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1

Fillit, Howard. "Future Therapeutic Developments of Estrogen Use." Journal of Clinical Pharmacology 35, no. 9S (September 1995): 25S—28S. http://dx.doi.org/10.1002/j.1552-4604.1995.tb04144.x.

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2

Martin-Jiménez, Cynthia, Diana Milena Gaitán-Vaca, Natalia Areiza, Valentina Echeverria, Ghulam Md Ashraf, Janneth González, Amirhossein Sahebkar, Luis Miguel Garcia-Segura, and George E. Barreto. "Astrocytes Mediate Protective Actions of Estrogenic Compounds after Traumatic Brain Injury." Neuroendocrinology 108, no. 2 (November 4, 2018): 142–60. http://dx.doi.org/10.1159/000495078.

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Traumatic brain injury (TBI) is a serious public health problem. It may result in severe neurological disabilities and in a variety of cellular metabolic alterations for which available therapeutic strategies are limited. In the last decade, the use of estrogenic compounds, which activate protective mechanisms in astrocytes, has been explored as a potential experimental therapeutic approach. Previous works have suggested estradiol (E2) as a neuroprotective hormone that acts in the brain by binding to estrogen receptors (ERs). Several steroidal and nonsteroidal estrogenic compounds can imitate
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3

Santen, Richard J., Risa Kagan, Corrado J. Altomare, Barry Komm, Sebastian Mirkin, and Hugh S. Taylor. "Current and Evolving Approaches to Individualizing Estrogen Receptor-Based Therapy for Menopausal Women." Journal of Clinical Endocrinology & Metabolism 99, no. 3 (March 1, 2014): 733–47. http://dx.doi.org/10.1210/jc.2013-3680.

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Context: Adding progestogens to estrogens changes the risk profile of hormonal therapy for menopausal women, and recent data support the need for progestogen-free options. Several current and evolving approaches to managing estrogen deficiency allow for progestogen omission. We review the mechanisms of estrogen activity and provide an overview of emerging and available estrogen receptor (ER)–based therapies. Evidence Acquisition: PubMed was searched for relevant English-language articles using keywords pertaining to estrogen deficiency, menopause, hormone therapy, and estrogen-only therapy. Pi
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4

Macciò, Antonio, and Clelia Madeddu. "Obesity, Inflammation, and Postmenopausal Breast Cancer: Therapeutic Implications." Scientific World JOURNAL 11 (2011): 2020–36. http://dx.doi.org/10.1100/2011/806787.

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Breast cancer is the female malignant neoplasia with the highest incidence in the industrialized world. Although early diagnosis has contributed to therapeutic success, breast cancer remains a major health issue. In the last few year the hormone therapy for estrogen-dependent breast cancer has evolved achieving significant clinical results; at the same time, it has enabled us to better define the role of estrogens in the etiopathogenesis of this tumour. Weight increase and obesity have been identified as the most important risk and prognostic factors for breast cancer in postmenopausal women.
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Mitra, Saikat, Mashia Subha Lami, Avoy Ghosh, Rajib Das, Trina Ekawati Tallei, Fatimawali, Fahadul Islam, et al. "Hormonal Therapy for Gynecological Cancers: How Far Has Science Progressed toward Clinical Applications?" Cancers 14, no. 3 (February 1, 2022): 759. http://dx.doi.org/10.3390/cancers14030759.

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In recent years, hormone therapy has been shown to be a remarkable treatment option for cancer. Hormone treatment for gynecological cancers involves the use of medications that reduce the level of hormones or inhibit their biological activity, thereby stopping or slowing cancer growth. Hormone treatment works by preventing hormones from causing cancer cells to multiply. Aromatase inhibitors, anti-estrogens, progestin, estrogen receptor (ER) antagonists, GnRH agonists, and progestogen are effectively used as therapeutics for vulvar cancer, cervical cancer, vaginal cancer, uterine cancer, and ov
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6

Gérard, Céline, Mélanie Mestdagt, Ekaterine Tskitishvili, Laudine Communal, Anne Gompel, Elisabete Silva, Jean-François Arnal, et al. "Combined Estrogenic and Antiestrogenic Properties of Estetrol on Breast Cancer may provide a Safe Therapeutic Window for the Treatment of Menopausal Symptoms." Journal of SAFOMS 3, no. 1 (2015): 31–33. http://dx.doi.org/10.5005/jsafoms-3-1-31.

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Abstract Increased risk of breast cancer is a critical side-effect associated with the use of a menopausal hormone therapy (MHT). Estetrol (E4) is a natural estrogen produced by the human fetal liver and is a promising compound for clinical use in MHT. However, its impact on breast cancer is controversial and poorly defined. In this preclinical study, we show that E4 acts as a weak estrogen by stimulating the growth of hormone-dependent breast cancer only at concentrations exceeding menopausal therapeutic needs. Estetrol (E4) presents also an antitumor activity by decreasing the strong prolife
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7

Hwang, Wu Jeong, Tae Young Lee, Nahrie Suk Kim, and Jun Soo Kwon. "The Role of Estrogen Receptors and Their Signaling across Psychiatric Disorders." International Journal of Molecular Sciences 22, no. 1 (December 31, 2020): 373. http://dx.doi.org/10.3390/ijms22010373.

