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Conjugated oestrogen

Amanda Tivnan, Tatjana Heilinger, Joanne Ramsey, Gemma O'Connor, Jenny Pokorny, Jann Sarkaria, Brett Stringer, Bryan Day, Andrew Boyd, Ella Kim, Holger Lode, Sally-Ann Cryan, Jochen Prehn
Aromatase is a critical enzyme in the irreversible conversion of androgens to oestrogens, with inhibition used clinically in hormone-dependent malignancies. We tested the hypothesis that targeted aromatase inhibition in an aggressive brain cancer called glioblastoma (GBM) may represent a new treatment strategy. In this study, aromatase inhibition was achieved using third generation inhibitor, Letrozole, encapsulated within the core of biodegradable poly lactic-co-glycolic acid (PLGA) nanoparticles (NPs). PLGA-NPs were conjugated to human/mouse chimeric anti-GD2 antibody ch14...
February 3, 2017: Oncotarget
Natalia Sutiman, Joanne Siok Liu Lim, Thomas E Muerdter, Onkar Singh, Yin Bun Cheung, Raymond Chee Hui Ng, Yoon Sim Yap, Nan Soon Wong, Peter Cher Siang Ang, Rebecca Dent, Werner Schroth, Matthias Schwab, Chiea Chuen Khor, Balram Chowbay
Tamoxifen (TAM) is an established endocrine treatment for all stages of oestrogen receptor (ER)-positive breast cancer. Its complex metabolism leads to the formation of multiple active and inactive metabolites. One of the main detoxification and elimination pathways of tamoxifen and its active metabolites, 4-hydroxytamoxifen (4-OHT) and endoxifen, is via glucuronidation catalysed by uridine 5'-diphospho-glucuronosyltransferases (UGTs). However, few studies have comprehensively examined the impact of variations in the genes encoding the major hepatic UGTs on the disposition of tamoxifen and its metabolites...
October 2016: Clinical Pharmacokinetics
Antonella Borrelli, Antonietta Schiattarella, Roberto Mancini, Alessandra Pica, Maria Laura Pollio, Maria Grazia Ruggiero, Patrizia Bonelli, Viviana De Luca, Franca Maria Tuccillo, Clemente Capasso, Enrico Gori, Marina Sanseverino, Andrea Carpentieri, Leila Birolo, Piero Pucci, Jean Rommelaere, Aldo Mancini
A 24-amino acid leader peptide of a new human recombinant manganese superoxide dismutase can enter cells and carry molecules. Here, we demonstrated that six of the 24 amino acids penetrate cells through a particular gate represented by a specific amino acid sequence of the oestrogen receptor (ER). We analysed the internalization of the synthetic hexapeptide and the cytotoxic activity of the hexapeptide conjugated to cisplatin on a cell line panel. In most cell lines, the hexapeptide delivered an amount of cisplatin that was 2 to 8 times greater than that released by cisplatin when the drug was used alone...
January 4, 2016: Scientific Reports
S A Mitchell, A Paine, M Moffatt, T A Neale, M E Orme, C Hawes
No abstract text is available yet for this article.
November 2015: Value in Health: the Journal of the International Society for Pharmacoeconomics and Outcomes Research
Xiaojuan Chai, Yan Guo, Mengxi Jiang, Bingfang Hu, Zhigang Li, Jie Fan, Meihong Deng, Timothy R Billiar, Heidi R Kucera, Nilesh W Gaikwad, Meishu Xu, Peipei Lu, Jiong Yan, Haiyan Fu, Youhua Liu, Lushan Yu, Min Huang, Su Zeng, Wen Xie
Sepsis is the host's deleterious systemic inflammatory response to microbial infections. Here we report an essential role for the oestrogen sulfotransferase (EST or SULT1E1), a conjugating enzyme that sulfonates and deactivates estrogens, in sepsis response. Both the caecal ligation and puncture (CLP) and lipopolysaccharide models of sepsis induce the expression of EST and compromise the activity of oestrogen, an anti-inflammatory hormone. Surprisingly, EST ablation sensitizes mice to sepsis-induced death. Mechanistically, EST ablation attenuates sepsis-induced inflammatory responses due to compromised oestrogen deactivation, leading to increased sepsis lethality...
August 10, 2015: Nature Communications
Ting Qu, Shi-Mao Zhang, Lin-Lin Yu, Sheng Zhang, Dong-Zhi Yuan, Qian Xu, Jin-Hu Zhang, Ya-Ping He, Li-Min Yue
Integrins are the dominant and final adhesion molecules in the attachment process between the blastocysts and endometrium. It is necessary for oestrogen to rapidly activate mouse blastocysts so that they attach to the endometrial epithelium. Our previous study suggested that oestrogen can rapidly induce an increase in intracellular calcium in mouse blastocysts via G-protein-coupled receptor 30 (GPR30). Thus, we deduced that integrins may be involved in GPR30 mediation of the fast effect of oestrogen on mouse blastocysts in implantation...
