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https://www.readbyqxmd.com/read/28431277/endocrine-disruption-by-environmental-gestagens-in-amphibians-a-short-review-supported-by-new-in%C3%A2-vitro-data-using-gonads-of-xenopus-laevis
#1
REVIEW
Andrea Ziková, Claudia Lorenz, Frauke Hoffmann, Wibke Kleiner, Ilka Lutz, Matthias Stöck, Werner Kloas
Endocrine disruption caused by various anthropogenic compounds is of persisting concern, especially for aquatic wildlife, because surface waters are the main sink of these so-called endocrine disruptors (ED). In the past, research focused on (anti)estrogenic, (anti)androgenic, and (anti)thyroidal substances, affecting primarily reproduction and development in vertebrates; however, other endocrine systems might be also targeted by ED. Environmental gestagens, including natural progestogens (e.g. progesterone (P4)) and synthetic progestins used for contraception, are supposed to affect vertebrate reproduction via progesterone receptors...
April 5, 2017: Chemosphere
https://www.readbyqxmd.com/read/28430630/estrogen-and-androgen-converting-enzymes-17%C3%AE-hydroxysteroid-dehydrogenase-and-their-involvement-in-cancer-with-a-special-focus-on-17%C3%AE-hydroxysteroid-dehydrogenase-type-1-2-and-breast-cancer
#2
REVIEW
Erik Hilborn, Olle Stål, Agneta Jansson
Sex steroid hormones such as estrogens and androgens are involved in the development and differentiation of the breast tissue. The activity and concentration of sex steroids is determined by the availability from the circulation, and on local conversion. This conversion is primarily mediated by aromatase, steroid sulfatase, and 17β-hydroxysteroid dehydrogenases. In postmenopausal women, this is the primary source of estrogens in the breast. Up to 70-80% of all breast cancers express the estrogen receptor-α, responsible for promoting the growth of the tissue...
February 20, 2017: Oncotarget
https://www.readbyqxmd.com/read/28429243/slco1b1-polymorphisms-and-plasma-estrone-conjugates-in-postmenopausal-women-with-er-%C3%A2-breast-cancer-genome-wide-association-studies-of-the-estrone-pathway
#3
Tanda M Dudenkov, James N Ingle, Aman U Buzdar, Mark E Robson, Michiaki Kubo, Irada Ibrahim-Zada, Anthony Batzler, Gregory D Jenkins, Tracy L Pietrzak, Erin E Carlson, Poulami Barman, Matthew P Goetz, Donald W Northfelt, Alvaro Moreno-Aspita, Clark V Williard, Krishna R Kalari, Yusuke Nakamura, Liewei Wang, Richard M Weinshilboum
BACKGROUND: Estrone (E1), the major circulating estrogen in postmenopausal women, promotes estrogen-receptor positive (ER+) breast tumor growth and proliferation. Two major reactions contribute to E1 plasma concentrations, aromatase (CYP19A1) catalyzed E1 synthesis from androstenedione and steroid sulfatase (STS) catalyzed hydrolysis of estrone conjugates (E1Cs). E1Cs have been associated with breast cancer risk and may contribute to tumor progression since STS is expressed in breast cancer where its activity exceeds that of aromatase...
April 20, 2017: Breast Cancer Research and Treatment
https://www.readbyqxmd.com/read/28427772/seasonal-variations-of-aromatase-and-estrogen-receptors-expression-in-the-testis-of-free-ranging-sand-rats
#4
Rafik Menad, Souaâd Smaï, Xavier Bonnet, Thérèse Gernigon-Spychalowicz, Elara Moudilou, Farida Khammar, Jean-Marie Exbrayat
An increasing number of studies revealed the importance of estrogen in male reproduction. However, most research was conducted in laboratory rodents subjected to standardized environmental conditions. Therefore, seasonal regulations of estrogen pathways remain poorly understood under natural conditions. Using immunohistochemistry, the expression of several molecules involved in the functioning of testis (i.e. 17-β estradiol [E2], P450 aromatase, estrogen receptors ESR1, ESR2, and GPER1 [also known as GPR30]) were investigated in free-ranging fat sand rats, Psammomys obesus, during the breeding and resting seasons...
