当前位置： SCI文献检索 > MOLECULAR AND CELLULAR ENDOCRINOLOGY期刊下所有文献 > The inhibitor of connexin Cx36 channels, mefloquine, inhibits voltage-dependent Ca2+ channels and insulin secretion.

The inhibitor of connexin Cx36 channels, mefloquine, inhibits voltage-dependent Ca2+ channels and insulin secretion.

Abstract：

:The antimalarial agent, mefloquine, inhibits the function of connexin Cx36 gap junctions and hemichannels and has thus become a tool to investigate their physiological relevance in pancreatic islets. In view of earlier reports on a KATP channel-block by mefloquine, the specificity of mefloquine as a pharmacological tool was investigated. Mouse pancreatic islets and single beta cells were used to measure membrane potential, whole cell currents, Ca2+ channel activity, cytosolic Ca2+ concentration ([Ca2+]i) and insulin secretion. Mefloquine was tested in the concentration range of 5-50 μM 25 μM mefloquine was as effective as 500 μM tolbutamide to depolarize the plasma membrane of beta cells, but did not induce action potentials. Rather, it abolished tolbutamide-induced action potentials and the associated increase of [Ca2+]i. In the range of 5-50 μM mefloquine inhibited voltage-dependent Ca2+ currents in primary beta cells as effectively as 1 μM nisoldipine, a specific blocker of L-type Ca2+ channels. The Ca2+ channel opening effect of Bay K8644 was completely antagonized by mefloquine. Likewise, the increase of [Ca2+]i and of insulin secretion stimulated by 40 mM KCl, but not that by 30 mM glucose was antagonized by 50 μM mefloquine. Neither at 5 μM nor at 50 μM did mefloquin stimulate insulin secretion at basal glucose. In conclusion, mefloquine blocks KATP channels and L-type Ca2+ channels in pancreatic beta cells in the range from 5 to 50 μM. Thus it inhibits depolarization-induced insulin secretion, but in the presence of a stimulatory glucose concentration additional effects of mefloquine, possibly on intracellular Ca2+ mobilization, and the metabolic amplification by glucose permit a sustained rate of secretion.

journal_name

Mol Cell Endocrinol

journal_title

Molecular and cellular endocrinology

authors

Seemann N,Welling A,Rustenbeck I

doi

10.1016/j.mce.2017.11.024

subject

Has Abstract

pub_date

2018-09-05 00:00:00

pages

97-106

eissn

0303-7207

issn

1872-8057

pii

S0303-7207(17)30610-X

journal_volume

472

pub_type

杂志文章

相关文献

MOLECULAR AND CELLULAR ENDOCRINOLOGY文献大全
  • Heme oxygenase-1 is induced by thyroid hormone and involved in thyroid hormone preconditioning-induced protection against renal warm ischemia in rat.

    abstract：:Thyroid hormone pretreatment was indicated to increase tissue tolerance to ischemia-reperfusion injury (IRI) in various organs, but the underlying molecular mechanisms remains largely unknown. Induction of heme oxygenase-1 (HO-1) protects organs against IRI. The present study investigated the effect of thyroid hormone...

    journal_title：Molecular and cellular endocrinology

    pub_type： 杂志文章

    doi：10.1016/j.mce.2011.03.019

    authors： Li F,Lu S,Zhu R,Zhou Z,Ma L,Cai L,Liu Z

    更新日期：2011-06-06 00:00:00

  • Molecular and functional studies of 4 candidate loci in Pendred syndrome and nonsyndromic hearing loss.

    abstract：:Patients with PS or non-syndromic deafness were submitted to genetic/functional analyzes of SLC26A4, of its binding domain for FOXI1 (FOXI1-DBD), of the transcription activator FOXI1, and of the potassium channel KCNJ10. SLC26A4 was the most frequently mutated gene. An altered intracellular localization with immunocyt...

    journal_title：Molecular and cellular endocrinology

    pub_type： 杂志文章

    doi：10.1016/j.mce.2012.01.013

    authors： Cirello V,Bazzini C,Vezzoli V,Muzza M,Rodighiero S,Castorina P,Maffini A,Bottà G,Persani L,Beck-Peccoz P,Meyer G,Fugazzola L

    更新日期：2012-04-04 00:00:00

  • 17B-hydroxysteroid dehydrogenases as acyl thioester metabolizing enzymes.

