Abstract:
:Thyroid hormone receptors (TRs) are nuclear receptors that are activated by thyroid hormone ligands and co-regulator proteins. Two receptor subtypes, TRalpha and TRbeta, have been suggested to play a role in numerous physiological functions. However, specificity of receptor subtype function and co-regulator interaction is unclear due to the lack of TR subtype-specific ligands. Five TR ligands were evaluated for their selectivity and interaction with the TR subtypes. A multiplex assay was used to identify co-regulator peptide interaction, and biochemical assays were used to characterize ligand-receptor specificity. In the biochemical assay, rank order ligand potencies were similar in the presence of co-activator peptides, SRC1-2 and SRC3-2, and the co-repressor peptide, NCoR1-2, with T3 and Triac potencies greater in the presence of the co-repressor. The potency of Tetrac was similar regardless of the co-regulator used while T4 and rT3 demonstrated selectivity for TRalpha subtype. The rank order among TR ligands at either receptor subtype in the biochemical assay correlated with the multiplex assay. These assays can be used to identify new ligands that can provide further insight into TR biology.
journal_name
Steroidsjournal_title
Steroidsauthors
Koury EJ,Pawlyk AC,Berrodin TJ,Smolenski CL,Nagpal S,Deecher DCdoi
10.1016/j.steroids.2008.11.014subject
Has Abstractpub_date
2009-02-01 00:00:00pages
270-6issue
2eissn
0039-128Xissn
1878-5867pii
S0039-128X(08)00302-4journal_volume
74pub_type
杂志文章相关文献
STEROIDS文献大全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::Bile acid salts are biosurfactants which form mixed micelles with phospholipids in vertebrates. These mixed micelles are suitable for solubilisation of cholesterol. For therapeutic purposes some bile acid salts as sodium ursocholate are used. However, bile acid anions possess low capacity for solubilisation of cholest...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/j.steroids.2014.04.018
更新日期:2014-08-01 00:00:00
abstract::Endochondral bone formation is a precise and highly ordered process whose exact regulatory framework is still being elucidated. Multiple regulatory pathways are known to be involved. In some cases, regulation impacts gene expression, resulting in changes in chondrocyte phenotypic expression and extracellular matrix sy...
journal_title:Steroids
pub_type: 杂志文章,评审
doi:10.1016/j.steroids.2017.12.003
更新日期:2019-02-01 00:00:00
abstract::The hydrolysis of 108 esters of norethisterone (17 alpha-ethynyl-17 beta-hydroxyestr-4-en-3-one) was studied in vitro using a rabbit liver preparation. Introduction of a double or triple bond into a straight-chain ester did not inhibit hydrolysis but a marked reduction in hydrolysis was produced on replacement of a me...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/0039-128x(83)90110-1
更新日期:1983-03-01 00:00:00
abstract::This paper describes three simple and short methods for the conversion of cholic acid into cholylaldehyde with protected hydroxyl groups. The first method involves lithium aluminum hydride reduction of the tetrahydropyranyl ether of methyl cholate and oxidation of the resulting primary alcohol with pyridinium chloroch...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/0039-128x(82)90140-4
更新日期:1982-06-01 00:00:00
abstract::A mechanistic study on the nucleophilic substitution of a strictly geometric 21-bromo-3alpha-hydroxyl-3beta-methoxymethyl-5alpha-pregnan-20-one was described. Reaction of the alpha-bromoketone with excess lithium imidazole followed by the addition of extra bases including n-butyllithium, methyllithium, lithium piperid...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/j.steroids.2006.07.004
更新日期:2006-11-01 00:00:00
abstract::Given the close resemblance of the ring A structure of prednisolone and prednisone on the one hand, and of androstadienedione on the other, the transformation of cortisol and cortisone into prednisolone and prednisone in cattle faeces was evaluated. A simple method that does not involve extraction but only the 1:100 d...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/j.steroids.2010.01.016
更新日期:2010-04-01 00:00:00
abstract::Steroid hormones are involved in the regulation of a variety of processes like embryonic development, sex differentiation, metabolism, immune responses, circadian rhythms, stress response, and reproduction in vertebrates. Teleost fishes and humans show a remarkable conservation in many developmental and physiological ...