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Increasing evidence suggests estrogen and estrogen signaling pathway disturbances across psychiatric disorders. Estrogens are not only crucial in sexual maturation and reproduction but are also highly involved in a wide range of brain functions, such as cognition, memory, neurodevelopment, and neuroplasticity. To add more, the recent findings of its neuroprotective and anti-inflammatory effects have grown interested in investigating its potential therapeutic use to psychiatric disorders. In this review, we analyze the emerging literature on estrogen receptors and psychiatric disorders in cellu
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8

Zhao, Zhuo, Hao Wang, Jewell A. Jessup, Sarah H. Lindsey, Mark C. Chappell, and Leanne Groban. "Role of estrogen in diastolic dysfunction." American Journal of Physiology-Heart and Circulatory Physiology 306, no. 5 (March 1, 2014): H628—H640. http://dx.doi.org/10.1152/ajpheart.00859.2013.

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The prevalence of left ventricular diastolic dysfunction (LVDD) sharply increases in women after menopause and may lead to heart failure. While evidence suggests that estrogens protect the premenopausal heart from hypertension and ventricular remodeling, the specific mechanisms involved remain elusive. Moreover, whether there is a protective role of estrogens against cardiovascular disease, and specifically LVDD, continues to be controversial. Clinical and basic science have implicated activation of the renin-angiotensin-aldosterone system (RAAS), linked to the loss of ovarian estrogens, in th
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9

Farkas, Szidónia, Adrienn Szabó, Anita Emőke Hegyi, Bibiána Török, Csilla Lea Fazekas, Dávid Ernszt, Tamás Kovács, and Dóra Zelena. "Estradiol and Estrogen-like Alternative Therapies in Use: The Importance of the Selective and Non-Classical Actions." Biomedicines 10, no. 4 (April 6, 2022): 861. http://dx.doi.org/10.3390/biomedicines10040861.

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Estrogen is one of the most important female sex hormones, and is indispensable for reproduction. However, its role is much wider. Among others, due to its neuroprotective effects, estrogen protects the brain against dementia and complications of traumatic injury. Previously, it was used mainly as a therapeutic option for influencing the menstrual cycle and treating menopausal symptoms. Unfortunately, hormone replacement therapy might be associated with detrimental side effects, such as increased risk of stroke and breast cancer, raising concerns about its safety. Thus, tissue-selective and no
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10

Sulaymanova, R. T. "EXPERIMENTAL MODELS OF TRANSGENERATIONAL EFFECTS OF THE INFLUENCE OF ESTROGENS ON THE MORPHOLOGY OF REPRODUCTIVE ORGANS IN POSTNATAL ONTOGENESIS." Morphological newsletter 27, no. 1 (March 30, 2019): 36–44. http://dx.doi.org/10.20340/mv-mn.19(27).01.36-44.

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In the modern clinical practice there is an increase in the use of hormones, their analogues and substances with hormone-like action in medical practice for the regulation of the menstrual cycle, conception, prevention, maintenance and resolution of pregnancy. According to official reports, in recent years, the number of annual cycles of assisted reproductive technology with hormonal support has increased six times in the country. The purpose of the review is to summarize current data on the effects of experimental and clinical effects of various doses of estrogens and drugs with estrogenic ef
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11

Normanno, Nicola, Massimo Di Maio, Ermelinda De Maio, Antonella De Luca, Andrea de Matteis, Antonio Giordano, Francesco Perrone, and _. _. "Mechanisms of endocrine resistance and novel therapeutic strategies in breast cancer." Endocrine-Related Cancer 12, no. 4 (December 2005): 721–47. http://dx.doi.org/10.1677/erc.1.00857.

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Tamoxifen has been the mainstay of hormonal therapy in both early and advanced breast cancer patients for approximately three decades. The availability of novel compounds such as aromatase inhibitors (AIs) and fulvestrant, with different mechanism of action, is changing the scenario of endocrine treatment of postmenopausal breast cancer patients. In this review article, we have summarized the current knowledge of the mechanisms of resistance to endocrine therapy, in order to derive information that might be useful for therapeutic intervention. We propose that resistance to endocrine therapy is
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12

Elloso, M. Merle, Kristen Phiel, Ruth A. Henderson, Heather A. Harris, and Steven J. Adelman. "Suppression of experimental autoimmune encephalomyelitis using estrogen receptor-selective ligands." Journal of Endocrinology 185, no. 2 (May 2005): 243–52. http://dx.doi.org/10.1677/joe.1.06063.

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Estrogens have been shown to modulate disease activity in experimental autoimmune encephalomyelitis (EAE), the mouse model for multiple sclerosis. Consistent with these findings, the severity of disease is reduced in pregnant women with multiple sclerosis when levels of estrogens are high. Estrogens bind to two known estrogen receptors (ER), ERα and ERβ. The relative contribution of these receptors to estrogen-mediated suppression of EAE was explored using ER-selective ligands. The ER antagonist ICI 182 780 reversed the suppressive effects of 17β-estradiol (E2), demonstrating that the protecti
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13

Manyonda, Isaac, Vikram S Talaulikar, Roxanna Pirhadi, and Joseph Onwude. "Progestogens are the problem in hormone replacement therapy: Time to reappraise their use." Post Reproductive Health 26, no. 1 (December 25, 2019): 26–31. http://dx.doi.org/10.1177/2053369119876490.

