Abstract：
:To identify new pathways of estrogen action and novel estrogen receptor α (ERα) biomodulators, we performed high throughput screening and used follow on assays and bioinformatics to identify small molecule ERα inhibitors with a novel mode of action. These studies led to identification of rapid extranuclear activation of the endoplasmic reticulum stress sensor, the unfolded protein response (UPR), as a new pathway of estrogen-ERα action. Moreover, increasing evidence indicates that the mechanism underlying anticipatory activation of the UPR is shared among steroid and peptide hormones and is conserved from insects to humans. It is likely that this newly unveiled extranuclear pathway is used by diverse mitogenic hormones to prepare cells for the increased protein folding load that will occur during subsequent cell proliferation. Demonstrating biological relevance, elevated expression of a UPR gene signature in ERα positive breast cancer is a powerful new prognostic marker tightly correlated with subsequent resistance to tamoxifen, tumor recurrence and poor survival. In addition, overexpression of epidermal growth factor receptor and HER2/neu is positively correlated with increased UPR activation in breast cancer. This review describes recent research that demonstrates the importance of anticipatory UPR activation in therapy resistant tumors and discusses a promising small molecule biomodulator that inhibits tumor growth by tuning this UPR signaling pathway.
journal_name
Steroidsjournal_title
Steroidsauthors
Zheng X,Andruska N,Yu L,Mao C,Kim JE,Livezey M,Helferich WG,Shapiro DJdoi
10.1016/j.steroids.2016.03.014subject
Has Abstractpub_date
2016-10-01 00:00:00pages
2-6eissn
0039-128Xissn
1878-5867pii
S0039-128X(16)00081-7journal_volume
114pub_type
杂志文章,评审相关文献
STEROIDS文献大全abstract：:A series of chemiluminescent 17beta-estradiol probes were synthesized. Relative equilibrium dissociation constants (K(D)) for the interaction of an anti-E(2) Fab fragment for the probes in solution were evaluated using a single E(2)-analog biosensor surface on a BIAcore surface plasmon resonance instrument. The result...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/s0039-128x(00)00091-x
更新日期：2000-06-01 00:00:00
abstract：:A new technique that permits measurement of Androgen-Binding Protein (ABP) is validated by reproducibility, linearity and correlation studies. Using this apparatus allowing Scatchard plot analysis, it is also possible to measure association and dissociation rate constants. In addition, it is a very useful tool for a r...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/0039-128x(88)90174-2
更新日期：1988-10-01 00:00:00
abstract：:Aldosterone induces fibrotic changes in cardiovascular tissues but its effects have usually been demonstrated in models of pre-existing renal injury and/or hypertension. This study tests the hypothesis that aldosterone can directly induce vascular fibrotic changes in the absence of prior renal injury or hypertension. ...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/j.steroids.2012.12.007
更新日期：2013-03-01 00:00:00
abstract：:Two new sterols, (24E)-24-n-propylidenecholesterol and 24 epsilon-n-propylcholesterol, were isolated from a cultured marine Chrysophyte. Since most of the steroids found in marine invertebrates are unchanged or modified sterols of algal or symbiotic origin, the discovery of these two unusual sterols in a unicellular a...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/0039-128x(80)90104-x
更新日期：1980-02-01 00:00:00
abstract：:Oxidative stress is thought to play a crucial role in the pathogenesis of chronic diabetic complications. We investigated the protective effects of 17 beta-estradiol (E2) on alloxan-induced stress oxidant, hepatic dysfunction and histological changes in male rats liver and pancreas. Our results showed that 17 beta-est...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/j.steroids.2007.12.026
更新日期：2008-05-01 00:00:00
abstract：:This study describes a new approach using stable isotope methodology in evaluating 11beta-HSD activities in vivo based on urinary excretion of cortisol, cortisone, and their A-ring reduced metabolites. The method involved the measurement of deuterium-labeled cortisol and its deuterium-labeled metabolites by GC/MS simu...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/s0039-128x(99)00086-0
更新日期：2000-02-01 00:00:00
abstract：:Three new pregnane steroids, 2beta,3beta,5beta-trihydroxy-pregn-20-en-6-one (1), 3beta-hydroxy-5alpha-pregn-7,20-dien-6-one (2), and 3beta-acetoxy-5alpha-pregn-7,20-dien-6-one (3) were isolated from the twigs and leaves of Turraea pubescens, and were structurally elucidated on the basis of spectroscopic data and chemi...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/j.steroids.2006.04.010
更新日期：2006-08-01 00:00:00
