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https://www.readbyqxmd.com/read/28185712/the-effect-of-selective-estrogen-receptor-modulators-on-type-2-diabetes-onset-in-women-basic-and-clinical-insights
#1
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...
January 20, 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
#2
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
#3
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...
January 31, 2017: Food Additives & Contaminants. Part A, Chemistry, Analysis, Control, Exposure & Risk Assessment
https://www.readbyqxmd.com/read/28131133/combined-pharmacologic-therapy-in-postmenopausal-osteoporosis
#4
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
#5
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
https://www.readbyqxmd.com/read/28117994/novel-selective-estrogen-receptor-downregulators-serds-developed-against-treatment-resistant-breast-cancer
#6
Rui Xiong, Jiong Zhao, Lauren M Gutgesell, Yueting Wang, Sue Lee, Bhargava Karumudi, Huiping Zhao, Yunlong Lu, Debra A Tonetti, Gregory R J Thatcher
Resistance to the selective estrogen receptor modulator tamoxifen and to aromatase inhibitors that lower circulating estradiol occurs in up to 50% of patients, generally leading to an endocrine-independent ER+ phenotype. Selective ER downregulators (SERDs) are able to ablate ER and thus, theoretically, to prevent survival of both endocrine-dependent and -independent ER+ tumors. The clinical SERD fulvestrant is hampered by intramuscular administration and undesirable pharmacokinetics. Novel SERDs were designed using the 6-OH-benzothiophene (BT) scaffold common to arzoxifene and raloxifene...
February 10, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28117364/selective-inhibition-of-ebola-entry-with-selective-estrogen-receptor-modulators-by-disrupting-the-endolysosomal-calcium
#7
Hanlu Fan, Xiaohong Du, Jingyuan Zhang, Han Zheng, Xiaohui Lu, Qihui Wu, Haifeng Li, Han Wang, Yi Shi, George Gao, Zhuan Zhou, Dun-Xian Tan, Xiangdong Li
The Ebola crisis occurred in West-Africa highlights the urgency for its clinical treatments. Currently, no Food and Drug Administration (FDA)-approved therapeutics are available. Several FDA-approved drugs, including selective estrogen receptor modulators (SERMs), possess selective anti-Ebola activities. However, the inhibitory mechanisms of these drugs remain elusive. By analyzing the structures of SERMs and their incidental biological activity (cholesterol accumulation), we hypothesized that this incidental biological activity induced by SERMs could be a plausible mechanism as to their inhibitory effects on Ebola infection...
January 24, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28112739/acquired-cyp19a1-amplification-is-an-early-specific-mechanism-of-aromatase-inhibitor-resistance-in-er%C3%AE-metastatic-breast-cancer
#8
Luca Magnani, Gianmaria Frigè, Raffaella Maria Gadaleta, Giacomo Corleone, Sonia Fabris, Hermannus Kempe, Pernette J Verschure, Iros Barozzi, Valentina Vircillo, Sung-Pil Hong, Ylenia Perone, Massimo Saini, Andreas Trumpp, Giuseppe Viale, Antonino Neri, Simak Ali, Marco Angelo Colleoni, Giancarlo Pruneri, Saverio Minucci
Tumor evolution is shaped by many variables, potentially involving external selective pressures induced by therapies. After surgery, patients with estrogen receptor (ERα)-positive breast cancer are treated with adjuvant endocrine therapy, including selective estrogen receptor modulators (SERMs) and/or aromatase inhibitors (AIs). However, more than 20% of patients relapse within 10 years and eventually progress to incurable metastatic disease. Here we demonstrate that the choice of therapy has a fundamental influence on the genetic landscape of relapsed diseases...
