Abstract：
:Interaction of tamoxifen, trioxifene and LY117018 with cytosol-estrogen receptors from immature rat uteri was compared. Determination of relative binding affinity (RBA) by competition with [3H] estradiol under various assay conditions revealed that the RBA of LY117018 increased with temperature while that of trioxifene declined. Furthermore, the RBA values of tamoxifen and trioxifene observed after 24 h of incubation at 4 degrees C were significantly lower than those obtained with 1-h incubations. However RBA values obtained with 1- or 24-h incubations of LY117018 at 4 degrees C were similar. The complex formed by estradiol or LY117018 at 4 degrees was relatively stable for 24 h, while significant dissociation of tamoxifen and trioxifene was detected under these conditions. At 30 degrees C estradiol displayed a biphasic pattern of dissociation, but tamoxifen and trioxifene dissociated rapidly and little evidence of a stable phase was apparent. By contrast, the complex formed by LY117018 exhibited greater stability than that of estradiol at 30 degrees C. These results establish a relationship between shifts in competition curves (RBA) and rates of dissociation relative to estradiol; and clearly reveal that LY117018 has different binding characteristics than tamoxifen and trioxifene.
journal_name
Mol Cell Endocrinoljournal_title
Molecular and cellular endocrinologyauthors
Black LJ,Jones CD,Goode RLdoi
10.1016/0303-7207(81)90105-2subject
Has Abstractpub_date
1981-04-01 00:00:00pages
95-103issue
1eissn
0303-7207issn
1872-8057journal_volume
22pub_type
杂志文章abstract：:mRNA differential display polymerase chain reaction analysis was used to screen systematically for novel androgen-regulated genes in the human prostatic adenocarcinoma cell line LNCaP. A 232 bp PCR fragment was found to be consistently down-regulated by the synthetic androgen R1881. Sequencing revealed complete identi...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/s0303-7207(99)00113-6
更新日期：1999-09-10 00:00:00
abstract：:We have studied a 15-year-old girl (P1) suffering from the Hutchinson-Gilford syndrome (progeria) associated with a severe insulin resistance. Insulin binding activity to P1 erythrocytes was 85% reduced when compared to that measured in ten normal controls matched for sex and age. This finding was confirmed in Epstein...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/0303-7207(91)90239-o
更新日期：1991-01-01 00:00:00
abstract：:The androgen receptor (AR), which mediates androgen action in the cell, belongs to the superfamily of nuclear receptors, a large group of transcription factors. Recent studies have described how the AR acts on specific target genes. The receptor's specificity of action depends on its regulation at different levels: ex...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章,评审
doi：10.1016/s0303-7207(02)00364-7
更新日期：2002-12-30 00:00:00
abstract：:HE6 (GPR64) is a highly conserved, tissue-specific heptahelical receptor of the human epididymis. The seven transmembrane (TM7) domains are a hallmark of G-protein-coupled receptors (GPCRs) which have a proven history of being excellent therapeutic targets. Of all currently marketed drugs, >30% are modulators of speci...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章,评审
doi：10.1016/j.mce.2005.12.023
更新日期：2006-05-16 00:00:00
abstract：:1,25-Dihydroxyvitamin D(3) (1,25D(3)), the active metabolite of vitamin D(3), inhibits breast cancer cell growth in vivo and in vitro. To examine mechanisms of 1,25D(3) induced growth arrest and apoptosis, cell lines were established from DMBA induced mammary tumors derived from vitamin D(3) receptor knockout (VDRKO) ...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/s0303-7207(02)00416-1
更新日期：2003-02-28 00:00:00
abstract：:Ghrelin is a peptide hormone that was originally isolated from the stomach as the endogenous ligand for the growth hormone secretagogue receptor (GHSR). Ghrelin has many functions, including the regulation of appetite and gut motility, growth hormone release from the anterior pituitary and roles in the cardiovascular ...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章,评审
doi：10.1016/j.mce.2011.04.013
更新日期：2011-06-20 00:00:00
abstract：:Inhibin production by cultured granulosa cells from immature diethylstilbestrol (DES)-primed rats was studied in relation to estradiol and progesterone production. The inhibin content in culture media was assayed with a specific radioimmunoassay (RIA) using an antibody to porcine 32 kDa inhibin that recognizes rat inh...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/0303-7207(87)90156-0
更新日期：1987-12-01 00:00:00
abstract：:Metastatic renal cell carcinomas (RCC) remain highly resistant to systemic therapy. RCCs are highly vascular tumors, which overproduce angiogenic peptides such as vascular endothelial growth factor (VEGF) even under normoxic conditions. A potential suggested role of antiangiogenic therapeutic strategies is the treatme...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/j.mce.2004.07.013
更新日期：2004-10-29 00:00:00
abstract：:Cardiovascular effects of parathyroid hormone (PTH) have been recently described. Pharmacological doses of PTH both reduce arterial pressure and increase blood flow of vascular beds. Two possible cellular mechanisms were investigated: (a) transmembrane Ca2+ fluxes and (b) cyclic AMP response in vascular smooth muscle....
