Meproadifen enhances activation and desensitization of the acetylcholine receptor-ionic channel complex (AChR): single channel studies.

Abstract:

:The effects of the quaternary agent meproadifen on ACh-activated channel currents were studied on myoballs cultured from hind limb muscles of neonatal rats. Meproadifen (0.02-0.1 microM) combined with ACh (0.1-0.3 microM) in the patch pipette caused an increase, followed by a decrease, in the frequency of channel openings. At concentrations greater than 0.2 microM the initial phase was not detected and a rapid and marked reduction in the opening frequency was observed. Meproadifen (up to 2.5 microM) produced no change in the duration or conductance of the open state of ACh-activated channels. In addition, this agent induced the appearance of events with a marked increase in the 'noise' during the opening phase. The lack of effect under inside-out patch conditions suggested that meproadifen binds to a site located at the external portion of the nicotinic macromolecule and has no access to it through the cell membrane. This study indicated that non-competitive antagonists such as meproadifen can facilitate receptor activation and desensitization.

journal_name

FEBS Lett

journal_title

FEBS letters

authors

Aracava Y,Albuquerque EX

doi

10.1016/0014-5793(84)81171-0

subject

Has Abstract

pub_date

1984-09-03 00:00:00

pages

267-74

issue

2

eissn

0014-5793

issn

1873-3468

pii

0014-5793(84)81171-0

journal_volume

174

pub_type

杂志文章
  • Crystallization of cytochrome P-450scc from bovine adrenocortical mitochondria.

    abstract::Cytochrome P-450scc (P-450scc), a cholesterol side-chain cleavage enzyme from bovine adrenocortical mitochondria, has been crystallized for the first time. Upon removal of glycerol from the solution of the native enzyme complexed with pyridoxal 5'-phosphate (PLP) by microdialysis against distilled water, reddish and p...

    journal_title:FEBS letters

    pub_type: 杂志文章

    doi:10.1016/0014-5793(88)81350-4

    authors: Iwamoto Y,Tsubaki M,Hiwatashi A,Ichikawa Y

    更新日期:1988-06-06 00:00:00

  • Identification of the genes responsive to etoposide-induced apoptosis: application of DNA chip technology.

    abstract::DNA chip technology was used in an attempt to identify target genes responsible for apoptosis induced by etoposide, a p53 activating topoisomerase II inhibitor used clinically as an antitumor agent. 62 Individual mRNAs whose mass changed significantly were identified after screening oligonucleotide arrays capable of d...

    journal_title:FEBS letters

    pub_type: 杂志文章

    doi:10.1016/s0014-5793(99)00136-2

    authors: Wang Y,Rea T,Bian J,Gray S,Sun Y

    更新日期:1999-02-26 00:00:00

  • Spectroelectrochemistry of P700 in native photosystem I particles and diethyl ether-treated thylakoid membranes from spinach and Thermosynechococcus elongatus.

    abstract::The redox potentials (E(composite function')) of P700 in intact and diethyl ether-treated thylakoid membranes as well as native photosystem (PS) I particles from spinach and Thermosynechococcus elongatus have been measured by a spectroelectrochemistry with an error range of +/-2-3 mV. Stepwise removal of antenna pigme...

    journal_title:FEBS letters

    pub_type: 杂志文章

    doi:10.1016/j.febslet.2008.02.075

    authors: Zhang Y,Nakamura A,Kuroiwa Y,Kato Y,Watanabe T

    更新日期:2008-04-02 00:00:00

  • In memory of Professor Leonor Michaelis in Nagoya: great contributions to biochemistry in Japan in the first half of the 20th century.

    abstract::Leonor Michaelis spent the years of 1922-1926 as Professor of Biochemistry of the Aichi Medical College (now Graduate School of Medicine, Nagoya University) in Nagoya, Japan. Michaelis succeeded in gathering many bright young biochemists from all over Japan into his laboratory, and made tremendous contributions to the...

