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https://www.readbyqxmd.com/read/29035723/raloxifene-reduces-the-risk-of-local-alveolar-bone-destruction-in-a-mouse-model-of-periodontitis-combined-with-systemic-postmenopausal-osteoporosis
#1
Ryota Ichimaru, Tsukasa Tominari, Shosei Yoshinouchi, Chiho Matsumoto, Kenta Watanabe, Michiko Hirata, Yukihiro Numabe, Gillian Murphy, Hideaki Nagase, Chisato Miyaura, Masaki Inada
OBJECTIVE: Periodontitis is characterized by local inflammation leading to tooth loss and severe destruction of alveolar bone. Raloxifene is a selective estrogen receptor modulator (SERM) that halts estrogen deficiency-induced systemic bone loss in postmenopausal osteoporosis without the side effects of cancer in breast and uterus. In this study, we examined the effects of raloxifene on alveolar bone mass in a mouse model with estrogen deficiency-induced periodontitis. METHODS: Periodontitis was induced by the injection of lipopolysaccharide (LPS) into the lower gingiva in ovariectomized (OVX) mice, and the alveolar bone and femur bone mineral density (BMD) were analyzed by dual-energy X-ray absorptiometry...
September 29, 2017: Archives of Oral Biology
https://www.readbyqxmd.com/read/29034111/molecular-characterization-of-diarrheagenic-escherichia-coli-in-children-less-than-5-years-of-age-with-diarrhea-in-ouagadougou-burkina-faso
#2
Ali Konaté, René Dembélé, Assèta Kagambèga, Issiaka Soulama, Wendpoulomdé A D Kaboré, Emmanuel Sampo, Haoua Cissé, Antoine Sanou, Samuel Serme, Soumanaba Zongo, Cheikna Zongo, Alio Mahamadou Fody, Nathalie K Guessennd, Alfred S Traoré, Amy Gassama-Sow, Nicolas Barro
Diarrheagenic Escherichia coli (DEC) is important bacteria of children's endemic and epidemic diarrhea worldwide. The aim of this study was to determine the prevalence of DEC isolated from stool samples collected from children with acute diarrhea living in Ouagadougou, Burkina Faso. From August 2013 to October 2015, stool samples were collected from 315 children under 5 years of age suffering from diarrhea in the "Centre Médical avec Antenne Chirurgicale (CMA)" Paul VI and the CMA of Schiphra. E. coli were isolated and identified by standard microbiological methods, and the 16-plex PCR method was used to further characterize them...
September 2017: European Journal of Microbiology & Immunology
https://www.readbyqxmd.com/read/29032175/the-effect-of-raloxifene-on-bone-marrow-adipose-tissue-and-bone-turnover-in-postmenopausal-women-with-osteoporosis
#3
Kerensa Beekman, Annegreet G Veldhuis-Vlug, Martin den Heijer, Mario Maas, Ania M Oleksik, Michael W Tanck, Susan M Ott, Rob J Van't Hof, Paul Lips, Peter H Bisschop, Nathalie Bravenboer
In patients with postmenopausal osteoporosis low bone volume is associated with high bone marrow adipose tissue (MAT). Moreover, high MAT is associated with increased fracture risk. This suggests an interaction between MAT and bone turnover, however literature remains equivocal. Estrogen treatment decreases MAT, but the effect of raloxifene, a selective estrogen receptor modulator (SERM) registered for treatment of postmenopausal osteoporosis, on MAT is not known. The aim of this study is 1] to determine the effect of raloxifene on MAT and 2] to determine the relationship between MAT and bone turnover in patients with osteoporosis...
October 11, 2017: Bone
https://www.readbyqxmd.com/read/28981741/comparative-risks-for-cancer-associated-with-use-of-calcitonin-bisphosphonates-or-selective-estrogen-receptor-modulators-among-osteoporosis-patients-a-population-based-cohort-study
#4
Fei-Yuan Hsiao, William Wei-Yuan Hsu
Background: This population-based cohort study was to compare the risks of incident cancer in osteoporosis patients who used bisphosphonates, calcitonin or selective estrogen receptor modulators (SERMs). Methods: We identified 9995 patients who were diagnosed with osteoporosis and prescribed osteoporosis drugs (bisphosphonate (n = 4675), calcitonin (n = 3993) and SERMs (n = 1327)) between 1 January 2000 and 31 December 2006 in Taiwan's National Health Insurance Research Database...
