Abstract：
:Androgen receptor mRNA was translated in vitro, and androgen- and antiandrogen-bound receptor complexes were studied using limited proteolytic digestion by trypsin. Partial proteolysis of androgen-bound receptor protein resulted in a 29-kDa proteolysis-resisting fragment, whereas antiandrogen binding stabilised a 35-kDa fragment. Both fragments contain the entire ligand binding domain, and the 35-kDa fragment extended into the hinge region of the receptor. Several antiandrogens show agonistic properties for a mutated androgen receptor (LNCaP cell variant); trypsin digestion of antiandrogen-bound mutated receptor also resulted in a 29-kDa fragment. Our results point to an important difference between antiandrogens and antagonists of other steroid hormone receptors. Antiandrogens result in protection of both the hinge region and C-terminus of the androgen receptor agonist proteolytic attack, whereas other studies showed that antiestrogens and antiprogestagens expose the C-terminal end of the ligand binding domain of their respective receptors to protease. Differences in conformation of the hinge region distinguish androgen-bound from antiandrogen-bound receptor complexes, which represents an important feature of antiandrogen action.
journal_name
Mol Cell Endocrinoljournal_title
Molecular and cellular endocrinologyauthors
Kuil CW,Mulder Edoi
10.1016/0303-7207(94)90112-0subject
Has Abstractpub_date
1994-06-01 00:00:00pages
R1-5issue
1-2eissn
0303-7207issn
1872-8057pii
0303-7207(94)90112-0journal_volume
102pub_type
杂志文章abstract：:Two cAMP-dependent protein kinase activities can be separated from rat thyroid cytosol. Their elution properties during the gel chromatography, as well as their sedimentation coefficients after sucrose-gradient ultracentrifugation and their capacity to dissociate in the presence of histones, suggest they are like the ...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/0303-7207(79)90102-3
更新日期：1979-05-01 00:00:00
abstract：:The binding of vasopressin, angiotensin II and prazosin (alpha 1-adrenergic antagonist) to purified heavy (GH) and (intermediate + light) (GI + L) rat liver Golgi fractions was studied. The three types of ligands showed a saturable and specific binding in Golgi fractions; the maximal specific binding of [3H]vasopressi...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/0303-7207(87)90119-5
更新日期：1987-05-01 00:00:00
abstract：:The role of estrogens produced by the testis may involve negative feedback regulation of androgen biosynthesis. Estrogens are also associated with contractile processes of seminiferous tubules, and might have mitogenic effects on Sertoli and Leydig cells. To investigate the location of aromatase (estrogen synthetase) ...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/s0303-7207(01)00444-0
更新日期：2001-06-10 00:00:00
abstract：:Using a combination of in vitro assays we have evaluated whether DDT metabolites can interact with the progesterone receptor pathway in yeast expressing human progesterone receptor (hPR) and in T47D human breast cancer cells which express endogenous hPR. In transactivation assays using both yeast and T47D cells, o,p'-...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/s0303-7207(96)04041-5
更新日期：1997-04-25 00:00:00
abstract：:LH and FSH act on gonadal cells to regulate steroidogenesis and gametogenesis. To model human reproductive disorders involving loss of LH function and to define LH-responsive genes, we produced knockout mice lacking the hormone-specific LHbeta subunit. LHbeta null mice are viable but demonstrate postnatal defects in g...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章,评审
doi：10.1016/j.mce.2006.10.020
更新日期：2007-04-15 00:00:00
abstract：:Bisphenol A (BPA) is widely used in consumer products and a potential endocrine disruptor linked with sexual precocity. However, its action and underlying mechanisms on male sexual maturation is unclear. In the present study, we used a unique in vivo ethane dimethane sulfonate (EDS)-induced Leydig cell regeneration mo...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/j.mce.2018.03.003
更新日期：2018-10-15 00:00:00
abstract：:The aims of the study were to characterize leptin and it is receptor (LEPR) proteins immunoexpression in ovine ovaries and to evaluate the effects of leptin on development of secondary follicles cultured in vitro. The ovaries were collected and fixed for immunohistochemical analysis. Additional pairs of ovaries were c...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/j.mce.2019.110506
更新日期：2019-09-15 00:00:00
abstract：:We studied the influence of thyroid hormones and vitamin A status on the regulation of UDP-glucuronosyltransferase (UGT) expression and the glucuronidation of thyroid hormones by UGTs. For this, we used an original model of rats fed with different vitamin A diets and implanted subcutaneously by osmotic minipumps deliv...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/s0303-7207(01)00681-5
