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https://www.readbyqxmd.com/read/29627127/the-action-of-estrogens-and-progestogens-in-the-young-female-breast
#1
Irene Zolfaroli, Juan J Tarín, Antonio Cano
Evidence from different sources sustains a pro-oncogenic role of hormones, estrogens and progestogens, on the breast. The issue is of interest for young women, who are exposed to the hormonal changes imposed by the ovarian cycle and, often, take hormones with contraceptive purposes. Experimental and clinical studies show that both estrogens and progesterone are involved in mammary development during puberty and lactation, the changes being observed across mammalian species, including humans. Estrogen receptors, and more particularly the alpha isoform, participate in molecular processes of stem cells differentiation and epithelial proliferation through paracrine actions implicating growth factors...
March 28, 2018: European Journal of Obstetrics, Gynecology, and Reproductive Biology
https://www.readbyqxmd.com/read/29617321/exosome-mediated-transfer-of-cancer-cell-resistance-to-antiestrogen-drugs
#2
Svetlana E Semina, Alexander M Scherbakov, Anna A Vnukova, Dmitry V Bagrov, Evgeniy G Evtushenko, Vera M Safronova, Daria A Golovina, Ludmila N Lyubchenko, Margarita V Gudkova, Mikhail A Krasil'nikov
Exosomes are small vesicles which are produced by the cells and released into the surrounding space. They can transfer biomolecules into recipient cells. The main goal of the work was to study the exosome involvement in the cell transfer of hormonal resistance. The experiments were performed on in vitro cultured estrogen-dependent MCF-7 breast cancer cells and MCF-7 sublines resistant to SERM tamoxifen and/or biguanide metformin, which exerts its anti-proliferative effect, at least in a part, via the suppression of estrogen machinery...
April 4, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29602124/radiative-response-of-biomass-burning-aerosols-over-an-urban-atmosphere-in-northern-peninsular-southeast-asia
#3
Shantanu Kumar Pani, Neng-Huei Lin, Somporn Chantara, Sheng-Hsiang Wang, Chanakarn Khamkaew, Tippawan Prapamontol, Serm Janjai
A large concentration of finer particulate matter (PM2.5 ), the primary air-quality concern in northern peninsular Southeast Asia (PSEA), is believed to be closely related to large amounts of biomass burning (BB) particularly in the dry season. In order to quantitatively estimate the contributions of BB to aerosol radiative effects, we thoroughly investigated the physical, chemical, and optical properties of BB aerosols through the integration of ground-based measurements, satellite retrievals, and modelling tools during the Seven South East Asian Studies/Biomass-burning Aerosols & Stratocumulus Environment: Lifecycles & Interactions Experiment (7-SEAS/BASELInE) campaign in 2014...
March 27, 2018: Science of the Total Environment
https://www.readbyqxmd.com/read/29582419/synthesis-and-biological-evaluation-of-novel-cyclopropyl-derivatives-as-subtype-selective-ligands-for-estrogen-receptor
#4
Zunyuan Wang, Yewei Yang, Xiaoliang Zheng, Tao Zhang, Wenhai Huang, Dongmei Yan, Wenjun Zhang, Xiaoju Wang, Zhengrong Shen
OBJECTIVES: Tamoxifen is the most commonly used selective estrogen receptor modulators (SERMs); however, patients often develop the acquired drug resistance on tamoxifen therapy. The aim of this study was to develop new SERMs. METHODS: Several novel cyclopropyl derivatives were designed and synthesized. The binding affinities of these compounds as well as the selectivity on subtype of estrogen receptor (ER) were assessed by fluorescence polarization. The antagonistic activity was also evaluated by dual-luciferase reporter assay...
March 27, 2018: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/29579190/27-hydroxycholesterol-is-an-estrogen-receptor-beta-selective-negative-allosteric-modifier-of-17%C3%AE-estradiol-binding
#5
Nicholas J E Starkey, Yufei Li, Sara K Drenkhahn-Weinaug, Jinghua Liu, Dennis B Lubahn
Estrogens bind to two nuclear estrogen receptor (ER) subtypes, ERα and ERβ, which are expressed in differing amounts in various tissues. The endogenous estrogen, 17β-estradiol (E2), binds to both subtypes with nearly equal affinity and is the prototypical agonist. SERMs (Selective Estrogen Receptor Modulators) may bind to both subtypes with equivalent affinities but have agonist activities in some tissues while having antagonist activities in others. We demonstrate here, that the first reported endogenous SERM, 27-hydroxycholesterol (27-OHC), binds preferentially (>100 fold) to ERβ over ERα...
March 19, 2018: Endocrinology
https://www.readbyqxmd.com/read/29574654/serms-promote-anti-inflammatory-signaling-and-phenotype-of-cd14-cells
#6
Lauri Polari, Anu Wiklund, Sofia Sousa, Lauri Kangas, Tero Linnanen, Pirkko Härkönen, Jorma Määttä
Signaling via estrogen receptors (ER) is recognized as an essential part of the immune regulation, and ER-mediated signaling is involved in autoimmune reactions. Especially ERα activation in immune cells has been suggested to skew cytokine production toward Th2/M2-type mediators, which can have protective effect on inflammatory diseases and reduce Th1 and Th17 responses. These effects are caused by increased alternative activation of macrophages and changes in the activation of different T cell populations...
