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关键词:'E2758'
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Sean Ekins et al.
Drug metabolism and disposition: the biological fate of chemicals, 38(12), 2302-2308 (2010-09-17)
Drug-induced liver injury (DILI) is one of the most important reasons for drug development failure at both preapproval and postapproval stages. There has been increased interest in developing predictive in vivo, in vitro, and in silico models to identify compounds
Prudencio T Agbohessi et al.
The Science of the total environment, 506-507, 567-584 (2014-12-01)
To determine the impact of agricultural pesticides used in cotton cultivation on the health status of fish living in a Beninese cotton basin, we compared the reproductive and hepatic systems of fish sampled from rivers located in both contaminated and
Prabin Dhangada Majhi et al.
Environmental health perspectives, 128(1), 17002-17002 (2020-01-16)
Endocrine-disrupting chemicals have been shown to have broad effects on development, but their mutagenic actions that can lead to cancer have been less clearly demonstrated. Physiological levels of estrogen have been shown to stimulate DNA damage in breast epithelial cells
Min Chen et al.
Gene, 543(2), 212-219 (2014-04-15)
PLIN1, a lipid droplet associated protein, has been implicated in playing a key role in the regulation of lipolysis and lipid storage in adipocytes. PLIN1 is found to be highly expressed in Leydig cells of testis, suggesting a potential role
Silvia Tapia-Gonzalez et al.
The Journal of endocrinology, 198(1), 219-230 (2008-05-08)
It has been previously reported that the neuroprotective hormone oestradiol reduces microglia inflammatory activity. The objective of this study was to test whether two selective oestrogen receptor modulators, tamoxifen and raloxifene, modulate in vivo the activation of microglia induced by
Cynthia D Selassie et al.
Journal of medicinal chemistry, 48(23), 7234-7242 (2005-11-11)
In this comprehensive study on the caspase-mediated apoptosis-inducing effect of 51 substituted phenols in a murine leukemia cell line (L1210), we determined the concentrations needed to induce caspase activity by 50% (I50) and utilized these data to develop the following
Meiqin Wu et al.
Zoological science, 31(4), 202-212 (2014-04-04)
The gene, vitellogenin (vtg) was cloned and characterized in the dojo loach (Misgurnus anguillicaudatus), an indigenous freshwater species in East Asia, in order to develop tools for detecting the effects of estrogenic endocrine-disrupting chemicals (EEDCs). Full-length cDNAs encoding seven distinct
Sophie Christin-Maitre et al.
Women's health (London, England), 9(1), 13-23 (2012-12-18)
Most combined oral contraceptive pills contain ethinyl estradiol (EE) with progestins. In order to minimize the pill's cardiovascular risks, the concept of using 17β-estradiol (E2), the endogenous estradiol, arose in the 1970s. Many attempts to develop a pill containing 17β-E2
Denis Habauzit et al.
Archives of biochemistry and biophysics, 541, 61-66 (2013-11-28)
The estrogen receptor (ER) is a transcription factor that binds under 17-β-estradiol (E2) stimulation as homodimer to a short DNA consensus sequence named estrogen response element (ERE). The ER/ERE interaction has been assessed by several research groups through different methodologies
Qiang Tan et al.
Bioorganic & medicinal chemistry letters, 15(6), 1675-1681 (2005-03-05)
The discovery, synthesis, and SAR of chromanes as ER alpha subtype selective ligands are described. X-ray studies revealed that the origin of the ER alpha-selectivity resulted from a C-4 trans methyl substitution to the cis-2,3-diphenyl-chromane platform. Selected compounds from this
Bruce Petrie et al.
Chemosphere, 113, 101-108 (2014-07-30)
The impact of solids retention time (SRT) on estrone (E1), 17β-estradiol (E2), estriol (E3) and 17α-ethinylestradiol (EE2) removal in an activated sludge plant (ASP) was examined using a pilot plant to closely control operation. Exsitu analytical methods were simultaneously used
Ni-Hao Gu et al.
Frontiers in cell and developmental biology, 9, 710407-710407 (2021-08-17)
Adenomyosis (AM) is a disease in which endometrial tissue invades the myometrium and has a 10-60% prevalence in reproductive-aged women. TSC2 regulates autophagy via mTOR1 signalling in colorectal cancer and endometrial carcinoma. Dysregulation of autophagy is implicated in adenomyosis pathogenesis.
V Carnevale et al.
Journal of endocrinological investigation, 28(2), 102-105 (2005-05-13)
Sex steroid hormones contribute to the physiological regulation of bone turnover in males. To address this issue, we investigated serum estradiol (E2), total testosterone (T), and DHEAS concentrations, along with serum levels of carboxy-terminal telopeptide of type I collagen (sCTx)
Fucui Ma et al.
Toxicology and applied pharmacology, 282(1), 68-76 (2014-12-03)
Both genetic and environmental factors contribute to neurodegenerative disorders. In a large number of neurodegenerative diseases (for example, Alzheimer's disease (AD)), patients do not carry the mutant genes. Other risk factors, for example the environmental factors, should be evaluated. 17β-trenbolone
Jian Liu et al.
Bioorganic & medicinal chemistry letters, 15(3), 715-718 (2005-01-25)
The ring oxygen and sulfur analogs of lasofoxifene, 1a and 1b, were synthesized in an attempt to impart ERalpha selectivity, as found in the closely related dihydrobenzoxathiin compound I, recently discovered in these laboratories. The resulting isochroman and isothiochroman compounds
Sze Wan Hung et al.