更新日期：2002-04-25 00:00:00
abstract：:Peroxisome proliferator-activated receptor gamma (PPARγ) is a key regulator of adipogenesis. It is also a central player in energy metabolism, inflammation and immunity. As an important nuclear transcription factor, PPARγ can regulate the expression and function of genes or biological processes directly or indirectly ...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/j.mce.2017.07.037
更新日期：2018-08-15 00:00:00
abstract：:1,25(OH)2D3 (vitamin D) is well-recognized as a neurosteroid that modulates multiple brain functions. A growing body of evidence indicates that vitamin D plays a pivotal role in brain development, neurotransmission, neuroprotection and immunomodulation. However, the precise molecular mechanisms by which vitamin D exer...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章,评审
doi：10.1016/j.mce.2017.05.035
更新日期：2017-09-15 00:00:00
abstract：:Transthyretin (TTR) is a plasma thyroid hormone (TH) binder that emerged from an ancient hydroxyisourate hydrolase by gene duplication. To know how an ancient TTR had high affinity for THs, molecular and TH binding properties of lamprey TTRs were investigated. In adult serum, the lipoprotein LAL was a major T3 binder ...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/j.mce.2018.02.012
更新日期：2018-10-15 00:00:00
abstract：:The diterpene forskolin was found to activate the adenylate cyclase system in intact tissue and membrane preparations of the immature rat ovary. The cyclic AMP (cAMP) response reached a maximal level after 5 min and no decline was observed even after 4 h of incubation. Forskolin stimulated production of both progester...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章,评审
doi：10.1016/0303-7207(83)90057-6
更新日期：1983-11-01 00:00:00
abstract：:Advanced glycation end products (AGEs), formed at an accelerated rate under diabetes, play a role in inflammation and fibrosis in mesangial areas in diabetic nephropathy (DN). However, the transcriptional modulator that mediates the cellular response to AGEs remains largely obscure. Our goal was to determine whether m...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/j.mce.2017.07.014
更新日期：2018-01-15 00:00:00
abstract：:Interaction of tamoxifen, trioxifene and LY117018 with cytosol-estrogen receptors from immature rat uteri was compared. Determination of relative binding affinity (RBA) by competition with [3H] estradiol under various assay conditions revealed that the RBA of LY117018 increased with temperature while that of trioxifen...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/0303-7207(81)90105-2
更新日期：1981-04-01 00:00:00
abstract：:The age-related evolution of the in vitro effects of a gonadotropin releasing hormone agonist ([D-Trp6]-GnRH) on the secretion of testosterone by the testis, cultured during 3 days on a Millipore filter floating on M199 medium, was studied during the perinatal period in the rat. The basal and luteinizing hormone (LH)-...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/0303-7207(91)90032-n
更新日期：1991-12-01 00:00:00
abstract：:Porcine Leydig cells in primary culture were incubated to equilibrium with increasing doses of either porcine luteinizing hormone (pLH) or human chorionic gonadotropin (hCG). Then, free and total high affinity gonadotropin receptors on the cell surface were dosed with [125I]hCG as tracer. In isotonic high salt medium,...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/0303-7207(91)90263-r
更新日期：1991-04-01 00:00:00
abstract：:Glucocorticoid hormones suppress circulating concentrations of thyrotrophin (TSH), but their effect on synthesis of TSH in the pituitary gland is unclear. We have examined the influence of the glucocorticoid dexamethasone on serum TSH, pituitary TSH content and TSH beta- and alpha-subunit mRNA concentrations in pituit...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/0303-7207(89)90064-6
更新日期：1989-06-01 00:00:00
abstract：:A peptide of unknown structure was found as a side product in a commercial preparation of the 1-34 fragment of bovine parathyroid hormone (PTH). CNBr cleavage and amino acid analysis showed that this peptide is the des-lys-13 form of 1-34 bovine PTH. The peptide thus represents a deletion mutant of PTH and structure-f...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/0303-7207(87)90037-2
更新日期：1987-06-01 00:00:00
abstract：:We have previously shown that osteocalcin synthesis is readily induced by 1,25-dihydroxyvitamin D3 (1,25(OH)2D3) in MG-63 human osteosarcoma cells (Mahonen et al. (1990) Biochim. Biophys. Acta 1048, 30-37). In the present study, the regulation of osteocalcin synthesis by other hormones of the steroid-thyroid hormone f...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/0303-7207(91)90269-x
