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https://www.readbyqxmd.com/read/29434492/sr-16234-a-novel-selective-estrogen-receptor-modulator-for-pain-symptoms-with-endometriosis-an-open-label-clinical-trial
#1
Tasuku Harada, Ikuko Ohta, Yusuke Endo, Hiroshi Sunada, Hisashi Noma, Fuminori Taniguchi
Background: SR-16234 is a selective estrogen receptor modulator (SERM) structurally different from approved SERM and has been reported to have estrogen receptor (ER) α antagonistic activity and strong affinity with a weak partial agonistic activity to ERβ receptor. SR-16234 showed strong inhibitory effects on transplanted endometrial cysts in the endometriosis model of rat and mouse. In this clinical trial, efficacy and safety of SR-16234 have been evaluated in endometriosis patients...
December 2017: Yonago Acta Medica
https://www.readbyqxmd.com/read/29428397/pyk2-deficiency-potentiates-osteoblast-differentiation-and-mineralizing-activity-in-response-to-estrogen-and-raloxifene
#2
Sumana Posritong, Jung Min Hong, Pierre P Eleniste, Patrick W McIntyre, Jennifer L Wu, Evan R Himes, Vruti Patel, Melissa A Kacena, Angela Bruzzaniti
Bone remodeling is controlled by the actions of bone-degrading osteoclasts and bone-forming osteoblasts (OBs). Aging and loss of estrogen after menopause affects bone mass and quality. Estrogen therapy, including selective estrogen receptor modulators (SERMs), can prevent bone loss and increase bone mineral density in post-menopausal women. Although investigations of the effects of estrogen on osteoclast activity are well advanced, the mechanism of action of estrogen on OBs is still unclear. The proline-rich tyrosine kinase 2 (Pyk2) is important for bone formation and female mice lacking Pyk2 (Pyk2-KO) exhibit elevated bone mass, increased bone formation rate and reduced osteoclast activity...
February 8, 2018: Molecular and Cellular Endocrinology
https://www.readbyqxmd.com/read/29407951/design-synthesis-and-biological-evaluation-of-novel-indole-benzimidazole-hybrids-targeting-estrogen-receptor-alpha-er-%C3%AE
#3
Ramit Singla, Kunj Bihari Gupta, Shishir Upadhyay, Monisha Dhiman, Vikas Jaitak
In the course of efforts to develop novel selective estrogen receptor modulators (SERMs), indole-benzimidazole hybrids were designed and synthesised by fusing the indole nucleus with benzimidazole. All the compounds were first inspected for anti-proliferative activity using ER-α responsive T47D breast cancer cell lines and ER-α binding assay. From this study, two representative bromo substituted compounds 5f and 8f were found to be most active and thus were escalated for gene expression studies for targeting ER-α...
February 1, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29393992/medical-treatment-of-epistaxis-in-hereditary-hemorrhagic-telangiectasia-an-evidence-based-review
#4
Ashleigh A Halderman, Matthew W Ryan, Christopher Clark, Raj Sindwani, Douglas D Reh, David M Poetker, Rosangela Invernizzi, Bradley F Marple
BACKGROUND: Hereditary hemorrhagic telangiectasia (HHT) is an autosomal dominant hereditary disorder resulting in vascular dysplasia and formation of arteriovenous malformations. Recurrent epistaxis is a hallmark of the disease. An array of medical therapies are used in this patient population, but robust evidence-based recommendations regarding the medical treatment of epistaxis are lacking. This systematic review was performed to look at the current literature and make meaningful evidence-based recommendations...
February 2, 2018: International Forum of Allergy & Rhinology
https://www.readbyqxmd.com/read/29383334/effects-of-toremifene-a-selective-estrogen-receptor-modulator-on-spontaneous-and-stimulated-gh-secretion-igf-i-and-igf-binding-proteins-in-healthy-elderly-subjects
#5
Ferdinand Roelfsema, Rebecca J Yang, Paul Y Takahashi, Dana Erickson, Cyril Y Bowers, Johannes D Veldhuis
Context: Estrogens amplify spontaneous and stimulated growth hormone (GH) secretion, whereas they diminish GH-dependent insulin-like growth factor (IGF)-I in a dose-dependent manner. Selective estrogen receptor modulators (SERMs), including tamoxifen and toremifene, are widely adjunctively used in breast and prostate cancer. Although some endocrine effects of tamoxifen are known, few data are available for toremifene. Objective: To explore sex-dependent effects of toremifene on spontaneous 10-hour overnight GH secretion, followed by GH-releasing hormone-ghrelin stimulation...
