receptor 2 (HER2)...
June 2018: Medicine (Baltimore)
https://www.readbyqxmd.com/read/29867779/znf423-a-new-player-in-estrogen-receptor-positive-breast-cancer
#3
REVIEW
Heather M Bond, Stefania Scicchitano, Emanuela Chiarella, Nicola Amodio, Valeria Lucchino, Annamaria Aloisio, Ylenia Montalcini, Maria Mesuraca, Giovanni Morrone
Preventive therapy can target hormone-responsive breast cancer (BC) by treatment with selective estrogen receptor modulators (SERMs) and reduce the incidence of BC. Genome-wide association studies have identified single nucleotide polymorphisms (SNPs) with relevant predictive values, SNPs in the ZNF423 gene were associated with decreased risk of BC during SERM therapy, and SNPs in the Cathepsin O gene with an increased risk. ZNF423, which was not previously associated with BC is a multifunctional transcription factor known to have a role in development, neurogenesis, and adipogenesis and is implicated in other types of cancer...
2018: Frontiers in Endocrinology
https://www.readbyqxmd.com/read/29861831/identification-of-estrogen-receptor-%C3%AE-antagonists-from-natural-products-via-in-vitro-and-in-silico-approaches
#4
Xiaocong Pang, Weiqi Fu, Jinhua Wang, De Kang, Lvjie Xu, Ying Zhao, Ai-Lin Liu, Guan-Hua Du
Estrogen receptor α (ER α ) is a successful target for ER-positive breast cancer and also reported to be relevant in many other diseases. Selective estrogen receptor modulators (SERMs) make a good therapeutic effect in clinic. Because of the drug resistance and side effects of current SERMs, the discovery of new SERMs is given more and more attention. Virtual screening is a validated method to high effectively to identify novel bioactive small molecules. Ligand-based machine learning methods and structure-based molecular docking were first performed for identification of ER α antagonist from in-house natural product library...
2018: Oxidative Medicine and Cellular Longevity
https://www.readbyqxmd.com/read/29797697/aromatase-inhibitors-letrozole-for-subfertile-women-with-polycystic-ovary-syndrome
#5
REVIEW
Sebastian Franik, Stephanie M Eltrop, Jan Am Kremer, Ludwig Kiesel, Cindy Farquhar
BACKGROUND: Polycystic ovary syndrome (PCOS) is the most common cause of infrequent periods (oligomenorrhoea) and absence of periods (amenorrhoea). It affects about 4% to 8% of women worldwide and often leads to anovulatory subfertility. Aromatase inhibitors (AIs) are a class of drugs that were introduced for ovulation induction in 2001. Since about 2001 clinical trials have reached differing conclusions as to whether the AI letrozole is at least as effective as the first-line treatment clomiphene citrate (CC)...
May 24, 2018: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/29793000/effect-of-a-bisphosphonate-and-selective-estrogen-receptor-modulator-on-bone-remodeling-in-streptozotocin-induced-diabetes-and-ovariectomized-rat-model
#6
Young-Seok Lee, Rishab Gupta, Jeong-Taik Kwon, Dae-Chul Cho, Ye Jin Seo, Sung Young Seu, Eui Kyun Park, Inbo Han, Chi-Heon Kim, Joo-Kyung Sung, Kyoung-Tae Kim
BACKGROUND CONTEXT: Diabetes and menopause can cause severe osteoporosis. In general, menopause and diabetes can lead to an imbalance in bone turnover, which results in secondary osteoporosis. However, the efficacy of antiresorptive drugs against this form of osteoporosis has not been extensively evaluated. OBJECTIVE: The aim of this study was to determine the changes in vertebral bone remodeling when postmenopausal osteoporosis is accompanied by diabetes and the efficacy of bisphosphonates and selective estrogen-receptor modulators (SERMs) against these outcomes...
May 21, 2018: Spine Journal: Official Journal of the North American Spine Society
https://www.readbyqxmd.com/read/29790381/what-do-tsecs-provide-in-the-menopausal-hormone-therapy
#7
Placido Llaneza, Joaquim Calaf, Ana Rosa Jurado, Nicolas Mendoza, Borja Otero, Francisco Quereda, Rafael Sánchez-Borrego, Daniel Lubian
Tissue-selective estrogen complex (TSEC) is projected as a progestogen-free option for the treatment of estrogen deficiency symptoms in postmenopausal, non-hysterectomized women. TSEC combines the benefits of estrogen with a selective estrogen receptor modulator (SERM), in this case bazedoxifene acetate (BZA), which has an antagonistic effect on the endometrium, thus avoiding the use of progestins. The authorized TSEC combination (conjugated estrogens [CE] 0.45 mg/BZA 20 mg) for the alleviation of vasomotor symptoms has been demonstrated in randomized clinical trials compared with placebo or menopausal hormone therapy (MHT)...