abstract：:The metabolism of testosterone (T) was studied in normal adult male rats using a constant infusion of trace amounts of the 3H-steroid into a tail vein for 3 h in order to attain a state of equilibrium. Samples of plasma, liver, kidney, prostate, seminal vesicles and muscle were analysed for 3H-testosterone, 3H-5alpha-...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/0039-128x(75)90011-2
更新日期：1975-07-01 00:00:00
abstract：:Allopregnanolone (3α-THP) is one of the main reduced progesterone (P4) metabolites that is recognized as a neuroprotective and myelinating agent. 3α-THP also induces proliferation of different neural cells. It has been shown that P4 favors the progression of glioblastomas (GBM), the most common and aggressive primary ...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/j.steroids.2017.01.004
更新日期：2017-03-01 00:00:00
abstract：:The synthesis of delta 7,9(11)-lanostadiene derivatives functionalized at C(32) starting from 3 beta-acetoxy-7 alpha,32-epoxylanostan-11-one has been presented. The delta 7,9(11) moiety was efficiently introduced in three steps in 71% yield by the regioselective abstraction of allylic 8 beta hydrogen. The formyl group...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/s0039-128x(97)00075-5
更新日期：1997-11-01 00:00:00
abstract：:We have investigated the metabolism of deoxycorticosterone in A6 cells, a continuous cell line derived from the kidney of Xenopus laevis. A6 cells at confluence were incubated with serum-free culture media containing 2.5 microM [3H] deoxycorticosterone. When radioactive compounds in incubation media were separated by ...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/0039-128x(95)00038-r
更新日期：1995-07-01 00:00:00
abstract：:A first assay based on stable isotope dilution/gas chromatography-mass spectrometry (ID/GC-MS) has been developed for plasma 11-deoxycortisol (Reichstein's compound S), the leading hormonal marker of 11beta-hydroxylase deficiency. A suitable internal standard being unavailable, we synthesized dideuterated 11-deoxycort...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/s0039-128x(02)00052-1
更新日期：2002-09-01 00:00:00
abstract：:The use of the synthetic progestin medroxyprogesterone acetate (MPA) for estrus prevention in the dog can result in overproduction of growth hormone, suppression of plasma glucocorticoid levels, and the induction of mammary tumors. Proligestone (PROL) was claimed to be devoid of these unwanted side effects. In the pre...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/0039-128x(95)00216-d
更新日期：1996-03-01 00:00:00
abstract：:18,20-Epoxy-11 beta,17 alpha,20 beta,21-tetrahydroxypregn-4-en-3-one was synthesized by the application of hypoiodite reaction to the cortisol acetonide. The intermediary 18-iodo derivative was converted to the 11-oxo steroid by chromic acid prior to silver ion-assisted solvolysis. Removal of the protective group with...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/0039-128x(92)90095-q
更新日期：1992-09-01 00:00:00
abstract：:The use of steroid hormones as growth promoters remains illegal in Europe. A classical approach used to control their utilization consists to measure the parent drug in target biological matrices. However, this strategy may fail when the parent drug is submitted to extensive metabolism reactions. For urine and tissue ...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/j.steroids.2004.11.009
更新日期：2005-03-01 00:00:00
abstract：:The common disease asthma is characterized by the obstruction, inflammation and increased sensitivity of the airways. Glucocorticoids (GCs) are one of the most potent anti-inflammatory agents available for treating allergic disease. In this study, we report that the GC budesonide (BUD) can rapidly inhibit the histamin...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/j.steroids.2005.09.019
更新日期：2006-02-01 00:00:00
abstract：:Oleoyl-estrone (OE) induces a marked loss of body fat in rats by maintaining energy expenditure, body protein and blood glucose despite decreasing food intake. OE increases glucocorticoids, but they arrest OE lipid-mobilization. We studied here whether OE induces a direct effect on adrenal glands function as part of t...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/j.steroids.2009.09.009
更新日期：2010-01-01 00:00:00
abstract：:It has been shown by others that treatment with only progesterone is sufficient to induce implantation and maintain pregnancy in ovariectomized-adrenalectomized rabbits. Based on these results, it was deduced that induction of implantation in the rabbit does not require estrogen. In making this deduction, "blastocyst ...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/0039-128x(76)90017-9
更新日期：1976-10-01 00:00:00
abstract：:A radio-gas chromatographic method has been devised for the estimation of 11-oxotestosterone (17beta-hydroxyandrost-4-ene-3, 11-dione) in fish plasma samples which provides an independent means of validating the radioimmunoassay described earlier. Estimates of the concentration of 11-oxotestosterone in a sample of mal...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/s0039-128x(78)80009-9
