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Tatiana Traboulsi, Mohamed El Ezzy, James Gleason, Sylvie Mader
About 70% of breast tumors express estrogen receptor alpha (ERα), which mediates the proliferative effects of estrogens on breast epithelial cells, and are candidates for treatment with antiestrogens, steroidal or non-steroidal molecules designed to compete with estrogens and antagonize ERs. The variable patterns of activity of antiestrogens (AEs) in estrogen target tissues and the lack of systematic cross-resistance between different types of molecules have provided evidence for different mechanisms of action...
October 11, 2016: Journal of Molecular Endocrinology
Thillai V Sekar, Kira Foygel, Tarik F Massoud, Sanjiv S Gambhir, Ramasamy Paulmurugan
Estrogen receptor-α (ERα) plays an important role in normal and abnormal physiology of the human reproductive system by interacting with the endogenous ligand estradiol (E2). However, other ligands, either analogous or dissimilar to E2, also bind to ERα. This may create unintentional activation of ER signaling in reproductive tissues that can lead to cancer development. We developed a transgenic mouse model that constitutively expresses a firefly luciferase (FLuc) split reporter complementation biosensor (NFLuc-ER-LBDG521T-CFLuc) to simultaneously evaluate the dynamics and potency of ligands that bind to ERα...
October 10, 2016: Scientific Reports
Agnieszka Bratek, Krzysztof Krysta, Karolina Drzyzga, Justyna Barańska, Krzysztof Kucia
BACKGROUND: Gender differences in schizophrenia have been recognized for a long time and it has been widely accepted that sex steroid hormones, especially estradiol, are strongly attributed to this fact. Two hypotheses regarding estradiol action in psychoses gained special research attention - the estrogen protection hypothesis and hypoestrogenism hypothesis. A growing number of studies have shown benefits in augmenting antipsychotic treatment with estrogens or selective estrogen receptor modulators (SERM)...
September 2016: Psychiatria Danubina
Andrée-Anne Poirier, Mélissa Côté, Mélanie Bourque, Marc Morissette, Thérèse Di Paolo, Denis Soulet
Motor symptoms in Parkinson's disease (PD) are often preceded by nonmotor symptoms related to dysfunctions of the autonomic nervous system such as constipation, defecatory problems, and delayed gastric emptying. These gastrointestinal impairments are associated with the alteration of dopaminergic (DAergic) neurons in the myenteric plexus of the gut. Recently, we demonstrated the anti-inflammatory properties of estrogens to treat intestinal neurodegeneration in the 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) mouse model of PD...
August 16, 2016: Neurobiology of Aging
Mei Methawasin, Joshua G Strom, Rebecca E Slater, Vanessa Fernandez, Chandra Saripalli, Henk Granzier
BACKGROUND: Left ventricular (LV) stiffening contributes to heart failure with preserved ejection fraction (HFpEF), a syndrome with no effective treatment options. Increasing the compliance of titin in the heart has become possible recently through inhibition of the splicing factor RNA binding motif-20. Here, we investigated the effects of increasing the compliance of titin in mice with diastolic dysfunction. METHODS: Mice in which the RNA recognition motif (RRM) of one of the RNA binding motif-20 alleles was floxed and that expressed the MerCreMer transgene under control of the αMHC promoter (referred to as cRbm20(ΔRRM) mice) were used...
October 11, 2016: Circulation
María E Fernández-Suárez, Joan C Escolà-Gil, Oscar Pastor, Alberto Dávalos, Francisco Blanco-Vaca, Miguel A Lasunción, Javier Martínez-Botas, Diego Gómez-Coronado
Selective estrogen receptor modulators (SERMs) are widely prescribed drugs that alter cellular and whole-body cholesterol homeostasis. Here we evaluate the effect of SERMs on the macrophage-specific reverse cholesterol transport (M-RCT) pathway, which is mediated by HDL. Treatment of human and mouse macrophages with tamoxifen, raloxifene or toremifene induced the accumulation of cytoplasmic vesicles of acetyl-LDL-derived free cholesterol. The SERMs impaired cholesterol efflux to apolipoprotein A-I and HDL, and lowered ABCA1 and ABCG1 expression...
2016: Scientific Reports
Nicoletta Provinciali, Chen Suen, Barbara K Dunn, Andrea DeCensi
INTRODUCTION: Raloxifene is an estrogen receptor modulator which competes with estrogens for binding to the estrogen receptor . Based on the results of the STAR (Study of Tamoxifen And Raloxifene) trial, raloxifene has been approved by the U.S. Food and Drug Administration for the reduction of breast cancer (BC) risk in postmenopausal women at increased risk. AREAS COVERED: This analysis reviews the activity of raloxifene and the clinical trials for non-BC indications which led to investigate its use as BC preventive agent...