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/0303-7207(89)90231-1
更新日期：1989-11-01 00:00:00
abstract：:Evidence is accumulating that environmental chemicals (ECs) including endocrine-disrupting compounds (EDCs) can alter female reproductive development, fertility and onset of menopause. While not as clearly defined as in the male, this set of abnormalities may constitute an Ovarian Dysgenesis Syndrome with at least som...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章,评审
doi：10.1016/j.mce.2011.10.021
更新日期：2012-05-22 00:00:00
abstract：:In the frog Xenopus laevis, vitellogenin is the major estrogen-induced protein in the liver. We have characterized an additional secreted protein, of 45,000 Da and designated Ep45, which is also responsive to estrogen treatment. Like vitellogenin, Ep45 is not normally found in the plasma nor synthesized by the liver o...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/0303-7207(87)90064-5
更新日期：1987-01-01 00:00:00
abstract：:This report represents the joint efforts of three laboratories, one with a primary interest in understanding regulatory processes in the epididymal epithelium (TTT) and two with a primary interest in identifying and characterizing new contraceptive targets (DSJ and SAJ). We have developed a highly refined mouse epidid...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/j.mce.2005.12.042
更新日期：2006-05-16 00:00:00
abstract：:Estrogens are the primary female sex hormones and play important roles in both reproductive and non-reproductive systems. Estrogens can be synthesized in non-reproductive tissues such as liver, heart, muscle, bone and the brain. During the past decade, increasing evidence suggests that brain estrogen can not only be s...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章,评审
doi：10.1016/j.mce.2013.12.018
更新日期：2014-05-25 00:00:00
abstract：:Neonatal and adult rat islets, cultured for 7-9 days in the presence of 10.5 mM D-glucose, were incubated for 120 min with either D-glucose (2.8 and 16.7 mM) or L-leucine (1.0 and 20.0 mM). The total and anaerobic rates of glycolysis, as judged respectively through the generation of 3H2O from D-[5-3H]glucose and 14C-l...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/0303-7207(90)90045-a
更新日期：1990-10-01 00:00:00
abstract：:Glucose-dependent insulinotropic polypeptide (GIP) plays an important role in stimulating insulin release in the pancreas as well as inhibiting gastric acid secretion in the stomach. GIP has been found in specific endocrine cells located in the mucosal layer of the small intestine and in the submandibular salivary gla...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/s0303-7207(99)00106-9
更新日期：1999-08-20 00:00:00
abstract：:The synthesis and phosphorylation of H1 histones were studied in organ cultures of midpregnant mouse mammary glands exposed to various combinations of insulin, cortisol and prolactin over a 48-h period. The synthesis of specific H1 histone subtypes was changed only when all three hormones were present, and the effect ...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/0303-7207(87)90137-7
更新日期：1987-11-01 00:00:00
abstract：:We recently cloned and sequenced two kilobases of the upstream flanking region of the mouse tissue transglutaminase gene. Transfection experiments showed that this region of the transglutaminase flanking sequence was sufficient to mediate a 4-fold induction in reporter gene expression by retinoic acid. The goal of the...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/0303-7207(96)03826-9
更新日期：1996-07-01 00:00:00
abstract：:We studied the ontogeny of GH receptor mRNA levels and the effect of exogenous estradiol administration on GH receptor mRNA levels in rabbit liver. A solution hybridization-RNase protection assay revealed a predominant 370-base long protected band corresponding to the mRNA encoding the transmembrane GH receptor, and a...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/0303-7207(94)90072-8
更新日期：1994-07-01 00:00:00
abstract：:Many genes that are required for fertility have been identified in model organisms (). Mutations in these genes cause infertility due to defects in development of the germ cell lineage, but the organism is otherwise healthy. Although human reproduction is undoubtedly as complex as that of other organisms, very few fer...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章,评审
doi：10.1016/s0303-7207(01)00646-3
更新日期：2001-11-26 00:00:00
