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E2758

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Takamitsu Onitsuka et al.
Anticancer research, 31(3), 855-860 (2011-04-19)
Positive expression of estrogen receptor (ER) beta is correlated with a favorable prognosis for patients with epidermal growth factor receptor (EGFR) mutations and predicts a good clinical outcome for patients with lung cancer after treatment with an EGFR-tyrosine kinase inhibitor
Shoudong Guo et al.
Biochimica et biophysica acta, 1841(6), 836-846 (2014-03-08)
Both sphingosine 1-phosphate (S1P) and estrogen have been documented to play endothelial protective roles. However, it remains unclear whether estrogen could regulate the anabolism of the bioactive molecule S1P and the underlying mechanisms. In this study, 108 healthy participants were
Qi Li et al.
Reproduction (Cambridge, England), 160(4), 511-519 (2020-07-23)
Endometriosis (EMs) is an estrogen (E2)-dependent inflammatory disorder. Although EMs is considered a benign disease, it presents with malignant characteristics, such as migration and invasion. An increasing number of studies have shown that aberrantly expressed circular RNAs (circRNAs) play an
New insights into metabolic regulation via bifurcated function of estrogen receptor α.
Tsutomu Wada et al.
Diabetes, 62(12), 3996-3998 (2013-11-23)
Sandra Haider et al.
Endocrinology, 160(10), 2282-2297 (2019-07-11)
The human endometrium is the inner lining of the uterus consisting of stromal and epithelial (secretory and ciliated) cells. It undergoes a hormonally regulated monthly cycle of growth, differentiation, and desquamation. However, how these cyclic changes control the balance between
Abbie S Ireland et al.
Cancer cell, 38(1), 60-78 (2020-06-01)
Small cell lung cancer (SCLC) is a neuroendocrine tumor treated clinically as a single disease with poor outcomes. Distinct SCLC molecular subtypes have been defined based on expression of ASCL1, NEUROD1, POU2F3, or YAP1. Here, we use mouse and human
Martin J Kelly et al.
Frontiers in neuroendocrinology, 33(4), 376-387 (2012-08-09)
It is well known that many of the actions of estrogens in the central nervous system are mediated via intracellular receptor/transcription factors that interact with steroid response elements on target genes. However, there now exists compelling evidence for membrane estrogen
Susan H Corbett et al.
Southern medical journal, 107(7), 433-436 (2014-07-11)
To identify trends in compounding pharmacies with a focus on women's health and, more specifically, the types and combinations of medications used in the treatment of vulvodynia. This survey study was conducted with 653 nonchain pharmacies that compound medications. Each
Lourdes Santana et al.
Journal of medicinal chemistry, 51(21), 6740-6751 (2008-10-07)
The work provides a new model for the prediction of the MAO-A and -B inhibitor activity by the use of combined complex networks and QSAR methodologies. On the basis of the obtained model, we prepared and assayed 33 coumarin derivatives
Simone Bertini et al.
European journal of medicinal chemistry, 46(6), 2453-2462 (2011-04-13)
In a continuing effort to improve the subtype selectivity and agonist potency of estrogen receptor β (ERβ) ligands, we have designed and developed a thus far unexplored structural series obtained by molecular refinements of monoaryl-substituted salicylaldoximes (Salaldox B). The most
K Murakami et al.
Maturitas, 33(1), 71-80 (1999-12-10)
Age-related changes of steroid levels in the central nervous system (CNS) are not well understood. To investigate whether steroidal conditions in the CNS of women change with aging and menopause, steroid levels have been measured in serum and cerebrospinal fluid
Joel S Finkelstein et al.
The New England journal of medicine, 369(11), 1011-1022 (2013-09-13)
Current approaches to diagnosing testosterone deficiency do not consider the physiological consequences of various testosterone levels or whether deficiencies of testosterone, estradiol, or both account for clinical manifestations. We provided 198 healthy men 20 to 50 years of age with
Heather M Moore et al.
Molecular cancer therapeutics, 19(1), 292-303 (2019-09-20)
The PI3K signaling pathway serves as a central node in regulating cell survival, proliferation, and metabolism. PIK3CA, the gene encoding the PI3K catalytic subunit p110-alpha, is commonly altered in breast cancer resulting in the constitutive activation of the PI3K pathway.
Nicholas B Struntz et al.
Cell chemical biology, 26(5), 711-723 (2019-03-19)
The transcription factor Max is a basic-helix-loop-helix leucine zipper (bHLHLZ) protein that forms homodimers or interacts with other bHLHLZ proteins, including Myc and Mxd proteins. Among this dynamic network of interactions, the Myc/Max heterodimer has crucial roles in regulating normal
Ayelet Ziv-Gal et al.
Reproductive toxicology (Elmsford, N.Y.), 100, 7-16 (2020-12-29)
The mammalian oviduct is a central organ for female reproduction as it is the site of fertilization and it actively transports the embryo to the uterus. The oviduct is responsive to ovarian steroids and thus, it is a potential target
Gonadal steroids and body composition, strength, and sexual function in men.