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Combined (estrogen and a progestogen) hormone replacement therapy (cHRT) is associated with an increased risk of breast cancer, while estrogen replacement therapy is not. Whatever the underlying mechanism, it is the progestogen in cHRT that seems to increase the risk. Fear of breast cancer is a major limiting factor in the use of hormone replacement therapy, and when women discontinue cHRT because of side effects, the latter are often attributable to the progestogen component. cHRT is given to women with an intact uterus to protect against the effects of un-opposed estrogen such as an increase
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14

Carroll, Kelli J., Michael C. Dovey, Claire C. Cutting, James M. Harris, Lea M. Vedder, Wolfram Goessling, and Trista E. North. "Estrogen Receptors 1 and 2 Have Stage-Specific Effects on Hematopoietic Stem Cell Regulation In Zebrafish." Blood 116, no. 21 (November 19, 2010): 1617. http://dx.doi.org/10.1182/blood.v116.21.1617.1617.

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Abstract Abstract 1617 The intrinsic signaling pathways regulating hematopoietic stem cells (HSC) are increasingly well recognized. However, less is known about how in utero exposure to common environmental xenobiotic compounds may alter HSC development and increase the risk of carcinogenesis. RUNX1 (AML1), required for definitive HSC induction in all vertebrates, is the target of frequent chromosomal alterations associated with leukemia. Through a chemical genetic screen for modifiers of runx1 expression in the zebrafish, estrogen-related compounds were identified. Here, we found that exposur
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15

Petrie, Whitney K., Megan K. Dennis, Chelin Hu, Donghai Dai, Jeffrey B. Arterburn, Harriet O. Smith, Helen J. Hathaway, and Eric R. Prossnitz. "G Protein-Coupled Estrogen Receptor-Selective Ligands Modulate Endometrial Tumor Growth." Obstetrics and Gynecology International 2013 (2013): 1–17. http://dx.doi.org/10.1155/2013/472720.

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Endometrial carcinoma is the most common cancer of the female reproductive tract. GPER/GPR30 is a 7-transmembrane spanning G protein-coupled receptor that has been identified as the third estrogen receptor, in addition to ERαand ERβ. High GPER expression is predictive of poor survival in endometrial and ovarian cancer, but despite this, the estrogen-mediated signaling pathways and specific estrogen receptors involved in endometrial cancer remain unclear. Here, employing ERα-negative Hec50 endometrial cancer cells, we demonstrate that GPER mediates estrogen-stimulated activation of ERK and PI3K
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16

Yakushevskaya, O. V. "Continuous combined low-dose hormone replacement therapy in perimenopause: an algorithm of choice." Meditsinskiy sovet = Medical Council, no. 3 (April 15, 2021): 113–18. http://dx.doi.org/10.21518/2079-701x-2021-3-113-118.

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In the age of broad medical options, women’s health has received sufficient attention. The different periods of a woman’s life are characterised by specific physiological changes, based on the age-related characteristics of the reproductive system. The onset of menopause can have a negative impact on health in varying degrees. Clinicians have a clear understanding of the effects of estrogen deficiency and the therapeutic options for managing it with menopausal hormone therapy (MHT) and alternative methods of treatment. However, to date, methods for optimising and individualising the correction
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17

Carroll, Kelli J., Michael C. Dovey, Claire C. Cutting, Lea Vedder Sheward, James M. Harris, Wolfram Goessling, and Trista E. North. "Hematopoietic Stem Cell Formation in Zebrafish Is Regulated in a Temporally Distinct Manner by Estrogen Receptor 2." Blood 118, no. 21 (November 18, 2011): 1268. http://dx.doi.org/10.1182/blood.v118.21.1268.1268.

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Abstract Abstract 1268 The intrinsic signaling pathways regulating hematopoietic stem cells (HSC) are increasingly understood; in contrast, less is known about the potential effect of exposure to environmental factors, such as xenoestrogens, on the formation of HSCs. RUNX1 (AML1) is a highly conserved transcription factor that is required for definitive HSC induction and is also the target of many chromosomal alterations in leukemia. Through a chemical genetic screen, estrogen-related compounds were identified as modifiers of runx1 expression in the zebrafish. Exposure to 17b-estradiol (E2) th
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18

Kareva, Kareva E. N., and Smetnik A. A. Smetnik. "Estrogen-like and antioxidant properties of resveratrol in clinical pharmacology and therapeutic use." Akusherstvo i ginekologiia 12_2021 (December 24, 2021): 37–48. http://dx.doi.org/10.18565/aig.2021.12.37-48.

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19

Acharya, Asha, Ila Das, Des Chandhok, and Tapas Saha. "Redox Regulation in Cancer: A Double-edged Sword with Therapeutic Potential." Oxidative Medicine and Cellular Longevity 3, no. 1 (2010): 23–34. http://dx.doi.org/10.4161/oxim.3.1.10095.

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Oxidative stress, implicated in the etiology of cancer, results from an imbalance in the production of reactive oxygen species (ROS) and cell’s own antioxidant defenses. ROS deregulate the redox homeostasis and promote tumor formation by initiating an aberrant induction of signaling networks that cause tumorigenesis. Ultraviolet (UV) exposures, γ-radiation and other environmental carcinogens generate ROS in the cells, which can exert apoptosis in the tumors, thereby killing the malignant cells or induce the progression of the cancer growth by blocking cellular defense system. Cancer stem cells
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20

Compston, Juliet E. "Sex Steroids and Bone." Physiological Reviews 81, no. 1 (January 1, 2001): 419–47. http://dx.doi.org/10.1152/physrev.2001.81.1.419.

