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Showing 1-30 of 376 results for "E2257" within Papers
Robert E McDevitt et al.
Bioorganic & medicinal chemistry letters, 15(12), 3137-3142 (2005-05-07)
The syntheses of a series of 2-arylindene-1-ones as potent ligands of ERbeta and ERalpha are described. Several compounds exhibited high potency and moderate selectivity for the ERbeta receptor. X-ray and modeling studies were used to understand ligand binding orientation and
Sarah El Hajj Chehadeh et al.
American journal of physiology. Endocrinology and metabolism, 307(11), E1009-E1019 (2014-10-09)
Early deficiency of the methyl donors folate and vitamin B12 produces hyperhomocysteinemia and cognitive and motor disorders in 21-day-old rat pups from dams fed a diet deficient in methyl donors during gestation and lactation. These disorders are associated with impaired
Paiboon Nuntanakorn et al.
Journal of natural products, 69(3), 314-318 (2006-03-28)
A new lignan, actaealactone (1), and a new phenylpropanoid ester derivative, cimicifugic acid G (2), together with 15 known polyphenols, protocatechuic acid, protocatechualdehyde, p-coumaric acid, caffeic acid, methyl caffeate, ferulic acid, ferulate-1-methyl ester, isoferulic acid, 1-isoferuloyl-beta-d-glucopyranoside, fukinolic acid, and cimicifugic
Frank Z Stanczyk et al.
Contraception, 87(6), 706-727 (2013-02-05)
The need to seek improved combined oral contraceptive (COC) efficacy, with fewer health risks and better acceptability, has been ongoing since the introduction of COCs more than 50 years ago. New progestin formulations combined with lower doses of ethinyl estradiol
A L Chernyshova et al.
Voprosy onkologii, 59(1), 65-71 (2013-07-03)
We conducted a comparative investigation of the hormonal status (LH, FSH, estradiol, progesterone, testosterone, prolactin, SHBG), energy status (leptin, ghrelin, insulin), and carbohydrate and lipid metabolism in patients with endometrial hyperplasia and neoplasia (168 patients) with or without metabolic syndrome
Chinnasamy Ramesh et al.
Journal of medicinal chemistry, 53(3), 1004-1014 (2010-01-01)
A series of iodo-substituted tetrahydro-3H-cyclopenta[c]quinolines was synthesized as potential targeted imaging agents for the G protein-coupled estrogen receptor GPR30. The affinity and specificity of binding to GPR30 versus the classical estrogen receptors ER alpha/beta and functional responses associated with ligand-binding
Kevin D Dykstra et al.
Bioorganic & medicinal chemistry letters, 17(8), 2322-2328 (2007-02-10)
A novel class of indole ligands for estrogen receptor alpha have been discovered which exhibit potent affinity and high selectivity. Substitution of the bazedoxifene skeleton to the linker present in the HTS lead 1a provided 22b which was found to
Nuha Al-Zaubai et al.
The Journal of pharmacology and experimental therapeutics, 351(1), 172-180 (2014-08-01)
Inflammation has been implicated in tumor initiation, angiogenesis, and metastasis, and linked to the development of more aggressive, therapy-resistant estrogen receptor (ER)-positive breast cancer. Resolvin D2 (RvD2) is a potent anti-inflammatory lipid mediator. As RvD2 may be synthesized within breast
Kiran K Soma et al.
The Journal of steroid biochemistry and molecular biology, 145, 261-272 (2014-06-15)
Historically, research on the neuroendocrinology of aggression has been dominated by the paradigm that the brain receives sex steroid hormones, such as testosterone (T), from the gonads, and then these gonadal hormones modulate behaviorally relevant neural circuits. While this paradigm
Richard A DeFazio et al.
The Journal of neuroscience : the official journal of the Society for Neuroscience, 34(49), 16296-16308 (2014-12-05)
Gonadotropin-releasing hormone (GnRH) secretion is regulated by estradiol feedback. This feedback switches from negative to positive in females; this switch depends on time of day in many species. Estradiol feedback is likely conveyed via afferents. Kisspeptin neurons of the arcuate
M Evagelatou et al.
Clinical and experimental immunology, 98(2), 203-209 (1994-11-01)
Effects of oestradiol (E2) have been studied on the in vitro T cell-dependent differentiation of B cells from peripheral blood and spleen using normal donors and patients with the antibody deficiency disease CVID. We also studied whether it modifies T
Ming Zhao et al.
Bioorganic & medicinal chemistry, 17(10), 3680-3689 (2009-04-24)
To explore the structural dependence of the oral potency and side effect of estrogen-RGD peptide conjugates, here six novel conjugates were prepared via introducing RGD-tetrapeptides into both 3- and 17-positions of estradiol, and introducing RGD-octapeptides into 3-position of estrone. In
R A Lobo et al.
The Journal of reproductive medicine, 37(1), 77-84 (1992-01-01)
The pharmacokinetics of oral 17 beta-estradiol (E2) were evaluated: only a limited amount of information is available on the subject. Because of the first passage hepatic effect, the blood levels of estrone (E1) are greater than those of E2; similar
Sandrine Marchais-Oberwinkler et al.
Journal of medicinal chemistry, 51(15), 4685-4698 (2008-07-18)
17beta-Estradiol (E2) is implicated in the genesis and the development of estrogen-dependent diseases. Its concentration is mainly regulated by 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1), which catalyzes the reduction of the weak estrogen estrone (E1) to the highly potent E2. This
Michael A Cant et al.