    abstract：:17β-Hydroxysteroid dehydrogenases (HSD17B) catalyze the oxidation/reduction of 17β-hydroxy/keto group in position C17 in C18- and C19 steroids. Most HSD17Bs are also catalytically active with substrates other than steroids. A subset of these enzymes is able to process thioesters of carboxylic acids. This group of enzy...

    journal_title：Molecular and cellular endocrinology

    pub_type： 杂志文章,评审

    doi：10.1016/j.mce.2018.11.012

    authors： Hiltunen JK,Kastaniotis AJ,Autio KJ,Jiang G,Chen Z,Glumoff T

    更新日期：2019-06-01 00:00:00

  • Changes in endonuclease activity during growth and regression of the Shionogi mammary carcinoma.

    abstract：:Autodigestion of nuclei isolated from the androgen-dependent Shionogi mouse mammary carcinoma revealed the presence of endogenous endonuclease activity which was stimulated by Ca2+ and Mg2+ and generated a repeating pattern of DNA fragments with an average monomeric size of 179 base pairs. The nuclear concentration of...

    journal_title：Molecular and cellular endocrinology

    pub_type： 杂志文章

    doi：10.1016/0303-7207(86)90144-9

    authors： Giles MG,Rennie PS,Bruchovsky N

    更新日期：1986-05-01 00:00:00

  • The thyroid hormone receptor recruits NCoR via widely spaced receptor-interacting domains.

    abstract：:The nuclear receptor corepressor (NCoR) interacts with the DNA-bound thyroid receptor (TR) homodimer through two of its three receptor-interacting domains (RIDs). One of these RIDs must be the most N-terminal, termed N3, which preferentially works with the next closest RID, N2. Interestingly, the spacing between the R...

    journal_title：Molecular and cellular endocrinology

    pub_type： 杂志文章

    doi：10.1016/j.mce.2009.02.028

    authors： Astapova I,Dordek MF,Hollenberg AN

    更新日期：2009-08-13 00:00:00

  • The progesterone receptor antagonist, onapristone has differential effects on the timing and control of the luteolytic mechanism depending on timing of administration in sheep.

    abstract：:Cyclic ewes were treated with control vehicle or progesterone receptor antagonist (onapristone; 100mg i.m. twice daily) during either early (day 3-5) or late (day 12-14) luteal phase and plasma samples collected for hormone analysis and to determine endogenous and oxytocin induced PGF2α release. On day 14 and 17, ewes...

    journal_title：Molecular and cellular endocrinology

    pub_type： 杂志文章

    doi：10.1016/j.mce.2013.06.001

    authors： Mann GE,Wathes DC,Robinson RS

    更新日期：2013-08-25 00:00:00

  • Potential action of IGF-1 and EGF on androgen receptor nuclear transfer and transactivation in normal and cancer human prostate cell lines.

    abstract：:This work was designed to determine whether IGF-1 and EGF modulate nuclear transfer and transactivation of the androgen receptor (AR) in human prostate cell lines (PNT1A and DU-145). We first characterized the IGF-1 and EGF receptors by ligand-binding assays with [125I] IGF-1 and [125I] EGF in a normal human prostate ...

    journal_title：Molecular and cellular endocrinology

    pub_type： 杂志文章

    doi：10.1016/s0303-7207(02)00374-x

    authors： Orio F Jr,Térouanne B,Georget V,Lumbroso S,Avances C,Siatka C,Sultan C

    更新日期：2002-12-30 00:00:00

  • Iron overload induces hypogonadism in male mice via extrahypothalamic mechanisms.

    abstract：INTRODUCTION:Iron overload leads to multiple organ damage including endocrine organ dysfunctions. Hypogonadism is the most common non-diabetic endocrinopathy in primary and secondary iron overload syndromes. AIM:To explore the molecular determinants of iron overload-induced hypogonadism with specific focus on hypothal...

    journal_title：Molecular and cellular endocrinology

    pub_type： 杂志文章

    doi：10.1016/j.mce.2017.06.019

    authors： Macchi C,Steffani L,Oleari R,Lettieri A,Valenti L,Dongiovanni P,Romero-Ruiz A,Tena-Sempere M,Cariboni A,Magni P,Ruscica M

    更新日期：2017-10-15 00:00:00

  • A potential role of galectin-1 in promoting mouse trophoblast stem cell differentiation.

    abstract：:Galectin-1 is highly expressed in blastocysts and trophoblast giant cells during implantation, and dysregulated galectin-1 is associated with many pregnancy-related abnormalities. Elevated galectin-1 contributes to cancer cells invasion. Here, we found that galectin-1 is expressed in mouse oocytes, preimplantation emb...

    journal_title：Molecular and cellular endocrinology

    pub_type： 杂志文章

    doi：10.1016/j.mce.2017.11.003

    authors： You JL,Wang W,Tang MY,Ye YH,Liu AX,Zhu YM

    更新日期：2018-07-15 00:00:00

  • Immunolocalization of leptin and its receptor in the sheep ovary and in vitro effect of leptin on follicular development and oocyte maturation.

