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E2758
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Eugen Dhimolea et al.
Cancer cell, 39(2), 240-256 (2021-01-09)
Treatment-persistent residual tumors impede curative cancer therapy. To understand this cancer cell state we generated models of treatment persistence that simulate the residual tumors. We observe that treatment-persistent tumor cells in organoids, xenografts, and cancer patients adopt a distinct and
Fengxia Wu et al.
Aquatic toxicology (Amsterdam, Netherlands), 155, 43-51 (2014-06-30)
We studied the effects of endocrine disrupting compounds nonylphenol (NP) and letrozole (LE) on the male goldfish Carassius aumtus. Exposure to NP (20 μg l(-1)) alone caused a significant up-regulation in the expression of aromatase, estrogen receptors and vitellogenin (VTG)
Arunoday Bhan et al.
Journal of molecular biology, 426(20), 3426-3441 (2014-08-05)
Enhancer of Zeste homolog 2 (EZH2), a methyltransferase specific to histone 3 lysine 27, is a critical player in gene silencing and is overexpressed in breast cancer. Our studies demonstrate that EZH2 is transcriptionally induced by estradiol in cultured breast
Mitochondria impact brain function and cognition.
Martin Picard et al.
Proceedings of the National Academy of Sciences of the United States of America, 111(1), 7-8 (2013-12-25)
David Sedlák et al.
Journal of medicinal chemistry, 53(10), 4290-4294 (2010-04-23)
To identify novel estrogen receptor ligands a series of substituted 17alpha-arylestradiols were synthesized using the catalytic [2 + 2 + 2]cyclotrimerization of 17alpha-ethynylestradiol with various 1,7-diynes in the presence of Wilkinson's catalysts [Rh(PPh(3))(3)Cl]. The compounds were subjected to competitive binding
Phedias Diamandis et al.
Nature chemical biology, 3(5), 268-273 (2007-04-10)
The identification of self-renewing and multipotent neural stem cells (NSCs) in the mammalian brain holds promise for the treatment of neurological diseases and has yielded new insight into brain cancer. However, the complete repertoire of signaling pathways that governs the
Steffen Renner et al.
Nature chemical biology, 5(8), 585-592 (2009-06-30)
The structure- and chemistry-based hierarchical organization of library scaffolds in tree-like arrangements provides a valid, intuitive means to map and navigate chemical space. We demonstrate that scaffold trees built using bioactivity as the key selection criterion for structural simplification during
Mei Yang et al.
Cell reports, 31(12), 107803-107803 (2020-06-25)
The function of enhancer RNAs (eRNAs) in transcriptional regulation remains obscure. By analyzing the genome-wide nascent transcript profiles in breast cancer cells, we identify a special group of eRNAs that are essential for estrogen-induced transcriptional repression. Using eRNAs of TM4SF1
Meimei Liu et al.
General and comparative endocrinology, 280, 115-122 (2019-04-20)
Estradiol is an important sex steroid hormone that involved in regulation of animal lipid metabolism. However, the effect of estradiol on lipid metabolism in swimming crab (Portunus trituberculatus) is unclear. The present study investigated the effect of four concentrations of
R R Wilkening et al.
Bioorganic & medicinal chemistry letters, 16(13), 3489-3494 (2006-04-25)
Synthesis and derivatization of a series of substituted tetrahydrofluorenone analogs giving potent, ERbeta subtype selective ligands are described. Several analogs possessing ERbeta binding affinities comparable to 17beta-estradiol but with greater than 75-fold selectivity over ERalpha are reported.
Molecular mechanism of estrogen-estrogen receptor signaling
Yacsar P, et al.
Reproductive medicine and biology, 16(1), 4-20 (2017)
Maria-Angeles Arevalo et al.
Nature reviews. Neuroscience, 16(1), 17-29 (2014-11-27)
Hormones regulate homeostasis by communicating through the bloodstream to the body's organs, including the brain. As homeostatic regulators of brain function, some hormones exert neuroprotective actions. This is the case for the ovarian hormone 17β-oestradiol, which signals through oestrogen receptors
Hina Mir et al.
Oncotarget, 6(12), 9985-9998 (2015-04-19)
Lung cancer (LuCa) is the leading cause of cancer-related deaths worldwide regardless of the gender. High mortality associated with LuCa is due to metastasis, molecular mechanisms of which are yet to be defined. Here, we present evidence that chemokine receptor
Donna D Yu et al.
Bioorganic & medicinal chemistry letters, 15(5), 1311-1313 (2005-02-17)
In order to develop agonist ligands that are specific for the estrogen-related receptors ERRbeta/gamma, a hydrazone with a 4-hydroxy group at one phenyl ring and a 4-diethylamino moiety at the other phenyl ring was synthesized. We demonstrate that compound 3
Laura Piccardi et al.
Aviation, space, and environmental medicine, 84(10), 1092-1094 (2013-11-23)
Discordant findings have been reported about the change in pregnant women's cognitive test performance. Visuo-spatial abilities, which are crucial in terrestrial/flight navigation, could be influenced by hormonal variations. A 32-yr-old Italian Air Force pilot underwent a 2-D Mental Rotation Task
Alice Meides et al.
