Androgen receptor isoforms AR-A and AR-B display functional differences in cultured human bone cells and genital skin fibroblasts.

Abstract:

:Two isoforms of the androgen receptor (AR-A and AR-B), differing by a lack of the first 187 amino acids in the NH2-terminal transactivation domain of AR-A, are expressed in connective tissue and bone. Transient transfections of normal human osteoblastic cells (HOB) and of genital skin fibroblasts defective in AR (GSF-540) were utilized to compare the functional properties of AR isoforms in mesenchymal tissues. Overexpression of AR-B or AR-A did not significantly affect type I collagen secretion. However, overexpression of AR-B (but not AR-A) restored androgen-dependent DNA synthesis in AR-defective fibroblasts and increased DHT-mediated DNA synthesis three-fold in osteoblastic cells. Overexpression of AR-A did not affect DHT action but reduced DHT-dependent DNA synthesis when transfected together with AR-B. The need for an NH2-terminal sequence of the AR for complete receptor function was demonstrated using electrophoretic mobility shift assay. A peptide coding for the amino terminus of the complete AR was able to decrease the binding affinity of AR-B and increase the binding affinity of AR-A to the androgen response element. Our results suggest that AR-A lacks the ability to stimulate cell proliferation possibly due to reduced binding of AR co-activating proteins to the truncated N-terminal transactivation domain rather than due to impaired stability of the AR-A isoform.

journal_name

Steroids

journal_title

Steroids

authors

Liegibel UM,Sommer U,Boercsoek I,Hilscher U,Bierhaus A,Schweikert HU,Nawroth P,Kasperk C

doi

10.1016/j.steroids.2003.08.016

subject

Has Abstract

pub_date

2003-12-01 00:00:00

pages

1179-87

issue

14

eissn

0039-128X

issn

1878-5867

pii

S0039128X03001831

journal_volume

68

pub_type

杂志文章

相关文献

STEROIDS文献大全
  • Cytotoxic 9,11-secosteroids from the South China Sea gorgonian Subergorgia suberosa.

    abstract::Ten new 9,11-secosteroids, subergorgols A-J (1-10), including two pairs of epimers (3/4, and 6/7), along with three known analogues (11-13) were isolated from the South China Sea gorgonian Subergorgia suberosa. The structures of these compounds were elucidated on the basis of extensive spectroscopic analyses and compa...

    journal_title:Steroids

    pub_type: 杂志文章

    doi:10.1016/j.steroids.2013.05.009

    authors: Zhang G,Tang X,Cheng C,Gong K,Zhang X,Zhu H,Wu R,Li P,Li G

    更新日期:2013-09-01 00:00:00

  • Highly sensitive determination of estrone and estradiol in human serum by liquid chromatography-electrospray ionization tandem mass spectrometry.

    abstract::A highly sensitive and specific quantification method of estrone and estradiol in human serum was described based upon the use of picolinoyl derivatization and liquid chromatography-electrospray ionization mass spectrometry (LC-ESI-MS) in a positive mode. Estrogens were treated with picolinoyl chloride hydrochloride o...

    journal_title:Steroids

    pub_type: 杂志文章

    doi:10.1016/j.steroids.2007.07.003

    authors: Yamashita K,Okuyama M,Watanabe Y,Honma S,Kobayashi S,Numazawa M

    更新日期:2007-10-01 00:00:00

  • Progesterone inhibition of voltage-gated calcium channels is a potential neuroprotective mechanism against excitotoxicity.

    abstract::The therapeutic use of progesterone following traumatic brain injury has recently entered phase III clinical trials as a means of neuroprotection. Although it has been hypothesized that progesterone protects against calcium overload following excitotoxic shock, the exact mechanisms underlying the beneficial effects of...

    journal_title:Steroids

    pub_type: 杂志文章

    doi:10.1016/j.steroids.2011.02.013

    authors: Luoma JI,Kelley BG,Mermelstein PG

    更新日期:2011-08-01 00:00:00

  • 1H and 13C NMR characteristics of synthetic derivatives of steroid sapogenins. Part III. 16Beta,23:23,26-diepoxy side chains.

    abstract::The full assignments of the (1)H and (13)C NMR signals of steroids bearing the 16beta,23:23,26-diepoxy side chain are provided. Differentiation of the diasterotopic H-26 pair was achieved with the aid of NOESY experiments. The main substituent and steric effects associated with this moiety and their influence on the c...

