Journal ArticleDOI
Valproic acid and its derivatives enhanced estrogenic activity but not androgenic activity in a structure dependent manner.
Sandra Stempin,Susanne Andres,Maja Bumke Scheer,Ariane Rode,Heinz Nau,Albrecht Seidel,Alfonso Lampen +6 more
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TLDR
It is indicated that VPA and its derivatives affect estrogen signaling with a structural specificity, while the (anti-)androgenic effects of these compounds are not structurally correlated.About:
This article is published in Reproductive Toxicology.The article was published on 2013-12-01. It has received 8 citations till now. The article focuses on the topics: Estrogen receptor & Androgen receptor.read more
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Histone deacetylase inhibitors induce proteolysis of activated CDC42-associated kinase-1 in leukemic cells.
TL;DR: HDACs sustain the ACK1-STAT3 signaling node and leukemic cell growth and Dasatinib and HDACi combinations produce beneficial antileukemic effects.
Journal ArticleDOI
Influence of waterborne gallic and pelargonic acid exposures on biochemical and reproductive parameters in the zebrafish (Danio rerio).
TL;DR: Neither significant variation in reproductive performances were detected following zebrafish exposure to gallic or pelargonic acid, and additional investigations concerning the mode of application and the environmental fate of these substances may warrant their further use in freshwater systems at concentrations compatible with biocidal/allelochemical effects.
Journal ArticleDOI
In Silico Computational Transcriptomics Reveals Novel Endocrine Disruptors in Largemouth Bass ( Micropterus salmoides).
Danilo Basili,Jiliang Zhang,Jiliang Zhang,John Herbert,Kevin J. Kroll,Nancy D. Denslow,Christopher J. Martyniuk,Francesco Falciani,Philipp Antczak +8 more
TL;DR: A dynamic model of ovary development linking gene transcription to key physiological end points, such as gonadosomatic index, plasma levels of estradiol and vitellogenin, in largemouth bass is developed, the first study of a dynamic model that links gene expression patterns across stages of ovarian development.
Journal ArticleDOI
Sex-related differences of urethane and sodium valproate effects on Ki-67 expression in urethane-induced lung tumors of mice.
Donatas Stakišaitis,Raminta Mozūraitė,Dovilė Kavaliauskaitė,Lina Šlekienė,Ingrida Balnytė,Nomeda Juodžiukynienė,Angelija Valančiūtė +6 more
TL;DR: Gonadectomy with NaVP treatment decreased Ki-67(+) in adenocarcinomas for mice of both sexes, and a sex-related effect of NaVP on progression in urethane-induced BALB/c mice lung tumors is indicated.
Journal ArticleDOI
The use of 3D cultures of MCF-10A and MCF-12A cells by high content screening for effect-based analysis of non-genotoxic carcinogens
TL;DR: The parallel use of both cell lines allows the identification of estrogenic properties of a given test compound, and the strong estrogen 17β-estradiol had no effect on acinus formation of estrogen receptor (ER)-negative MCF-10A cells, but yielded largerMCF-12A (ER-positive) acini.
References
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Journal ArticleDOI
Comparison of the ligand binding specificity and transcript tissue distribution of estrogen receptors alpha and beta
George G.J.M. Kuiper,Bo Carlsson,Kaj Grandien,Eva Enmark,Johan Häggblad,Stefan K. Nilsson,Jan-Åke Gustafsson +6 more
TL;DR: The messenger RNA expression of both ER subtypes in rat tissues by RT-PCR is investigated and the ligand binding specificity of the ER sub types is compared, revealing a single binding component for 16β-estradiol with high affinity.
Journal ArticleDOI
Interaction of estrogenic chemicals and phytoestrogens with estrogen receptor beta.
George G. J. M. Kuiper,J.G. Lemmen,Bo Carlsson,J. Christopher Corton,Stephen Safe,Paul T. van der Saag,Bart van der Burg,Jan-Åke Gustafsson +7 more
TL;DR: The estrogenic activity of environmental chemicals and phytoestrogens in competition binding assays with ERα or ERβ protein, and in a transient gene expression assay using cells in which an acute estrogenic response is created by cotransfecting cultures with recombinant human ERβ complementary DNA (cDNA) in the presence of an estrogen-dependent reporter plasmid are investigated.
Journal ArticleDOI
Firefly luciferase gene: structure and expression in mammalian cells.
TL;DR: Assaying the expression of luciferase provides a rapid and inexpensive method for monitoring promoter activity and is estimated to be from 30- to 1,000-fold more sensitive than assaying chloramphenicol acetyltransferase expression.
PatentDOI
DIFFERENTIAL LIGAND ACTIVATION OF ESTROGEN RECEPTORS ER$g(a) AND ER$g(b) AT AP1 SITES
Peter J. Kushner,Jan-Ake Gustafsson,George G.J.M. Kuiper,Stefan K. Nilsson,Kolja Paech,Thomas S. Scanlan,Paul W. Webb +6 more
TL;DR: In this article, a cell comprising an estrogen receptor beta (ER beta ), AP1 proteins, and a construct comprising a promoter comprising an AP1 site which regulates expression of a first reporter gene is contacted with the test compound and changes in expression levels of the reporter gene are detected indicating whether the test compounds activate transcription, inactivate transcription or have no effect at the AP1 sites.
Journal ArticleDOI
Estrogen receptor null mice: what have we learned and where will they lead us?
John F. Couse,Kenneth S. Korach +1 more
TL;DR: The recent successful generation of double knockout, or alpha beta ERKO mice of both sexes, suggests that this receptor is also not essential to survival and was most likely not a compensatory factor in the survival of the alpha ERKO.