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Sex steroids are essential for skeletal development and the maintenance of bone health throughout adult life, and estrogen deficiency at menopause is a major pathogenetic factor in the development of osteoporosis in postmenopausal women. The mechanisms by which the skeletal effects of sex steroids are mediated remain incompletely understood, but in recent years there have been considerable advances in our knowledge of how estrogens and, to a lesser extent androgens, influence bone modeling and remodeling in health and disease. New insights into estrogen receptor structure and function, recent
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21

Benagiano, Giuseppe, and Ivo Brosens. "The Endometrium in Adenomyosis." Women's Health 8, no. 3 (May 2012): 301–12. http://dx.doi.org/10.2217/whe.12.8.

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Eutopic and ectopic endometria of women with adenomyosis show a series of metabolic and molecular abnormalities that increase angiogenesis and proliferation, decrease apoptosis, allow local production of estrogens, create progesterone resistance, and impair cytokine expression. These changes enhance the ability of the endometrium to infiltrate the junctional zone myometrium and the growth of ectopic tissue. In addition, in these subjects several immunological abnormalities have been observed, together with an increased production of ‘free radicals’ leading to excessive growth of endometrial st
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22

Velez, Maria A., Timothy F. Burns, and Laura P. Stabile. "The estrogen pathway as a modulator of response to immunotherapy." Immunotherapy 11, no. 13 (September 2019): 1161–76. http://dx.doi.org/10.2217/imt-2019-0024.

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Lung cancer is the leading cause of cancer deaths worldwide, with a 5-year survival rate of about 18%. Thus, there is a great need for novel therapeutic approaches to treat non-small-cell lung cancer (NSCLC). Immune checkpoint inhibitors (ICIs) have improved outcomes for a subset of patients, especially those with high programmed death-ligand 1 expression and/or high tumor mutational burden, but have failed in the majority of patients. Increasing evidence suggests that the estrogen signaling pathway may be a therapeutic target in metastatic NSCLC and that the estrogen pathway may play a role i
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23

Kuznetsova, I. V. "Transition period of estrogen-progestogen hormone therapy." Medical alphabet 3, no. 25 (November 19, 2019): 6–10. http://dx.doi.org/10.33667/2078-5631-2019-3-25(400)-6-10.

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Combined hormonal contraception is an effective method of preventing pregnancy and at the same time has a number of therapeutic effects. The need for contraception persists until the final cessation of menstrual function, but at an older fertile age, the selection of a hormonal agent becomes a daunting task. Over the past years, a woman has accumulated factors that can complicate the use of hormonal drugs, and, on the other hand, new problems arise in the transitional period of life, which combined contraceptives can solve. An equally relevant topic is the question of stopping the use of combi
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24

Biggar, Robert J. "Molecular Pathways: Digoxin Use and Estrogen-Sensitive Cancers—Risks and Possible Therapeutic Implications: Figure 1." Clinical Cancer Research 18, no. 8 (February 24, 2012): 2133–37. http://dx.doi.org/10.1158/1078-0432.ccr-11-1389.

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25

Zhao, Hong, Ling Zhou, Anna Junjie Shangguan, and Serdar E. Bulun. "Aromatase expression and regulation in breast and endometrial cancer." Journal of Molecular Endocrinology 57, no. 1 (July 2016): R19—R33. http://dx.doi.org/10.1530/jme-15-0310.

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Long-term exposure to excess estrogen increases the risk of breast cancer and type 1 endometrial cancer. Most of the estrogen in premenopausal women is synthesized by the ovaries, while extraovarian subcutaneous adipose tissue is the predominant tissue source of estrogen after menopause. Estrogen and its metabolites can cause hyperproliferation and neoplastic transformation of breast and endometrial cells via increased proliferation and DNA damage. Several genetically modified mouse models have been generated to help understand the physiological and pathophysiological roles of aromatase and es
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26

Foster, Paul A., L. W. Lawrence Woo, Barry V. L. Potter, Michael J. Reed, and Atul Purohit. "The Use of Steroid Sulfatase Inhibitors as a Novel Therapeutic Strategy Against Hormone-Dependent Endometrial Cancer." Endocrinology 149, no. 8 (May 1, 2008): 4035–42. http://dx.doi.org/10.1210/en.2008-0223.

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The past few years have seen an increase in the reported incidence of endometrial carcinoma, one of the most frequently diagnosed malignancies of the female genital tract. Estrogen production is vital for the mitogenesis of endometrial tumors. Inhibition of steroid sulfatase (STS), an enzyme responsible for the synthesis of steroids with estrogenic properties, may represent a novel therapeutic target for this type of cancer. This study investigates the effects of STX64 (also known as 667Coumate and BN83495) and STX213, two potent STS inhibitors, on hormone-dependent endometrial cancer cell gro
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27

Zhao, Liqin, Zisu Mao та Roberta Diaz Brinton. "A Select Combination of Clinically Relevant Phytoestrogens Enhances Estrogen Receptor β-Binding Selectivity and Neuroprotective Activities in Vitro and in Vivo". Endocrinology 150, № 2 (1 лютого 2009): 770–83. http://dx.doi.org/10.1210/en.2008-0715.