February 1, 2018: Journal of the Endocrine Society
https://www.readbyqxmd.com/read/29371332/the-impact-of-27-hydroxycholesterol-on-endometrial-cancer-proliferation
#6
Douglas A Gibson, Frances Collins, Fiona L Cousins, Arantza Esnal Zufiaurre, Philippa T Saunders
Endometrial cancer (EC) is the most common gynaecological malignancy. Obesity is a major risk factor for EC and is associated with elevated cholesterol. 27-Hydroxycholesterol (27HC) is a cholesterol metabolite that functions as an endogenous agonist for Liver X Receptor (LXR) and a selective estrogen receptor modulator (SERM). Exposure to estrogenic ligands increases risk of developing EC however the impact of 27HC on EC is unknown. Samples of stage 1 EC (n=126) were collected from post-menopausal women undergoing hysterectomy...
January 25, 2018: Endocrine-related Cancer
https://www.readbyqxmd.com/read/29360794/estrogen-and-androgen-blockade-for-advanced-prostate-cancer-in-the-era-of-precision-medicine
#7
REVIEW
Tetsuya Fujimura, Kenichi Takayama, Satoru Takahashi, Satoshi Inoue
Androgen deprivation therapy (ADT) has been widely prescribed for patients with advanced prostate cancer (PC) to control key signaling pathways via androgen receptor (AR) and AR-collaborative transcriptional factors; however, PC gradually acquires a lethal phenotype and results in castration-resistant PC (CRPC) during ADT. Therefore, new therapeutic strategies are required in clinical practice. In addition, ARs; estrogen receptors (ERs; ERα and ERβ); and estrogen-related receptors (ERRs; ERRα, ERRβ, and ERRγ) have been reported to be involved in the development or regulation of PC...
January 23, 2018: Cancers
https://www.readbyqxmd.com/read/29357976/variation-in-natural-exposure-to-anopheles-mosquitoes-and-its-effects-on-malaria-transmission
#8
Wamdaogo M Guelbéogo, Bronner Pamplona Gonçalves, Lynn Grignard, John Bradley, Samuel S Serme, Joel Hellewell, Kjerstin Lanke, Soumanaba Zongo, Nuno Sepúlveda, Issiaka Soulama, Dimitri W Wangrawa, Laith Yakob, N'Falé Sagnon, Teun Bousema, Chris Drakeley
Variation in biting frequency by Anopheles mosquitoes can explain some of the heterogeneity in malaria transmission in endemic areas. In this study in Burkina Faso, we assessed natural exposure to mosquitoes by matching the genotype of blood meals from 1066 mosquitoes with blood from residents of local households. We observed that the distribution of mosquito bites exceeded the Pareto rule (20/80) in two of the three surveys performed (20/85, 76, and 96) and, at its most pronounced, is estimated to have profound epidemiological consequences, inflating the basic reproduction number of malaria by 8-fold...
January 23, 2018: ELife
https://www.readbyqxmd.com/read/29330437/a-computational-assay-of-estrogen-receptor-%C3%AE-antagonists-reveals-the-key-common-structural-traits-of-drugs-effectively-fighting-refractory-breast-cancers
#9
Matic Pavlin, Angelo Spinello, Marzia Pennati, Nadia Zaffaroni, Silvia Gobbi, Alessandra Bisi, Giorgio Colombo, Alessandra Magistrato
Somatic mutations of the Estrogen Receptor α (ERα) occur with an up to 40% incidence in ER sensitive breast cancer (BC) patients undergoing prolonged endocrine treatments. These polymorphisms are implicated in acquired resistance, disease relapse, and increased mortality rates, hence representing a current major clinical challenge. Here, multi-microseconds (12.5 µs) molecular dynamics simulations revealed that recurrent ERα polymorphisms (i. e. L536Q, Y537S, Y537N, D538G) (mERα) are constitutively active in their apo form and that they prompt the selection of an agonist (active)-like conformation even upon antagonists binding...
January 12, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29330027/selective-estrogen-receptor-modulator-ormeloxifene-suppresses-embryo-implantation-via-inducing-mir-140-and-targeting-insulin-like-growth-factor-1-receptor-in-rat-uterus
#10
Vijay K Sirohi, Kanchan Gupta, Rohit Kumar, Vinay Shukla, Anila Dwivedi
Ormeloxifene, the non-steroidal SERM contraceptive, inhibits endometrial receptivity and embryo implantation via countering nidatory estrogen. However, the molecular mechanism of ormeloxifene action responsible for its contraceptive efficacy still remains unclear. Herein, we aimed to identify the miRNAs modulated under the influence of ormeloxifene and to explore their role in endometrial receptivity and embryo implantation. By doing microRNA sequencing analysis, a total of 168 miRNAs were found to be differentially expressed in uterine tissue of ormeloxifene-treated rats, on day 5 (10:00 h) of pregnancy i...