    journal_title:FEBS letters

    pub_type: 传,历史文章,杂志文章

    doi:10.1016/j.febslet.2013.04.020

    authors: Nagatsu TT

    更新日期:2013-09-02 00:00:00

  • Do the major human glutathione S-transferases have fatty acid ethyl ester synthase activity?

    abstract::Two fatty acid ethyl ester (FAEE) synthase isoenzymes purified from human myocardium were reported to be glutathione S-transferases (GST) [(1989) Proc. Natl. Acad. Sci. USA 86, 4470-4473; and (1989) J. Clin. Invest. 84, 1942-1946]. In the present study, the FAEE synthase activity of several purified and well character...

    journal_title:FEBS letters

    pub_type: 杂志文章

    doi:10.1016/0014-5793(90)81438-t

    authors: Suzuki T,Kovacs MS,Board PG

    更新日期:1990-11-26 00:00:00

  • Regulation of acetylcholine receptor gene expression in rats treated with alpha-bungarotoxin.

    abstract::Regulation of acetylcholine receptor (AChR) gene expression was analyzed in alpha-bungarotoxin (alpha-BTX) treated rats. A reduction in available 125I-alpha-BTX binding sites was accompanied by an increase in the various AChR transcripts. The increase in the AChR alpha-, beta- epsilon- and delta-subunit mRNAs was simi...

    journal_title:FEBS letters

    pub_type: 杂志文章

    doi:10.1016/0014-5793(91)80487-n

    authors: Asher O,Provenzano C,Fuchs S

    更新日期:1991-05-06 00:00:00

  • Involvement of uncoupled antenna chlorophylls in photoinhibition in thylakoids.

    abstract::Evidence is presented, by means of both fluorescence and action spectroscopy, that a small, spectroscopically heterogeneous population of both Chl a and Chl b molecules is present in isolated spinach thylakoids and is active in photoinhibition. The broadness of the action spectrum suggests that degraded or incompletel...

    journal_title:FEBS letters

    pub_type: 杂志文章

    doi:10.1016/s0014-5793(01)02174-3

    authors: Santabarbara S,Neverov KV,Garlaschi FM,Zucchelli G,Jennings RC

    更新日期:2001-02-23 00:00:00

  • Molecular cloning and expression of a novel truncated form of chicken trkC.

    abstract::The trk family of tyrosine protein kinase genes serves crucial roles for the development of the nervous system and the survival of neurons. The members of this gene family, trk, trkB and trkC, bind a distinct neurotrophin of the nerve growth factor (NGF) gene family, and trigger the intracellular signals which elicit ...

    journal_title:FEBS letters

    pub_type: 杂志文章

    doi:10.1016/0014-5793(93)80216-h

    authors: Okazawa H,Kamei M,Kanazawa I

    更新日期:1993-08-23 00:00:00

  • The endoproteolytic processing of alphavbeta5 integrin is involved in cytoskeleton remodelling and cell migration.

    abstract::We previously showed that the post-translational cleavage of alphav subunit is essential for integrin-dependent signalling and cell adhesion. Here, we report that blocking alphav subunit cleavage by expression of alpha1-PDX, a convertase inhibitor, modified the capacity of cells to change shape, via a remodelling of t...

    journal_title:FEBS letters

    pub_type: 杂志文章

    doi:10.1016/s0014-5793(03)01467-4

    authors: Berthet V,Rigot V,Nejjari M,Marvaldi J,Luis J

    更新日期:2004-01-16 00:00:00

  • Evaluation of metal-conjugated compounds as inhibitors of 3CL protease of SARS-CoV.

    abstract::3C-like (3CL) protease is essential for the life cycle of severe acute respiratory syndrome-coronavirus (SARS-CoV) and therefore represents a key anti-viral target. A compound library consisting of 960 commercially available drugs and biologically active substances was screened for inhibition of SARS-CoV 3CL protease....

