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https://www.readbyqxmd.com/read/28319725/antiestrogen-use-in-breast-cancer-patients-reduces-the-risk-of-subsequent-lung-cancer-a-population-based-study
#1
Sung-Chao Chu, Chia-Jung Hsieh, Tso-Fu Wang, Mun-Kun Hong, Tang-Yuan Chu
BACKGROUND: There is accumulating epidemiological and preclinical evidence that estrogen might be a driver of lung cancer. Breast cancer survivors can offer a unique patient cohort to examine the effect of antiestrogen therapy on lung cancer carcinogenesis because many of these women would have received long-term selective estrogen receptor modulators (SERMs) and/or aromatase inhibitors (AIs) as adjuvant treatment. Our hypothesis is that estrogens play a role in lung cancer development, and that antiestrogen therapy would affect the incidence of subsequent lung cancer among breast cancer survivors...
March 17, 2017: Cancer Epidemiology
https://www.readbyqxmd.com/read/28283546/functional-association-of-oestrogen-receptors-with-hpv-infection-in-cervical-carcinogenesis
#2
REVIEW
Balaji Ramachandran
Repeated parity and usage of oral contraceptives have demonstrated an increased risk of cervical cancer (CC) in HPV-infected women. These lifestyle observations raise the likelihood that oestrogens and HPV infection might act synergistically to affect cancers of the cervix. In vivo studies have indicated the requirement of oestrogens and ERα in the development of atypical squamous metaplasia followed by cervical intraepithelial neoplasia (CIN) I, II and III. CIN II and III are precancerous cervical lesions that can progress over time to CC as an invasive carcinoma...
April 2017: Endocrine-related Cancer
https://www.readbyqxmd.com/read/28281842/opportunities-and-challenges-of-long-term-anti-estrogenic-adjuvant-therapy-treatment-forever-or-intermittently
#3
Poulomi Bhattacharya, Balkees Abderrahman, V Craig Jordan
Extended adjuvant (5-10 years) therapy targeted to the estrogen receptor (ER) has significantly decreased mortality from breast cancer (BC). Areas covered: Translational research advanced clinical testing of extended adjuvant therapy with tamoxifen or aromatase inhibitors (AIs). Short term therapy or non-compliance increase recurrence, but surprisingly recurrence and death does not increase dramatically after 5 years of adjuvant therapy stops. Expert commentary: Compliance ensures optimal benefit from extended antihormone adjuvant therapy...
April 2017: Expert Review of Anticancer Therapy
https://www.readbyqxmd.com/read/28261281/induction-of-mitochondrial-apoptotic-pathway-by-raloxifene-and-estrogen-in-human-endometrial-stromal-thesc-cell-line
#4
Ivana Nikolic, Marija Andjelkovic, Milan Zaric, Ivanka Zelen, Petar Canovic, Zoran Milosavljevic, Marina Mitrovic
INTRODUCTION: Endometrial hyperplasia is a condition that occurs as a result of hormonal imbalance between estrogen and progesterone. Morphological disturbance of endometrial cells occurs consequently leading towards endometrial cancer. In therapy of endometrial hyperplasia SERMs are used to supress effects of locally high estrogen level in uterus. There is strong evidence suggesting that estrogen could be involved in cell death - apoptosis. There are no experimental data demstrating the direct apoptotic effect of both raloxifene and estrogen on the ThESC cell line...
March 1, 2017: Archives of Medical Science: AMS
https://www.readbyqxmd.com/read/28252426/adjuvant-hormonal-therapy-as-a-cause-of-bone-loss-in-patients-with-breast-cancer-review-of-literature
#5
N Khachidze, E Giorgadze, M Tsagareli
Adjuvant (hormonal) therapy is the main method of treatment after surgery in hormone (estrogen and/or progesterone) positive breast cancer patients. The goal of above mentioned treatment is to reduce or block the level of estrogen and progesterone. ultiple clinical trials have revealed that hormonal therapy in breast cancer patients affect bone mineral density (BMD). Authors have analyzed data obtained from several clinical trials conducted in several countries (including Georgia). The final conclusion is that selective estrogen receptor modulators (SERMs) have negative effect on BMD in pre-menopausal women and aromatase inhibitors (anastrozole, letrozole, exemestane) are associated with significant bone loss in post-menopausal women...
January 2017: Georgian Medical News
https://www.readbyqxmd.com/read/28246081/the-4ps-of-breast-cancer-chemoprevention-putting-proven-principles-into-practice
#6
EDITORIAL
V Craig Jordan
The pioneering Royal Marsden Tamoxifen Prevention Trial recruited 2,471 eligible high-risk women to be randomized to either placebo or tamoxifen (20 mg daily) for 8 years. Breast cancer incidence was evaluated at a median of 18.4 years from the start of the study. There was a 32% reduction in estrogen/progesterone receptor (ER/PR)-positive breast cancers after tamoxifen treatment finished. Translational research, to study "the good, the bad, and the ugly of tamoxifen" in the 1980s, subsequently ensured women's safety from possible increases in osteoperosis, coronary heart disease, and endometrial cancer...
February 28, 2017: Cancer Prevention Research
https://www.readbyqxmd.com/read/28228354/effect-of-tamoxifen-on-spermatogenesis-and-testicular-steroidogenesis
#7
Rachna Verma, Amitabh Krishna
The aim of this study was to evaluate the effects of in vivo and in vitro treatments with selective estrogen receptor modulator (SERM), tamoxifen on testicular functions. The testis treated with tamoxifen, in vivo or in vitro, showed dose-dependent regressive changes in spermatogenesis. This study showed that the decreased estrogenic effect due to tamoxifen may be directly responsible for decreased testicular expression of aromatase, which in turn may be responsible for decreased synthesis of estradiol in the testis...
February 19, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28185712/the-effect-of-selective-estrogen-receptor-modulators-on-type-2-diabetes-onset-in-women-basic-and-clinical-insights
#8
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...
April 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
#9
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
#10
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...
April 2017: Food Additives & Contaminants. Part A, Chemistry, Analysis, Control, Exposure & Risk Assessment
https://www.readbyqxmd.com/read/28131133/combined-pharmacologic-therapy-in-postmenopausal-osteoporosis
#11
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
#12
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
#13
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
#14
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
#15
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...
March 2017: Nature Genetics
https://www.readbyqxmd.com/read/28107349/using-breast-cancer-risk-associated-polymorphisms-to-identify-women-for-breast-cancer-chemoprevention
#16
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
#17
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
#18
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...
February 7, 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
#19
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
#20
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
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