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E2257

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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
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
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
Improving in vitro maturation and pregnancy outcome in cattle using a novel oocyte shipping and maturation system not requiring a CO2 gas phase
Barcelo-Fimbres M, et al.
Theriogenology, 84(1), 109-117 (2015)
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)
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)
R R Greb et al.
The Journal of clinical endocrinology and metabolism, 90(8), 4866-4872 (2005-05-12)
FSH is essential for follicular maturation. Data from ovarian hyperstimulation cycles suggest that FSH action is attenuated by a frequent single nucleotide polymorphism of the FSH receptor gene exchanging Asn for Ser at codon 680. We hypothesized that the FSH
B Zumoff et al.
Arteriosclerosis (Dallas, Tex.), 2(1), 58-67 (1982-01-01)
Plasma concentrations and urinary excretions of various hormones and hormone metabolites were measured in four groups. Group 1 was composed of 13 men with prior myocardial infarction; Group 2 contained 35 clinically normal men; Group 3 consisted of 44 men
Yuko Ando et al.
Bioorganic & medicinal chemistry letters, 16(22), 5849-5854 (2006-09-02)
A novel oxazine ring formation method was established using the reaction of 2-acetyl-(E)-3-styrylcarbonylaminobenzo[b]furans (4) with Vilsmeier-Haack-Arnold reagent to afford (E and Z)-((E)-2-styrylbenzo[b]furo[3,2-d][1,3]oxazin-4-ylideno)acetaldehydes (5). (Z)-4-(8-Bromo-(E)-2-styrylbenzo[b]furo[3,2-d][1,3]oxazin-4-ylideno)but-(E)-2-enoic acid ethyl ester (6b), derived from (Z)-5a, showed significantly potent anti-osteoclastic bone resorption activity comparable to
Coadministrating luteolin minimizes the side effects of the aromatase inhibitor letrozole.
Li F, Wong TY, Lin SM, et al.
Journal of Pharmacology and Experimental Therapeutics, 351(2), 270-277 (2014)
17 beta-estradiol/levonorgestrel transdermal system. A viewpoint by Lee P. Shulman.
Lee P Shulman
Treatments in endocrinology, 3(5), 325-326 (2004-08-28)
Determination of 17 beta-estradiol in pharmaceutical preparation by UV spectrophotometry and high performance liquid chromatography methods
Yilmaz B and Kadioglu Y
Arabian Journal of Chemistry, 10, S1422-S1428 (2017)
L B Tankó et al.
Journal of internal medicine, 258(6), 544-553 (2005-11-30)
To investigate how variation in the dose of the progestogen influence the impact of 17beta-oestradiol plus drospirenone (DRSP) treatment on adipose tissue and its secretor function with direct implications for atherogenic metabolites. Randomized, double-blind, placebo-controlled trial. Primary care, single study
Yung-Luen Yu et al.
The Journal of biological chemistry, 280(33), 29533-29542 (2005-06-22)
In the interleukin 3-dependent hematopoietic cell line Ba/F3, inhibition of mitogen-activated protein kinase, a member of the MAPK/c-Jun N-terminal kinase/stress-activated protein kinase kinase family that plays an important role in cell growth and death control, rapidly leads to severe apoptosis.
K J Elliott et al.
British journal of sports medicine, 39(1), 15-19 (2004-12-25)
To examine the effects of oral contraceptive use on maximum force production in young women. In the study, 21 female subjects (14 pill users and seven eumenorrheic controls) took part. All pill using subjects had been taking a combined, monophasic
Seiro Satohisa et al.
Endocrinology, 155(8), 3005-3016 (2014-06-01)
Adduction of a nitric oxide (NO) moiety (NO(•)) to cysteines termed as S-nitrosylation (SNO) has emerged as a crucial mechanism for NO signaling crucial for mediating the vascular effects of estrogens. Mitochondrion is a known vascular risk factor; however, the
Shiladitya Sengupta et al.
Proceedings of the National Academy of Sciences of the United States of America, 117(36), 22183-22192 (2020-08-23)
Among several reversible epigenetic changes occurring during transcriptional activation, only demethylation of histones and cytosine-phosphate-guanines (CpGs) in gene promoters and other regulatory regions by specific demethylase(s) generates reactive oxygen species (ROS), which oxidize DNA and other cellular components. Here, we
Latanya M Scott et al.
Bioorganic & medicinal chemistry letters, 21(2), 730-733 (2011-01-05)
Shp2 protein tyrosine phosphate (PTP) is a novel target for anticancer drug discovery. We identified estramustine phosphate as a Shp2 PTP inhibitor from the National Cancer Institute Approved Oncology Drug set. A focused structure-activity relationship study indicated that the 17-phosphate
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
Vincent M Carroll et al.
Journal of medicinal chemistry, 55(1), 528-537 (2011-11-30)
Two estrogen receptor (ER) subtypes, ERα and ERβ, mediate the actions of estrogens in diverse reproductive and nonreproductive target tissues. ER subtype-selective ligands, which bind to and activate these subtypes differentially, have proved to be useful in elucidating which actions
D Fraser et al.
British journal of obstetrics and gynaecology, 98(12), 1277-1282 (1991-12-01)
To investigate the presence of an oestradiol receptor-related protein (P29) in skin and skin organelles, and to assess changes in its content during the normal menstrual cycle. An observational study. King's College School of Medicine and Dentistry, London. Twenty-one premenopausal
Kathryn J Grive et al.
Developmental biology, 392(1), 42-51 (2014-05-20)
Primary ovarian insufficiency (POI) affects 1% of women under the age of 40 and is associated with premature ovarian follicle depletion. TAF4b deficiency in adult female mouse models results in hallmarks of POI including stereotyped gonadotropin alterations indicative of early
Zhonghua Shi et al.
Endocrinology, 155(5), 1982-1990 (2014-03-08)
Omental adipose tissue plays a central role in insulin resistance in gestational diabetes mellitus (GDM), and the molecular mechanisms leading to GDM remains vague. Evidence demonstrates that maternal hormones, such as estradiol, contribute to insulin resistance in GDM. In this
Zhichao Liu et al.
PLoS computational biology, 7(12), e1002310-e1002310 (2011-12-24)
Drug-induced liver injury (DILI) is a significant concern in drug development due to the poor concordance between preclinical and clinical findings of liver toxicity. We hypothesized that the DILI types (hepatotoxic side effects) seen in the clinic can be translated
Bu B Yeap et al.
The Journal of clinical endocrinology and metabolism, 99(1), E9-18 (2013-11-22)
Testosterone (T) levels decline with age and lower T has been associated with increased mortality in aging men. However, the associations of its metabolites, dihydrotestosterone (DHT) and estradiol (E2), with mortality are poorly defined. We assessed associations of T, DHT
Jeongsoo Yoo et al.
Journal of medicinal chemistry, 48(20), 6366-6378 (2005-09-30)
Estrogen receptor beta (ERbeta), a less active ER subtype that appears to have a restraining effect on the more active ERalpha, could be a factor that determines the level of estrogen action in certain estrogen target tissues. ERbeta is found
Timothy A Blizzard et al.
Bioorganic & medicinal chemistry letters, 17(22), 6295-6298 (2007-09-25)
A series of androstene-3,5-diene derivatives were prepared. Despite lacking the C-3 hydroxyl previously believed necessary for ER activity, some of the analogs retained surprising affinity for ER-beta. For example, diene 4 retained excellent selectivity and potency as an ER-beta agonist
Gonadal steroids and body composition, strength, and sexual function in men.
Paul F Schellhammer
The New England journal of medicine, 369(25), 2456-2456 (2013-12-20)
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