October 1, 2017: Japanese Journal of Clinical Oncology
https://www.readbyqxmd.com/read/28978567/what-factors-influence-decision-making-about-breast-cancer-chemoprevention-among-high-risk-women
#5
EDITORIAL
Katherine D Crew
Estrogen exposure is one of the strongest risk factors for breast cancer development. Chemoprevention with selective estrogen receptor modulators (SERM), such as tamoxifen and raloxifene, has been shown in randomized controlled trials to reduce breast cancer incidence by up to 50% among high-risk women. Despite the strength of this evidence, there is significant underutilization of chemoprevention. Given the relatively few modifiable breast cancer risk factors, SERM use provides an important strategy for the primary prevention of this disease...
October 4, 2017: Cancer Prevention Research
https://www.readbyqxmd.com/read/28978566/nrg-oncology-national-surgical-adjuvant-breast-and-bowel-project-decision-making-project-1-results-decision-making-in-breast-cancer-risk-reduction
#6
Christine Holmberg, Hanna Bandos, Angela Fagerlin, Therese B Bevers, Tracy A Battaglia, D Lawrence Wickerham, Worta J McCaskill-Stevens
Selective estrogen receptor modulators (SERMs) reduce breast cancer risk. Adoption of SERMs as prevention medication remains low. This is the first study to quantify social, cultural, and psychologic factors driving decision making regarding SERM use in women counseled on breast cancer prevention options. A survey study was conducted with women counseled by a health care provider (HCP) about SERMs. A statistical comparison of responses was performed between those who decided to use and those who decided not to use SERMs...
October 4, 2017: Cancer Prevention Research
https://www.readbyqxmd.com/read/28978005/bazedoxifene-enhances-the-anti-tumor-effects-of-cisplatin-and-radiation-treatment-by-blocking-il-6-signaling-in-head-and-neck-cancer
#7
Arti Yadav, Bhavna Kumar, Theodoros N Teknos, Pawan Kumar
Recent studies have shown that IL-6 signaling plays an important role in the aggressive and metastatic phenotype of head and neck squamous cell carcinoma (HNSCC). Therefore, we hypothesized that targeting of IL-6 signaling in HNSCC could enhance the therapeutic efficacy of standard chemoradiation treatment. We used both in vitro and in vivo models to test the efficacy of Bazedoxifene (BZA), a drug that was originally developed as a newer-generation selective estrogen receptor modulator (SERM) for the treatment of postmenopausal osteoporosis...
September 15, 2017: Oncotarget
https://www.readbyqxmd.com/read/28962172/psoralen-stimulates-osteoblast-proliferation-through-the-activation-of-nuclear-factor-%C3%AE%C2%BAb-mitogen-activated-protein-kinase-signaling
#8
Feimeng Li, Qihuo Li, Xiaoqing Huang, Yunting Wang, Chana Ge, Yong Qi, Wei Guo, Hongtao Sun
Osteoporosis is a systemic skeletal disease that leads to increased bone fragility and susceptibility to fracture. Approximately 50% of postmenopausal women develop osteoporosis as a result of postmenopausal estrogen deficiency. To reduce fractures related to osteoporosis in women, previous studies have focused on therapeutic strategies that aim to increase bone formation or decrease bone resorption. However, pharmacological agents that aim to improve bone fracture susceptibility exhibit side effects. Current studies are investigating natural alternatives that possess the benefits of selective estrogen receptor modulators (SERMs) without the adverse effects...
September 2017: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/28948818/new-molecules-modulating-bone-metabolism-new-perspectives-in-the-treatment-of-osteoporosis
#9
I Zofkova, J Blahos
In this review the authors outline traditional antiresorptive pharmaceuticals, such as bisphosphonates, monoclonal antibodies against RANKL, SERMs, as well as a drug with an anabolic effect on the skeleton, parathormone. However, there is also a focus on non-traditional strategies used in therapy for osteolytic diseases. The newest antiosteoporotic pharmaceuticals increase osteoblast differentiation via BMP signaling (harmine), or stimulate osteogenic differentiation of mesenchymal stem cells through Wnt/beta-catenin (icarrin, isoflavonoid caviunin, or sulfasalazine)...
September 26, 2017: Physiological Research
https://www.readbyqxmd.com/read/28942113/novel-serms-based-on-3-aryl-4-aryloxy-2h-chromen-2-one-skeleton-a-possible-way-to-dual-er%C3%AE-vegfr-2-ligands-for-treatment-of-breast-cancer
#10
Guoshun Luo, Xinyu Li, Guoqing Zhang, Chengzhe Wu, Zhengpu Tang, Linyi Liu, Qidong You, Hua Xiang
There is considerable interest in developing new SERMs as multifunctional agents in women's health. Development of dual selective estrogen receptor modulators/VEGFR-2 inhibitors (SERMs/V-2I) has been an attractive strategy for the discovery of new breast cancer therapeutic agents. Our previous efforts led to the preparation of a series of 3-aryl-4-anilino-2H-chromen-2-ones endowed with potent estrogen receptor binding affinity and anti-proliferative efficacy. In this study, various structurally related 3-aryl-4-anilino/aryloxy-2H-chromen-2-one analogues were rationally designed, synthesized and evaluated as a new chemo-type of dual ERα and VEGFR-2 inhibitors...