    journal_title:FEBS letters

    pub_type: 杂志文章

    doi:10.1016/j.febslet.2004.08.015

    authors: Hsu JT,Kuo CJ,Hsieh HP,Wang YC,Huang KK,Lin CP,Huang PF,Chen X,Liang PH

    更新日期:2004-09-10 00:00:00

  • Carbohydrate-induced modulation of cell membrane. VIII. Agglutination with mammalian lectin galectin-1 increases osmofragility and membrane fluidity of trypsinized erythrocytes.

    abstract::Interaction of lectins with cell surface determinants may alter membrane properties. Using trypsinized rabbit erythrocytes as model we tested the capacity of an endogenous lectin in this respect. Galectin-1 is a member of an adhesion/growth-regulatory family known to interact for example with ganglioside GM(1) and als...

    journal_title:FEBS letters

    pub_type: 杂志文章

    doi:10.1016/j.febslet.2006.02.006

    authors: Gupta RK,Pande AH,Gulla KC,Gabius HJ,Hajela K

    更新日期:2006-03-06 00:00:00

  • The X protein of hepatitis B virus binds to the F box protein Skp2 and inhibits the ubiquitination and proteasomal degradation of c-Myc.

    abstract::The HBx protein of hepatitis B virus is involved in deregulation of cell cycle and development of hepatocellular carcinoma. Since c-Myc also plays an important role in cell proliferation and tumor development, we studied its regulation by HBx in a human hepatoma cell line. Co-expression of HBx and c-Myc resulted in in...

    journal_title:FEBS letters

    pub_type: 杂志文章

    doi:10.1016/j.febslet.2005.12.034

    authors: Kalra N,Kumar V

    更新日期:2006-01-23 00:00:00

  • The detection and characterization of G-proteins in the eyespot of Chlamydomonas reinhardtii.

    abstract::The presence of G-proteins in the eyespot fraction of Chlamydomonas reinhardtii is shown. This fraction is capable of binding (GTP gamma[35S], possesses the GTPase activity and interacts with antibodies raised against a highly conserved peptide of most G-proteins' alpha-subunit. Cross-reaction with a 24-kDa protein is...

    journal_title:FEBS letters

    pub_type: 杂志文章

    doi:10.1016/0014-5793(90)81251-i

    authors: Korolkov SN,Garnovskaya MN,Basov AS,Chunaev AS,Dumler IL

    更新日期:1990-09-17 00:00:00

  • Nitric oxide protects blood-brain barrier in vitro from hypoxia/reoxygenation-mediated injury.

    abstract::A cell culture model of blood-brain barrier (BBB, coculture of rat brain endothelial cells with rat astrocytes) was used to investigate the effect of nitric oxide (.NO) on the damage of the BBB induced by hypoxia/reoxygenation (H/R). Permeability coefficient of fluorescein across the endothelium was used as a marker o...

    journal_title:FEBS letters

    pub_type: 杂志文章

    doi:10.1016/s0014-5793(98)00173-2

    authors: Utepbergenov DI,Mertsch K,Sporbert A,Tenz K,Paul M,Haseloff RF,Blasig IE

    更新日期:1998-03-13 00:00:00

  • Energetic aspects of intramolecular coupling between the nucleotide binding site and the distal switch II region of the yeast RAS2 protein.

    abstract::We have studied the interaction of the yeast RAS2 protein with guanine nucleotides using energetic parameters for the dissociation of RAS.nucleotide complexes. The results indicated that a Gly-->Ser substitution at position 82 led to an altered interaction with GppNHp and, to a lesser extent, also with GDP. It was als...

    journal_title:FEBS letters

    pub_type: 杂志文章

    doi:10.1016/0014-5793(94)00521-4

    authors: De Vendittis E,Fasano O

    更新日期:1994-06-27 00:00:00

  • Binding of IL-4 to the IL-13Ralpha(1)/IL-4Ralpha receptor complex leads to STAT3 phosphorylation but not to its nuclear translocation.