September 1, 2016: Expert Review of Clinical Pharmacology
Jing Sun, Wei Jia Sun, Zheng Yang Li, Ling Li, Yue Wang, Yu Zhao, Cong Wang, Li Ren Yu, Ling Zhi Li, Yong Liang Zhang
Daidzein is a major dietary source of isoflavones found in Leguminosae, and belongs to the family of diphenolic compounds. The estrogenic effects of daidzein to prompt bone formation and prevent bone resorption have been observed in animal models and cultured cells. In our study, we studied the effects of daidzein, raloxifene and E2 on expression of the osteoblast-produced bone regulatory factors OPG, RANKL and IL-6 in human osteoblastic MG-63 cells. Results suggest that treatment with daidzein, raloxifene and E2 increased the levels of OPG and decreased those of RANKL and IL-6...
August 27, 2016: International Immunopharmacology
Ki-Chan An
Selective estrogen receptor modulators (SERMs) are now being used as a treatment for breast cancer, osteoporosis and postmenopausal symptoms, as these drugs have features that can act as an estrogen agonist and an antagonist, depending on the target tissue. After tamoxifen, raloxifene, lasofoxifene and bazedoxifene SERMs have been developed and used for treatment. The clinically decisive difference among these drugs (i.e., the key difference) is their endometrial safety. Compared to bisphosphonate drug formulations for osteoporosis, SERMs are to be used primarily in postmenopausal women of younger age and are particularly recommended if there is a family history of invasive breast cancer, as their use greatly reduces the incidence of this type of cancer in women...
August 2016: Asian Spine Journal
Javier Labad, Lourdes Martorell, Elena Huerta-Ramos, Jesús Cobo, Elisabet Vilella, Elena Rubio-Abadal, Gemma Garcia-Pares, Marta Creus, Cristian Núñez, Laura Ortega, Eva Miquel, Judith Usall
Several double-blind clinical trials have reported improvement in positive, negative and cognitive symptoms of schizophrenia with raloxifene, a selective receptor estrogen modulator. However, there are some inconsistencies in replicating findings between studies of different countries. The failure to replicate these findings may result from genetic factors that could explain some of the variability in the treatment response. However, pharmacogenetic studies exploring this topic in women with schizophrenia are lacking...
October 2016: European Neuropsychopharmacology: the Journal of the European College of Neuropsychopharmacology
Nicoletta Bivi, Haitao Hu, Balagopalakrishna Chavali, Michael J Chalmers, Christopher T Reutter, Gregory L Durst, Anna Riley, Masahiko Sato, Matthew R Allen, David B Burr, Jeffrey A Dodge
No abstract text is available yet for this article.
September 15, 2016: Bioorganic & Medicinal Chemistry
Zuzana E Haarhoff, Melissa A Kramer, Tatyana A Zvyaga, Jun Zhang, Priyadeep Bhutani, Murali Subramanian, A David Rodrigues
1. Members of the cytochrome P450 3A (CYP3A) subfamily metabolize numerous compounds and serve as the loci of drug-drug interactions (DDIs). Because of high amino acid sequence identity with human CYP3A, the cynomolgus monkey has been proposed as a model species to support DDI risk assessment. 2. Therefore, the objective of this study was to evaluate 35 known inhibitors of human CYP3A using human (HLM) and cynomolgus monkey (CLM) liver microsomes. Midazolam was employed as substrate to generate IC50 values (concentration of inhibitor rendering 50% inhibition) in the absence and presence of a preincubation (30 mins) with NADPH...
August 8, 2016: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
Woochang Hwang, Jaejoon Choi, Mijin Kwon, Doheon Lee
BACKGROUND: It is necessary to evaluate the efficacy of individual drugs on patients to realize personalized medicine. Testing drugs on patients in clinical trial is the only way to evaluate the efficacy of drugs. The approach is labour intensive and requires overwhelming costs and a number of experiments. Therefore, preclinical model system has been intensively investigated for predicting the efficacy of drugs. Current computational drug sensitivity prediction approaches use general biological network modules as their prediction features...
2016: BMC Bioinformatics
Risa B Burns, Mara A Schonberg, Nadine M Tung, Howard Libman
In November 2013, the U.S. Preventive Services Task Force issued a guideline on medications for risk reduction of primary breast cancer in women. Although mammography can detect early cases, it cannot prevent development of breast cancer. Tamoxifen and raloxifene are selective estrogen receptor modulators that have been shown to reduce the risk for estrogen receptor-positive breast cancer and are approved by the U.S. Food and Drug Administration (FDA) for this indication. However, neither medication reduces the risk for estrogen receptor-negative breast cancer or all-cause mortality...
