Abstract：
:Experimental data indicate that metal ions such as Na(+), Ca(2+) and Mg(2+), which are present in millimolar concentrations in the extracellular environment, modulate binding of ligands to plasma membrane receptors. Here, we briefly review structural studies that demonstrate that various types of ligands, including peptide hormones and drugs, bind metal ions, in particular Ca(2+), in the lipid milieu. We propose that the metal ion-bound forms of ligands represent their bioactive conformations. With a view to understanding the mechanism of modulation of ligand-receptor interactions by metal ions, we have computed a homology model of the mu-opioid receptor, a G protein-coupled receptor (GPCR), and performed docking of specific agonist and antagonist ligands in the receptor. This resulted in the formation of a ligand-metal ion-receptor (ternary) complex which accounted for the data on the structure-activity relationships of ligands and mutation data on the receptor. Based on experimental and modeling data, we have proposed a general mechanism of activation of GPCRs by their corresponding ligands wherein metal ions play a pivotal role. Studies on overexpressed segments of mu-receptor are in progress to verify the above proposal.
journal_name
Mol Cell Endocrinoljournal_title
Molecular and cellular endocrinologyauthors
Ananthanarayanan VS,Kerman Adoi
10.1016/j.mce.2005.11.023keywords:
subject
Has Abstractpub_date
2006-02-26 00:00:00pages
53-9issue
1-2eissn
0303-7207issn
1872-8057pii
S0303-7207(05)00428-4journal_volume
246pub_type
杂志文章,评审abstract：:Apolipoprotein E (APOE) deficient mice exhibit unexplained hypercorticosteronemia. Given that APOE is also produced locally within the adrenals, we evaluated the effect of adrenal-specific APOE deficiency on the glucocorticoid function. Hereto, one adrenal containing or lacking APOE was transplanted into adrenalectomi...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/j.mce.2019.04.001
更新日期：2019-06-15 00:00:00
abstract：:Proinsulin folding imperfections cause extensive beta-cell defects known in diabetes. Here, we investigated whether exenatide can alleviate such defects in proinsulin conversion, beta-cell survival, and insulin secretion, in the Ins2+/Akita beta-cells that have a spontaneous mutation (Cys 96 Tyr) in the insulin 2 gene...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/j.mce.2016.09.015
更新日期：2017-01-05 00:00:00
abstract：:Primary aldosteronism (PA) encompasses a broad, heterogeneous group of disorders including both sporadic and familial forms (familial hyperaldosteronism type I, II and III). PA is the most common form of secondary hypertension and associated with a higher rate of cardiovascular complications, compared with essential h...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章,评审
doi：10.1016/j.mce.2014.09.015
更新日期：2015-01-05 00:00:00
abstract：:Characteristics of the alpha-adrenergic stimulation of ACTH, beta-endorphin + beta-LPH and alpha-MSH release were studied in rat anterior pituitary cells in primary culture. Parallel changes of ACTH, beta-endorphin + beta-LPH and alpha-MSh release were found under all stimulatory and inhibitory conditions by natural a...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/0303-7207(81)90038-1
更新日期：1981-06-01 00:00:00
abstract：:Recently, a remarkable progress has been made in our understanding about the role of sex steroids in male physiology. In this paper, we consider the clinical aspects of congenital estrogen deficiency - notably, estrogen resistance and aromatase deficiency - in men and we discuss both well-established and supposed estr...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章,评审
doi：10.1016/s0303-7207(01)00432-4
更新日期：2001-06-10 00:00:00
abstract：:The so-called calcium antagonist D-600 and agents that enhance the influx of calcium ions into nerve terminals during action potentials (4-aminopyridine, tetraethylammonium, guanidine) interact with alpha-adrenoceptors. The interaction was revealed by binding experiments in vitro with the alpha 2- and alpha 1-specific...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/0303-7207(80)90054-4
更新日期：1980-09-01 00:00:00
abstract：:Metabolic syndrome (MetS) is a disease composed of different risk factors such as obesity, type 2 diabetes or dyslipidemia. The prevalence of this syndrome is increasing worldwide in parallel with the rise in obesity. Nonalcoholic fatty liver disease (NAFLD) is now the most frequent chronic liver disease in western co...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章,评审
doi：10.1016/j.mce.2015.02.018
更新日期：2015-12-15 00:00:00