    abstract::Interleukin-4 (IL-4) is a pleiotropic cytokine, which acts on both hematopoietic and non-hematopoietic cells, through different types of receptor complexes. In this study, we report that in human B cells, IL-4 caused rapid phosphorylation of Janus kinase (JAK) 1 and JAK3 tyrosine kinases. In keratinocytes, the hematop...

    journal_title:FEBS letters

    pub_type: 杂志文章

    doi:10.1016/s0014-5793(99)01680-4

    authors: Wery-Zennaro S,Letourneur M,David M,Bertoglio J,Pierre J

    更新日期:1999-12-24 00:00:00

  • Human interferon-gamma lacking 23 COOH-terminal amino acids is biologically active.

    abstract::We constructed five mutated cDNAs encoding human interferon-gamma (IFN-gamma) derivatives lacking 19-23 COOH-terminal residues and expressed them in Escherichia coli. All the derivatives were purified to homogeneity. They showed substantially the same order of antiviral activity in vitro as the intact molecule, and be...

    journal_title:FEBS letters

    pub_type: 杂志文章

    doi:10.1016/0014-5793(88)80671-9

    authors: Sakaguchi M,Honda S,Ozawa M,Nishimura O

    更新日期:1988-03-28 00:00:00

  • Direction of aminoacylated transfer RNAs into antibiotic synthesis and peptidoglycan-mediated antibiotic resistance.

    abstract::Prokaryotic aminoacylated-transfer RNAs often need to be efficiently segregated between translation and other cellular biosynthetic pathways. Many clinically relevant bacteria, including Streptococcus pneumoniae, Staphylococcus aureus, Enterococcus faecalis and Pseudomonas aeruginosa direct some aminoacylated-tRNA spe...

    journal_title:FEBS letters

    pub_type: 杂志文章,评审

    doi:10.1016/j.febslet.2013.07.036

    authors: Shepherd J,Ibba M

    更新日期:2013-09-17 00:00:00

  • The respiration-driven active sodium transport system in E. coli does not function with lithium.

    abstract::Comparison of respiration-driven active transport of alkali cations from E. coli cells loaded with Na+ or Li+ showed that Li+ could not be expelled from the cells like Na+. K+ accumulation, which was fast in Na+-loaded cells, was strongly inhibited in Li+-loaded cells, despite high membrane potential and respiratory r...

    journal_title:FEBS letters

    pub_type: 杂志文章

    doi:10.1016/0014-5793(96)00531-5

    authors: Verkhovskaya ML,Verkhovsky MI,Wikström M

    更新日期:1996-06-17 00:00:00

  • Effects of detyrosinated tubulin on Na+,K+-ATPase activity and erythrocyte function in hypertensive subjects.

    abstract::Formation of tubulin/Na(+),K(+)-ATPase (NKA) complex in erythrocytes of hypertensive subjects results in a 50% reduction in NKA activity. We demonstrate here that detyrosinated tubulin, which is increased in hypertensive erythrocytes membranes, enhances the inhibitory effect of acetylated tubulin on NKA activity. More...

    journal_title:FEBS letters

    pub_type: 杂志文章

    doi:10.1016/j.febslet.2014.12.022

    authors: Amaiden MR,Santander VS,Monesterolo NE,Nigra AD,Rivelli JF,Campetelli AN,Pie J,Casale CH

    更新日期:2015-01-30 00:00:00

  • Polymyxin B, a novel inhibitor of red cell Ca2+-activated K+ channel.

    abstract::Polymyxin B (PXB), a cyclic peptide antibiotic, in concentrations 0.1-3.0 mg/ml (0.08-4.0 mmol/l), inhibited the K+ efflux induced by opening of the Ca2+-activated K+ channel (the Gárdos effect) in intact human red blood cells. The inhibition was observed when the Gárdos effect was elicited by Ca2+ in the presence of ...