May 8, 2015: Reproduction, Fertility, and Development
M Ghazanfarpour, R Latifnejad Roudsari, G Treglia, R Sadeghi
Current systematic review evaluated the efficacy of topical isoflavones to relieve vaginal symptoms in menopausal women. MEDLINE (1966 to January 2014), Scopus (1990 to January 2014), and the Cochrane Central Register of Controlled Trials (The Cochrane Library issue 1, 2013) were searched using keywords 'isoflavone and vagina'. Relevant studies were reviewed by two independent reviewers. Only randomised controlled trials (RCTs) were included in the systematic review. Out of 115 potentially relevant publications, four studies met the inclusion criteria...
2015: Journal of Obstetrics and Gynaecology: the Journal of the Institute of Obstetrics and Gynaecology
Robert W Schwenk, Christian Baumeier, Brian Finan, Oliver Kluth, Christine Brauer, Hans-Georg Joost, Richard D DiMarchi, Matthias H Tschöp, Annette Schürmann
AIMS/HYPOTHESIS: Oestrogens have previously been shown to exert beta cell protective, glucose-lowering effects in mouse models. Therefore, the recent development of a glucagon-like peptide-1 (GLP-1)-oestrogen conjugate, which targets oestrogen into cells expressing GLP-1 receptors, offers an opportunity for a cell-specific and enhanced beta cell protection by oestrogen. The purpose of this study was to compare the effects of GLP-1 and GLP-1-oestrogen during beta cell failure under glucolipotoxic conditions...
March 2015: Diabetologia
Young-Hoon Ko, Sook-Haeng Joe, Woong Cho, Jeong-Hyun Park, Jung-Jae Lee, In-Kwa Jung, Leen Kim, Seung-Hyun Kim
Objective. The purpose of this investigation was to assess the cognitive effects of adjuvant hormone replacement therapy (HRT) when used to treat premenopausal women with chronic schizophrenia using an 8-week, double-blind, placebo-controlled, randomized trial. Method. Women of childbearing age with chronic schizophrenia were recruited and randomized into placebo and HRT groups, the latter of which was administered 0.625 mg of conjugated oestrogen with 2.5 mg of medroxyprogesterone acetate daily. Each group contained 14 subjects...
2006: International Journal of Psychiatry in Clinical Practice
R Cao, J Chen, X Zhang, Y Zhai, X Qing, W Xing, L Zhang, Y S Malik, H Yu, X Zhu
BACKGROUND: Myosin X (MYO10) was recently reported to promote tumour invasion by transporting integrins to filopodial tips in breast cancer. However, the role of MYO10 in tumours remains poorly defined. Here, we report that MYO10 is required in invadopodia to mediate invasive growth and extracellular matrix degradation, which depends on the binding of MYO10's pleckstrin homology domain to PtdIns(3,4,5)P3. METHODS: The expression of MYO10 and its associations with clinicopathological and biological factors were examined in breast cancer cells and breast cancer specimens (n=120)...
July 29, 2014: British Journal of Cancer
Jiajia Wang, Yongfeng Wang, Ting Wang, Kai Cui, Lianhong Wang, Rong Ji
Steroid oestrogens are typical endocrine-disrupting compounds in the environment and are excreted from the human and animals mainly as conjugates, including sulfate and glucuronide salts. The oestrogen conjugates are largely biologically inactive, but they can be de-conjugated and release free oestrogens, which usually exhibit strong oestrogenicity. Therefore, it is important to study the fate of oestrogen conjugates in the environment. However, because of the complexity of environmental matrixes, time-consuming pre-treatments of samples are usually required to reduce the interference of the matrixes...
June 15, 2014: Journal of Labelled Compounds & Radiopharmaceuticals
Shai Libson, Marc Lippman
Breast cancer is the most frequently diagnosed cancer in women and ranks second among causes for cancer related death in women. The ability to identify and diagnose breast cancer has improved markedly. Treatment decisions which were based in the past predominantly on the anatomic extent of the disease are shifting to the underlying biological mechanisms. Gene array technology has led to the recognition that breast cancer is a heterogeneous disease composed of different biological subtypes, and genetic profiling enables response to chemotherapy to be predicted...
February 2014: International Review of Psychiatry
Monica Mazzarino, Mariangela Biava, Xavier de la Torre, Ilaria Fiacco, Francesco Botrè
The use of selective oestrogen receptor modulators has been prohibited since 2005 by the World Anti-Doping Agency regulations. As they are extensively cleared by hepatic and intestinal metabolism via oxidative and conjugating enzymes, a complete investigation of their biotransformation pathways and kinetics of excretion is essential for the anti-doping laboratories to select the right marker(s) of misuse. This work was designed to characterize the chemical reactions and the metabolizing enzymes involved in the metabolic routes of clomiphene, tamoxifen and toremifene...