Vita Birzniece
The New England journal of medicine, 369(25), 2455-2455 (2013-12-20)
Andrew L LaFrate et al.
Bioorganic & medicinal chemistry, 17(10), 3528-3535 (2009-04-28)
Steroidal bivalent ligands for the estrogen receptor (ER) were designed using crystal structures of ERalpha dimers as a template. The syntheses of several 17alpha-ethynylestradiol-based bivalent ligands with varying linker compositions and lengths are described. The binding affinities of these bivalent
Aldehyde oxidase: an enzyme of emerging importance in drug discovery.
David C Pryde et al.
Journal of medicinal chemistry, 53(24), 8441-8460 (2010-09-22)
Dulce Mesa-Siverio et al.
Bioorganic & medicinal chemistry, 16(6), 3387-3394 (2008-02-05)
Five new dibenzylbutane type lignans (1-5) were isolated from the stem bark of Iryanthera lancifolia. Their structures were determined by extensive 1D and 2D NMR spectroscopic studies and chemical evidence. Seventeen of the isolated compounds were tested for their estrogenic
Fortune Kohen et al.
Journal of medicinal chemistry, 50(25), 6405-6410 (2007-11-10)
The isoflavones biochanin A ( 1a), genistein ( 1b), and daidzein ( 4) at concentrations >20 microM inhibit cell growth of various cancer cell lines. To enhance the antiproliferative activities of these compounds, we synthesized three analogs, 2-[3-carboxy-(6-tert-butoxycarbonylamino)-hexylamino-propyl]-7,5-dihydroxy-4'-methoxyisoflavone ( 3a)
Nicola J Clegg et al.
Journal of medicinal chemistry, 48(19), 5989-6003 (2005-09-16)
Estrogen receptors (ERs) control transcription of genes important for normal human development and reproduction. The signaling networks are complex, and there is a need for a molecular level understanding of the roles of receptor subtypes ERalpha and ERbeta in normal
George Barreto et al.
Endocrinology, 150(11), 5010-5015 (2009-10-03)
After brain injury, astrocytes acquire a reactive phenotype characterized by a series of morphological and molecular modifications, including the expression of the cytoskeletal protein vimentin. Previous studies have shown that estradiol down-regulates reactive astrogliosis. In this study we assessed whether
Wenbo Li et al.
Nature, 498(7455), 516-520 (2013-06-04)
The functional importance of gene enhancers in regulated gene expression is well established. In addition to widespread transcription of long non-coding RNAs (lncRNAs) in mammalian cells, bidirectional ncRNAs are transcribed on enhancers, and are thus referred to as enhancer RNAs
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Linhao Ruan et al.
Science advances, 6(32), eabc7288-eabc7288 (2020-08-22)
Proteostasis declines with age, characterized by the accumulation of unfolded or damaged proteins. Recent studies suggest that proteins constituting pathological inclusions in neurodegenerative diseases also enter and accumulate in mitochondria. How unfolded proteins are managed within mitochondria remains unclear. Here
Valentino Martina et al.
Clinical endocrinology, 64(3), 260-264 (2006-02-21)
Several clinical and population-based studies suggest that dehydroepiandrosterone (DHEA) and its sulphate (DHEA-S) play a protective role against atherosclerosis and coronary artery disease in human. However, the mechanisms underlying this action are still unknown. It has recently been suggested that
Aniruddha Das et al.
Archives of sexual behavior, 43(7), 1403-1415 (2014-03-07)
Using nationally representative data from the 2005-2006 U.S. National Social Life, Health, and Aging Project, this study queried relationship, sexual, and sex hormone patterns among married evangelical women and men aged 57-85, relative to those in other religions. Results suggested
Christine Cadot et al.
Bioorganic & medicinal chemistry, 15(2), 714-726 (2006-11-18)
A series of estrone and estradiol derivatives having an N-butyl,methyl heptanamide side chain at C6-position were synthesized, tested as inhibitors of type 1 17beta-HSD and assessed for their possible estrogenic activity. A better type 1 17beta-HSD inhibition was obtained for
Dan Tong et al.
Biology of reproduction, 80(6), 1099-1106 (2009-01-30)
Expression of GJA1 (commonly known as connexin43 or Cx43), a major myometrial gap junction protein, is upregulated before the onset of delivery, suggesting an essential role for Cx43-mediated gap junctional intercellular communication (GJIC) in normal uterine contraction during parturition. To
Shigeo Hayashi et al.
Bioorganic & medicinal chemistry, 18(21), 7675-7699 (2010-09-30)
Neuropathic pain is a serious chronic disorder caused by lesion or dysfunction in the nervous systems. Endogenous nociceptin/orphanin FQ (N/OFQ) peptide and N/OFQ peptide (NOP) receptor [or opioid-receptor-like-1 (ORL1) receptor] are located in the central and peripheral nervous systems, the
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