Abstract:
:The hormone 1alpha,25(OH)2vitamin D3 (1,25-D) produces biological responses via both genomic and rapid mechanisms. The genomic responses are linked to a nuclear receptor, while the rapid responses are believed to utilize other signal transduction pathways that are likely linked to a putative cell membrane receptor for 1,25-D. The natural seco-steroid, 1,25-D, is capable of facile rotation about its 6,7 single carbon bond to permit generation of a continuum of potential ligand shapes extending from the 6-s-cis (6C) to the 6-s-trans (6T). To identify the shape of the conformer(s) that can serve as agonists for the genomic and rapid responses, we synthesized two families of analogs that were locked in either the 6T or 6C conformation. We found that 6T-locked analogs were inactive or significantly less active than 1,25-D in both rapid responses (transcaltachia or the rapid stimulation of intestinal Ca2+ absorption in perfused chick intestine, stimulation of whole cell chloride currents in osteoblastic ROS 17/2.8 cells, and stimulation of phosphorylation of mitogen-activated protein kinase in promyelocytic NB4 leukemic cells) and in genomic responses (induction of osteocalcin in human MG-63 osteoblastic cells). For genomic responses, the 6C-locked analogs bound poorly to the nuclear receptor and were much less potent than 1,25-D. In contrast, the 6C-locked analogs were potent agonists of the three rapid responses studied and had activities equivalent to 1,25-D. These results demonstrate that the signal transduction pathways that support rapid and genomic responses can discriminate between different shapes of the conformationally flexible 1,25-D.
journal_name
Steroidsjournal_title
Steroidsauthors
Norman AW,Song X,Zanello L,Bula C,Okamura WHdoi
10.1016/s0039-128x(98)00091-9subject
Has Abstractpub_date
1999-01-01 00:00:00pages
120-8issue
1-2eissn
0039-128Xissn
1878-5867pii
S0039-128X(98)00091-9journal_volume
64pub_type
杂志文章,评审相关文献
STEROIDS文献大全abstract::Phytochemical analysis of the fruits of Raphia vinifera led to the isolation of four new steroidal saponins (1-4), along with six known secondary metabolites (6-10). The structures of the isolated compounds were determined based on the analyses of NMR and mass spectrometric data, and chemical degradation reactions. Am...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/j.steroids.2020.108724
更新日期:2020-11-01 00:00:00
abstract::Significant changes in % free serum E2, T and P were observed during the annual cycle of the turtle. In contrast no significant changes in SHBG affinity constants (2.29-4.48 x 10(8) M-7) were found and binding capacity for estradiol 17B was between 3.47 and 3.96 x 10(-7) M except in preovulatory animals (2.00 +/- 0.25...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/0039-128x(88)90144-4
更新日期:1988-10-01 00:00:00
abstract::Seventeen cholesteryl alkyl ethers were synthesized through alcoholysis of cholesterol p-toluenesulfonate. This method was found superior to the etherification of sodium or potassium cholesterylate with alkyl halides or methanesulfonates, especially for the preparation of long-chain unsaturated aklyl ethers of [7(m)-3...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/0039-128x(80)90109-9
更新日期:1980-01-01 00:00:00
abstract::Radioactive mestranol (ME) and/or ethynylestradiol (EE) were administered to women in Nigeria, Sri Lanka, and the USA, and the types and patterns of radioactive urinary conjugates examined by Sephadex LH-20 chromatography. There are no differences in the total excretion of urinary radioactivity over 3 days. Consistent...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/0039-128x(80)90001-x
更新日期:1980-09-01 00:00:00
abstract::Parathyroid hormone-related protein (PTHrP) increases the growth and osteolytic potential of prostate cancer cells, making it important to control PTHrP expression in these cells. We show that 1,25-dihydroxyvitamin D3 (1,25(OH)2D3) and its non-hypercalcemic analog, EB1089, decrease PTHrP mRNA and cellular protein leve...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/j.steroids.2005.08.009
更新日期:2006-02-01 00:00:00
abstract::In an endeavour to develop potent anti-tumor agents from diosgenin, a series of C-6 derived 1,2,3-triazolyl derivatives were designed and synthesized by employing Cu(I) catalyzed Huisgen 1,3-dipolar cycloaddition reaction of novel azides - (22R,25R)-6β-azidospirostan-3β,5α-diol and 6β-azido-7α-hydroxyspirosta-1,4-dien...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/j.steroids.2019.108460
更新日期:2019-11-01 00:00:00
abstract::We report the synthesis of 3 beta,15 beta,17 alpha-trihydroxy-5-pregnen-20- one (1) from 3 beta,15 beta-dihydroxy-5,16-pregnadien-20-one (11) in 7 steps using boronate derivatives as a means of protecting the 17,20-glycol side-chain of steroid intermediates. 16 alpha,17 alpha-Epoxy-3 beta,15 beta-dihydroxy-5- pregnen-...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/0039-128x(95)00169-q