    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

    authors： Macedo TJS,Santos JMS,Bezerra MÉS,Menezes VG,Gouveia BB,Barbosa LMR,Lins TLBG,Monte APO,Barberino RS,Batista AM,Barros VRP,Wischral A,Queiroz MAA,Araújo GGL,Matos MHT

    更新日期：2019-09-15 00:00:00

  • Effect of transfer RNA from various sources on placental messenger RNA translation.

    abstract：:Poly(A+)-containing mRNA from human term placenta was used to direct protein synthesis in a nuclease-treated rabbit reticulocyte lysate, which is dependent on mRNA and tRNA for maximal activity. The major protein product was human pre-placental lactogen (hPL). Addition of tRNA from rabbit liver, rabbit reticulocyte, h...

    journal_title：Molecular and cellular endocrinology

    pub_type： 杂志文章

    doi：10.1016/0303-7207(83)90212-5

    authors： Kelly SJ,Loria J,Gyves MT,Ilan J

    更新日期：1983-02-01 00:00:00

  • High-affinity binding of the antiestrogen [3H]tamoxifen to the 8S estradiol receptor.

    abstract：:The interaction of tamoxifen (ICI 46,474), a synthetic antiestrogen, with uterine cytosol proteins of immature calf and rat has been studied directly using the tritiated compound labeled with a high specific activity. The binding complexes were measured by the dextrancoated charcoal, protamine sulfate and hydroxyapati...

    journal_title：Molecular and cellular endocrinology

    pub_type： 杂志文章

    doi：10.1016/0303-7207(78)90006-0

    authors： Capony F,Rochefort H

    更新日期：1978-07-01 00:00:00

  • Specific DNA binding and transactivation potential of recombinant, purified Stat5.

    abstract：:The signal transducers and activators of transcriptions (Stats) are central mediators of cytokine responses especially in hematopoietic cells. The detailed molecular mechanisms of Stat activation, particularly the role of post-translational modifications and co-operation with cellular transcription factors are subject...

    journal_title：Molecular and cellular endocrinology

    pub_type： 杂志文章

    doi：10.1016/s0303-7207(01)00588-3

    authors： Beisenherz-Huss C,Mundt M,Herrala A,Vihko P,Schubert A,Groner B

    更新日期：2001-10-25 00:00:00

  • Cyclic AMP stimulates the gene expression of a non-selective cation channel, mNSC1, in pancreatic beta-cell line, MIN6.

    abstract：:Mouse non-selective cation channel 1 (mNSC 1) cDNA from mouse pancreatic beta-cell line, MIN6, have recently been cloned. Since the number of non-selective cation channel in pancreatic duct cells has been reported to increase 9-fold in 5 h incubation with cAMP, the effect of cAMP on the gene expression of mNSC1 in MIN...

    journal_title：Molecular and cellular endocrinology

    pub_type： 杂志文章

    doi：10.1016/s0303-7207(99)00214-2

    authors： Satoh J,Kutsuwada K,Ohki G,Imai M,Kobayashi M,Suzuki M

    更新日期：2000-02-25 00:00:00

  • Prostaglandin E2 increases adenosine 3',5'-monophosphate concentration and binding-site occupancy, and stimulates serotonin-N-acetyltransferase activity in rat pineal glands in vitro.

    abstract：:The effects of prostaglandins (PGs) on rat pineal metabolism were examined in vitro. PGE2 (0.01-1 microM) increased the activity of serotonin-N-acetyltransferase (SNAT), the stimulation curve exhibiting a maximum at 0.1 microM. PGE1 increased SNAT activity only at the highest dose (1 microM) whereas PGF2 alpha, 15-ket...

    journal_title：Molecular and cellular endocrinology

    pub_type： 杂志文章

    doi：10.1016/0303-7207(81)90066-6

    authors： Ritta MN,Cardinali DP

    更新日期：1981-08-01 00:00:00

  • Sites of glandular kallikrein gene expression in fetal mice.