journal_title:Steroids
pub_type: 杂志文章,评审
doi:10.1016/j.steroids.2015.06.011
更新日期:2015-11-01 00:00:00
abstract::Steroid delta 4-5 alpha- and delta 4-5 beta-reductase activity was determined in 16 human mammary tumors and 8 DMBA-induced rat mammary tumors using a spectrophotometric assay. Steroid delta 4-5 alpha-reductase was present in all tumors investigated while delta 4-5 beta-reductase was detected in only 6 estrogen recept...
journal_title:Steroids
pub_type: 历史文章,杂志文章
doi:10.1016/s0039-128x(79)80010-0
更新日期:1979-01-01 00:00:00
abstract::This study examined the role of protein kinase C enzymatic activity as a physiologic determinant of stromal cell death in decidua basalis (DB) during pregnancy. The expression of epidermal growth factor receptor (EGF-R) and Bcl2 was used as an indicator of stromal cell proliferation/survival, whereas Bax and the occur...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/s0039-128x(99)00044-6
更新日期:1999-09-01 00:00:00
abstract::Inhibitors of estrogen 2-hydroxylase can be utilized in studying the kinetics of this cytochrome P450 enzyme complex and in elucidating the structural requirements of the active site. The conversion of estrogens to 2-hydroxyestrogens in rat liver microsomal preparations was examined using two radiotracer assays, the c...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/s0039-128x(83)90120-4
更新日期:1983-07-01 00:00:00
abstract::Six naturally occurring C27 ecdysteroids were isolated and identified from the tobacco hornworm during pupal-adult development five days after peak titer of molting hormone activity. In order of decreasing quantities the hormones were: 20,26-dihydroxyecdysone, 3-epi-20-hydroxyecdysone, 20hydroxyecdysone, 3-epi-20,26-d...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/0039-128x(79)90084-9
更新日期:1979-09-01 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::The first convenient chemical synthesis of 7alpha-hydroxyandrost-4-ene-3,17-dione is reported. Androsta-4,6-diene3, 17-dione was converted into its 6alpha, 7alpha-epoxy-derivative; reduction of the epoxide with aluminum amalgam gave 7alpha-hydroxyandrost-4-ene-3,17-dione. This reducing agent is more efficient than chr...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/s0039-128x(76)90096-9
更新日期:1976-05-01 00:00:00
abstract::Inhibition of 5alpha-reduction of testosterone by an anti-androgen TSAA-291 (16beta-ethyl-17beta-hydroxy-4-estren-3-one) was studied in rat ventral prostates and the metabolic conversion of 3H-TSAA-291 was examined both in vitro and in vivo. In the in vitro experiment using nuclear 5alpha-reductase of the prostate, 5a...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/0039-128x(81)90021-0
更新日期:1981-07-01 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::The formation of a horseradish peroxidase-testosterone conjugate for the enzyme-linked immunoassay of testosterone was investigated, using tritiated testosterone to follow the reaction. The formation of testosterone-3-(carboxymethyl) oxime-peroxidase by the mixed anhydride method was found to give a conjugate of high ...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/0039-128x(77)90021-6
更新日期:1977-05-01 00:00:00
abstract::17beta-estradiol exerts an antiapoptotic action in skeletal muscle cells through extranuclear ERalpha and beta. This protective action, mainly involves a non-genomic mechanism of ERK1/2 and PI3K/Akt activation and BAD phosphorylation. ERbeta plays a major role in the inhibition of apoptosis by 17beta-estradiol at the ...