January 23, 2017: Nature Genetics
https://www.readbyqxmd.com/read/28107349/using-breast-cancer-risk-associated-polymorphisms-to-identify-women-for-breast-cancer-chemoprevention
#9
Elad Ziv, Jeffrey A Tice, Brian Sprague, Celine M Vachon, Steven R Cummings, Karla Kerlikowske
BACKGROUND: Breast cancer can be prevented with selective estrogen receptor modifiers (SERMs) and aromatase inhibitors (AIs). The US Preventive Services Task Force recommends that women with a 5-year breast cancer risk ≥3% consider chemoprevention for breast cancer. More than 70 single nucleotide polymorphisms (SNPs) have been associated with breast cancer. We sought to determine how to best integrate risk information from SNPs with other risk factors to risk stratify women for chemoprevention...
2017: PloS One
https://www.readbyqxmd.com/read/28098599/is-there-a-serm-in-your-menopause-toolkit
#10
James H Liu
Over the past 3 decades, compounds called selective estrogen receptor modulators (SERMs) have been developed that block the estrogen receptor in some tissues (estrogen receptor antagonists) or stimulate the estrogen receptor in other tissues (estrogen receptor agonists). This Practice Pearl focuses on SERMs that clinicians can use for menopausal patients.
January 16, 2017: Menopause: the Journal of the North American Menopause Society
https://www.readbyqxmd.com/read/28060751/the-small-heat-shock-protein-b8-hspb8-modulates-proliferation-and-migration-of-breast-cancer-cells
#11
Margherita Piccolella, Valeria Crippa, Riccardo Cristofani, Paola Rusmini, Mariarita Galbiati, Maria Elena Cicardi, Marco Meroni, Nicola Ferri, Federica F Morelli, Serena Carra, Elio Messi, Angelo Poletti
Breast cancer (BC) is one of the major causes of cancer death in women and is closely related to hormonal dysregulation. Estrogen receptor (ER)-positive BCs are generally treated with anti hormone therapy using antiestrogens or aromatase inhibitors. However, BC cells may become resistant to endocrine therapy, a process facilitated by autophagy, which may either promote or suppress tumor expansion. The autophagy facilitator HSPB8 has been found overexpressed in some BC. Here we found that HSPB8 is highly expressed and differentially modulated by natural or synthetic selective ER modulators (SERMs), in the triple-positive hormone-sensitive BC (MCF-7) cells, but not in triple-negative MDA-MB-231 BC cells...
January 2, 2017: Oncotarget
https://www.readbyqxmd.com/read/28054434/in-vitro-phase-i-metabolism-of-selective-estrogen-receptor-modulators-in-horse-using-ultra-high-performance-liquid-chromatography-high-resolution-mass-spectrometry
#12
Karen Y Kwok, George H M Chan, Wai Him Kwok, Jenny K Y Wong, Terence S M Wan
Selective estrogen receptor modulators (SERMs) are chemicals that possess the anti-oestrogenic activities that are banned "in" and "out" of competition by the World Anti-Doping Agency (WADA) in human sports, and by the International Federation of Horseracing Authorities (IFHA) in horseracing. SERMs can be used as performance enhancing drugs to boost the level of androgens or to compensate for the adverse effects as a result of extensive use of androgenic anabolic steroids (AASs). SERMs have indeed been abused in human sports; hence, a similar threat can be envisaged in horseracing...
January 5, 2017: Drug Testing and Analysis
https://www.readbyqxmd.com/read/28032978/exploring-the-structural-compliancy-versus-specificity-of-the-estrogen-receptor-using-isomeric-three-dimensional-ligands
#13
Naina Sharma, Kathryn E Carlson, Jerome C Nwachukwu, Sathish Srinivasan, Abhishek Sharma, Kendall W Nettles, John A Katzenellenbogen
The estrogen receptors (ERs) bind with high affinity to many structurally diverse ligands by significantly distorting the contours of their ligand-binding pockets. This raises a question: To what degree is ER able to distinguish between structurally related regioisomers and enantiomers? We have explored the structural compliance and specificity of ERα with a set of ligands having a 7-oxa-bicyclo[2.2.1]hept-5-ene sulfonate core and basic side chains typical of selective ER modulators (SERMs). These ligands have two regioisomers, each of which is a racemate of enantiomers...