May 23, 2018: Gynecological Endocrinology
https://www.readbyqxmd.com/read/29772410/estrogenic-properties-of-coumarins-and-meroterpene-from-the-fruits-of-cullen-corylifolium-experimental-and-computational-studies
#8
Tiehua Zhang, Shuning Zhong, Ligang Hou, Tiezhu Li, XiaoJia Xing, Tianzhu Guan, Jie Zhang, Yongjun Wang
Coumarins and meroterpene from the fruits of Cullen corylifolium were evaluated for their ability to bind and activate human estrogen receptor α (hERα) by a combination of in vitro studies and molecular dynamics simulations. The recombinant hERα ligand binding domain (hERα-LBD) was produced in BL21 (DE3)pLysS and the fluorescence polarization (FP) assay was performed to determine the binding affinities of coumarins and meroterpene with receptor protein. These compounds displayed distinct binding potency toward hERα-LBD, generally increased with their increasing molecular length and Connolly solvent-excluded volume (CSEV)...
May 14, 2018: Phytochemistry
https://www.readbyqxmd.com/read/29755856/the-guiding-role-of-bone-metabolism-test-in-osteoporosis-treatment
#9
REVIEW
Wei Zhang, Guo-Ji Yang, Shi-Xian Wu, Dong-Qing Li, Ying-Bo Xu, Cheng-Hong Ma, Jun-Ling Wang, Wei-Wen Chen
Osteoporosis (OP) and osteoporotic fractures are becoming a serious health care issue in the world. Calcium and vitamin D are the basic treatment for osteoporosis. Nonetheless, they do not effectively reduce the incidences of fracture. Currently approved treatments for osteoporosis include selective estrogen receptor modulators (SERMs), bisphosphonates, denosumab, teriparatide, calcitonin and others. However, the appearance of some adverse effects including atypical fracture and breast cancer has limited long-term treatments above mentioned...
2018: American Journal of Clinical and Experimental Immunology
https://www.readbyqxmd.com/read/29751107/estrogens-and-selective-estrogen-receptor-modulators-differentially-antagonize-runx2-in-st2-mesenchymal-progenitor-cells
#10
Yonatan Amzaleg, Jie Ji, Donlaporn Kittivanichkul, Anna E Törnqvist, Sara Windahl, Elias Sabag, Aysha B Khalid, Hal Sternberg, Michael West, John A Katzenellenbogen, Susan A Krum, Nyam-Osor Chimge, Dustin E Schones, Yankel Gabet, Claes Ohlsson, Baruch Frenkel
Estrogens attenuate bone turnover by inhibiting both osteoclasts and osteoblasts, in part through antagonizing Runx2. Apparently conflicting, stimulatory effects in osteoblast lineage cells, however, sway the balance between bone resorption and bone formation in favor of the latter. Consistent with this dualism, 17ß-estradiol (E2) both stimulates and inhibits Runx2 in a locus-specific manner, and here we provide evidence for such locus-specific regulation of Runx2 by E2 in vivo. We also demonstrate dual, negative and positive, regulation of Runx2-driven alkaline phosphatase (ALP) activity by increasing E2 concentrations in ST2 osteoblast progenitor cells...
May 8, 2018: Journal of Steroid Biochemistry and Molecular Biology
https://www.readbyqxmd.com/read/29742257/a-serm-increasing-the-expression-of-the-osteoblastogenesis-and-mineralization-related-proteins-and-improving-quality-of-bone-tissue-in-an-experimental-model-of-osteoporosis
#11
Fernanda Costa Yogui, Gustavo Antonio Correa Momesso, Leonardo Perez Faverani, Tarik Ocon Braga Polo, Gabriel Ramalho-Ferreira, Jaqueline Suemi Hassumi, Ana Cláudia Rossi, Alexandre Rodrigues Freire, Felippe Bevilacqua Prado, Roberta Okamoto
Raloxifene is an antiresorptive drug, selective estrogen receptor modulator (SERM) used in the treatment of osteoporosis. Objective To evaluate proteins related to bone repair at the peri-implant bone in a rat model of osteoporosis treated with raloxifene. Material and Methods 72 rats were divided into three groups: SHAM (healthy animals), OVX (ovariectomized animals), and RLX (ovariectomized animals treated with raloxifene). Raloxifene was administered by gavage (1 mg/kg/day). Tibial implantation was performed 30 days after ovariectomy, and animals were euthanized at 14, 42, and 60 days postoperatively...
