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 has recently been determined in complex with its natural substrate androstenedione in the high-spin ferric state of heme. Hydrogen bond forming interactions and tight packing hydrophobic side chains closely complement puckering of the steroid backbone, thereby providing the molecular basis for the androgenic specificity of aromatase. In the crystal, aromatase molecules are linked by a head-to-tail intermolecular interaction via a surface loop between helix D and helix E of one aromatase molecule that penetrates the heme-proximal cavity of the neighboring, crystallographically related molecule, thus forming in tandem a polymeric aromatase chain. This intermolecular interaction is similar to the aromatase-cytochrome P450 reductase coupling and is driven by electrostatics between the negative potential surface of the D-E loop region and the positively charged heme-proximal cavity. This loop-to-proximal site link in aromatase is rather unique--there are only a few of examples of somewhat similar intermolecular interactions in the entire P450 structure database. Furthermore, the amino acids involved in the intermolecular contact appear to be specific for aromatase. Higher order organization of aromatase monomers may have implications in lipid integration and catalysis.
journal_name
Steroidsjournal_title
Steroidsauthors
Ghosh D,Jiang W,Lo J,Egbuta Cdoi
10.1016/j.steroids.2011.02.030subject
Has Abstractpub_date
2011-07-01 00:00:00pages
753-8issue
8eissn
0039-128Xissn
1878-5867pii
S0039-128X(11)00070-5journal_volume
76pub_type
杂志文章相关文献
STEROIDS文献大全abstract：:20S-hydroxyvitamin D3 (20S-(OH)D3), an in vitro product of vitamin D3 metabolism by the cytochrome P450scc, was recently isolated, identified and shown to possess antiproliferative activity without inducing hypercalcemia. The enzymatic production of 20S-(OH)D3 is tedious, expensive, and cannot meet the requirements fo...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/j.steroids.2010.05.021
更新日期：2010-12-01 00:00:00
abstract：:Nucleocytoplasmic shuttling of glucocorticoid receptors (GRs) is disrupted in v-mos-transformed cells leading to the redistribution of hormone-bound receptors from the nuclear to cytoplasmic compartments. We show here that GRs from v-mos-transformed cells are hyperphosphorylated on a specific peptide and maintain horm...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/0039-128x(94)00068-n
更新日期：1995-05-01 00:00:00
abstract：:The syntheses of 15beta-carboxyethylmercapto-5alpha-dihydrotestosterone, 15beta-carbosyethylmercapto-5alpha-androstane-3beta, 17beta-diol and 15beta-carboxyethylmercapto-5alpha-androstane-3alpha, 17beta-diol and the preparation of their bovine serum albumin (BSA) conjugates are described. These conjugates were employe...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/0039-128x(77)90037-x
更新日期：1977-02-01 00:00:00
abstract：:Data in animal models and surveys in humans have revealed psychiatric complications of long-term anabolic androgenic steroid abuse. However, the neurobiochemical mechanisms behind the observed behavioral changes are poorly understood. The aim of the present study was to investigate the effects of nandrolone decanoate ...
journal_title：Steroids
pub_type： 杂志文章
doi：
更新日期：2014-01-01 00:00:00
abstract：:A heretofore unknown metabolite of vitamin D3 was isolated from the 1 alpha, 24, 25-trihydroxyvitamin D3 fraction of lipid extracts obtained from plasma of rats which were given intravenous or oral doses of 100 pmol/100 g of either 1 alpha-hydroxyvitamin D3 or 1 alpha, 23-dihydroxyvitamin D3. Doses of 25-250 pmoles of...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/0039-128x(80)90065-3
更新日期：1980-07-01 00:00:00
abstract：:Progesterone and its polar metabolite(s) trigger the meiotic divisions in the amphibian oocyte through a non-genomic signaling system at the plasma membrane. Published site-directed mutagenesis studies of ouabain binding and progesterone-ouabain competition studies indicate that progesterone binds to a 23 amino acid e...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/j.steroids.2012.04.012
更新日期：2012-09-01 00:00:00
abstract：:Brassinosteroids (BRs) control several important agronomic traits, such as strengthening resistance to diverse adversity, improving the quality, and increasing crop yield. Their chemical structures and varieties, specific methods for the evaluation of bioactivities, structure-activity relationships, potential novel co...