April 17, 2017: Acta Histochemica
https://www.readbyqxmd.com/read/28427518/controversies-in-clinicopathological-characteristics-and-treatment-strategies-of-male-breast-cancer-a-review-of-the-literature
#5
REVIEW
Agnese Losurdo, Selene Rota, Giuseppe Gullo, Giovanna Masci, Rosalba Torrisi, Giulia Bottai, Monica Zuradelli, Wolfgang Gatzemeier, Armando Santoro
Male breast cancer (MaBC) is a rare disease, accounting for less than 1% of malignancies in men. For this reason, literature data on its clinicopathological characteristics are very heterogeneous and treatment strategies have mostly been extrapolated from the female counterpart. However, immunohistochemical peculiarities of MaBC have recently emerged, defining it as a distinct entity from female breast cancer (FBC), thus requiring a tailored clinical approach. MaBC appears to be more often hormone receptor positive than FBC, while data on HER2 status still remain inconclusive, indicating a possible higher incidence of HER2 alterations...
May 2017: Critical Reviews in Oncology/hematology
https://www.readbyqxmd.com/read/28427017/aromatase-inhibitors-and-apoptotic-inducers-design-synthesis-anticancer-activity-and-molecular-modeling-studies-of-novel-phenothiazine-derivatives-carrying-sulfonamide-moiety-as-hybrid-molecules
#6
Mostafa M Ghorab, Mansour S Alsaid, Nermin Samir, Ghada A Abdel-Latif, Aiten M Soliman, Fatma A Ragab, Dalal A Abou El Ella
Hybrid molecules are used as anticancer agents to improve effectiveness and diminish drug resistance. So, the current study aimed to introduce twenty novel phenothiazine sulfonamide hybrids 5-22, 24 and 25 of promising anticancer activity. Compounds 11 and 13 revealed more potent anticancer properties (IC50 8.1 and 8.8 μM) than that of the reference drug (doxorubicin, IC50 = 9.8 μM) against human breast cancer cell line (T47D). To determine the mechanism of their anticancer activity, compounds 5, 6, 7, 11, 13, 14, 16, 17, 19 and 22 that showed promising activity on T47D, were evaluated for their aromatase inhibitory effect...
April 15, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28424084/durable-complete-remission-with-aromatase-inhibitor-therapy-in-a-patient-with-metastatic-uterine-carcinosarcoma-with-poor-performance-status-and-coagulation-disorders-a-case-report
#7
P Martin-Romano, M Jurado, M A Idoate, L Arbea, J L Hernandez-Lizoain, D Cano, J A Paramo, S Martin-Algarra
BACKGROUND: Chemotherapy is considered the most appropriate treatment for metastatic uterine sarcoma, despite its limited efficacy. No other treatment has been conclusively proved to be a real alternative, but some reports suggest that anti-hormonal therapy could be active in a small subset of patients. We report the case of a patient with metastatic uterine carcinosarcoma with positive hormonal receptors and a complete pathological response. CASE PRESENTATION: A 54-year-old white woman presented to our emergency room with hypovolemic shock and serious vaginal bleeding...
April 19, 2017: Journal of Medical Case Reports
https://www.readbyqxmd.com/read/28423398/treatment-restarting-after-discontinuation-of-adjuvant-hormone-therapy-in-breast-cancer-patients
#8
Wei He, Karin E Smedby, Fang Fang, Henrik Olsson, Sara Margolin, Per Hall, Kamila Czene
Background: Over half of breast cancer patients discontinue their adjuvant hormone therapy, permanently or temporarily. We aimed to identify predictors of treatment restarting after discontinuation of adjuvant hormone therapy and to test the hypothesis that treatment restarting is associated with better breast cancer outcomes. Methods: We conducted a population-based cohort study by linking data from the Stockholm-Gotland Breast Cancer Register, the Swedish Prescribed Drug Register, and a self-reported questionnaire...