February 17, 2017: ACS Chemical Biology
https://www.readbyqxmd.com/read/28030966/systemic-drugs-that-influence-titanium-implant-osseointegration
#14
Dragos Apostu, Ondine Lucaciu, Gheorghe Dan Osvald Lucaciu, Bogdan Crisan, Liana Crisan, Mihaela Baciut, Florin Onisor, Grigore Baciut, Radu Septimiu Câmpian, Simion Bran
Titanium implants are widely used on an increasing number of patients in orthopedic and dental medicine. Despite the good survival rates of these implants, failures that lead to important socio-economic consequences still exist. Recently, research aimed at improving implant fixation, a process called osseointegration, has focused on a new, innovative field: systemic delivery of drugs. Following implant fixation, patients receive systemic drugs that could either impair or enhance osseointegration; these drugs include anabolic and anti-catabolic bone-acting agents in addition to new treatments...
January 23, 2017: Drug Metabolism Reviews
https://www.readbyqxmd.com/read/27974229/selective-estrogen-receptor-modulators-and-the-vitamin-d-analogue-eldecalcitol-block-bone-loss-in-male-osteoporosis
#15
Yuiko Sato, Toshimi Tando, Mayu Morita, Kana Miyamoto, Tami Kobayashi, Ryuichi Watanabe, Takatsugu Oike, Morio Matsumoto, Masaya Nakamura, Takeshi Miyamoto
Rapid increases in the number of elderly people have dramatically increased the number of female and male osteoporosis patients. Osteoporosis often causes bone fragility fractures, and males exhibit particularly poor prognosis after these fractures, indicating that control of osteoporosis is crucial to maintain quality of men's lives. However, osteoporosis therapies available for men have lagged behind advances available for women. Here, we show that three selective estrogen receptor modulators (SERMs), namely, raloxifene, bazedoxifene, and tamoxifen, plus the vitamin D analogue ED71, also called eldecalcitol, completely block orchiectomy-induced, testosterone-depleted bone loss in male mice in vivo...
January 22, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/27941208/-current-views-on-the-interaction-between-the-treatment-of-osteoporosis-and-cardiovascular-diseases
#16
Tomasz Zapolski, Andrzej Wysokiński
The most common medical conditions after menopause are osteoporosis and atherosclerotic disease. Traditionally these two conditions were considered unrelated and their coexistence has been attributed to independent processess exclusively reated to age. The possible link between cardiovascular disease and osteoporosis stimulates today to analyse not only the evidence of a possible association, but also to identify mutual beneficial and adverse effects of drugs used in these two diseases. That's why, the focus on the interference between osteoporosis treatment and drugs used for atherosclerosis is made...
2016: Wiadomości Lekarskie: Organ Polskiego Towarzystwa Lekarskiego
https://www.readbyqxmd.com/read/27941109/assessing-acceptability-of-a-diagnostic-and-malaria-treatment-package-delivered-by-community-health-workers-in-malaria-endemic-settings-of-burkina-faso-nigeria-and-uganda
#17
Ayodele S Jegede, Frederick O Oshiname, Armande K Sanou, Jesca Nsungwa-Sabiiti, IkeOluwapo O Ajayi, Mohamadou Siribié, Chinenye Afonne, Luc Sermé, Catherine O Falade
BACKGROUND:  The efficacy of artemisinin-based combination therapy (ACT) and rectal artesunate for severe malaria in children is proven. However, acceptability of a package of interventions that included use of malaria rapid diagnostic tests (RDTs), ACTs, and rectal artesunate when provided by community health workers (CHWs) is uncertain. This study assessed acceptability of use of CHWs for case management of malaria using RDTs, ACTs, and rectal artesunate. METHODS:  The study was carried out in Burkina Faso, Nigeria, and Uganda in 2015 toward the end of an intervention using CHWs to provide diagnosis and treatment...