abstract：:The cell line MD-IGF-1, containing an ovine IGF-1 cDNA driven by the mouse mammary tumor virus-long terminal repeat (MMTV-LTR) promoter, was used to study expression of IGF-1 linked to the MMTV-LTR in bovine mammary epithelial cells in response to various hormonal and substratum stimuli. Acute sensitivity of the MMTV-...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/0303-7207(93)90105-s
更新日期：1993-10-01 00:00:00
abstract：:The pineal hormone melatonin modulates constitutive protein secretion from melanoma M2R cells. Nanomolar concentrations of melatonin inhibited protein secretion early after plating or at low cell density, but facilitated it late after plating or at high cell density. Inhibition by melatonin of adenylate cyclase is the...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/0303-7207(95)03592-u
更新日期：1995-08-11 00:00:00
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journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章,评审
doi：10.1016/j.mce.2012.11.020
更新日期：2013-05-22 00:00:00
abstract：:The enzyme 3beta-hydroxysteroid dehydrogenase/isomerase (3beta-HSD) is essential for the biosynthesis of all active steroid hormones. The 3beta-HSD enzyme consists in multiple isoforms, each the product of a distinct gene. In the mouse, six tissue-specific isoforms have been identified. These isoforms are expressed in...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章,评审
doi：10.1016/s0303-7207(01)00689-x
更新日期：2002-02-22 00:00:00
abstract：:Basal and gonadotropin stimulated adenylate cyclase activity was assessed in testicular tissues obtained from men (20-80 years). A disparity was observed in the gonadotropin responsiveness of the human testicular adenylate cyclase system to hFSH and hCG stimulation. Of the tissues analyzed, 61% were FSH responsive and...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/0303-7207(85)90006-1
更新日期：1985-08-01 00:00:00
abstract：:In a model of pulmonary hypertension induced by a single injection of monocrotaline (MCT), we observed a time-dependent right ventricular hypertrophy, which became apparent in treated rats 21 days after administration of MCT and progressed through day 45. Associated with this right ventricular hypertrophy were time-de...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/0303-7207(89)90011-7
更新日期：1989-04-01 00:00:00
abstract：:Elaboration of a multicellular organism requires highly efficient coordination between proliferation and developmental processes. Accordingly, the embryonic cell cycle exhibits a high degree of plasticity; however, the mechanisms underlying its regulation in vivo remain largely unknown. The purpose of this review is t...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章,评审
doi：10.1016/j.mce.2007.11.008
更新日期：2008-01-30 00:00:00
abstract：:Estrogens are synthesized from C19 steroids by a unique form of cytochrome P450, aromatase cytochrome P-450 (P-450AROM; the product of the CYP19 gene). We have shown that tissue-specific expression of human P-450AROM is determined, in part, by the use of alternative promoters. Previous methods of analysis for determin...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/0303-7207(93)90227-b
更新日期：1993-11-01 00:00:00
abstract：:The mechanism by which hCG increases the rat testicular vascular permeability was studied by injecting the testes with hCG (0.1-100 ng) together with testicular interstitial fluid (150 mul) or with the fluid alone (control) and measuring the uptake of i.v. injected [125I]hCG and the interstitial fluid volume in the te...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/0303-7207(86)90138-3
更新日期：1986-05-01 00:00:00
abstract：:Effects of insulin-like growth factor I on the expression of the immediate-early gene c-fos in adrenomedullary tissue were assessed in bovine chromaffin cells in primary culture. The expression of c-fos mRNA and FOS protein were studied by Northern blot and immunofluorescence microscopy. IGF-I induced c-fos mRNA expre...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/0303-7207(94)90205-4
更新日期：1994-12-01 00:00:00
abstract：:Estrogen receptors (ers) not only are activated by hormones but also interact with many human-derived environmental contaminants. Here, we present evidence for four expressed er genes in Atlantic salmon cDNA - two more ers (erα2 and erβ2) than previously published. To determine if er gene expression differs between tw...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/j.mce.2014.11.009
更新日期：2015-01-15 00:00:00
abstract：:The crucial effects of androgens on the male skeleton are at least partly mediated via the androgen receptor (AR). In addition to hormone binding, the AR activity is regulated by post-translational modifications, including SUMOylation. SUMOylation is a reversible modification in which Small Ubiquitin-related MOdifier ...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/j.mce.2018.09.008