January 9, 2018: Journal of Steroid Biochemistry and Molecular Biology
https://www.readbyqxmd.com/read/29321530/the-effect-of-raloxifene-augmentation-in-men-and-women-with-a-schizophrenia-spectrum-disorder-a-systematic-review-and-meta-analysis
#11
REVIEW
Janna de Boer, Merel Prikken, Wan U Lei, Marieke Begemann, Iris Sommer
Recognizing the robust sex differences in schizophrenia prevalence, the selective estrogen receptor modulator (SERM) raloxifene is a likely candidate for augmentation therapy in this disorder. Therefore, a systematic search was performed using PubMed (Medline), Embase, PsychInfo, and Cochrane Database of Systematic Reviews. Randomized controlled trials investigating the effect of raloxifene in schizophrenia spectrum disorders were included in the quantitative analyses. Outcome measures were psychotic symptom severity, depression, and cognition...
January 10, 2018: NPJ Schizophrenia
https://www.readbyqxmd.com/read/29318649/treatment-related-changes-in-bone-turnover-and-fracture-risk-reduction-in-clinical-trials-of-anti-resorptive-drugs-a-meta-regression
#12
Douglas C Bauer, Dennis M Black, Mary L Bouxsein, Li-Yung Lui, Jane A Cauley, Anne E de Papp, Andreas Grauer, Sundeep Khosla, Charles E McCulloch, Richard Eastell
Few pooled analyses of antiresorptive (AR) treatment trials relate short-term changes in bone turnover markers (BTMs) to subsequent fracture reduction. Such information would be useful to assess new ARs or novel dosing regimens. In the Foundation for the National Institutes of Health (FNIH) Bone Quality project, we analyzed individual-level data from 28,000 participants enrolled in 11 bisphosphonate (BP) and three selective estrogen receptor modulator (SERM) placebo-controlled fracture endpoint trials. Using BTM results for two bone formation markers (bone-specific alkaline phosphatase [bone ALP] and pro-collagen I N-propeptide [PINP]) and two bone resorption markers (N-terminal and C-terminal telopeptide of type I collagen) and incident fracture outcome data, we performed a meta-regression relating the mean net effect of treatment on change in bone turnover (active minus placebo % difference after 3 to 12 months) to the log of study-wide fracture risk reduction, and used linear regression to plot the best fitting line...
January 10, 2018: Journal of Bone and Mineral Research: the Official Journal of the American Society for Bone and Mineral Research
https://www.readbyqxmd.com/read/29289555/selective-estrogen-receptor-modulators-serms-and-selective-estrogen-receptor-degraders-serds-in-cancer
#13
REVIEW
Hitisha K Patel, Teeru Bihani
Breast cancer is the most frequently diagnosed cancer in women, with estrogen receptor positive (ER+) breast cancer making up approximately 75% of all breast cancers diagnosed. Given the dependence on active ER signaling in these tumors, the predominant treatment strategy has been to inhibit various aspects of this pathway including directly antagonizing ER with the use of selective estrogen receptor modulators (SERMs) and selective estrogen receptor degraders (SERDs). Interestingly, the dependence on ER for breast cancer growth is often retained even after progression through several lines of antiestrogen therapy, making ER a bonafide biomarker for this cancer subtype and driving the continued research and development of novel ER-targeted therapeutics to treat this patient population...
December 28, 2017: Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/29228306/25s-rdna-genotype-and-antifungal-susceptibility-of-clinical-candida-albicans-in-ouagadougou-burkina-faso
#14
Adama Zida, Soulama Issiaka, Bamba Sanata, Serme S Samuel, Sangare Ibrahim, Sawadogo Marcel, Guiguemde Thierry, Traore Lady Kady, Guiguemde T Robert
The present investigation aimed to assess the prevalence of genotypes of C. albicans in Ouagadougou and to analyze the relationship between the genetic diversity and antifungal susceptibility. Ninety-six clinical strains are included. They were diagnosed as C. albicans using germ tube test, chlamydospore formation, and Api-Candida test. Genotyping was performed using PCR targeting 25S rDNA. Antifungal susceptibilities were tested based on the disk diffusion method. The genotypes A (85.4%) was predominant followed by genotypes B (10...
December 8, 2017: Medical Mycology: Official Publication of the International Society for Human and Animal Mycology
https://www.readbyqxmd.com/read/29210666/a-newly-synthetized-ferrocenyl-derivative-selectively-induces-apoptosis-in-all-lymphocytes-through-mitochondrial-estrogen-receptors
#15
Marjan Aghvami, Jalal Pourahmad, Afshin Zarghi, Peyman Eshghi, Mohammad Hadi Zarei, Shabnam Farzaneh, Fatemeh Sattari
BACKGROUND: Estrogens, as the main female steroid hormones have multiple proven effects on reproductive and non- reproductive systems. Expression of ERα and ERβ, two dominant estrogen receptors, in peripheral blood mononuclear cells in certain B-cell malignancies and the existence of estrogens receptors on mitochondria is open to question that estrogen likely has an impact on the cancerous lymphocytes life span. Acute lymphoblastic leukemia (ALL) is the frequent pediatric malignity which is recurrent and hardly curable in many cases...