journal_title:Steroids
pub_type: 杂志文章,评审
doi:10.1016/j.steroids.2007.12.027
更新日期:2008-10-01 00:00:00
abstract::This paper revealed the expression pattern of ERα in the ovoviviparous teleost, Sebastes schlegeli. In this paper, we isolated the cDNA encoding for estrogen receptor alpha of black rockfish (S. schlegeli) from its ovary, named as black rockfish ERα (brfERα). The cDNA sequence of brfERα consists of 2972bp with an open...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/j.steroids.2011.09.014
更新日期:2011-12-20 00:00:00
abstract::While the neuroprotective benefits of estrogen and progesterone in critical illness are well established, the data regarding the effects of androgens are conflicting. Surgical repair of congenital heart disease is associated with significant morbidity and mortality, but there are scant data regarding the postoperative...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/j.steroids.2013.11.003
更新日期:2014-03-01 00:00:00
abstract::Gene therapy based on gene delivery is a promising strategy for the treatment of various human diseases such as cancer. Cationic lipids represent one of the important synthetic gene delivery systems. There is a great interest in imaging of gene therapy using the biomedical imaging technique positron emission tomograph...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/j.steroids.2010.04.009
更新日期:2010-10-01 00:00:00
abstract::The crystal structure of a Li(+) salt of a glucosyl derivative of lithocholic acid (lithium 3α-(α-d-glucopyranosyl)-5β-cholan-24-oate) has been solved. The crystal belongs to the orthorhombic system, P212121 spatial group, and includes acetone and water in the structure with a 1:1:2 stoichiometry. Monolayers, having a...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/j.steroids.2016.07.001
更新日期:2016-09-01 00:00:00
abstract::The synthesis of seco-D and D-homo digitalis derivatives, from the carda-14,20(22)-dienolide 1, is described. Selective ozonolysis gave the seco-D 14-ketoaldehyde 2a. Modification of the two carbonyl groups and of the alpha, beta-unsaturated lactone ring of the seco-D 14-ketoaldehyde 2a allowed preparation of derivati...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/s0039-128x(96)00117-1
更新日期:1996-10-01 00:00:00
abstract::A radioimmunoassay for the quantitation of the sum of free, glucuronidated and urine is described. The method is reliable and accurate. Using this method, urinary excretion of 16 alpha-hydroxyestrone was determined in normal men, premenopausal women, and postmenopausal women. The values were compared to the urinary ex...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/0039-128x(89)90144-x
更新日期:1989-01-01 00:00:00
abstract::A radioimmunoassay technique has been developed for the measurement of cortisol in a single methylene chloride extract of human plasma without chromatography. The antiserum, obtained by immunizing rabbits with cortisol-3-carboxymethyl-oxime conjugated to bovine serum albumin, had a high affinity (KA = 1.8 X 10(9) 1/mo...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/0039-128x(75)90057-4
更新日期:1975-11-01 00:00:00
abstract::Three protein fractions of the cytosol of the chick parathyroid glands, which had the sedimentation constants of 2.5 S, 3.7 S and 5.5 S, were found to bind with 1 alpha,25-dihydroxyvitamin D3. Among these proteins, the 3.7 S protein was assumed to be the specific receptor protein. The 3.7 S receptor protein was also ...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/0039-128x(82)90125-8
更新日期:1982-01-01 00:00:00
abstract::Dioscorea panthaica is a traditional Chinese medicinal herb used in the treatment of various physiological conditions, including cardiovascular disease, gastropathy and hypertension. Steroidal saponins (SS) are the main active ingredients of this herb and have effects on myocardial ischemia and cancer. The phytochemic...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/j.steroids.2014.12.023
更新日期:2015-03-01 00:00:00
abstract::A variety of compounds, including the selective estrogen receptor (ER) modulators tamoxifen and raloxifene, phytoestrogens such as genistein, and xenoestrogens such as bisphenol, bind to the estrogen receptor and elicit biological responses. Structural studies have linked the altered activity of compounds such as 4-hy...
journal_title:Steroids
pub_type: 杂志文章,评审
doi:10.1016/j.steroids.2004.03.014
更新日期:2004-06-01 00:00:00
abstract::A radioimmunological method was developed for determining total and free corticosterone in rat plasma. This method was used to determine the dose-response curve of corticosterone and to measure the elimination and study the half-lives of total and free corticosterone in rat plasma with a dose of 5 mg/kg. The eliminati...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/0039-128x(88)90056-6
更新日期:1988-05-01 00:00:00
abstract::A number of progesterone derivatives, having a 17 alpha-acetoxy group and various functions at C-3 and C-6, interact at the cardiac glycoside (CG) binding site, using [3H]ouabain in a radioligand binding assay (RBA) with membranes from dog myocardium. We now report on results of structure-activity studies concerned wi...
journal_title:Steroids
pub_type: 杂志文章
doi:10.1016/0039-128x(87)90012-2
更新日期:1987-04-01 00:00:00