journal_title：Steroids
pub_type： 杂志文章,评审
doi：10.1016/j.steroids.2017.05.005
更新日期：2017-08-01 00:00:00
abstract：:Using beta-sitosterol as a starting material, (6E)-hydroximino-24-ethylcholest-4-en-3-one (1), a natural steroidal oxime from Cinachyrella alloclada and C. apion, was synthesized in four steps with a high overall yield. First, beta-sitosterol (5a) is transformed into the corresponding 24-ethylcholest-4-en-3,6-dione (6...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/j.steroids.2007.10.007
更新日期：2008-03-01 00:00:00
abstract：:A novel epoxy sterol isolated from the marine mollusc Planaxis sulcatus has been identified as 9 alpha,11 alpha-epoxycholest-7-ene-3 beta,5 alpha,6 beta-triol by spectrometric methods. ...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/0039-128x(88)90216-4
更新日期：1988-07-01 00:00:00
abstract：:1,25-Dihydroxyvitamin D(3) (1,25D) regulates gene transcription through a nuclear vitamin D receptor (VDR) which acts as a ligand-regulated transcription factor. Some structural vitamin D analogs (VDAs) are selective in their biological actions, because they retain cell-differentiating potential, while their calcemic ...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/j.steroids.2008.06.010
更新日期：2008-12-22 00:00:00
abstract：:A series of final twelve propanoyloxy derivatives of 5β-cholan-24-oic acid (O-propanoyl derivatives of cholic acid) as potential drug absorption modifiers (skin penetration enhancers, intestinal absorption promoters) was generated by multistep synthesis. Structure confirmation of all generated compounds was accomplish...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/j.steroids.2013.02.001
更新日期：2013-05-01 00:00:00
abstract：:Glycyrrhizic acid (GZA) and glycyrrhetinic acid (GRA) can be determined rapidly and precisely by high-performance liquid chromatography (HPLC) in biological fluids and tissues from experimental animals and humans. From plasma and tissues, GZA and GRA are extracted by organic solvents and the extracts can directly be u...
journal_title：Steroids
pub_type： 杂志文章,评审
doi：10.1016/0039-128x(94)90088-4
更新日期：1994-02-01 00:00:00
abstract：:The applications of sterically crowed trialkyksilyl ether derivatives to the analysis and characterization by thin-layer chromatography, gas chromatography and mass spectrometry, of metabolites of 2alpha, 3alpha-cyclopropano-5alpha-androstan-17beta-ol in the rabbit are described. These derivatives are complementary to...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/0039-128x(77)90013-7
更新日期：1977-05-01 00:00:00
abstract：:Using 1 alpha,2 alpha-oxido-cholesta-5,7-diene-3 beta,25-diol (2) as a starting material, the provitamins of calcitriol with an additional 2 beta-chloro-, 2 beta-fluoro-, and 2 beta-methoxy-substituent (3,4,5) are obtained by transdiaxial opening of the oxirane ring with nucleophiles. An efficient irradiation process ...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/s0039-128x(98)00072-5
更新日期：1998-12-01 00:00:00
abstract：:Neutral steroids are difficult to analyse using desorption ionisation methods coupled with mass spectrometry (MS). However, steroids with an unhindered ketone group can readily be derivatised with the Girard P (GP) reagent to give GP hydrazones. Steroid GP hydrazones contain a quaternary nitrogen atom and are readily ...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/j.steroids.2005.08.002
更新日期：2006-01-01 00:00:00
abstract：:The effect of cortisol and prostaglandin inhibitors on the growth and development of germinating mung bean, Vigna radiata L. Wilzek, cv. Jumbo was investigated. Cortisol, indomethacin, and a mixture of cortisol with aspirin, or benoxaprofen significantly increased radicle length and the number of lateral roots as comp...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/0039-128x(85)90052-2
更新日期：1985-08-01 00:00:00
abstract：:(24R and 24S)-5beta-cholestane-3alpha,7alpha,24,25-tetrols were prepared by osmium tetroxide oxidation of 5beta-cholest-24-ene-3alpha,7alpha-diol. The resulting diastereomeric tetrols were separated by thin-layer chromatography, their purity ascertained by melting point, gas-liquid chromatography and mass spectra and ...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/0039-128x(78)90022-3
更新日期：1978-01-01 00:00:00
abstract：BACKGROUND:Congenital adrenal hyperplasia (CAH) caused by 21-hydroxylase deficiency (21OHD) is an autosomal recessive disorder due to mutation in the CYP21A2 gene. OBJECTIVE:To elucidate the genetic basis of 21-hydroxylase-deficient CAH in Hong Kong Chinese patients. PATIENTS AND METHODS:Mutational analysis of the CY...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/j.steroids.2011.04.010
更新日期：2011-09-01 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：:A new spirostane steroidal saponin, govanoside A (1) along with three known compounds borassoside E (2) pennogenin (3) and diosgenin (4) were isolated from rhizomes of Trillium govanianum. Their structures were elucidated through 1D, 2D-NMR spectroscopic data analysis and acid hydrolysis. Compound (2) in genus Trilliu...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/j.steroids.2015.10.013
更新日期：2015-12-01 00:00:00
abstract：:Dehydroepiandrosterone (DHEA) is a multifunctional steroid with a broad range of biological effects in humans and animals. DHEA can be converted to multiple oxygenated metabolites in the brain and peripheral tissues. The mechanisms by which DHEA exerts its effects are not well understood. However, evidence that the ef...