June 2013: Analytical and Bioanalytical Chemistry
Matthias Barton
PURPOSE OF REVIEW: Oestrogens are important modulators of lipid metabolism, inflammation and vascular homeostasis. Endogenous oestrogens contribute to the low prevalence of atherosclerotic vascular disease in premenopausal women with intact ovarian function, and cessation of oestrogen production following menopause increases cardiovascular risk. Orally administered oestrogens such as postmenopausal hormone therapy increase HDL and reduce LDL cholesterol levels, and they increase triglyceride levels...
June 2013: Current Opinion in Lipidology
June D Cody, Madeleine Louisa Jacobs, Karen Richardson, Birgit Moehrer, Andrew Hextall
BACKGROUND: It is possible that oestrogen deficiency may be an aetiological factor in the development of urinary incontinence in women. This is an update of a Cochrane review first published in 2003 and subsequently updated in 2009. OBJECTIVES: To assess the effects of local and systemic oestrogens used for the treatment of urinary incontinence. SEARCH METHODS: We searched the Cochrane Incontinence Group Specialised Register of trials (searched 21 June 2012) which includes searches of MEDLINE, the Cochrane Central Register of Controlled Trials (CENTRAL) and handsearching of journals and conference proceedings, and the reference lists of relevant articles...
2012: Cochrane Database of Systematic Reviews
Mark Tarleton, Jayne Gilbert, Jennette A Sakoff, Adam McCluskey
We previously reported the discovery of a simple conjugated cyano pharmacophore which had led to the development of (Z)-2-(3,4-dichlorophenyl)-3-(4-nitrophenyl)acrylonitrile, as a selective inhibitor of oestrogen receptor positive (ER+ve) human breast cancer cell line, MCF-7. Further exploration though modification of the acrylonitrile and aromatic substituents has highlighted key structural components necessary for broad spectrum cytotoxicity. The acrylic acid derivates (Z)-2-(3,4-dichlorophenyl)-3-(4-nitrophenyl)acrylic acid and (Z)-2-(3,4-dichlorophenyl)-3-(4-methoxyphenyl)acrylic acid (9) were inactive; confirming the importance of the cyanide moiety...
November 2012: European Journal of Medicinal Chemistry
James I Raeside, Heather L Christie, Rudolf O Waelchli, Keith J Betteridge
The embryo proper in early equine pregnancy has recently been shown to have a remarkable capacity for metabolism of oestrogens. High concentrations of oestrogens in yolk-sac fluid could provide substrate for local metabolism in tissues of the embryo proper and this activity could have significance for early development. Due to the high level of oestrogen metabolism in the embryo proper we examined the possibility that it could also biosynthesise oestrogens. Conceptuses were collected in the fourth week of pregnancy (n=23) and the embryo was separated from extraembryonic tissues for incubation with [(3)H]androstenedione...
2012: Reproduction, Fertility, and Development
Richard M England, Esther Masiá, Vanessa Giménez, Rut Lucas, María J Vicent
We report here the first examples of Polymer Therapeutics synthesised with the intention of inhibiting Hypoxia Inducible Factor-1 (HIF-1), a transcription factor heavily involved in numerous cell processes under a low oxygen environment. Four compounds were selected for use in these systems; Diethylstilbestrol (DES), Bisphenol A (BIS), Dienestrol (DIENES) and Hexestrol (HEX), which were chosen from a large family of similar molecules known as Stilbenes. These are non-steroidal molecules with structural similarities to oestrogen, and of which DES and BIS have previously been reported for HIF-1 inhibition...
December 28, 2012: Journal of Controlled Release: Official Journal of the Controlled Release Society
Ketan Gajjar, Pierre L Martin-Hirsch, Francis L Martin
Cancers in hormone-responsive tissues (e.g., breast, ovary, endometrium, prostate) occur at high incidence rates worldwide. However, their genetic basis remains poorly understood. Studies to date suggest that endogenous/exogenous oestrogen and environmental carcinogens may play a role in development and/or progression of hormone-induced cancers via oxidative oestrogen metabolism. Cytochrome P450 1B1 is a key enzyme in its oestrogen metabolism pathway, giving rise to hydroxylation and conjugation. Although CYP1B1 is expressed in many cancers, particularly high levels of expression are observed in oestrogen-mediated disease...
November 1, 2012: Cancer Letters
Marina Badia-Fabregat, Carlos E Rodríguez-Rodríguez, Pablo Gago-Ferrero, Alba Olivares, Benjamí Piña, M Silvia Díaz-Cruz, Teresa Vicent, Damià Barceló, Glòria Caminal
Ultraviolet (UV) filters are xenobiotic compounds that can enter the environment through the liquid effluent of wastewater treatment plants (WWTPs) and through adsorption in the sludge by-product because of their high hydrophobicity, as the sludge is subsequently applied as a fertiliser. A solid-state treatment of WWTP sludge with the white-rot fungus Trametes versicolor is reported in the present work as a feasible method for UV filter degradation, with reductions ranging from 87% in the case of 3-(4'-methylbenzylidene) camphor (4-MBC) to 100% for benzophenone-3 (BP3) and its metabolite 4,4'-dihydroxybenzophenone (4DHB)...
August 15, 2012: Journal of Environmental Management
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