March 24, 2018: Inflammation
https://www.readbyqxmd.com/read/29559388/from-pathogenesis-to-clinical-practice-emerging-medical-treatments-for-endometriosis
#7
REVIEW
Sara Clemenza, Flavia Sorbi, Ivo Noci, Tommaso Capezzuoli, Irene Turrini, Carlo Carriero, Nicolò Buffi, Massimiliano Fambrini, Felice Petraglia
Endometriosis is a chronic disease, and a lifelong management plan should be developed by using pharmacological treatment and surgical procedures. The pathogenesis of endometriosis is complicated and has not been definitively established. The mechanisms involved are numerous, and their understanding is constantly evolving. Currently, the first-line drugs act by blocking ovarian function, creating an hypoestrogenic environment. The blockade of estrogen secretion and receptor activity and the activation of progesteron receptors are the main target of several current drugs, as well as those under development...
February 15, 2018: Best Practice & Research. Clinical Obstetrics & Gynaecology
https://www.readbyqxmd.com/read/29547405/fracture-risk-and-treatment-in-chronic-kidney-disease
#8
Kelsey Connelly, David Collister, Navdeep Tangri
PURPOSE OF REVIEW: Chronic kidney disease (CKD) is associated with the development of mineral bone disorder (MBD), osteoporosis, and fragility fractures. The purpose of this review is to provide an update on recent findings in the diagnosis and treatment of osteoporosis in patients with CKD. RECENT FINDINGS: Multiple observational studies have shown that bone mineral density measurement using DEXA is equally predictive in CKD stages 1-3, as in the general population...
March 15, 2018: Current Opinion in Nephrology and Hypertension
https://www.readbyqxmd.com/read/29533367/tissue-selective-estrogen-complex-tsec-a-review
#9
James H Pickar, Matthieu Boucher, Diana Morgenstern
OBJECTIVE: This review describes historical development of selective estrogen receptor modulators (SERMs) and their combination with estrogens, termed a tissue selective estrogen complex (TSEC), and considers the potential for future TSEC development. METHODS: This narrative review is based on literature identified on PubMed and the TSEC research and development experience of the authors. RESULTS: SERMs have estrogenic and antiestrogenic effects in various tissues; however, no single agent has achieved an optimal balance of agonist and antagonist effects for the treatment of menopausal symptoms...
March 12, 2018: Menopause: the Journal of the North American Menopause Society
https://www.readbyqxmd.com/read/29530558/-new-medical-treatments-for-painful-endometriosis-cngof-has-endometriosis-guidelines
#10
G Legendre, L Delbos, E Hudon, N Chabbert-Buffet, S Geoffron, M Sauvan, H Fernandez, P-E Bouet, P Descamps
OBJECTIVE: The objective of this work is to evaluate the place of new treatments in the management of endometriosis outside the context of infertility. METHODS: A review of the literature was conducted by consulting Medline data until July 2017. RESULTS: Dienogest is effective compared to placebo in short term (NP2) and long term (NP4) for the treatment of painful endometriosis. In comparison with GnRH agonists, dienogest is also effective in terms of decreased pain and improved quality of life in non-operated patients (NP2) as well as for recurrence of lesions and symptomatology postoperatively (NP2)...
March 9, 2018: Gynecologie, Obstetrique, Fertilite & Senologie
https://www.readbyqxmd.com/read/29508640/the-use-of-selective-estrogen-receptor-modulators-on-bone-health-in-men
#11
Sok Kuan Wong, Nur-Vaizura Mohamad, Putri Ayu Jayusman, Ahmad Nazrun Shuid, Soelaiman Ima-Nirwana, Kok-Yong Chin
Selective estrogen receptor modulators (SERMs) represent a class of drugs that act as agonist or antagonist for estrogen receptor in a tissue-specific manner. The SERMs drugs are initially used for the prevention and treatment of osteoporosis in postmenopausal women. Bone health in prostate cancer patients has become a significant concern, whereby patients undergo androgen deprivation therapy is often associated with deleterious effects on bone. Previous preclinical and epidemiological findings showed that estrogens play a dominant role in improving bone health as compared to testosterone in men...
March 6, 2018: Aging Male: the Official Journal of the International Society for the Study of the Aging Male
https://www.readbyqxmd.com/read/29501737/transdermal-delivery-of-raloxifene-hcl-via-ethosomal-system-formulation-advanced-characterizations-and-pharmacokinetic-evaluation
#12
Syed Mahmood, Uttam Kumar Mandal, Bappaditya Chatterjee
Raloxifene HCl belongs to a class of selective estrogen receptor modulators (SERMs) which is used for the management of breast cancer. The major problem reported with raloxifene is its poor bioavailability which is only up to 2%. The main objective of the present work was to formulate raloxifene loaded ethosomal preparation for transdermal application and compare it with an oral formulation of the drug. Five ethosomal formulations with different concentrations of ethanol and a conventional liposomes formulation were prepared by rotary evaporation method...
February 28, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29482944/synthesis-and-biological-evaluation-of-4-6-diaryl-2-pyrimidinamine-derivatives-as-anti-breast-cancer-agents
#13
Linyi Liu, Zhichao Tang, Chengze Wu, Xinyu Li, Ali Huang, Xiang Lu, Qidong You, Hua Xiang
Breast cancer is the most frequently diagnosed cancers and the leading causes of cancer death among females worldwide. Estrogen receptor positive has been identified as the predominant internal reasons, involving in more than 70% breast cancer patients and SERMs which competes with estradiol for the binding to ERα in breast tissue are widely used in the treatment of ER+ breast cancer, such as tamoxifen, raloxifene. However, many SERMs may cause negative side effects due to their estrogenic activity in other tissues and approximate 50% of patients with ER-positive tumors either initially do not respond or become resistant to these drugs...
December 30, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29434492/sr-16234-a-novel-selective-estrogen-receptor-modulator-for-pain-symptoms-with-endometriosis-an-open-label-clinical-trial
#14
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
#15
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
#16
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
#17
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
#18
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
#19
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
#20
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
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