更新日期：1978-05-01 00:00:00
abstract：:Catalytic cycloalumination of (3β,5α)-3-vinylcholestane and (3α,5α)-3-allylcholestane with Et3Al catalyzed by Cp2ZrCl2 was performed for the first time to give previously unknown aluminacyclopentanes in ∼90% yield; these products were converted in situ to carbo- and heterocyclic (5α)-cholestane derivatives. ...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/j.steroids.2016.01.015
更新日期：2016-04-01 00:00:00
abstract：:Aromatase (CYP19A1) is an integral membrane enzyme that catalyzes the removal of the 19-methyl group and aromatization of the A-ring of androgens. All human estrogens are synthesized from their androgenic precursors by this unique cytochrome P450. The crystal structure of active aromatase purified from human placenta ...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/j.steroids.2011.02.030
更新日期：2011-07-01 00:00:00
abstract：:This study examines the distribution of 5 alpha-reductase and 3 alpha(beta)-hydroxysteroid dehydrogenase activities throughout the intact hyperplastic prostate gland and relate these measurements to the fibromuscular/epithelial composition and to the gross glandular morphology. The relative capacities of the stroma an...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/0039-128x(83)90015-6
更新日期：1983-01-01 00:00:00
abstract：:Sertoli cells isolated from 17 day old rats were maintained in culture and incubated with [14C]-progesterone for 20 h. The cells and media were extracted with ether/chloroform and the extracts chromatographed two-dimensionally on TLC and the radioactive metabolites visualized by autoradiography. Nine of the metabolite...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/s0039-128x(80)80009-2
更新日期：1980-05-01 00:00:00
abstract：:Fermentation of mesterolone (1) with Cunninghamella blakesleeana yielded four new metabolites, 1α-methyl-1β,11β,17β-trihydroxy-5α-androstan-3-one (2), 1α-methyl-7α,11β,17β-trihydroxy-5α-androstan-3-one (3), 1α-methyl-1β,6α,17β-trihydroxy-5α-androstan-3-one (4) and 1α-methyl-1β,11α,17β-trihydroxy-5α-androstan-3-one (5)...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/j.steroids.2014.01.001
更新日期：2014-04-01 00:00:00
abstract：:The role of an estrogen-binding protein similar to a known mammalian estrogen receptor (ER) is described in the estradiol-dependent reproduction of the helminth parasite Taenia crassiceps. Previous results have shown that 17-β-estradiol induces a concentration-dependent increase in bud number of in vitro cultured cyst...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/j.steroids.2011.05.003
更新日期：2011-09-01 00:00:00
abstract：:The 3alpha,5alpha- and 3alpha,5beta-reduced derivatives of progesterone, deoxycorticosterone, dehydroepiandrosterone and testosterone enhance GABAergic neurotransmission and produce inhibitory neurobehavioral and anti-inflammatory effects. Despite substantial information on the progesterone derivative (3alpha,5alpha)-...
journal_title：Steroids
pub_type： 临床试验,杂志文章
doi：10.1016/j.steroids.2008.12.015
更新日期：2009-04-01 00:00:00
abstract：:Hydroxycitric acid (HCA), a dietary-derived weight loss supplement, competitively inhibits ATP citrate lyase (ACLY). Tamoxifen (TAM) is the most frequently used therapy for estrogen receptor (ER)-positive breast cancer patients, but its application was restricted due to efficacy related issues. Lipid metabolic reprogr...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/j.steroids.2020.108656
更新日期：2020-08-01 00:00:00
abstract：:Recent reports demonstrate neurotrophic properties of dehydroepiandrosterone sulfate (DHEAS) in men at rest, as well as profound neurotrophic responses to stress in both men and women. Little is known of neuroprotective-neurotrophic effects of DHEAS during stress exposure, either in men or women. This translational st...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/j.steroids.2014.05.011
更新日期：2014-09-01 00:00:00
abstract：:A significant dose-response relationship between gonadotropin-releasing hormone (GnRH) and time to luteinizing hormone (LH) peak, peak serum LH and total serum LH was obtained in prepubertal Holstein heifers (28 weeks of age) (Experiment 1). For the second experiment, the effect of steroid feedback on the anterior pit...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/0039-128x(86)90082-6
更新日期：1986-02-01 00:00:00
abstract：:Synthetic transformations of steroids for drug discovery and improvement of drug effectiveness have been an important part of modern medicinal chemistry and pharmaceutical sciences. Pentacyclic triterpenoids, being represented in the nature by various structures and biogenetically related to steroids, can largely expa...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/j.steroids.2018.10.005
更新日期：2018-12-01 00:00:00