International journal of cancer, 135(12), 2749-2759 (2014-03-29)
Matrix metalloproteinases like MMP-13 cleave and remodel the extracellular matrix and thereby play a crucial role in tumor progression in vivo. Using a highly selective inhibitor to block MMP-13 protein activity, we demonstrate a striking inhibitory effect on invasive tumor
Claudia Rivera-Guevara et al.
Bioorganic & medicinal chemistry, 18(15), 5593-5601 (2010-07-14)
Tamoxifen is a selective estrogen receptor modulator widely used in oncology and reproductive endocrinology. In order to decrease its non-desirable effects and elucidate mechanisms of action, permanently charged tamoxifen derivatives (PCTDs) have been reported. Whether PCTDs have genomic effects remains
Naseem Ahmed et al.
Bioorganic & medicinal chemistry letters, 17(11), 3212-3216 (2007-03-24)
Different flavone-, indole-, and furan-17beta-estradiol conjugates, linked via alkyl spacer chains extending from the 17alpha-position of the estradiol moiety, were synthesized by Pd-catalyzed cross-coupling reactions. Structures were assigned based on spectroscopic data. In vitro competitive binding assays for the estrogen
A F De Nicola et al.
Mini reviews in medicinal chemistry, 12(11), 1081-1089 (2012-07-26)
Besides their effects on reproduction, estrogens exert neuroprotective effects for brain diseases. Thus, estrogens ameliorate the negative aspects of aging and age-associated diseases in the nervous system, including hypertension. Within the brain, the hippocampus is sensitive to the effects of
S Lu et al.
Climacteric : the journal of the International Menopause Society, 22(4), 395-402 (2019-02-20)
Objective: This study was designed to investigate associations between menopausal age and the DNA methylation levels of stearoyl-coenzyme A desaturase 1 (SCD1, selected by the Illumina Human Methylation 450 K Bead Chip) and explore the changes in mRNA levels of SCD1
Sara Schubert et al.
Aquatic toxicology (Amsterdam, Netherlands), 157, 141-149 (2014-12-03)
Transient exposure of brown trout embryos from fertilization until hatch (70 days) to 17β-estradiol (E2) was investigated. Embryos were exposed to 3.8 and 38.0 ng/L E2 for 2h, respectively, under four scenarios: (A) exposure once at the day of fertilization
Timothy A Blizzard et al.
Bioorganic & medicinal chemistry letters, 17(10), 2944-2948 (2007-04-24)
A series of bridged androstenediol derivatives was prepared. The bridged compounds exhibited reduced ER-beta selectivity relative to uncyclized analogs.
Li Ma et al.
Cancer letters, 355(1), 96-105 (2014-09-15)
Sorafenib is the approved systemic drug of choice for advanced hepatocellular carcinoma (HCC), but has demonstrated limited benefits because of drug resistance. 2-Methoxyestradiol (2ME2) has been shown to be a promising anticancer drug against various types of cancers and acts
Jiangyuan Liu et al.
European journal of medicinal chemistry, 44(4), 1689-1704 (2008-11-14)
To enhance the potency, reduce the side effects and improve oral property of estradiol in estrogen replacement therapy (ERT), 6 novel estradiol-RGD octapeptide conjugates have been prepared. In an ovariectomized mouse osteoporotic model, at an oral dosage of 110.3 nmol/kg
Cecilia Martin et al.
The Journal of neuroscience : the official journal of the Society for Neuroscience, 34(17), 6047-6056 (2014-04-25)
The adipocyte-derived hormone leptin plays a critical role in the central transmission of energy balance to modulate reproductive function. However, the neurocircuitry underlying this interaction remains elusive, in part due to incomplete knowledge of first-order leptin-responsive neurons. To address this
Jarmila Sulcová et al.
Clinical chemistry and laboratory medicine, 43(2), 221-227 (2005-04-22)
Twenty-one healthy male volunteers aged 20-70 years were given transdermally 25 mg of 7-oxo-dehydroepiandrosterone daily in the form of an emulgel for 8 consecutive days. Morning blood was collected as follows: before application, and after the first, fourth and eighth
N Chabbert-Buffet et al.
La Revue du praticien, 49(12), 1270-1276 (1999-09-17)
The physiology of the hypothalamus-pituitary-gonadal axis includes endocrine interactions between the hypothalamopituitary system and the gonads, as well as paracrine interactions within the various endocrine glands of the reproductive system (pituitary, ovary, testis). The pulsatile secretion of GnRH by the
Jennifer L Robinson et al.
Scientific reports, 8(1), 8527-8527 (2018-06-06)
Temporomandibular joint degenerative disease (TMJ-DD) is a chronic form of TMJ disorder that specifically afflicts people over the age of 40 and targets women at a higher rate than men. Prevalence of TMJ-DD in this population suggests that estrogen loss
M P Mira-Escolano et al.
BJOG : an international journal of obstetrics and gynaecology, 121(11), 1359-1364 (2014-09-25)
Animal models have suggested that anogenital distance (AGD) at birth reflects androgen levels during in utero development and predicts adult AGD. A recent study showed an association between perineal length and androgen levels in men, suggesting that serum testosterone levels
Qiaoying Lv et al.
Cancer letters, 442, 137-147 (2018-11-14)
Continuous estrogen signaling is thought to be the main mechanism causing endometrial cancer (EC). Studies have demonstrated that CD163+ macrophages could promote the development of estrogen-dependent EC, but the mechanisms involved remain unclear. We found that CD163+ macrophages were the
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