    journal_title:Steroids

    pub_type: 杂志文章

    doi:10.1016/j.steroids.2008.01.027

    authors: Vázquez-Ramírez I,Macías-Alonso M,Arcos-Ramos RO,Ruíz-Pérez KM,Solano-Ramírez DO,Iglesias Arteaga MA

    更新日期:2008-07-01 00:00:00

  • Taccasubosides A-D, four new steroidal glycosides from Tacca subflabellata.

    abstract::By analyzing the steroidal content of fresh whole plants of Tacca subflabellata (Taccaceae), we isolated one sapogenin and eight glycosides with four kinds of steroidal skeletons including four new glycosides, named taccasubosides A-D (1-4), together with five known compounds. Among them, compound 1 is the first penta...

    journal_title:Steroids

    pub_type: 杂志文章

    doi:10.1016/j.steroids.2011.04.003

    authors: Li L,Ni W,Li XR,Hua Y,Fang PL,Kong LM,Pan LL,Li Y,Chen CX,Liu HY

    更新日期:2011-09-01 00:00:00

  • Synthesis of 13,14-secotestosterone derivatives.

    abstract::A number of testosterone analogs with a 13,14-secosteroidal fragment have been prepared from (13S)-13-iodo-6beta-methoxy-3alpha, 5-cyclo-13,14-seco-5alpha-androstan-14,17-dione. The key steps involved stereoselective deiodination of the starting compound with triphenylphosphine and selective protection of the 17-keto ...

    journal_title:Steroids

    pub_type: 杂志文章

    doi:10.1016/j.steroids.2004.04.010

    authors: Khripach VA,Zhabinskii VN,Kuchto AI,Zhiburtovich YY,Fando GP,Lyakhov AS,Govorova AA,Groen MB,van der Louw J,de Groot A

    更新日期:2004-07-01 00:00:00

  • Novel action of estrone on vascular tissue: regulation of NOS and COX activity.

    abstract::The hypothesis tested in the present work is that estrone non-genomically regulates aortic nitric oxide synthase (NOS) and cyclooxygenase (COX) activities in female rats, and that such regulation depends on ovarian function. We found that physiological concentrations of estrone (E(1)) (0.1-10nM) significantly increase...

    journal_title:Steroids

    pub_type: 杂志文章

    doi:10.1016/j.steroids.2004.10.012

    authors: Selles J,Polini N,Alvarez C,Massheimer V

    更新日期:2005-04-01 00:00:00

  • The use of 6alpha-and 6beta-carboxymethyl testosterone-bovine serum albumin conjugates in radioimmunoassay for testosterone.

    abstract::The synthesis of 6alpha- and 6beta-testosterone-bovine serum albumin (BSA) conjugates is described. 6beta-Carboxymethyl-4-androstene-3,17-dione was prepared by a route analogous to that described earlier for 6beta-carboxymethyl progesterone. Sodium borohydride reduction of the 3 and 17 keto groups and subsequent selec...

    journal_title:Steroids

    pub_type: 杂志文章

    doi:10.1016/s0039-128x(75)80004-3

    authors: Jones CD,Mason NR

    更新日期:1975-01-01 00:00:00

  • Design, synthesis and biological evaluation of novel 5α, 8α-endoperoxide steroidal derivatives with hybrid side chain as anticancer agents.

    abstract::A series of novel 5α, 8α-endoperoxide steroidal hybrid derivatives containing isatin or indole substituents on the C-17 side chain were synthesized and characterized. The preliminary anti-proliferative activity of the compounds against HepG2, MCF-7, HT-29 and HeLa cell lines were investigated. Compounds 7g and 7l disp...

    journal_title:Steroids

    pub_type: 杂志文章

    doi:10.1016/j.steroids.2019.108471

    authors: Li H,Wang H,Wang J,Lin Y,Ma Y,Bu M

    更新日期:2020-01-01 00:00:00

  • Distribution and metabolism of F6-1,25(OH)2 vitamin D3 and 1,25(OH)2 vitamin D3 in the bones of rats dosed with tritium-labeled compounds.