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We have previously shown that a number of naturally occurring phytoestrogens and derivatives were effective to induce some measures of neuroprotective responses but at a much lower magnitude than those induced by the female gonadal estrogen 17β-estradiol. In the present study, we sought to investigate whether a combination of select phytoestrogens could enhance neural responses without affecting the reproductive system. We performed a range of comparative analyses of the estrogen receptor (ER) α/β binding profile, and in vitro to in vivo estrogenic activities in neural and uterine tissues indu
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28

Kuznetsova, I. V., L. V. Evsyukova, and V. A. Konovalov. "Combined oral contraception: is there a resource for increased use?" Medical Council, no. 12 (July 29, 2018): 146–51. http://dx.doi.org/10.21518/2079-701x-2018-12-146-151.

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Combined oral contraceptives (COCs) are a highly effective method for preventing unintended pregnancy, but unfortunately, the resource of their contraceptive and therapeutic potential is not used enough, and global unintended pregnancies account for about 40%. The reasons for the lack of proper distribution of COCs are insufficient awareness of the beneficial properties of contraception, along with exaggerated fears of the adverse effects of hormone intake both among women and among doctors. This problem can only be overcome by providing adequate information to health professionals regarding t
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29

Gucalp, Ayca, and Tiffany A. Traina. "Triple-Negative Breast Cancer: Adjuvant Therapeutic Options." Chemotherapy Research and Practice 2011 (June 21, 2011): 1–13. http://dx.doi.org/10.1155/2011/696208.

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Triple-negative breast cancer (TNBC), a subtype distinguished by negative immunohistochemical assays for expression of the estrogen and progesterone receptors (ER/PR) and human epidermal growth factor receptor-2(HER2) represents 15% of all breast cancers. Patients with TNBC generally experience a more aggressive clinical course with increased risk of disease progression and poorer overall survival. Furthermore, this subtype accounts for a disproportionate number of disease-related mortality in part due to its aggressive natural history and our lack of effective targeted agents beyond conventio
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30

Hahn, S. E., L. A. da Cruz, D. Sayegh, A. Ferry, K. O’Reilly, D. S. Pereira, D. B. Rubinstein, H. Findlay, and D. S. Young. "Therapeutic monoclonal antibodies target phenotypically-differing human breast cancer." Journal of Clinical Oncology 25, no. 18_suppl (June 20, 2007): 13510. http://dx.doi.org/10.1200/jco.2007.25.18_suppl.13510.

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13510 Background: CD44 (an adhesion molecule and stem cell antigen), CD59 (a complement-inhibitory molecule), MCSP (an adhesion and cell-cell interactions), and Trop-2 (EpCam a related signaling molecule) represent a group of biologically-significant cancer proteins acting through distinct mechanisms. We have described Abs with in vitro and in vivo cancer suppressive activity to this group of targets. However, their effectiveness depends on the phenotype of malignant cells; cell response should correlate with expression of its Ag, and tumor cells represent a heterogeneous group of non-synchron
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31

Monaco, Alessandra, Fabrizio Licitra, Martina Di Gisi, Giovanni Galasso, Marzia Di Donato, Pia Giovannelli, Antimo Migliaccio та Gabriella Castoria. "ERβ in Triple-Negative Breast Cancer: Emerging Concepts and Therapeutic Possibilities". Endocrines 2, № 3 (13 вересня 2021): 356–65. http://dx.doi.org/10.3390/endocrines2030033.

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Despite the improvements in diagnostic and therapeutic approaches, breast cancer still remains one of the world’s leading causes of death among women. Particularly, triple negative breast cancer (TNBC) is characterized by aggressiveness, metastatic spreading, drug resistance and a very high percentage of death in patients. Nowadays, identification of new targets in TNBC appears very compelling. TNBC are considered negative for the estrogen receptor alpha (ERα) expression. Nevertheless, they often express ERβ and its variants. As such, this TNBC subtype still responds to estrogens. While the ER
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32

shen, Tian, Helia Nasrollahi Sanchez, Hong Zan, and Paolo Casali. "Short-chain fatty acid HDAC inhibitor-mediated downregulation of AID expression and class switch DNA recombination is relieved by estrogen through modulation of selected microRNAs." Journal of Immunology 196, no. 1_Supplement (May 1, 2016): 127.12. http://dx.doi.org/10.4049/jimmunol.196.supp.127.12.

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Abstract Estrogen contributes to the elevated antibody response to vaccines in women and the female bias of autoimmune responses, likely by increasing class-switched and hypermutated antibodies and pathogenic autoantibodies. As we have shown, estrogen potentiates the induction of AID, which is critical for class switch DNA recombination (CSR) and somatic hypermutation (SHM), through upregulation of HoxC4. Estrogen may also alter AID gene expression through epigenetic modifications. As we have also shown, short-chain fatty acid (SCFA) histone deacetylase inhibitors (HDIs), including valproic ac
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33

Cannataro, Roberto, and Erika Cione. "Nutritional Supplements and Lipedema: Scientific and Rational Use." Nutraceuticals 2, no. 4 (October 3, 2022): 270–77. http://dx.doi.org/10.3390/nutraceuticals2040020.