journal_title：Steroids
pub_type： 杂志文章,评审
doi：10.1016/j.steroids.2011.09.008
更新日期：2012-01-01 00:00:00
abstract：:In the present study, synthesis and antineoplastic activity of phenylacetic acid and benzoic acid nitrogen mustard conjugates of various steroidal oximes are reported for the first time. The conjugation was achieved through a more stable oxime-ester linkage and the resulting newly synthesized conjugates were evaluated...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/j.steroids.2017.04.005
更新日期：2017-07-01 00:00:00
abstract：:There are currently two main candidates for the membrane receptor for 1,25(OH)2D3: the 1,25D3-MARRS protein/ERp57; and the classical VDR. The 1,25D3-MARRS protein is essential for hormone-stimulated phosphate and calcium uptake in chick intestinal cells, whereas the VDR is not. The 1,25D3-MARRS protein also shows a hi...
journal_title：Steroids
pub_type： 杂志文章,评审
doi：10.1016/j.steroids.2005.02.005
更新日期：2005-05-01 00:00:00
abstract：BACKGROUND AND AIMS:Calcitriol, an active vitamin D metabolite, has a limited application in bone repair because of its undesirable hypercalcaemic action. However it has emerged that lithocholic acid (LCA) is a non-calcaemic vitamin D receptor ligand but whether this steroid can support osteoblast maturation has not be...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/j.steroids.2009.07.005
更新日期：2009-11-01 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：:The adverse effects of hypercortisolism on the human brain have been highlighted in previous studies of Cushing's disease (CD). However, the reversibility of brain damage after the resolution of hypercortisolism remains unclear. Thus, we studied the potential volumetric reversibility in biochemically remitted CD patie...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/j.steroids.2019.108457
更新日期：2019-11-01 00:00:00
abstract：:Key to the production of biologically active steroids is the enzyme 3 beta-hydroxysteroid dehydrogenase-isomerase. Some controversy has arisen concerning the subcellular distribution of this enzyme within steroidogenic cells. The distribution of 3 beta-hydroxysteroid dehydrogenase-isomerase was assessed in subcellular...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/0039-128x(91)90056-2
更新日期：1991-06-01 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：:Traditional interpretation of GC-MS output involved the semi-quantitative estimation of outstanding low or high specific metabolites and the ratio between metabolites. Here, we utilize a systems biology approach to steroid metabolomics of a complex steroid-related disorder, using an all-inclusive analysis of the stero...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/j.steroids.2014.07.003
更新日期：2014-10-01 00:00:00
abstract：:It has been previously demonstrated that 1,25 dihydroxyvitamin D(3) (1,25-D(3)) exerts inhibitory effects in breast cancer cells. The aim of this study was to determine whether mitogen-activated protein kinase (MAPK) pathways are associated with 1,25-D(3)-induced cell death in breast cancer. We used three breast cell ...
journal_title：Steroids
pub_type： 杂志文章
doi：10.1016/j.steroids.2010.07.007
更新日期：2010-12-12 00:00:00