August 2, 2016: Annals of Internal Medicine
Ann V Schwartz
Diabetes is characterized by increased fracture risk and by reduced bone strength for a given density. Contributing factors may include lower bone turnover and accumulation of advanced glycation endproducts. There are concerns that the pharmacological therapies for osteoporosis, particularly anti-resorptive therapies that suppress bone turnover, may not be as effective in the setting of diabetes. This review considers clinical trials and observational studies that have assessed the efficacy of anti-resorptive and anabolic therapies in diabetic patients...
July 26, 2016: Calcified Tissue International
Gabriel Ramalho-Ferreira, Leonardo Perez Faverani, Gustavo Antonio Correa Momesso, Eloá Rodrigues Luvizuto, Igor de Oliveira Puttini, Roberta Okamoto
OBJECTIVES: The aim of this study is to evaluate the alendronate and raloxifene influence in the alveolar healing process of osteoporotic rats. MATERIALS AND METHODS: Sixty-four female rats were divided in four groups: sham rats (SHAM), ovariectomized rats and no medical treatment (OVX NT), ovariectomized rats and submitted to alendronate treatment (OVX ALE), and ovariectomized and submitted to raloxifene treatment (OVX RAL). The histomorphometrical and immunohistochemical analysis was performed...
July 27, 2016: Clinical Oral Investigations
M R Meyer, M Barton
In premenopausal women, endogenous estrogens are associated with reduced prevalence of arterial hypertension, coronary artery disease, myocardial infarction, and stroke. Clinical trials conducted in the 1990s such as HERS, WHI, and WISDOM have shown that postmenopausal treatment with horse hormone mixtures (so-called conjugated equine estrogens) and synthetic progestins adversely affects female cardiovascular health. Our understanding of rapid (nongenomic) and chronic (genomic) estrogen signaling has since advanced considerably, including identification of a new G protein-coupled estrogen receptor (GPER), which like the "classical" receptors ERα and ERβ is highly abundant in the cardiovascular system...
2016: Advances in Pharmacology
Jayashri Kulkarni, Emorfia Gavrilidis, Stella M Gwini, Roisin Worsley, Jasmin Grigg, Annabelle Warren, Caroline Gurvich, Heather Gilbert, Michael Berk, Susan R Davis
IMPORTANCE: A substantial proportion of women with schizophrenia experience debilitating treatment-refractory symptoms. The efficacy of estrogen in modulating brain function in schizophrenia has to be balanced against excess exposure of peripheral tissue. Raloxifene hydrochloride is a selective estrogen receptor modulator (mixed estrogen agonist/antagonist) with potential psychoprotective effects and fewer estrogenic adverse effects. OBJECTIVE: To determine whether adjunctive raloxifene therapy reduces illness severity in women with refractory schizophrenia...
September 1, 2016: JAMA Psychiatry
Walter Lemmo
A 66-year-old patient presented with acute recurrent metastatic estrogen and progesterone receptor-positive, Her-2/neu-negative breast cancer, bone lesions (lumbar spine, pelvis), pulmonary nodules, hepatic metastasis, elevated cancer antigen 15 and liver enzymes, dyspepsia, and diarrhea. The patient had been taking raloxifene for approximately 8 years. After discontinuation, clinical parameters and symptoms improved rapidly without oncological therapy or other forms of treatment. Three months after raloxifene discontinuation, capecitabine was initiated by the treating oncologist who deemed an anti-estrogen withdrawal effect (AEWE) implausible...
September 2016: Integrative Cancer Therapies
Adam R Brentnall, Jack Cuzick, Helen Byers, Corrinne Segal, Caroline Reuter, Simone Detre, Ivana Sestak, Anthony Howell, Trevor J Powles, William G Newman, Mitchell Dowsett
A case-control study from two randomised breast cancer prevention trials of tamoxifen and raloxifene (P-1 and P-2) identified single-nucleotide polymorphisms (SNPs) in or near genes ZNF423 and CTSO as factors which predict which women will derive most anti-cancer benefit from selective oestrogen receptor modulator (SERM) therapy. In this article, we further examine this question using blood samples from two randomised tamoxifen prevention trials: the International Breast Cancer Intervention Study I (IBIS-I) and the Royal Marsden trial (Marsden)...
August 2016: Breast Cancer Research and Treatment
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