October 1, 2017: Journal of the National Cancer Institute
https://www.readbyqxmd.com/read/28423275/single-or-multiple-access-channels-to-the-cyp450s-active-site-an-answer-from-free-energy-simulations-of-the-human-aromatase-enzyme
#9
Alessandra Magistrato, Jacopo Sgrignani, Rolf Krause, Andrea Cavalli
Cytochromes P450 (CYP450), in particular CYP19A1 and CYP17A1, are key clinical targets of breast and prostate anticancer therapies, critical players in drug metabolism and their overexpression in tumours is associated with drug resistance. In these enzymes ligands (substrates, drugs) metabolism occurs in deeply buried active sites accessible only via several gruelling channels, whose exact biological role remains unclear. Gaining direct insights on the mechanism by which ligands travel in and out, is becoming increasingly important given that channels are involved in the modulation of binding/dissociation kinetics and the specificity of ligands toward a CYP450...
April 19, 2017: Journal of Physical Chemistry Letters
https://www.readbyqxmd.com/read/28420031/the-ventromedial-hypothalamic-nucleus-in-the-zebra-finch-taeniopygia-guttata-afferent-and-efferent-projections-in-relation-to-the-control-of-reproductive-behaviour
#10
J Martin Wild
Sex-specific mating behaviors occur in a variety of mammals, with the medial preoptic nucleus (POM) and the ventromedial hypothalamic nucleus (VMH) mediating control of male and female sexual behaviour, respectively. In birds, likewise, POM is predominantly involved in the control of male reproductive behaviour, but the degree to which VMH is involved in female reproductive behaviour is unclear. Here, in male and female zebra finches, a combination of aromatase immunohistochemistry and conventional tract tracing facilitated the definition of two separate but adjacent nuclei in the basal hypothalamus: an oblique band of aromatase-positive (AR+) neurons, and ventromedial to this, an ovoid, aromatase-negative (AR-) nucleus...
April 18, 2017: Journal of Comparative Neurology
https://www.readbyqxmd.com/read/28417244/ribociclib-first-global-approval
#11
Yahiya Y Syed
Ribociclib is an oral, small-molecule inhibitor of cyclin-dependent kinase (CDK) 4 and 6 that is under development by Novartis for the treatment of cancer. CDKs play an important role in cell cycle progression and cellular proliferation, and inhibition of these kinases with ribociclib results in G1 phase cell-cycle arrest. Ribociclib, in combination with an aromatase inhibitor, was recently approved in the USA for the first-line treatment of advanced breast cancer and has been submitted for approval in the EU for this indication...
April 17, 2017: Drugs
https://www.readbyqxmd.com/read/28416639/absent-progesterone-receptor-expression-in-the-lymph-node-metastases-of-er-positive-her2-negative-breast-cancer-is-associated-with-relapse-on-tamoxifen
#12
Cameron E Snell, Madeline Gough, Kathryn Middleton, Michael Hsieh, Lauren Furnas, Brenton Seidl, Kristen Gibbons, Christopher Pyke, Catherine Shannon, Natasha Woodward, Jane E Armes
AIMS: Progesterone receptor (PR) expression is prognostic in early stage breast cancer. There are several reports of discordant expression between primary tumour and axillary lymph node (ALN) metastasis expression of oestrogen receptor (ER) and PR. We sought to determine whether expression of these biomarkers in the synchronous ALN metastases of ER positive (+), HER2 negative (-) breast cancer could provide more accurate prognostic information. METHODS: The retrospective cohort included 229 patients from a single institution with ER+, HER2- breast cancer who had synchronous ALN metastatic disease (2005-2014)...