更新日期:1996-01-01 00:00:00
abstract::C17-20Lyase and 21-hydroxylase activities were measured during late gestation in the rhesus monkey (Macaca mulatta) fetal adrenal. Activities were assessed in 10,000 x g supernatants with 17-hydroxyprogesterone and NADPH as substrates. Although conversion of [14C]17-hydroxyprogesterone to [14C]androstenedione was note...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/0039-128x(81)90036-2
更新日期:1981-08-01 00:00:00
abstract::4- to 8-cell mouse PIE's (preimplantation embryos) were cultured in vitro for 48 hr in media containing various concentrations of the anti-estrogen CI-628. Graded effects of the various concentrations were observed with the highest concentration (1.5 microng/ml) being 100% effective in blocking development to the blas...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/0039-128x(77)90005-8
更新日期:1977-03-01 00:00:00
abstract::Sleep apnea is a disorder, which increasingly affects people worldwide. Whether the associated hypoxic events during sleep are central or obstructive in origin, the end result is excessive daytime sleepiness and an increased risk for several comorbidities, such as cardiovascular and neurodegenerative disorders. Sleep ...
journal_title:Steroids
pub_type: 杂志文章,评审
doi:10.1016/j.steroids.2017.12.006
更新日期:2018-05-01 00:00:00
abstract::Some properties of immunoreactive estradiol secreted by adrenals and ovaries of immature female rats were studied. It was shown that adrenals and ovaries of 15-day-old animals secrete approximately equal amounts of immunoreactive estradiol, with thin-layer chromatogram of immunoreactive material being identical for bo...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/0039-128x(92)90004-s
更新日期:1992-04-01 00:00:00
abstract::During the periparturient period, dairy cows are subjected to physiological changes that may induce immunosuppression and an increased susceptibility of the animal to bacterial infections such as mastitis. The incidence of clinical environmental mastitis is high during the last period of gestation, at parturition and ...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/s0039-128x(03)00040-0
更新日期:2003-05-01 00:00:00
abstract::20-Hydroxyecdysterone - (2β,3β,5β,22R)-2,3,14,20,22,25-hexahydroxycholest-7-en-6-one was isolated in satisfactory yield using ethanol extraction from the aerial part of Silene wolgensis (Hornem.) Otth; sometimes Silene wolgensis (Willd.) Bess. ex Spreng. The complexation of the phytoecdysteroid with β-cyclodextrin was...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/j.steroids.2018.11.007
更新日期:2019-07-01 00:00:00
abstract::The mass spectral elimination of water in epimeric 1,3-diols of vitamin D3 (colecalciferol) series has been investigated. It was found that the mass spectra of these steroisomers differ sharply in the relative intensities of the ions M-H2O (m/e 382) and a-H2O (m/e +/- 34), where ion a (formed via formal cleavage of th...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/0039-128x(79)90039-4
更新日期:1979-05-01 00:00:00
abstract::The addition of molybdate to rabbit liver cytosol increased significantly the affinity of the glucocorticoid receptor for [3H] dexamethasone without influencing the concentration of binding sites. This effect was concentration dependent. Analysis of the binding data by curve-fitting and Scatchard plot revealed the occ...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/s0039-128x(84)90088-6
更新日期:1984-08-01 00:00:00
abstract::11 beta-hydroxysteroid dehydrogenase (11 beta-HSD), the enzyme that catalyzes the conversion of biologically active glucocorticoids to their inactive metabolites, was shown to be located exclusively in Leydig cells of the rat testis, and its appearance was associated with the developmental rise in testosterone. Thus, ...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/s0039-128x(96)00225-5
更新日期:1997-03-01 00:00:00
abstract::The effect of a substituent in the 12-position of progestagens was studied. To this end, various approaches toward the preparation of 12 beta-alkyl- and 12-alkylidenenorpregnanes were investigated. Eventually, the desired compounds 17 beta-hydroxy-12 beta-methyl-18a-homo-19-nor-17 alpha-pregn-4-en-20-yn-3-one (37) and...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/0039-128x(92)90020-a
更新日期:1992-11-01 00:00:00
abstract:BACKGROUND:A high-throughput, sensitive, specific, mass spectrometry-based method for quantitating estrone (E1), estradiol (E2), and testosterone (T) in postmenopausal human serum has been developed for clinical research. The method consumes 100μl human serum for each measurement (triplicates consume 300μl) and does no...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/j.steroids.2015.01.007