December 5, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/29207335/tamoxifen-a-pioneering-drug-an-update-on-the-therapeutic-potential-of-tamoxifen-derivatives
#16
REVIEW
Shagufta, Irshad Ahmad
Tamoxifen (ICI 46 474), trans-1-(4-β-dimethylaminoethoxyphenyl)-1,2-diphenylbut-1-ene, is the most commonly used drug for the treatment of estrogen receptor positive breast cancer and has been saving lives worldwide for the past four decades. Tamoxifen is considered a pioneering drug due to its ubiquitous use in both treatment and chemoprevention of breast cancer and also for research addressing novel selective estrogen receptor modulators (SERMs). Tamoxifen is cost effective, lifesaving, and devoid of major side effects in the majority of patients...
November 24, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29198894/design-synthesis-and-biological-evaluation-of-novel-indole-xanthendione-hybrids-as-selective-estrogen-receptor-modulators
#17
Ramit Singla, Kunj Bihari Gupta, Shishir Upadhyay, Monisha Dhiman, Vikas Jaitak
Ground breaking clinical therapeutic advances in the treatment of breast cancer (BC) is the introduction of selective estrogen receptor modulators (SERMs). We have expeditiously designed and synthesized indole-xanthendione hybrids by coalescing the indole nucleus with xanthendione. All the compounds were first screened for anti-proliferative activity, cytotoxicity and ER-α binding affinity by utilizing ER-α dominant T47D BC cell lines, PBMCs and ER-α competitor assay kit. From this study, two representative compounds 6e and 6f showing most promising activity were advanced for gene expression studies for targeting ER-α...
November 30, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/29183806/the-antagonist-properties-of-bazedoxifene-after-acute-treatment-are-shifted-to-stimulatory-action-after-chronic-exposure-in-the-liver-but-not-in-the-uterus
#18
Mélissa Buscato, Coralie Fontaine, Aurélie Fabre, Alexia Vinel, Marie-Cécile Valera, Emmanuelle Noirrit, Maeva Guillaume, Bernard Payrastre, Raphaël Métivier, Jean-François Arnal
A promising alternative to conventional hormone therapy for postmenopausal symptoms is treatment combining Bazedoxifene (BZA), a third-generation selective estrogen receptor modulator (SERM), and conjugated equine estrogen (CE). This combination is also known as a tissue-selective estrogen complex (TSEC). Understanding the tissue-specific actions of SERMs and the TSEC remains a major challenge to try to predict their clinical effects. The aim of this study was to compare acute versus chronic treatment with BZA, CE or CE + BZA in two major targets of estrogens, the uterus and the liver...
November 25, 2017: Molecular and Cellular Endocrinology
https://www.readbyqxmd.com/read/29183790/17%C3%AE-estradiol-and-tamoxifen-protect-mice-from-manganese-induced-dopaminergic-neurotoxicity
#19
Edward Pajarillo, James Johnson, Judong Kim, Pratap Karki, Deok-Soo Son, Michael Aschner, Eunsook Lee
Chronic exposure to manganese (Mn) causes neurotoxicity, referred to as manganism, with common clinical features of parkinsonism. 17β-estradiol (E2) and tamoxifen (TX), a selective estrogen receptor modulator (SERM), afford neuroprotection in several neurological disorders, including Parkinson's disease (PD). In the present study, we tested if E2 and TX attenuate Mn-induced neurotoxicity in mice, assessing motor deficit and dopaminergic neurodegeneration. We implanted E2 and TX pellets in the back of the neck of ovariectomized C57BL/6 mice two weeks prior to a single injection of Mn into the striatum...
November 26, 2017: Neurotoxicology
https://www.readbyqxmd.com/read/29160416/agonistic-activity-of-tamoxifen-a-selective-estrogen-receptor-modulator-serm-on-arthritic-ovariectomized-mice
#20
L A S Silva, F B Felix, J M D Araujo, E V Souza, E A Camargo, R Grespan
Arthritis is positively associated with the decline of sex hormones, especially estrogen. Tamoxifen (TMX) is a selective estrogen receptor modulator, possessing agonist or antagonistic activity in different tissues. Thus, the objective of this study was to investigate the effect of TMX on the zymosan-induced arthritis model. Female Swiss normal and ovariectomized (OVX) mice were divided into groups and treated for five days with TMX (0.3, 0.9 or 2.7 mg/kg) or 17-β-estradiol (E2, 50 µg/kg). On the fifth day, arthritis was induced and 4 h later, leukocyte migration into joint cavities was evaluated...
November 13, 2017: Brazilian Journal of Medical and Biological Research, Revista Brasileira de Pesquisas Médicas e Biológicas
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