April 17, 2017: Journal of Clinical Pathology
https://www.readbyqxmd.com/read/28414904/in-silico-prediction-of-chemicals-binding-to-aromatase-with-machine-learning-methods
#13
Hanwen Du, Yingchun Cai, Hongbin Yang, Hongxiao Zhang, Yuhan Xue, Guixia Liu, Yun Tang, Weihua Li
Environmental chemicals may affect endocrine systems through multiple mechanisms, one of which is via effects on aromatase (also known as CYP19A1), an enzyme critical for maintaining the normal balance of estrogens and androgens in the body. Therefore, rapid and efficient identification of aromatase-related endocrine disrupting chemicals (EDCs) is important for toxicology and environment risk assessment. In this study, on the basis of the Tox21 10K compound library, in silico classification models for predicting aromatase binders/non-binders were constructed by machine learning methods...
April 17, 2017: Chemical Research in Toxicology
https://www.readbyqxmd.com/read/28414121/neural-derived-estradiol-regulates-brain-plasticity
#14
REVIEW
Iñigo Azcoitia, Maria Angeles Arevalo, Luis M Garcia-Segura
In addition to be an ovarian hormone, estradiol is a neurosteroid synthesized by neural cells. The brain is a steroidogenic tissue that metabolizes testosterone to estradiol. The last step in the synthesis of estradiol is catalyzed by the enzyme aromatase, which is widely expressed in the brain of male and female animals and humans. Studies that have manipulated the expression or the activity of aromatase have revealed that brain-derived estradiol acts as a neuromodulator and regulates different forms of brain plasticity in male and female animals...
April 13, 2017: Journal of Chemical Neuroanatomy
https://www.readbyqxmd.com/read/28413771/management-of-aromatase-inhibitor-associated-bone-loss-aibl-in-postmenopausal-women-with-hormone-sensitive-breast-cancer-joint-position-statement-of-the-iof-cabs-ects-ieg-esceo-ims-and-siog
#15
REVIEW
Peyman Hadji, Matti S Aapro, Jean-Jacques Body, Michael Gnant, Maria Luisa Brandi, Jean Yves Reginster, M Carola Zillikens, Claus-C Glüer, Tobie de Villiers, Rod Baber, G David Roodman, Cyrus Cooper, Bente Langdahl, Santiago Palacios, John Kanis, Nasser Al-Daghri, Xavier Nogues, Erik Fink Eriksen, Andreas Kurth, Rene Rizzoli, Robert E Coleman
BACKGROUND: Several guidelines have been reported for bone-directed treatment in women with early breast cancer (EBC) for averting fractures, particularly during aromatase inhibitor (AI) therapy. Recently, a number of studies on additional fracture related risk factors, new treatment options as well as real world studies demonstrating a much higher fracture rate than suggested by randomized clinical controlled trials (RCTs). Therefore, this updated algorithm was developed to better assess fracture risk and direct treatment as a position statement of several interdisciplinary cancer and bone societies involved in the management of AI-associated bone loss (AIBL)...
June 2017: Journal of Bone Oncology
https://www.readbyqxmd.com/read/28412323/single-cpg-site-methylation-controls-estrogen-receptor-gene-transcription-and-correlates-with-hormone-therapy-resistance
#16
Kouki Tsuboi, Takamasa Nagatomo, Tatsuyuki Gohno, Toru Higuchi, Shunta Sasaki, Natsu Fujiki, Masafumi Kurosumi, Hiroyuki Takei, Yuri Yamaguchi, Toshifumi Niwa, Shin-Ichi Hayashi
Hormone therapy is the most effective treatment for patients with estrogen receptor α-positive breast cancers. However, although resistance occurs during treatment in some cases and often reflects changed estrogen receptor α status, the relationship between changes in estrogen receptor α expression and resistance to therapy are poorly understood. In this study, we identified a mechanism for altered estrogen receptor α expression during disease progression and acquired hormone therapy resistance in aromatase inhibitor-resistant breast cancer cell lines...