    abstract::26,26,26,27,27,27-Hexafluo-1,25(OH)2 vitamin D3, the hexafluorinated analog of 1,25(OH)2 vitamin D3, has been reported to be several times more potent than the parent compound regarding some vitamin D actions. The reason for enhanced biologic activity in the kidneys and small intestine appears to be related to F6-1,25...

    journal_title:Steroids

    pub_type: 杂志文章

    doi:10.1016/s0039-128x(98)00055-5

    authors: Komuro S,Kanamaru H,Nakatsuka I,Yoshitake A

    更新日期:1998-10-01 00:00:00

  • Hyfraxins A and B, cytotoxic ergostane-type steroid and lanostane triterpenoid glycosides from the invasive ash dieback ascomycete Hymenoscyphus fraxineus.

    abstract::A virulent culture of Hymenoscyphus fraxineus, the causal agent of ash dieback, was investigated for its production of secondary metabolites in a 70 L batch fermentation. Chemical analysis of the mycelial extract by means of flash chromatography and preparative HPLC led to the isolation of a new ergostane-type steroid...

    journal_title:Steroids

    pub_type: 杂志文章

    doi:10.1016/j.steroids.2018.03.007

    authors: Surup F,Halecker S,Nimtz M,Rodrigo S,Schulz B,Steinert M,Stadler M

    更新日期:2018-07-01 00:00:00

  • Synthesis and biological evaluation of novel sarsasapogenin derivatives as potential anti-tumor agents.

    abstract::Based on the fact that timosaponin A-III (TA-III) exhibits potent cytotoxic effects and has been considered as a potential anti-tumor agent, a range of novel sarsasapogenin derivatives 1, 2a-2g, 3, 4, 5, 6a-6g have been synthesized by a simple and facile synthetic route. The in vitro cytotoxic activity of these synthe...

    journal_title:Steroids

    pub_type: 杂志文章

    doi:10.1016/j.steroids.2014.09.007

    authors: Yin Y,Zhao XC,Wang SJ,Gao PY,Li LZ,Ikejima T,Song SJ

    更新日期:2015-01-01 00:00:00

  • Insulin alters the effects of follicle stimulating hormone on aromatase in bovine granulosa cells in vitro.

    abstract::It is known that follicle-stimulating hormone (FSH) and insulin stimulate estradiol secretion from cultured non-luteinizing granulosa cells. The interaction between these hormones is less well understood. Granulosa cells from small (2-4 mm) bovine follicles were cultured in serum-free medium to determine if cytochrome...

    journal_title:Steroids

    pub_type: 杂志文章

    doi:10.1016/s0039-128x(00)00218-x

    authors: Bhatia B,Price CA

    更新日期:2001-06-01 00:00:00

  • Mass spectrometry and stability of t-butyldimethylsilylethers of some estrogens and androstanes.

    abstract::In addition to using radioimmunoassays for the determination of estrogens and other steroids, the possibility of using mass fragmentography for analysis was investigated. t-Butyldimethylsilyl chloride was selected as a reagent for derivatisation because it forms rather stable silylethers. In all the mass-spectra obrai...

    journal_title:Steroids

    pub_type: 杂志文章

    doi:10.1016/0039-128x(79)90013-8

    authors: Ballhorn L,Mueller WF,Korte F

    更新日期:1979-04-01 00:00:00

  • Cation channels are involved in brassinosteroid signalling in higher plants.

    abstract::Brassinosteroids (BRs) are an important class of plant hormones with a multitude of functions. They have been intensively investigated for their biosynthesis, distribution and physiological functions. The aim of this study was to examine possible effects of BRs on the plant plasma membrane cation conductances and Ca(2...

    journal_title:Steroids

    pub_type: 杂志文章

    doi:10.1016/j.steroids.2014.10.008

    authors: Straltsova D,Chykun P,Subramaniam S,Sosan A,Kolbanov D,Sokolik A,Demidchik V

    更新日期:2015-05-01 00:00:00

  • Uptake and metabolism of androgens by bovine spermatozoa.

    abstract::Spermatozoa from bovine ejaculates and cauda epiditymidis were incubated with either tritiated 17 beta-hydroxy-5 alpha-androstane-3-one (DHT) or 5 alpha-androstane-3 alpha, 17 beta-diol (3 alpha-diol). Examination of the medium incubations demonstrated metabolic conversion of both DHT and 3 alpha-diol when these steri...