2018: Journal of Applied Oral Science: Revista FOB
https://www.readbyqxmd.com/read/29730442/towards-optimization-of-estrogen-receptor-modulation-in-medicine
#12
REVIEW
Marie-Cécile Valéra, Coralie Fontaine, Marion Dupuis, Emmanuelle Noirrit-Esclassan, Alexia Vinel, Maeva Guillaume, Pierre Gourdy, Françoise Lenfant, Jean-François Arnal
Women now spend more than one-third of their lives in the postmenopausal years, and the decline of endogenous estrogen production during menopause is accompanied by a series of functional disorders that affect the quality of life. These symptoms could be alleviated or even totally suppressed by menopausal hormone therapy (MHT), initially based on natural estrogens extracted from the urine of pregnant mares (mainly in the USA, using the oral route) and later from the synthesis of the natural estrogen, 17β-estradiol (mainly in Europe, in particular using the transdermal route)...
May 3, 2018: Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/29721807/potential-association-with-early-changes-in-serum-calcium-level-after-starting-or-switching-to-denosumab-combined-with-eldecalcitol
#13
Tsuyoshi Asano, Tomohiro Shimizu, Daisuke Takahashi, Masahiro Ota, Dai Sato, Hiroki Hamano, Shigeto Hiratsuka, Masahiko Takahata, Norimasa Iwasaki
The aims of this study are to investigate changes in serum calcium (Ca) level after switching from either non-therapy, bisphosphonate, selective estrogen receptor modulators (SERM) or teriparatide treatments to a combination therapy of denosumab (DMAb), and eldecalcitol, and the association between early changes in serum calcium and changes in bone metabolic markers and bone mineral density (BMD). 129 patients with postmenopausal osteoporosis (32 non-pretreatment, 50 bisphosphonates, 18 SERM, and 29 teriparatide) were recruited and switched to DMAb plus eldecalcitol...
May 2, 2018: Journal of Bone and Mineral Metabolism
https://www.readbyqxmd.com/read/29720397/increased-long-qt-and-torsade-de-pointes-reporting-on-tamoxifen-compared-with-aromatase-inhibitors
#14
Virginie Grouthier, Benedicte Lebrun-Vignes, Andrew M Glazer, Philippe Touraine, Christian Funck-Brentano, Antoine Pariente, Carine Courtillot, Anne Bachelot, Dan M Roden, Javid J Moslehi, Joe-Elie Salem
OBJECTIVE: A prolonged QTc (LQT) is a surrogate for the risk of torsade de pointes (TdP). QTc interval duration is influenced by sex hormones: oestradiol prolongs and testosterone shortens QTc. Drugs used in the treatment of breast cancer have divergent effects on hormonal status. METHODS: We performed a disproportionality analysis using the European database of suspected adverse drug reaction (ADR) reports to evaluate the reporting OR (ROR χ2 ) of LQT, TdP and ventricular arrhythmias associated with selective oestrogen receptor modulators (SERMs: tamoxifen and toremifene) as opposed to aromatase inhibitors (AIs: anastrozole, exemestane and letrozole)...
May 2, 2018: Heart: Official Journal of the British Cardiac Society
https://www.readbyqxmd.com/read/29704771/new-approach-based-on-immunochemical-techniques-for-monitoring-of-selective-estrogen-receptor-modulators-serms-in-human-urine
#15
J-Pablo Salvador, Ester Vila-Roca, Núria Monfort, Rosa Ventura, M-Pilar Marco
Antiestrogenic compounds such as tamoxifen, toremifen and chlomifen are used illegally by athletes to minimize physical impacts such as gynecomastia resulting from the secondary effects of anabolic androgenic steroids, used to increase athletic efficiency unlawfully. The use of these compounds is banned by the World Anti-Doping Agency (WADA) and controls are made through analytical methodologies such as HPLC-MS/MS, which do not fulfil the sample throughput requirements. Moreover, compounds such as tamoxifen are also used to treat hormone receptor-positive breast cancer (ER + )...