更新日期：2019-01-05 00:00:00
abstract：:Recent evidence using GT1-7 cells indicates that GnRH pulsatility depends on exocytotic-release and gene transcription events. To determine whether calcium or DREAM may play a role in linking these processes, we used an L-type Ca(2+)-blocker (nimodipine) and found that not only GnRH gene expression (GnRH-GE) pulse act...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/j.mce.2006.12.040
更新日期：2007-03-15 00:00:00
abstract：:We have examined the relationship between extracellular Ca2+, cytosolic free Ca2+ and insulin release in the clonal beta-cell line HIT-T15. Glucose-stimulated insulin release was dependent on the extracellular Ca2+ concentration in a dose-related manner; the threshold medium Ca2+ concentration for glucose-stimulated i...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/0303-7207(89)90162-7
更新日期：1989-08-01 00:00:00
abstract：:Pioglitazone belongs to the class of drugs called thiazolidinediones (TZDs), which are widely used as insulin sensitizers in the treatment of diabetes. A major side effect of TZDs is fluid retention. The steroid hormone aldosterone also promotes sodium and fluid retention; however, the effect of pioglitazone on aldost...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/j.mce.2014.07.007
更新日期：2014-08-25 00:00:00
abstract：:Carbamylcholine and acetylcholine through a muscarinic type of receptor, KCl, ionophore A-23187 and NaF increased cyclic GMP accumulation in dog-thyroid slices. These effects were abolished in calcium-depleted slices, which findings confirm that Ca2+ is required for cyclic GMP accumulation. All these agents depressed ...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/0303-7207(79)90057-1
更新日期：1979-04-01 00:00:00
abstract：:We have studied the effect of the adenylate cyclase-stimulating agent forskolin on expression of components of the plasminogen activation system in the human fibrosarcoma cell line HT-1080. By enzyme-linked immunosorbent assays, forskolin was found to cause a 2 to 4-fold decrease in intracellular and culture medium le...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/0303-7207(90)90100-m
更新日期：1990-08-20 00:00:00
abstract：:Proteins synthesised by seminal vesicles of normal rats were labelled with [35S]methionine and were then separated using two-dimensional gel electrophoresis. Isoelectric focusing or nonequilibrium pH gradient electrophoresis were used in the first dimension followed by polyacrylamide gel electrophoresis under denaturi...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/0303-7207(81)90081-2
更新日期：1981-10-01 00:00:00
abstract：:In order to study the distribution of LH (HCG) receptors on luteal cells ferritin was coupled to ovine LH with glutaraldehyde and purified by gel chromatography. The conjugate (FELH) competed with 125I-hCG for binding to isolated luteal membranes and stimulated a dose-dependent release of progesterone (P) from isolate...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/0303-7207(79)90008-x
更新日期：1979-08-01 00:00:00
abstract：:Experiments were done to determine the actions of ACTH on the morphologic and functional characteristics of the zona fasciculata (ZF) and zona reticularis (ZR) in the guinea pig adrenal cortex. In control guinea pigs, a number of morphologic differences distinguished the ZF from the ZR, including the presence of far m...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/s0303-7207(98)00189-0
更新日期：1998-11-25 00:00:00
abstract：:Granulosa cells of small follicles differentiate in vitro in serum-free medium, resulting in increased estradiol secretion and abundance of mRNA encoding cytochrome P450aromatase (P450arom). We tested the hypothesis that differentiation in vitro also involves increased expression of 3beta- and 17beta-hydroxysteroid de...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/j.mce.2004.05.010
更新日期：2004-08-31 00:00:00
abstract：:As part of an ongoing study of the cell-specific expression of glandular kallikrein genes in mice, we have investigated cellular sites of expression of the renal/pancreatic kallikrein gene, mGK-6, during fetal life. Expression of alpha I and beta-subunit genes of Na+K+ATPase and bradykinin binding were used as an indi...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/0303-7207(92)90005-q
更新日期：1992-10-01 00:00:00
abstract：:To define the heparin-binding site of follistatin, the reduced and S-carboxymethylated recombinant human follistatin containing 288 amino acids was digested by Staphylococcus aureus V8. The digested product was subjected to sulfate cellufine column chromatography and the adsorbed peptide fragments eluted with a stepwi...
journal_title：Molecular and cellular endocrinology
pub_type： 杂志文章
doi：10.1016/0303-7207(92)90094-m
更新日期：1992-12-01 00:00:00