    journal_title:Steroids

    pub_type: 杂志文章

    doi:10.1016/0039-128x(78)90045-4

    authors: Djöseland O,Høglo S,Nyberg K,Hastings CD,Attramadal A

    更新日期:1978-03-01 00:00:00

  • Inhibition of 3beta-hydroxysteroid dehydrogenase-isomerase in mouse adrenal cells: a direct effect of testosterone.

    abstract::Gonadal steroids modulate adrenal gland size and function in a variety of species, and our previous studies demonstrate that circulating androgens suppress 3beta-hydroxysteroid dehydrogenase-isomerase (3betaHSD) activity in the adrenal cortex of male mice. The present study tests the hypothesis that androgens have a d...

    journal_title:Steroids

    pub_type: 杂志文章

    doi:10.1016/s0039-128x(02)00023-5

    authors: Stalvey JR

    更新日期:2002-07-01 00:00:00

  • Major cardiac surgery induces an increase in sex steroids in prepubertal children.

    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

    authors: Heckmann M,d'Uscio CH,de Laffolie J,Neuhaeuser C,Bödeker RH,Thul J,Schranz D,Frey BM

    更新日期:2014-03-01 00:00:00

  • 17 Beta-hydroxysteroid dehydrogenase in human breast cancer: analysis of kinetic and clinical parameters.

    abstract::In this study, we assessed the rate of estradiol degradation via the 17 beta-hydroxysteroid dehydrogenase (HSD) enzyme in breast tumors from postmenopausal women. We initially studied the effects of time, level of enzyme activity, amount of tissue assayed, and substrate concentration on the linearity of conversion of ...

    journal_title:Steroids

    pub_type: 杂志文章

    doi:10.1016/0039-128x(88)90020-7

    authors: Leszczynski D,Santner SJ,Feil PD,Santen RJ

    更新日期:1988-03-01 00:00:00

  • The synthesis of cholesteryl alkyl ethers.

    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

    authors: Halperin G,Gatt S

    更新日期:1980-01-01 00:00:00

  • Human mammary tumor cell proliferation: primary role of platelet-derived growth factor and possible synergism with human alpha-fetoprotein.

    abstract::Human mammary medullary carcinoma cells (passages 16 to 21) were cultured for 2 days to allow for attachment, followed by 6 days of culture in either fetal calf serum, human cord blood, human amniotic fluid, or growth factors in the presence or absence of purified human alpha-fetoprotein (AFP). When growth factors wer...

    journal_title:Steroids

    pub_type: 杂志文章

    doi:10.1016/0039-128x(91)90042-t

    authors: Leal JA,Gangrade BK,Kiser JL,May JV,Keel BA

    更新日期:1991-05-01 00:00:00

  • Clickable conjugates of bile acids and nucleosides: Synthesis, characterization, in vitro anticancer and antituberculosis studies.

    abstract::A series of clickable bile acid-nucleosides conjugates linked directly or via amino acid linker were synthesized, and characterized by spectroscopic techniques such as 1H NMR, 13C NMR, FT-IR, HRMS and HPLC. The synthesized compounds 6a-p were screened for their in vitro anticancer property against a panel of three can...

    journal_title:Steroids

    pub_type: 杂志文章

    doi:10.1016/j.steroids.2018.09.006

    authors: Agarwal DS,Siva Krishna V,Sriram D,Yogeeswari P,Sakhuja R

    更新日期:2018-11-01 00:00:00

  • Characterization of new conjugated metabolites in bile of rats administered 24,25-dihydroxyvitamin D(3) and 25-hydroxyvitamin D(3).

    abstract::The characterization of new conjugated vitamin D metabolites in rat bile was performed using HPLC, liquid chromatography/tandem mass spectrometry combined derivatization, and GC-MS. After the administration of 24,25-dihydroxyvitamin D(3) to rats, 23, 25-dihydroxy-24-oxovitamin D(3) 23-glucuronide, 3-epi-24, 25-dihydro...

    journal_title:Steroids

    pub_type: 杂志文章

    doi:10.1016/s0039-128x(00)00087-8

    authors: Higashi T,Miura K,Kikuchi R,Shimada K,Hiyamizu H,Ooi H,Iwabuchi Y,Hatakeyama S,Kubodera N

    更新日期:2000-05-01 00:00:00

  • Catalytic cyclometallation in steroid chemistry IV: Efficient method for the synthesis of tetrahydrothiophene, tetrahydroselenophen and cyclopentanone derivatives of (5α)-cholestane.