    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

    authors： Penschow JD,Coghlan JP

    更新日期：1992-10-01 00:00:00

  • Genetic control of murine limb morphogenesis: relationships with human syndromes and evolutionary relevance.

    abstract：:Over the past ten years, the discovery and functional characterisation of murine Hox genes has led to a better understanding of some of the molecular mechanisms underlying limb development. It has also shed some light on the potential genetic events which have accompanied the fin-to-limb transition, an evolutionary st...

    journal_title：Molecular and cellular endocrinology

    pub_type： 杂志文章,评审

    doi：10.1016/s0303-7207(98)00021-5

    authors： Kondo T,Hérault Y,Zákány J,Duboule D

    更新日期：1998-05-25 00:00:00

  • Cloning, sequence analysis, tissue distribution, and sex-specific expression of the neural form of P450 aromatase in juvenile sea bass (Dicentrarchus labrax).

    abstract：:The teleost brain is characterized by exceptionally high levels of aromatase, the enzyme that converts androgens into estrogens, and by its continuous growth throughout life. Gonadal estrogens have been implicated in sex differentiation and the control of reproduction in adult fish, but the role of neural estrogens du...

    journal_title：Molecular and cellular endocrinology

    pub_type： 杂志文章

    doi：10.1016/j.mce.2004.01.006

    authors： Blázquez M,Piferrer F

    更新日期：2004-04-30 00:00:00

  • The antiproliferative effect of tamoxifen in breast cancer cells: mediation by the estrogen receptor.

    abstract：:The effects of tamoxifen (Tam) and its 4-hydroxylated metabolite (OH-Tam) on the growth of two human breast cancer cell lines ( MCF7 and BT20 ) were evaluated by fluorometric DNA assay. The effects of the antiestrogens were dependent upon their concentrations and the nature of the cells. At concentrations below 4 micr...

    journal_title：Molecular and cellular endocrinology

    pub_type： 杂志文章

    doi：10.1016/0303-7207(84)90004-2

    authors： Bardon S,Vignon F,Derocq D,Rochefort H

    更新日期：1984-05-01 00:00:00

  • Functional analysis of LHbeta knockout mice.

    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

    authors： Kumar TR

    更新日期：2007-04-15 00:00:00

  • Thyrotropin but not epidermal growth factor down-regulates the isozyme I (PKa I) of cyclic AMP-dependent protein kinases in dog thyroid cells in primary cultures.

    abstract：:The activity of the two cAMP-dependent protein kinases (PKa I and PKa II) was evaluated in dog thyroid cells in primary cultures after a 6-day growth period induced by either thyrotropin (TSH) or epidermal growth factor (EGF). Although the total PKa activity was not affected in cells cultured in the presence of TSH or...

    journal_title：Molecular and cellular endocrinology

    pub_type： 杂志文章

    doi：10.1016/0303-7207(89)90188-3

    authors： Breton MF,Roger PP,Omri B,Dumont JE,Pavlovic-Hournac M

    更新日期：1989-01-01 00:00:00

  • Tyrosine hydroxylase induction in the young rat: control by thyroid hormones.

    abstract：:At 14 days of age, hypothyroid and normal rats are rendered hypoglycaemic by insulin injection and the subsequent induction in adrenal tyrosine hydroxylase (TH) is studied. Hypothyroidism impairs both the intensity and the time-course of adrenal TH induction. ...

    journal_title：Molecular and cellular endocrinology

    pub_type： 杂志文章

    doi：10.1016/0303-7207(84)90149-7

    authors： Gripois D,Valens M

    更新日期：1984-11-01 00:00:00

  • Immunocytochemical localization of prolactin receptors in rat liver cells: I. Dependence on sex and sex steroids.

    abstract：:The peculiarities of cellular and tissue distribution of prolactin receptors (PRLR) in the liver of female and male rats with different sex steroid status were investigated in paraplast-embedded tissue with the indirect immunoperoxidase technique. Two clones of antibodies directed outside the PRL-binding site (U6) or ...

    journal_title：Molecular and cellular endocrinology

    pub_type： 杂志文章

    doi：10.1016/0303-7207(94)90037-x

    authors： Smirnova OV,Petraschuk OM,Kelly PA

    更新日期：1994-10-01 00:00:00

  • Functional interactions of an upstream enhancer of the mouse glycoprotein hormone alpha-subunit gene with proximal promoter sequences.