September 14, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28933369/epigenetic-mechanisms-of-tamoxifen-resistance-in-luminal-breast-cancer
#11
REVIEW
Hany A Abdel-Hafiz
Breast cancer is one of the most common cancers and the second leading cause of cancer death in the United States. Estrogen receptor (ER)-positive cancer is the most frequent subtype representing more than 70% of breast cancers. These tumors respond to endocrine therapy targeting the ER pathway including selective ER modulators (SERMs), selective ER downregulators (SERDs) and aromatase inhibitors (AIs). However, resistance to endocrine therapy associated with disease progression remains a significant therapeutic challenge...
July 6, 2017: Diseases (Basel)
https://www.readbyqxmd.com/read/28930603/centchroman-a-safe-reversible-postcoital-contraceptive-with-curative-and-prophylactic-activity-in-many-disorders
#12
Ved P Kamboj, Suprabhat Ray, Nitya Anand
Centchroman (INN: Ormeloxifene), a reversible post-coital/weekly oral contraceptive (half-life of about 168 hours), designed and developed at CDRI, Lucknow is the only non-steroidal oral contraceptive in clinical use in the world today. Synthesized in 1967 and completing pre-clinical and clinical studies in 1989, this drug was approved for marketing in 1991, social marketing in 1995 and NFPW in April 2016. It acts by preventing implantation of blastocyst in endometrium. It is the only contraceptive which neither suppresses ovulation nor interferes with the hypothalamic-pituitary-ovarian axis...
January 1, 2018: Frontiers in Bioscience (Elite Edition)
https://www.readbyqxmd.com/read/28923174/27-hydroxycholesterol-an-endogenous-selective-estrogen-receptor-modulator
#13
REVIEW
Sisi He, Erik R Nelson
Estrogen receptors (ERs) mediate the actions of the steroidal estrogens, and are important for the regulation of several physiological and pathophysiological processes, including reproduction, bone physiology, cardiovascular physiology and breast cancer. The unique pharmacology of the ERs allows for certain ligands, such as tamoxifen, to elicit tissue- and context-specific responses, ligands now referred to as selective estrogen receptor modulators (SERMs). Recently, the cholesterol metabolite 27-hydroxychoelsterol (27HC) has been defined as an endogenous SERM, with activities in atherosclerosis, osteoporosis, breast and prostate cancers, and neural degenerative diseases...
October 2017: Maturitas
https://www.readbyqxmd.com/read/28890137/secular-trends-of-use-of-anti-osteoporotic-treatments-in-spain-a-population-based-cohort-study-including-over-1-5million-people-and-more-than-12years-of-follow-up
#14
Elisa Martín-Merino, Consuelo Huerta-Álvarez, Daniel Prieto-Alhambra, Arturo Álvarez-Gutiérrez, Dolores Montero-Corominas
OBJECTIVE: Different regulatory actions for anti-osteoporotic medication (AOM) were taken during the last years, including marketing of new drugs, safety warnings, or restrictions on the indications. We aimed to characterise the secular trends of AOM use in Spain from 2001 to 2013. METHODS: A cohort study using the Spanish Database for Pharmacoepidemiological Research in Primary Care (BIFAP), was performed. BIFAP includes anonym records for 4million patients. Participants entered the study when aged ≥50years in 2001-2013 and after 1year of data available, and were followed to an AOM prescription (including alendronate, other bisphosphonates, SERM (selective estrogen receptor modulators), strontium ranelate, teriparatide or denosumab), death, lost or the end of December 2013...
September 8, 2017: Bone
https://www.readbyqxmd.com/read/28882502/design-and-synthesis-of-benzoacridines-as-estrogenic-and-anti-estrogenic-agents
#15
Kohei Torikai, Rintaro Koga, Xiaohui Liu, Kaoru Umehara, Tatsuya Kitano, Kenji Watanabe, Tohru Oishi, Hiroshi Noguchi, Yasuyuki Shimohigashi
Estrogens play undisputedly important physiological roles, but lifetime exposure to estrogens has also been linked to the development of breast cancer. Moreover, imbalanced estrogen levels have been associated with various symptoms such as osteoporosis and menopausal disorders. For the improvement of such estrogen imbalances, estrogenic reagents with regulatory properties have shown promising potential. Herein, we report the construction of a 12-arylbenzoacridine library via a diversity-oriented strategy that furnished non-toxic estrogenic and anti-estrogenic agents...