Proceedings of the National Academy of Sciences of the United States of America, 111(1), 326-330 (2013-12-25)
The evolution of cooperation in animal and human societies is associated with mechanisms to suppress individual selfishness. In insect societies, queens and workers enforce cooperation by "policing" selfish reproduction by workers. Insect policing typically takes the form of damage limitation
S Freret et al.
Reproduction (Cambridge, England), 131(4), 783-794 (2006-04-06)
The aim of our study was to test whether a reduction in dietary intake could improve in vitro embryo production in superovulated overfed dairy heifers. Cumulus-oocyte complexes of 16 Prim' Holstein heifers (14 +/- 1 months old) were collected by
Patrycja Kurowska et al.
Reproduction (Cambridge, England) (2019-05-08)
Vaspin, also known as visceral adipose tissue-derived serine protease inhibitor, is a member of the serine protease inhibitor family. Its expression is associated with obesity, insulin resistance and type 2 diabetes, and elevated concentration is observed in polycystic ovary syndrome.
Xihua Chen et al.
Human reproduction (Oxford, England), 30(9), 2160-2170 (2015-06-27)
How is vascular endothelial growth factor (VEGF) expression regulated by hypoxia inducible factor 1 alpha (HIF1A) during menstruation? After progesterone (P4) withdrawal, HIF1A was activated and it directly up-regulated VEGF mRNA expression and this regulation was the highest during endometrium
Daniel N Weber et al.
Journal of toxicology and environmental health. Part A, 78(1), 50-66 (2014-11-27)
Developmental bisphenol A (BPA) exposure is associated with adverse behavioral effects, although underlying modes of action remain unclear. Because BPA is a suspected xenoestrogen, the objective was to identify sex-based changes in adult zebrafish social behavior developmentally exposed to BPA
Hasrat Ali et al.
Bioorganic & medicinal chemistry letters, 16(2), 317-319 (2005-11-09)
Nucleosides were coupled to estradiol via a 17alpha-ethynyl spacer group using Pd(II) as a catalyst. The conjugates were evaluated in vitro for estrogen receptor (ER) binding affinity and cytotoxicity against cell lines with and without ER. The highest receptor binding
R Scott Obach et al.
Drug metabolism and disposition: the biological fate of chemicals, 36(7), 1385-1405 (2008-04-23)
We present herein a compilation and trend analysis of human i.v. pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data. This data set provides the drug metabolism scientist with a
Nariaki Kokuho et al.
Laboratory investigation; a journal of technical methods and pathology, 99(6), 853-865 (2019-02-08)
Although mammalian target of rapamycin inhibitors (mTORi) are used to treat various malignancies, they frequently induce active alveolitis and dyslipidemia. Abnormal lipid metabolism affects alveolar surfactant function and results in pulmonary disorders; however, the pathophysiology of lung injury and its
Mahdi Golshan et al.
Aquatic toxicology (Amsterdam, Netherlands), 155, 73-83 (2014-07-06)
The fungicide vinclozolin (VZ) is in use globally and known to disrupt reproductive function in male. The present study tested the hypothesis that VZ disrupts testicular function in goldfish (Carassius auratus) by affecting brain-pituitary-testis axis. Goldfish were exposed to 100
Dongmei Zhang et al.
Pathology oncology research : POR, 27, 582443-582443 (2021-07-15)
The expression of Proline-, glutamic acid-, and leucine-rich protein 1 (PELP1) has been reported to be dysregulated in non-small cell lung carcinoma, especially in lung adenocarcinoma (LUAD). Therefore, we aimed to investigate the functional and prognostic roles of PELP1 in
Ca Leisinger et al.
Animal reproduction science, 150(1-2), 70-75 (2014-09-28)
The present study utilized a 2Ć2Ć2 factorial design examining age (old vs. young), follicle size (ā„2mm vs. <2mm) and media supplementation (with or without fetal bovine serum [FBS]) to determine factors that might affect in vitro maturation of alpaca oocytes.
M Gajecka
Polish journal of veterinary sciences, 16(2), 313-322 (2013-08-27)
The experiment involved 30 clinically healthy Beagle bitches aged approximately 70 days with an initial body weight of approximately 8 kg. The animals were randomly divided into two experimental groups (EI and EII) and a control group of 10 animals
Tony K L Kiang et al.
Pharmacology & therapeutics, 106(1), 97-132 (2005-03-23)
UDP-glucuronosyltransferase (UGT) enzymes catalyze the conjugation of various endogenous substances (e.g., bilirubin) and exogenous compounds (e.g., drugs). The human UGT superfamily is comprised of 2 families (UGT1 and UGT2) and 3 subfamilies (UGT1A, UGT2A, and UGT2B). Many of the individual
Wanying Sun et al.
Bioorganic & medicinal chemistry letters, 16(6), 1468-1472 (2006-01-18)
A series of 6H-benzo[c]chromen-6-one and 6H-benzo[c]chromene derivatives were prepared, and the affinity and selectivity for ERalpha and ERbeta was measured. Many of the analogs were found to be potent and selective ERbeta agonists. Bis hydroxyl at positions 3 and 8
Tomoko Soga et al.
Endocrinology, 155(5), 1944-1955 (2014-03-13)
Gonadotropin-inhibitory hormone (GnIH) neurons project to GnRH neurons to negatively regulate reproductive function. To fully explore the projections of the GnIH neurons, we created transgenic rats carrying an enhanced green fluorescent protein (EGFP) tagged to the GnIH promoter. With these
Sara GonzƔlez-Arranz et al.
Cells, 10(10) (2021-10-24)
During meiosis, the budding yeast polo-like kinase Cdc5 is a crucial driver of the prophase I to meiosis I (G2/M) transition. The meiotic recombination checkpoint restrains cell cycle progression in response to defective recombination to ensure proper distribution of intact
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