    abstract：:Transcription of the glycoprotein hormone alpha-subunit gene in the pituitary is governed by different promoter elements in thyrotropes and gonadotropes. We recently identified an upstream enhancer that directs a high level of cell type specific expression in transgenic mice and stimulates proximal promoter activity i...

    journal_title：Molecular and cellular endocrinology

    pub_type： 杂志文章

    doi：10.1016/s0303-7207(98)00110-5

    authors： Wood WM,Dowding JM,Sarapura VD,McDermott MT,Gordon DF,Ridgway EC

    更新日期：1998-07-25 00:00:00

  • Is human chorionic gonadotropin directly involved in the regulation of human implantation?

    abstract：:The regulation of human implantation is not fully understood. hCG as one of the earliest embryonal signals may be a major regulator in the parakrine embryo-endometrial communication. The expression of full-length hCG/LH-receptor mRNA could be demonstrated in human endometrium throughout the follicular and secretory ph...

    journal_title：Molecular and cellular endocrinology

    pub_type： 杂志文章,评审

    doi：10.1016/j.mce.2006.09.016

    authors： Licht P,Fluhr H,Neuwinger J,Wallwiener D,Wildt L

    更新日期：2007-04-15 00:00:00

  • The biology of progesterone receptor in the normal mammary gland and in breast cancer.

    abstract：:This paper reviews work on progesterone and the progesterone receptor (PR) in the mouse mammary gland that has been used extensively as an experimental model. Studies have led to the concept that progesterone controls proliferation and morphogenesis of the luminal epithelium in a tightly orchestrated manner at distinc...

    journal_title：Molecular and cellular endocrinology

    pub_type： 杂志文章,评审

    doi：10.1016/j.mce.2011.10.030

    authors： Obr AE,Edwards DP

    更新日期：2012-06-24 00:00:00

  • Autoimmune T-cell recognition sites of human thyrotropin receptor in Graves' disease.

    abstract：:Five overlapping synthetic peptides representing two regions of thyrotropin (TSH) binding sites of human thyrotropin receptor (TSHR) (peptides 12-30, 24-44, 308-328, 324-344 and 339-364) were investigated for their ability to cause proliferation of peripheral blood lymphocytes (PBL) from eight patients with Graves' di...

    journal_title：Molecular and cellular endocrinology

    pub_type： 杂志文章

    doi：10.1016/0303-7207(93)90077-w

    authors： Sakata S,Tanaka S,Okuda K,Miura K,Manshouri T,Atassi MZ

    更新日期：1993-03-01 00:00:00

  • Characterization and sub-cellular localization of SS1R, SS2R, and SS5R in human late-stage prostate cancer cells: effect of mono- and bi-specific somatostatin analogs on cell growth.

    abstract：:Somatostatin (SST) and SST receptors (SS1R, SS2R, SS3R, SS4R and SS5R) appear to play a significant role in the progression of human prostate cancer (PCa), which is associated with heterogeneity of SSRs expression and specific cell localization as we already demonstrated in the LNCaP cell line, an in vitro model of hu...

    journal_title：Molecular and cellular endocrinology

    pub_type： 杂志文章

    doi：10.1016/j.mce.2013.10.027

    authors： Ruscica M,Magni P,Steffani L,Gatto F,Albertelli M,Rametta R,Valenti L,Ameri P,Magnaghi V,Culler MD,Minuto F,Ferone D,Arvigo M

    更新日期：2014-02-15 00:00:00

  • The Klotho gene family as a regulator of endocrine fibroblast growth factors.

    abstract：:The Klotho gene encodes a single-pass transmembrane protein and functions as an aging-suppressor gene, which extends lifespan when overexpressed and accelerates the development of aging-like phenotypes when disrupted in mice. Fibroblast growth factor 23 (FGF23) is a bone-derived hormone that regulates phosphate and vi...

    journal_title：Molecular and cellular endocrinology

    pub_type： 杂志文章,评审

    doi：10.1016/j.mce.2008.10.052

    authors： Kurosu H,Kuro-O M

    更新日期：2009-02-05 00:00:00

  • Hormonal regulation of thyroidal protein phosphokinase activities. II. Differential sensitivity of type I and type II cAMP-dependent enzymes to the treatment of rats with thyroxine.

    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

    authors： Delbauffe D,Ohayon R,Pavlovic-Hournac M

    更新日期：1979-05-01 00:00:00