更新日期：1991-04-01 00:00:00
abstract：:Dopamine and somatostatin are both involved in the negative control of normal pituitary cells. Dopamine subtype 2 receptor (D2DR) and somatostatin receptor (sst) agonists, mainly directed to sst2, are used in the treatment of pituitary adenomas. Nevertheless, a majority of corticotroph and gonadotroph adenomas and a t...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章,评审
doi：10.1016/j.mce.2007.12.008
更新日期：2008-05-14 00:00:00
abstract：:Medullary thyroid carcinoma (MTC) is a rare neuroendocrine neoplasm of the parafollicular thyroid C cells. Although somatostatin receptors are expressed by MTCs, treatment with octreotide has shown poor efficacy, whereas recently pasireotide has demonstrated antiproliferative effects in persistent postoperative MTCs. ...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/j.mce.2020.111092
更新日期：2021-01-15 00:00:00
abstract：:Mammalian spermatozoa undergo several signaling and biochemical transformations in the female genital tract, collectively called capacitation. The capacitated spermatozoon binds to the egg zona pellucida, where it undergoes the acrosome reaction (AR), a process enabling it to penetrate and fertilize the egg. Actin pol...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章,评审
doi：10.1016/j.mce.2009.06.009
更新日期：2010-01-27 00:00:00
abstract：:The binding of thyrotropin (TSH) to the TSH receptor (TSHR) activates two signaling pathways: the cAMP-protein kinase A (PKA) and the protein kinase C (PKC) systems. We have recently demonstrated that TSH activates the Janus kinases (JAK)/signal transducer and activator of transcription (STAT) pathway via TSHR. This s...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/s0303-7207(02)00185-5
更新日期：2002-08-30 00:00:00
abstract：:While the transcriptional effects of glucocorticoid hormone manipulation on the pituitary pro-opiomelanocortin (POMC) gene have been documented, it is not yet clear whether glucocorticoids activate additional post-transcriptional mechanisms to regulate POMC gene expression. We have used RNA probes that span exon/intro...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/0303-7207(89)90029-4
更新日期：1989-10-01 00:00:00
abstract：:Thrombin and COX-2 regulating cardiac hypertrophy are via various signaling cascades. Several transcriptional factors including CREB involve in COX-2 expression. However, the interplay among thrombin, CREB, and COX-2 in primary human neonatal ventricular cardiomyocytes remains unclear. In this study, thrombin-induced ...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/j.mce.2015.04.005
更新日期：2015-07-05 00:00:00
abstract：:The cellular content of preuteroglobin mRNA in endometrium was measured by molecular hybridization to preuteroglobin cDNA, and compared with uteroglobin content in the uterine secretion as determined by radioimmunoassay. The following results were obtained. (1) A single injection of either estradiol or progesterone le...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/0303-7207(81)90051-4
更新日期：1981-02-01 00:00:00
abstract：:The transforming growth factor beta (TGF-beta) superfamily includes several closely related peptides including the activins and inhibins. Since we recently reported that TGF-beta 1 and beta 2 are potent inducers of steroid 5 alpha-reductase (5 alpha R), we have now studied the effects of these other peptides using pri...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/0303-7207(94)03430-2
更新日期：1995-01-01 00:00:00
abstract：:Prolactin (PRL) modulates proliferation in the mammary gland and other tissues, in part through inducing transcription of cyclin D1, a key regulator of G(1) phase cell cycle progression. We showed previously that PRL, via Jak2, induces binding of Stat5 to a distal GAS site (GAS1) in the cyclin D1 promoter. However, fu...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/j.mce.2005.04.006
更新日期：2005-07-15 00:00:00
abstract：:It is widely accepted that obesity is a major risk factor for the development of atherosclerosis. In this context, adipose tissue produces a variety of adipokines and releases free fatty acids, contributing to a chronic-low grade inflammation state implicated in vascular complications. In this study, we investigated t...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/j.mce.2012.06.010
更新日期：2012-10-15 00:00:00
abstract：:Over 20 mutations affecting the neurophysin moiety of the vasopressin prohormone, have been identified in families suffering from familial neurohypophysial diabetes insipidus (FNDI). Only one of these, NP87E-->stop, is located outside the central conserved domain implicated in sorting of the vasopressin prohormone. To...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/s0303-7207(00)00288-4
更新日期：2000-09-25 00:00:00