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Lipedema is a pathology of the adipose tissue, in evident female prevalence, diagnosed clinically and still of not well-defined etiopathogenesis. Indeed, an estrogen-related component is present, and an inflammatory state and a condition of edema are present in most cases; even pain seems to be a recurring feature, and insulin resistance is also often associated with lipedema. The therapeutic approach is finally becoming holistic. Therefore, with surgery, physiotherapy, and elastic compression therapy, the nutritional aspect of food supplementation is gaining much value. The objective of the p
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34

Kim, Kyung Hee, Derek Toomre, and Jeffrey R. Bender. "Splice isoform estrogen receptors as integral transmembrane proteins." Molecular Biology of the Cell 22, no. 22 (November 15, 2011): 4415–23. http://dx.doi.org/10.1091/mbc.e11-05-0416.

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In addition to enhancing or repressing transcription, steroid hormone receptors rapidly transduce kinase activation signals. On ligand engagement, an N-terminus–truncated splice isoform of estrogen receptor (ER) α, ER46, triggers membrane-initiated signals, resulting in endothelial nitric oxide synthase (eNOS) activation and endothelial NO production. The orientation of ER46 at the plasma membrane is incompletely defined. With the use of ecliptic pHluorin-fused ER46, total internal reflection fluorescence microscopy in live human endothelial cells illustrates that ER46 can topologically confor
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Chen, Shuhua, Jon Nilsen, and Roberta Diaz Brinton. "Dose and Temporal Pattern of Estrogen Exposure Determines Neuroprotective Outcome in Hippocampal Neurons: Therapeutic Implications." Endocrinology 147, no. 11 (November 1, 2006): 5303–13. http://dx.doi.org/10.1210/en.2006-0495.

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To address controversies of estrogen therapy, in vitro models of perimenopause and prevention vs. treatment modes of 17β-estradiol (E2) exposure were developed and used to assess the neuroprotective efficacy of E2 against β-amyloid-1–42 (Aβ1–42)-induced neurodegeneration in rat primary hippocampal neurons. Low E2 (10 ng/ml) exposure exerted neuroprotection in each of the perimenopausal temporal patterns, acute, continuous, and intermittent. In contrast, high E2 (200 ng/ml) was ineffective at inducing neuroprotection regardless of temporal pattern of exposure. Although high E2 alone was not tox
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Yukalchuk, D. Yu, D. M. Ponomarenko, T. N. Yukalchuk, S. S. Sidorova, A. V. Shevchuk, and A. M. Novopashin. "The Use of Alpelisib in Metastatic Estrogen-Receptor-Positive HER2/Neu-Negative Breast Cancer." Effective Pharmacotherapy 18, no. 13 (April 25, 2022): 121–16. http://dx.doi.org/10.33978/2307-3586-2022-18-13-12-16.

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The clinical case presented in the article demonstrates the effectiveness of orange in combination with fulvestrant in metastatic estrogen receptor-positive HER2/neu-negative breast cancer with a mutation in the PIK3CA gene. The resistance of hormone therapy requires the search for new therapeutic options. The results of the SOLAR-1 and BYLieve studies have shown not only the effectiveness of alpelisib, but also new types of toxicity characteristic of this therapy. At the moment, recommendations have been developed for the prevention and treatment of the most frequent adverse events, allowing
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Oualla, Karima, Heba M. El-Zawahry, Banu Arun, James M. Reuben, Wendy A. Woodward, Heba Gamal El-Din, Bora Lim, Nawfel Mellas, Naoto T. Ueno, and Tamer M. Fouad. "Novel therapeutic strategies in the treatment of triple-negative breast cancer." Therapeutic Advances in Medical Oncology 9, no. 7 (June 13, 2017): 493–511. http://dx.doi.org/10.1177/1758834017711380.

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Triple-negative breast cancer (TNBC) is a heterogeneous subtype of breast cancer that is defined by negative estrogen receptor (ER), progesterone receptor (PR) and human epidermal growth factor receptor 2 (HER2) status. Treating patients with TNBC remains clinically challenging, as patients are not candidates for endocrine or HER2-directed therapy. As a result, chemotherapy with traditional agents such as anthracyclines and taxanes remains the only available option with moderate success. Recent discoveries have revealed that TNBC is a heterogeneous disease at the clinical, histological and mol
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Bitirim, Ceylan V., Zeynep B. Ozer, and Kamil C. Akcali. "Estrogen receptor alpha regulates the expression of adipogenic genes genetically and epigenetically in rat bone marrow-derived mesenchymal stem cells." PeerJ 9 (September 10, 2021): e12071. http://dx.doi.org/10.7717/peerj.12071.

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Regulation of the efficacy of epigenetic modifiers is regarded as an important control mechanism in the determination and differentiation of stem cell fate. Studies are showing that the effect of estrogen is important in the differentiation of mesenchymal stem cells (MSCs) into adipocytes, osteocytes, and chondrocytes. Activation of certain transcription factors and epigenetic modifications in related genes play an active role in the initiation and completion of adipogenic differentiation. Understanding the role of estrogen in diseases such as obesity, which increases with the onset of menopau
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Ghuge, Rahul B., Prashant R. Murumkar, Kailash M. Choudhary, Karan D. Joshi, Monica Chauhan, Rahul R. Barot, and Mange R. Yadav. "Development of Steroidal Aromatase Inhibitors as Potential Anti-breast Cancer Agents." Current Enzyme Inhibition 16, no. 1 (May 4, 2020): 45–62. http://dx.doi.org/10.2174/1573408016666200212094804.