更新日期:2015-04-01 00:00:00
abstract::The chemoselectivity of rigid cyclic alpha,beta-unsaturated carbonyl group on the reducing agents was influenced by the ring size and steric factor. Cholesterol (cholest-5-en-3beta-ol) and dehydroepiandrosterone (DHEA) were oxidized with 2,3-dichloro-5,6-dicyano-1,4-benzoquinone to form 1,4,6-cholestatrien-3-one and 1...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/j.steroids.2006.12.008
更新日期:2007-04-01 00:00:00
abstract::Bioconversion of the aromatase inhibitor formestane (4-hydroxyandrost-4-ene-3,17-dione) (1) by the fungus Rhizopus oryzae ATCC 11145 resulted in a new minor metabolite 3,5α-dihydroxyandrost-2-ene-4,17-dione (2) and the known 4β,5α-dihydroxyandrostane-4,17-dione (3) as the major product. The structural elucidation and ...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/j.steroids.2016.07.003
更新日期:2016-09-01 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::Spinasterol and schottenol, two phytosterols present in argan oil and in cactus pear seed oil, were synthesized from commercially available stigmasterol by a four steps reactions. In addition, the effects of these phytosterols on cell growth and mitochondrial activity were evaluated on 158N murine oligodendrocytes, C6...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/j.steroids.2015.01.005
更新日期:2015-07-01 00:00:00
abstract:BACKGROUND:Chronic administration of exogenous glucocorticoids is often required in experimental research. We compared the efficacy and reliability of three different methods of continuous glucocorticoid administration in mice. MATERIALS AND METHODS:Male CD1 Swiss White mice aged 7-9 weeks received corticosterone (CS)...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/j.steroids.2008.11.009
更新日期:2009-02-01 00:00:00
abstract::Corticosteroids were used normally as anti-inflammatory drugs. However, in some area certain corticosteroids might be illegally used as growth promoting agent in feed, and as prohibited doping substances in game and sport for human or/and animal performance-enhancing. Synthesized structural similar corticosteroids wer...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/j.steroids.2020.108739
更新日期:2021-01-01 00:00:00
abstract::Bioassays were conducted to determine various endocrinological properties of two spirolactone derivatives, 4',5'-dihydrospiro-[estr-4-ene-17,2'(3'H)-furan]-3-one (Compound I) and dispiro[cyclopropane-1,6'-estr-4'-ene-17',2"(3"h)-furan]-3'-one (Compound II). They proved to be very potent estrogen antagonists in immatur...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/0039-128x(77)90123-4
更新日期:1977-06-01 00:00:00
abstract::Steroids with 4-ene-3,6-dione functionality have application in natural product chemistry, as synthetic intermediates and as aromatase inhibitors. Here, we report a two-phase oxidation of a range of steroidal 5-en-3beta-ols into corresponding 4-ene-3,6-diones using a modified Jones oxidation. The new reaction affords ...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/j.steroids.2005.07.007
更新日期:2006-01-01 00:00:00
abstract::Chronic kidney disease results in a reduction in 1,25-dihydroxyvitamin D3 (1,25(OH)2D3) synthesis and an accumulation of phosphorus in the blood, leading to secondary hyperparathyroidism and renal osteodystrophy. Vitamin D analogs that retain the ability to suppress PTH but that are less calcemic and phosphatemic than...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/j.steroids.2008.06.003
更新日期:2008-11-01 00:00:00
abstract::The preparation of 9alpha, 11xi-tritiated 17alpha-ethinyl estradiol, mestranol, estradiol-17beta, and norethindrone are described. Estrone-3-methyl ether was employed as starting material, and ethinylation with lithium acetylide-ethylene diamine resulted in 95% mestranol. Demethylation of mestranol with boron tribro...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/0039-128x(71)90028-6
更新日期:1971-08-01 00:00:00
abstract::A new synthesis of both epimeric forms of 26-cholestanoic acids and 26-alcohols containing a 3beta-hydroxy-Delta(5)- or a Delta(4)-3-keto-functionality in ring A is described starting from stigmasterol or (20S)-3beta-acetoxy-pregn-5-en-20-carboxylic acid. The obtained compounds are useful as standards for studies of c...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/j.steroids.2005.02.014
更新日期:2005-07-01 00:00:00
abstract::13beta-Ethyl-3-methoxy-17beta-ol-8,14-seco-1,3,5(10),8-gonatetraen-14-one (IIIa) was isolated and its participation in the well-known acidic cyclization process was established. ...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/0039-128x(75)90015-x
更新日期:1975-05-01 00:00:00