December 15, 2016: Clinical Infectious Diseases: An Official Publication of the Infectious Diseases Society of America
https://www.readbyqxmd.com/read/27941108/quantifying-and-valuing-community-health-worker-time-in-improving-access-to-malaria-diagnosis-and-treatment
#18
Joëlle Castellani, Borislava Mihaylova, IkeOluwapo O Ajayi, Mohamadou Siribié, Jesca Nsungwa-Sabiiti, Chinenye Afonne, Luc Sermé, Andrew Balyeku, Vanessa Kabarungi, Josephine Kyaligonza, Silvia M A A Evers, Aggie T G Paulus, Max Petzold, Jan Singlovic, Melba Gomes
BACKGROUND:  Community health workers (CHWs) are members of a community who are chosen by their communities as first-line, volunteer health workers. The time they spend providing healthcare and the value of this time are often not evaluated. Our aim was to quantify the time CHWs spent on providing healthcare before and during the implementation of an integrated program of diagnosis and treatment of febrile illness in 3 African countries. METHODS:  In Burkina Faso, Nigeria, and Uganda, CHWs were trained to assess and manage febrile patients in keeping with Integrated Management of Childhood Illness recommendations to use rapid diagnostic tests, artemisinin-based combination therapy, and rectal artesunate for malaria treatment...
December 15, 2016: Clinical Infectious Diseases: An Official Publication of the Infectious Diseases Society of America
https://www.readbyqxmd.com/read/27941107/malaria-rapid-diagnostic-tests-and-malaria-microscopy-for-guiding-malaria-treatment-of-uncomplicated-fevers-in-nigeria-and-prereferral-cases-in-3-african-countries
#19
Catherine O Falade, IkeOluwapo O Ajayi, Jesca Nsungwa-Sabiiti, Mohamadou Siribié, Amidou Diarra, Luc Sermé, Chinenye Afonne, Oyindamola B Yusuf, Zakaria Gansane, Ayodele S Jegede, Jan Singlovic, Melba Gomes
BACKGROUND:  The World Health Organization recommends that malaria treatment be based on demonstration of the infecting Plasmodium parasite specie. Malaria rapid diagnostic tests (RDTs) are recommended at community points of care because they are accurate and rapid. We report on parasitological results in a malaria study in selected rural communities in 3 African countries. METHODS:  In Nigeria, community health workers (CHWs) performed RDTs (SD-Bioline) and thick blood smears on all children suspected to have malaria...
December 15, 2016: Clinical Infectious Diseases: An Official Publication of the Infectious Diseases Society of America
https://www.readbyqxmd.com/read/27941105/compliance-with-malaria-rapid-diagnostic-testing-by-community-health-workers-in-3-malaria-endemic-countries-of-sub-saharan-africa-an-observational-study
#20
Jan Singlovic, IkeOluwapo O Ajayi, Jesca Nsungwa-Sabiiti, Mohamadou Siribié, Armande K Sanou, Ayodele S Jegede, Catherine O Falade, Luc Sermé, Zakaria Gansane, Chinenye Afonne, Vanessa Kabarungi, Josephine Kyaligonza, Joëlle Castellani, Max Petzold, Melba Gomes
BACKGROUND:  The World Health Organization recommends that all malaria management be based on parasitological identification. We monitored performance of trained community health workers (CHWs) in adhering to this recommendation to restrict artemisinin-based combination therapies (ACTs) to positive rapid diagnostic test (RDT)-confirmed cases in children in 3 malaria-endemic sub-Saharan African countries. METHODS:  In 33 villages in Burkina Faso, 45 villages in Nigeria, and 84 villages in Uganda, 265 CHWs were trained over a minimum of 3 days to diagnose malaria using RDTs (prepare, read, record results, and inform the patient about results) and treat RDT-confirmed uncomplicated malaria cases with ACTs...
December 15, 2016: Clinical Infectious Diseases: An Official Publication of the Infectious Diseases Society of America
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