August 24, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28868359/immune-mediator-pharmacogenomics-tcl1a-snps-and-estrogen-dependent-regulation-of-inflammation
#16
Ming-Fen Ho, Richard M Weinshilboum
This review describes the important functional implications of TCL1A single nucleotide polymorphisms (SNPs) discovered during pharmacogenomic studies of aromatase inhibitor-induced musculoskeletal adverse events that were subsequently shown to influence the expression of cytokines, chemokines, toll-like receptors (TLR), and NF-κB in a SNP and estrogen-dependent fashion. Functional genomic studies of these SNPs led to the discovery of novel mechanisms that may contribute to disease pathophysiology and which may also increase our understanding of pharmacogenomic aspects of regulation of the expression of inflammatory mediators...
August 2017: Journal of Nature and Science
https://www.readbyqxmd.com/read/28859903/bazedoxifene-and-raloxifene-protect-neocortical-neurons-undergoing-hypoxia-via-targeting-er%C3%AE-and-ppar-%C3%AE
#17
J Rzemieniec, E Litwa, A Wnuk, W Lason, M Kajta
Selective estrogen receptor modulators (SERMs) such as bazedoxifene and raloxifene are recognized to mainly act via estrogen receptors (ERs), but there is no study examining the involvement of PPAR-γ in their actions, especially in neurons undergoing hypoxia. Little is also known about age-dependent actions of the SERMs on neuronal tissue challenged with hypoxia. In this study, bazedoxifene and raloxifene protected neocortical cells against hypoxia at early and later developmental stages. Both SERMs evoked caspase-3-independent neuroprotection and increased protein levels of ERα (66 and 46 kDa isoforms) and PPAR-γ...
August 28, 2017: Molecular and Cellular Endocrinology
https://www.readbyqxmd.com/read/28856246/breast-cancer-chemoprevention-pharmacogenomics-deep-sequencing-and-functional-genomics-of-the-znf423-and-ctso-genes
#18
Duan Liu, Ming-Fen Ho, Daniel J Schaid, Steven E Scherer, Krishna Kalari, Mohan Liu, Joanna Biernacka, Vivien Yee, Jared Evans, Erin Carlson, Matthew P Goetz, Michiaki Kubo, D Lawrence Wickerham, Liewei Wang, James N Ingle, Richard M Weinshilboum
Our previous GWAS using samples from the NSABP P-1 and P-2 selective estrogen receptor modulator (SERM) breast cancer prevention trials identified SNPs in ZNF423 and near CTSO that were associated with breast cancer risk during SERM chemoprevention. We have now performed Next Generation DNA sequencing to identify additional SNPs that might contribute to breast cancer risk and to extend our observation that SNPs located hundreds of bp from estrogen response elements (EREs) can alter estrogen receptor alpha (ERα) binding in a SERM-dependent fashion...
2017: NPJ Breast Cancer
https://www.readbyqxmd.com/read/28834864/effects-of-tamoxifen-on-urinary-incontinence-case-report-and-review-of-literature
#19
Elshad Hasanov, Merve Hasanov, Issa M Kuria, Rovshan Hasanov, Reshad Rzazade, Eric Jonasch, Kadri Altundag
RATIONALE: Tamoxifen has been used in women with hormone receptor-positive breast cancer and has been shown to successfully reduce both recurrence and mortality. On the contrary, long-term use of tamoxifen has hormone-related urogenital side effects which decrease the quality of life of the patients. PATIENT CONCERNS: In this case report, we present a breast cancer patient receiving tamoxifen who developed urinary incontinence; we discuss the effects of tamoxifen on urinary incontinence, which decreases quality of life of the patients who were evaluated in our clinic...
August 2017: Medicine (Baltimore)
https://www.readbyqxmd.com/read/28830317/growth-hormone-secretagogue-treatment-in-hypogonadal-men-raises-serum-insulin-like-growth-factor-1-levels
#20
John T Sigalos, Alexander W Pastuszak, Andrew Allison, Samuel J Ohlander, Amin Herati, Mark C Lindgren, Larry I Lipshultz
Realizing the reported misuse of human growth hormone (GH), investigation of a safe alternative mechanism for increasing endogenous GH is needed. Several GH secretagogues are available, including GH-releasing peptides (GHRPs) GHRP-2 and GHRP-6, and the GH-releasing hormone analog, sermorelin (SERM). Insulin-like growth factor 1 (IGF-1) serves as a surrogate marker for GH. Here, the effect of GHRP/SERM therapy on IGF-1 levels is evaluated. A retrospective review of medical records was performed for 105 men on testosterone (T) therapy seeking increases in lean body mass and fat loss who were prescribed 100 mcg of GHRP-6, GHRP-2, and SERM three times daily...
August 1, 2017: American Journal of Men's Health
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