Frontiers in pharmacology, 12, 714790-714790 (2021-11-02)
Endometriosis is defined as endometrial tissues found outside the uterine cavity. ProEGCG is a prodrug of Epigallocatechin gallate (EGCG), a potent polyphenol found in green tea. It inhibits the development of endometriotic lesions of mouse model in vivo, with higher
Iu O Fedotova et al.
Eksperimental'naia i klinicheskaia farmakologiia, 76(5), 3-6 (2013-08-02)
The aim of this work was to study the effect of stimulation or blockade of Na7-cholinoreceptors with a low dose of 17beta-estradiol on the passive avoidance performance and behavior in the open-field test in adult ovariectomized (OVX) female rats. Agonist
Bharath Saravanan et al.
PLoS genetics, 16(1), e1008516-e1008516 (2020-01-07)
Unliganded Estrogen receptor alpha (ERα) has been implicated in ligand-dependent gene regulation. Upon ligand exposure, ERα binds to several EREs relatively proximal to the pre-marked, unliganded ERα-bound sites and affects transient but robust gene expression. However, the underlying mechanisms are
Hui-Chun Irene Su et al.
Cancer, 120(23), 3691-3698 (2014-08-02)
Endocrine measures of ovarian reserve before breast cancer treatment may predict postchemotherapy ovarian function, providing prognostic information at the time of cancer diagnosis. The objectives of this study were 1) to determine whether prechemotherapy levels of antimullerian hormone (AMH), follicle-stimulating
Jing Wu et al.
Toxicology letters, 232(3), 573-579 (2014-12-30)
T-2 toxin is a secondary metabolite produced by Fusarium genus and is a common contaminant in food and feedstuffs of cereal origin. In porcine granulosa cells(GC), T-2 toxin has been shown to inhibit the steroidogenesis; however, the mechanism has not
T Agrawal et al.
British journal of biomedical science, 70(2), 51-57 (2013-07-31)
Genital Chlamydia trachomatis infection creates a substantial reproductive health burden in women. The high incidence of asymptomatic infection often precludes timely antibiotic therapy to control the sequelae of infection, and therefore a vaccine is required. Dendritic cells (DC) are now
Francisco J Prado-Prado et al.
Bioorganic & medicinal chemistry, 18(6), 2225-2231 (2010-02-27)
There are many of pathogen parasite species with different susceptibility profile to antiparasitic drugs. Unfortunately, almost QSAR models predict the biological activity of drugs against only one parasite species. Consequently, predicting the probability with which a drug is active against
Estrogen synthesis and signaling pathways during aging: from periphery to brain
Cui J, et al.
Trends in Molecular Medicine, 19(3), 197-209 (2013)
Paola Gilli et al.
Journal of medicinal chemistry, 48(6), 2026-2035 (2005-03-18)
Drug-receptor binding thermodynamics has proved to be a valid tool for pharmacological and pharmaceutical characterization of molecular mechanisms of receptor-recognition phenomena. The large number of membrane receptors so far studied has led to the discovery of enthalpy-entropy compensation effects in
Jen-Liang Su et al.
The Journal of biological chemistry, 282(27), 19385-19398 (2007-05-22)
Osteoporosis is a major public health problem and the most obvious preventive strategy, hormone replacement therapy, has lost favor due to recent findings of the Women's Health Initiative regarding increased risks of breast cancer and cardiovascular disease. Resveratrol, a naturally
D Celestino Catão Da Silva et al.
Minerva ginecologica, 65(3), 297-302 (2013-05-22)
The aim of this paper was to compare the carotid intima-media thickness (IMT) in pre- and postmenopausal women and to evaluate the association between endogenous sex hormones, body fat distribution, and insulin resistance and the IMT. This cross-sectional study included
Namram Sushindrajit Singh et al.
Indian journal of experimental biology, 52(5), 496-503 (2014-05-24)
Resonance experiment was employed to investigate the mechanism of photoperiodic time measurement during initiation of ovarian growth and functions in the subtropical population of female tree sparrow (Passer montanus) at Shillong (Latitude 25 degrees 34 'N, Longitude 91 degrees 53
Harpreet Bhatia et al.
Ecotoxicology and environmental safety, 109, 143-151 (2014-09-07)
The aim of the present study was to evaluate the responses of female Murray rainbowfish (Melanotaenia fluviatilis) to the model anti-androgen, flutamide in a short-term exposure. Adult female Murray rainbowfish were exposed to nominal (measured) concentrations of 125 (104), 250
Lina Liu et al.
Evidence-based complementary and alternative medicine : eCAM, 2020, 4156145-4156145 (2020-07-14)
Xiao-Yao-San (XYS) decoction is a traditional Chinese medicine formula. This study aimed to investigate the effect of XYS on cognitive abilities and its underlying mechanism in ovariectomized rats. Female Sprague-Dawley rats were ovariectomized and treated with XYS (3 g/kg or 9 g/kg)
Inna V Ilina et al.
Journal of assisted reproduction and genetics, 38(2), 517-529 (2020-11-19)
To study whether the application of femtosecond laser pulses for zona pellucida (ZP) drilling of blastocysts at the embryonic or abembryonic poles can promote hatching to start immediately through the hole formed and ensure high hatching rates and embryo viability.
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