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Breast cancer is the most prevalent type of cancer and one of the leading causes of death among all the cancers affecting women worldwide. Preliminary cause of development of tumors in the breast cancer in post-menopausal women is mostly the increased estrogen levels in the body which could be the result of overexpression of aromatase CYP450 i.e. CYP19A1. Aromatase is the only enzyme present in humans that brings about aromatization of A-ring of 19-carbon androgens to form 18-carbon estrogens. Inhibiting aromatase enzyme thereby decreasing the estrogen levels in the postmenopausal women has be
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Downs, William V., Edward L. Perkins, William E. Burak, and Himangshu S. Bose. "ODP433 An increased in AIPB expression in Triple Negative (ER-/PR-/Her2-) Breast Tumors reduces estradiol synthesis." Journal of the Endocrine Society 6, Supplement_1 (November 1, 2022): A671. http://dx.doi.org/10.1210/jendso/bvac150.1388.

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Abstract Aromatase (estrogen synthetase) is a p450 family of enzymes that catalyzes testosterone to estradiol in presence of a cofactor NADPH. Aromatase is central for its role in reproduction and reproductive diseases for catalyzing the conversion of testosterone to estradiol by aromatase. Since aromatase is responsible for the synthesis of estrogens, it is essentially a rate limiting enzyme. Aromatase is expressed mainly in the ovaries of premenopausal women and placentas of pregnant women. Therapeutic approaches for controlling breast cancer proliferation include reducing estrogen by interf
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Wu, Malinda, Neha Arora, Viranuj Sueblinvong, William R. Hunt, and Vin Tangpricha. "Estrogen Supplementation Is Associated With Higher Quality of Life Scores in Women With Cystic Fibrosis." Journal of the Endocrine Society 5, Supplement_1 (May 1, 2021): A732. http://dx.doi.org/10.1210/jendso/bvab048.1489.

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Abstract Purpose: With rapid advancements in therapeutic options for patients with cystic fibrosis (CF), the median predicted survival has increased to 47 years along with the prevalence of non-pulmonary complications for patients with CF. Women with CF suffer irregular menses, sexual dysfunction and low bone mineral density. With increasing pregnancies among women with CF, they may consider contraception. Estrogen supplementation may modulate these outcomes and others. The purpose of this study was to explore the effects of supplemental estrogen use on quality of life (QOL) in CF. Methods: Wo
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Vorobiof, Daniel A. "Recent advances in the medical treatment of breast cancer." F1000Research 5 (November 29, 2016): 2786. http://dx.doi.org/10.12688/f1000research.9619.1.

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Over the past few decades, the systemic therapy of breast cancer (early and advanced) has changed considerably. For the past 40–50 years, and since the discovery and further therapeutic use of tamoxifen, a selective estrogen receptor modulator, breast cancer treatment has become the model for the development and success of tailored medical treatment. Much still needs to be done in improving outcomes for all patients with breast cancer, and especially for those who have advanced breast cancer, a challenging area for medical oncologists. Ongoing international clinical trials are currently evalua
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Gunther, Jillian R., Yuhong Du, Eric Rhoden, Iestyn Lewis, Brian Revennaugh, Terry W. Moore, Sung Hoon Kim, Raymond Dingledine, Haian Fu, and John A. Katzenellenbogen. "A Set of Time-Resolved Fluorescence Resonance Energy Transfer Assays for the Discovery of Inhibitors of Estrogen Receptor-Coactivator Binding." Journal of Biomolecular Screening 14, no. 2 (February 2009): 181–93. http://dx.doi.org/10.1177/1087057108329349.

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Therapeutic block of estrogen action is typically achieved with conventional antagonists (CAs), compounds that displace estradiol from the estrogen receptor (ER) and induce formation of an ER conformation that cannot bind to coactivator proteins, such as the steroid receptor coactivators (SRCs). As an alternative mode for blocking estrogen action, the authors seek small molecules that act as coactivator binding inhibitors (CBIs)—that is, they compete directly with SRC3 for interaction with estradiol-bound ER. CBIs would be interesting mechanistic probes of estrogen action and might also provid
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Li, Ang. "An Overview of Tumor Necrosis Factor-α on Pathophysiological Mechanisms, Relevant Therapeutic Status in Breast Cancer". Highlights in Science, Engineering and Technology 8 (17 серпня 2022): 472–80. http://dx.doi.org/10.54097/hset.v8i.1201.

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TNFα is an essential pro-inflammatory cytokine that is prevalent in the tumor microenvironment and is involved in mediating or activating many significant signaling pathways which result in inflammation, apoptosis, and tumor cell proliferation, survival, and invasiveness. In breast cancer, TNFα is involved throughout all stages from occurrence, development, procession, and metastasis to recurrence. Researchers have pointed out that TNFα plays a major role in the estrogen biosynthesis pathway, especially in the process of adipose tissue switching to estrogen. In the breast tumor microenvironmen
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Ray, Rinki, Christine M. Herring, Troy A. Markel, Paul R. Crisostomo, Meijing Wang, Brent Weil, Tim Lahm, and Daniel R. Meldrum. "Deleterious effects of endogenous and exogenous testosterone on mesenchymal stem cell VEGF production." American Journal of Physiology-Regulatory, Integrative and Comparative Physiology 294, no. 5 (May 2008): R1498—R1503. http://dx.doi.org/10.1152/ajpregu.00897.2007.