April 12, 2017: Journal of Steroid Biochemistry and Molecular Biology
https://www.readbyqxmd.com/read/28411130/ifitm1-suppression-blocks-proliferation-and-invasion-of-aromatase-inhibitor-resistant-breast-cancer-in%C3%A2-vivo-by-jak-stat-mediated-induction-of-p21
#17
Asona J Lui, Eric S Geanes, Joshua Ogony, Fariba Behbod, Jordan Marquess, Kelli Valdez, William Jewell, Ossama Tawfik, Joan Lewis-Wambi
Interferon induced transmembrane protein 1 (IFITM1) belongs to a family of interferon stimulated genes (ISGs) that is associated with tumor progression and DNA damage resistance, however, its role in endocrine resistance is not known. Here, we correlate IFITM1 expression with clinical stage and poor response to endocrine therapy in a tissue microarray consisting of 94 estrogen receptor (ER)-positive breast tumors. IFITM1 overexpression is confirmed in the AI-resistant MCF-7:5C cell line and not found in AI-sensitive MCF-7 cells...
April 12, 2017: Cancer Letters
https://www.readbyqxmd.com/read/28410957/fetal-alpha-5-reductase-val89leu-mutation-is-associated-with-late-miscarriage
#18
Beatriz Pérez-Nevot, Jose-Luis Royo, Miriam Cortés, Ana M Lendínez, Arturo Reyes-Palomares, Ana-José Jiménez, Maximiliano Ruiz-Galdón, Armando Reyes-Engel
The present study was undertaken to determine the role of different polymorphisms affecting the testosterone/oestrogen pathway in miscarriage. Alpha 5-reductase (SRD5A2) rs523349 and rs9282858, cytochrome P450 aromatase (CYP19A1) rs4646, rs10046 and rs2236722 and oestrogen receptor (ESR1) rs9340799, rs2234693 and rs6932902 polymorphisms were selected. The case group consisted of 94 samples of formalin-fixed and paraffin-embedded fetal tissue from a miscarriage at ≤24 weeks. The control group comprised a population of 331 young healthy subjects...
March 21, 2017: Reproductive Biomedicine Online
https://www.readbyqxmd.com/read/28407578/a-peek-into-the-drug-development-scenario-of-endometriosis-a-systematic-review
#19
REVIEW
Luxitaa Goenka, Melvin George, Maitrayee Sen
PURPOSE AND OBJECTIVE: Endometriosis is a gynaecological disease that is characterised by the presence of endometrium like tissue-epithelium and stroma that develops outside the uterine cavity, which is responsible for pelvic pain and infertility. Even though several medical therapies exist for the treatment of endometriosis, each of the drug class has its own limitations such as cost of treatment, side-effects and its short-term effect on the symptoms of endometriosis. In this review, we have attempted to summarize the current status and challenges of drug development for endometriosis...
April 10, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28407500/in-vitro-and-in-vivo-estrogenic-activity-of-bpa-bpf-and-bps-in-zebrafish-specific-assays
#20
Vincent Le Fol, Selim Aït-Aïssa, Manoj Sonavane, Jean-Marc Porcher, Patrick Balaguer, Jean-Pierre Cravedi, Daniel Zalko, François Brion
Bisphenol A (BPA) is a widely used chemical that has been extensively studied as an endocrine-disrupting chemical (EDC). Other bisphenols sharing close structural features with BPA, are increasingly being used as alternatives, increasing the need to assess associated hazards to the endocrine system. In the present study, the estrogenic activity of BPA, bisphenol S (BPS) and bisphenol F (BPF) was assessed by using a combination of zebrafish-specific mechanism-based in vitro and in vivo assays. The three bisphenols were found to efficiently transactivate all zebrafish estrogen receptor (zfER) subtypes in zebrafish hepatic reporter cell lines (ZELH-zfERs)...
April 11, 2017: Ecotoxicology and Environmental Safety
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