    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

    authors: D'yakonov VA,Tuktarova RA,Islamov II,Khalilov LM,Dzhemilev UM

    更新日期:2016-04-01 00:00:00

  • Synthesis of ursodeoxycholic acid from plant-source (20S)-21-hydroxy-20-methylpregn-4-en-3-one.

    abstract::A novel synthetic route of producing ursodeoxycholic acid (UDCA) was developed through multiple reactions from cheap and commercially available bisnoralcohol (BA). The key reaction conditions, including solvents, bases and reaction temperatures of the route were investigated and optimized. In the straightforward route...

    journal_title:Steroids

    pub_type: 杂志文章

    doi:10.1016/j.steroids.2020.108600

    authors: Wang J,Gu XZ,He LM,Li CC,Qiu WW

    更新日期:2020-05-01 00:00:00

  • New synthetic strategy for the synthesis of 24-epibrassinolide.

    abstract::The synthesis of (22E,24R)-5 alpha-ergosta-2,22-dien-6-one (2), a key intermediate to the preparation of 24-epibrassinolide (1), was achieved through the 3,6-diketone 8 in a 40% overall yield in five steps starting from ergosterol (3). ...

    journal_title:Steroids

    pub_type: 杂志文章

    doi:10.1016/s0039-128x(96)00087-6

    authors: Brosa C,Puig R,Comas X,Fernández C

    更新日期:1996-09-01 00:00:00

  • Hydroxysteroid sulfotransferase activity in the rat brain and liver as a function of age and sex.

    abstract::The high concentrations of dehydroepiandrosterone sulfate and pregnenolone sulfate in the mammalian brain, despite the blood-brain barrier's impermeability to these compounds, and the apparent independence of these concentrations from those in plasma prompted us to investigate whether enzymatic sulfation of dehydroepi...

    journal_title:Steroids

    pub_type: 杂志文章

    doi:10.1016/s0039-128x(97)00013-5

    authors: Rajkowski KM,Robel P,Baulieu EE

    更新日期:1997-05-01 00:00:00

  • Steroids and oxygen solubility.

    abstract::Determinations of oxygen solubility in serum were made utilizing various concentrations of corticosteroids in the serum. Within a certain concentration range dexamethasone and betamethasone caused an increase in oxygen solubility. None of the other steroids tested demonstrated this property. ...

    journal_title:Steroids

    pub_type: 杂志文章

    doi:10.1016/0039-128x(76)90041-6

    authors: Gainer JL,Kelly R

    更新日期:1976-09-01 00:00:00

  • Evidence for macromolecular synthesis in stimulation of the estrogen synthesizing system of the immature rat ovary by PMS.

    abstract::Exposure of immature rat ovaries to pregnant mare's serum gonadotropin (PMS) results in a prompt increase in testosterone and progesterone output but synthesis of estradiol (E2) increases only after a lag period of several hours. Actinomycin D (Act-D) given with PMS did not inhibit testosterone or progesterone product...

    journal_title:Steroids

    pub_type: 杂志文章

    doi:10.1016/0039-128x(77)90004-6

    authors: Soewoto H,Cheng HC,Johnson DC

    更新日期:1977-03-01 00:00:00

  • Development of a new sensitive and specific time-resolved fluoroimmunoassay (TR-FIA) of chlormadinone acetate in the serum of treated menopausal women.

    abstract::We describe the development of a serum chlormadinone acetate (CMA) time-resolved fluoroimmunoassay (TR-FIA). We prepared haptens (3-CMO-chlormadinone acetate and 6-chloropregna-4,6-dien-17,20-diol-3-one-20-hemisuccinate), biotinylated tracers (3(biotinylaminopropylamido) 3-CMO-chlormadinone acetate and 3-(6-chloropreg...

    journal_title:Steroids

    pub_type: 临床试验,杂志文章

    doi:10.1016/s0039-128x(02)00050-8

    authors: Fiet J,Giton F,Auzerie J,Galons H

    更新日期:2002-12-01 00:00:00