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Modulating the paracrine effects of bone marrow mesenchymal stem cells (BMSCs) may be important for the treatment of ischemic myocardial tissue. In this regard, endogenous estrogen may enhance BMSC vascular endothelial growth factor (VEGF) production. However, little information exists regarding the effect of testosterone on stem cell function. We hypothesized that 1) endogenous or exogenous estrogen will enhance stem cell production of VEGF and 2) endogenous or exogenous testosterone will inhibit BMSC VEGF production. BMSCs were collected from adult male, female, castrated male, and ovariecto
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Thabet, Romany H., Adel A. Gomaa, Laila M. Matalqah, and Erin M. Shalaby. "Vitamin D: an essential adjuvant therapeutic agent in breast cancer." Journal of International Medical Research 50, no. 7 (July 2022): 030006052211138. http://dx.doi.org/10.1177/03000605221113800.

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Low serum levels of vitamin D have been reported as a risk factor for breast cancer. This narrative review provides an update on the impact of vitamin D on hormone receptors, notably estrogen receptor subunits, and gives insights on possible therapeutic interventions to overcome breast cancer. In addition, evidence that supports the beneficial use of vitamin D as adjuvant treatment of breast cancer is summarized. Vitamin D deficiency is significantly widespread in patients with triple-negative tumors. Several studies have observed a possible modulatory effect of vitamin D or its analogues on t
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Komal S, Harikrishnan N, Gejalakshmi S, Kayalvizhi S, Hemamalini Baskaran, Priyanka J, Mohan Kumar A, and Sriram GM. "Novel herbs and drugs for endometriosis management: A review on current and futuristic therapies." International Journal of Research in Pharmaceutical Sciences 12, no. 2 (May 8, 2021): 1404–14. http://dx.doi.org/10.26452/ijrps.v12i2.4699.

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A disorder with estrogen dependency comprising of inflammatory lesions outside the uterus, causing pain and inflammation in pelvis and affecting women of reproductive age with infertility and post reproductive age is endometriosis. Endometriosis is viewed as public health issue with a major impact on quality of life of women. Medically advanced computational and chemical treatments are available to treat the progression of the disease by diagnostic imaging, clinical examinations, imaging and laparoscopy often leading to immediate surgery. A warrantable rethinking on the diagnosis and managemen
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Ciesielska, Aleksandra, Aida Kusiak, Agata Ossowska, and Magdalena Emilia Grzybowska. "Changes in the Oral Cavity in Menopausal Women—A Narrative Review." International Journal of Environmental Research and Public Health 19, no. 1 (December 27, 2021): 253. http://dx.doi.org/10.3390/ijerph19010253.

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Oral health awareness during the menopausal period is essential to minimize the inevitable inconveniences which may occur due to hormonal changes. The decrease in estrogen hormone concentration impacts the oral mucosa in a similar way to the vaginal mucosa due to the presence of estrogen receptors in both of these structures. An estrogen deficiency also affects the maturation process of the oral mucosal epithelium and can lead to its thinning and atrophy, making it more susceptible to local mechanical injuries, causing a change in pain tolerance and problems in the use of removable prosthetic
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Yu, Xinge, Angela C. Weyand, and Jordan A. Shavit. "Surprisingly Rapid Onset of Estrogen-Induced Venous Thrombosis in an Animal Model." Blood 132, Supplement 1 (November 29, 2018): 418. http://dx.doi.org/10.1182/blood-2018-99-120325.

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Abstract Venous thrombosis is a well-known complication of sex hormone therapy, with onset typically within weeks to months after initiation. Worldwide, more than 100 million pre-menopausal women use combined oral contraceptives, thus tens to hundreds of thousands develop thrombosis annually, resulting in significant morbidity and mortality. Estrogens are thought to be the major thrombotic risk, although the impact of progestins is less clear. It has been hypothesized that progestin effects may be secondary to mitigation of the estrogen effect. Although it is known that estrogens and progestin
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Lopez-Munoz, E., N. Garcia-Hernandez, R. I. Penaloza-Espinosa, M. E. Gomez-Del Toro, G. Zarco-Espinosa, S. Barroso-Bravo, F. Salamanca-Gomez, and D. J. Arenas-Aranda. "”BIK/NBK Gene Expression as a Possible Marker of Circulating Breast Cancer Cells in Blood“." Open Biomarkers Journal 4, no. 1 (October 14, 2011): 8–14. http://dx.doi.org/10.2174/1875318301104010008.

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The detection of circulating breast cancer cells in blood could be of special interest as an indicator of diagnosis and prognosis, and for the selection of treatment. In a previous report, our research group determined gene expression profiles in samples of breast cancer tissue, identifying over-expression of the BIK/NBK mRNA gene in 90% of the analyzed samples. In this paper, we analyze the BIK/NBK gene expression as a possible biomarker of circulating breast cancer cells in blood. We demonstrate that the BIK/NBK gene expression is not a significant biomarker in the detection of circulating b
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