abstract：:Steroidogenic activity in the mature corpus luteum of most mammals depends upon provision of cholesterol from the circulating lipoproteins. In cattle, as in many species, high-density lipoprotein (HDL) is the major lipoprotein involved. The recent identification of the scavenger receptor SR-BI as an HDL-receptor allow...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/s0303-7207(97)00173-1
更新日期：1997-10-31 00:00:00
abstract：:The detergent-soluble extract of rat ovary plasma membranes contained a Gs protein of about 100 kDa as shown by its elution behavior on a Bio Gel A-1.5m column. However, the cell membranes exposed to hCG (37 degrees C, 15 min) contained in addition a higher molecular weight Gs protein complex of 300 kDa comprised of h...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/0303-7207(91)90147-k
更新日期：1991-09-01 00:00:00
abstract：:Receptor-mediated Ca2+ entry was investigated in fura-2-loaded thyroid FRTL-5 cells. Activation of protein kinase C (PKC) by phorbol myristate acetate (PMA) attenuated the ATP-induced increase in intracellular free Ca2+ ([Ca2+]i). In PKC down-regulated cells, the ATP-induced increase in [Ca2+]i was increased compared ...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/0303-7207(93)90134-6
更新日期：1993-05-01 00:00:00
abstract：:Eppin (epididymal protease inhibitor) is a member of the whey acidic protein (WAP)-type four-disulfide core (WFDC) gene family. This study provides updated information on Eppin and the Eppin-like genes within the Eppin cluster on human chromosome 20. A virtual structural model of the Eppin protein demonstrates that th...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/j.mce.2005.12.039
更新日期：2006-05-16 00:00:00
abstract：:The present study examines the involvement of cAMP in the transduction of the short-term effect of gonadotropin-releasing hormone (GnRH) on gonadotropin release in the teleost fish, tilapia. A 5 min pulse of dibutyryl cyclic AMP (dbcAMP; 0.03-3 mM) or forskolin (0.1-10 microM) resulted in dose-dependent surges in tila...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/0303-7207(92)90256-6
更新日期：1992-06-01 00:00:00
abstract：:Ghrelin is the only known circulating hormone that acts on peripheral and central targets to increase food intake and promote adiposity. The present review focuses on the possible clinical relevance of ghrelin in the regulation of human feeding behavior in individuals with obesity and other eating disorders such as Pr...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章,评审
doi：10.1016/j.mce.2011.03.001
更新日期：2011-06-20 00:00:00
abstract：:Insulin-like growth factors (IGF-I and -II) promote cellular mitosis and differentiation and have been implicated in fetal and placental growth. Together with the IGF receptors and IGF binding proteins (IGFBPs) they form a complex network, with tissue specific activity. This review will discuss the data generated to e...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章,评审
doi：10.1016/s0303-7207(98)00041-0
更新日期：1998-05-25 00:00:00
abstract：:The high-density lipoprotein (HDL) pathway in rat adrenocortical cells was studied at the electron microscopic level in vitro via colloidal gold labelling. Steroid hormone assays were performed to confirm that the cells remained intact, viable, responsive to ACTH under the applied conditions, and to reveal the steroid...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/0303-7207(86)90062-6
更新日期：1986-02-01 00:00:00
abstract：:The effect of thyroid status on the postnatal development of the two molecular forms of Na+,K+-ATPase, distinguished kinetically on the basis of their ouabain sensitivity, was examined in rat brain. Hypothyroidism induced by PTU from day 1 postnatally significantly reduced the Na+,K+-ATPase activity in cerebellum (22-...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/0303-7207(85)90170-4
更新日期：1985-05-01 00:00:00
abstract：:Mammalian gonadotropins are highly selective. Charge differences between the Cys(10-11) sequence of FSHbeta and LHbeta/CGbeta seat-belt loops determine the ability of these hormones to interact with the LH-R. Selective FSH-R binding is mainly dependent on the presence of an FSHbeta-specific sequence between Cys(11-12)...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/j.mce.2004.06.011
更新日期：2004-09-30 00:00:00
abstract：:The activity of the hypothalamic-pituitary-adrenal (HPA) axis is characterized by an ultradian (pulsatile) pattern of hormone secretion. Pulsatility of glucocorticoids has been found critical for optimal transcriptional, neuroendocrine and behavioral responses. This review will focus on the mechanisms underlying the o...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章,评审
doi：10.1016/j.mce.2015.02.005
更新日期：2015-06-15 00:00:00