April 22, 2018: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/29627127/the-action-of-estrogens-and-progestogens-in-the-young-female-breast
#16
Irene Zolfaroli, Juan J Tarín, Antonio Cano
Evidence from different sources sustains a pro-oncogenic role of hormones, estrogens and progestogens, on the breast. The issue is of interest for young women, who are exposed to the hormonal changes imposed by the ovarian cycle and, often, take hormones with contraceptive purposes. Experimental and clinical studies show that both estrogens and progesterone are involved in mammary development during puberty and lactation, the changes being observed across mammalian species, including humans. Estrogen receptors, and more particularly the alpha isoform, participate in molecular processes of stem cells differentiation and epithelial proliferation through paracrine actions implicating growth factors...
March 28, 2018: European Journal of Obstetrics, Gynecology, and Reproductive Biology
https://www.readbyqxmd.com/read/29617321/exosome-mediated-transfer-of-cancer-cell-resistance-to-antiestrogen-drugs
#17
Svetlana E Semina, Alexander M Scherbakov, Anna A Vnukova, Dmitry V Bagrov, Evgeniy G Evtushenko, Vera M Safronova, Daria A Golovina, Ludmila N Lyubchenko, Margarita V Gudkova, Mikhail A Krasil'nikov
Exosomes are small vesicles which are produced by the cells and released into the surrounding space. They can transfer biomolecules into recipient cells. The main goal of the work was to study the exosome involvement in the cell transfer of hormonal resistance. The experiments were performed on in vitro cultured estrogen-dependent MCF-7 breast cancer cells and MCF-7 sublines resistant to SERM tamoxifen and/or biguanide metformin, which exerts its anti-proliferative effect, at least in a part, via the suppression of estrogen machinery...
April 4, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29602124/radiative-response-of-biomass-burning-aerosols-over-an-urban-atmosphere-in-northern-peninsular-southeast-asia
#18
Shantanu Kumar Pani, Neng-Huei Lin, Somporn Chantara, Sheng-Hsiang Wang, Chanakarn Khamkaew, Tippawan Prapamontol, Serm Janjai
A large concentration of finer particulate matter (PM2.5 ), the primary air-quality concern in northern peninsular Southeast Asia (PSEA), is believed to be closely related to large amounts of biomass burning (BB) particularly in the dry season. In order to quantitatively estimate the contributions of BB to aerosol radiative effects, we thoroughly investigated the physical, chemical, and optical properties of BB aerosols through the integration of ground-based measurements, satellite retrievals, and modelling tools during the Seven South East Asian Studies/Biomass-burning Aerosols & Stratocumulus Environment: Lifecycles & Interactions Experiment (7-SEAS/BASELInE) campaign in 2014...
August 15, 2018: Science of the Total Environment
https://www.readbyqxmd.com/read/29582419/synthesis-and-biological-evaluation-of-novel-cyclopropyl-derivatives-as-subtype-selective-ligands-for-estrogen-receptor
#19
Zunyuan Wang, Yewei Yang, Xiaoliang Zheng, Tao Zhang, Wenhai Huang, Dongmei Yan, Wenjun Zhang, Xiaoju Wang, Zhengrong Shen
OBJECTIVES: Tamoxifen is the most commonly used selective estrogen receptor modulators (SERMs); however, patients often develop the acquired drug resistance on tamoxifen therapy. The aim of this study was to develop new SERMs. METHODS: Several novel cyclopropyl derivatives were designed and synthesized. The binding affinities of these compounds as well as the selectivity on subtype of estrogen receptor (ER) were assessed by fluorescence polarization. The antagonistic activity was also evaluated by dual-luciferase reporter assay...
March 27, 2018: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/29579190/27-hydroxycholesterol-is-an-estrogen-receptor-%C3%AE-selective-negative-allosteric-modifier-of-17%C3%AE-estradiol-binding
#20
Nicholas J E Starkey, Yufei Li, Sara K Drenkhahn-Weinaug, Jinghua Liu, Dennis B Lubahn
Estrogens bind to two nuclear estrogen receptor (ER) subtypes, ERα and ERβ, which are expressed in differing amounts in various tissues. The endogenous estrogen, 17β-estradiol (E2), binds to both subtypes with nearly equal affinity and is the prototypical agonist. Selective estrogen receptor modulators (SERMs) may bind to both subtypes with equivalent affinities but have agonist activities in some tissues while having antagonist activities in others. In the present study, we demonstrate that the first reported endogenous SERM, 27-hydroxycholesterol (27-OHC), binds preferentially (>100-fold) to ERβ over ERα...
May 1, 2018: Endocrinology
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