    journal_title:FEBS letters

    pub_type: 杂志文章

    doi:10.1016/0014-5793(87)81152-3

    authors: Varecka L,Peterajová E,Pogády J

    更新日期:1987-12-10 00:00:00

  • In vivo oxidation-reduction kinetics of OxyR, the transcriptional activator for an oxidative stress-inducible regulon in Escherichia coli.

    abstract::The OxyR protein is a transcriptional activator for a subset of peroxide stress-inducible genes, most of which are involved in defense systems against oxidative stress. Recently, it was demonstrated that purified OxyR has one intramolecular disulfide bond, which led to the proposal that the reversible disulfide bond f...

    journal_title:FEBS letters

    pub_type: 杂志文章

    doi:10.1016/s0014-5793(99)01013-3

    authors: Tao K

    更新日期:1999-08-20 00:00:00

  • Interference with protein binding at AP2 sites by sequence-specific methylation in the late E2A promoter of adenovirus type 2 DNA.

    abstract::The in vitro methylation of the +6, +24, and -215 located 5'-CCGG-3' sequences in the late E2A promoter of adenovirus type 2 (Ad2) DNA abrogates promoter function. 5-Methyldeoxycytidine (5-mC) at positions +6 and +24 in both or either of the two DNA complements in the late E2A promoter abolishes the formation of a hig...

    journal_title:FEBS letters

    pub_type: 杂志文章

    doi:10.1016/0014-5793(91)80391-f

    authors: Hermann R,Doerfler W

    更新日期:1991-04-09 00:00:00

  • Low temperature perception in plants: effects of cold on protein phosphorylation in cell-free extracts.

    abstract::Activities of prevalent protein phosphatases decreased by nearly 95% and those of individual protein kinases were differentially reduced at low temperature. Inhibition of phosphatase activity at temperatures below 12 degrees C resulted in marked hyperphosphorylation of a 58-kDa protein (PP58). The temperature threshol...

    journal_title:FEBS letters

    pub_type: 杂志文章

    doi:10.1016/s0014-5793(97)00589-9

    authors: Monroy AF,Labbé E,Dhindsa RS

    更新日期:1997-06-30 00:00:00

  • The monofunctional glycosyltransferase of Escherichia coli is a member of a new class of peptidoglycan-synthesising enzymes.

    abstract::Using conserved fingerprints in the glycosyltransferase (GTase) domain of high-molecular-weight penicillin-binding proteins (PBP), a gene (mgt) encoding a putative monofunctional glycosyltransferase has been identified in Haemophilus influenzae and in other bacteria] species. Here we report the cloning of the homologo...

    journal_title:FEBS letters

    pub_type: 杂志文章

    doi:10.1016/0014-5793(96)00809-5

    authors: Di Berardino M,Dijkstra A,Stüber D,Keck W,Gubler M

    更新日期:1996-08-26 00:00:00

  • The seventh zinc finger motif of A20 is required for the suppression of TNF-α-induced apoptosis.

    abstract::The ubiquitin-editing enzyme A20 suppresses nuclear factor-κB (NF-κB) activation and tumor necrosis factor-α (TNF-α)-induced apoptosis in a deubiquitinating and ubiquitin ligase activity-dependent manner. Although recent studies revealed that A20 regulates NF-κB independently of its enzymatic activity through its seve...

    journal_title:FEBS letters

    pub_type: 杂志文章

    doi:10.1016/j.febslet.2015.04.022

    authors: Yamaguchi N,Yamaguchi N

    更新日期:2015-05-22 00:00:00

  • Studies on the substrate for hepatic lipogenesis in the rat.

    abstract::The contribution of hepatic glycogen to lipogenesis was studied in isolated, intact rat hepatocytes. To establish its importance as a substrate for lipogenesis, the glycogen of isolated hepatocytes was prelabelled with 14C from glucose. Evidence is presented that neither glucose nor glycogen constitute major sources o...

    journal_title:FEBS letters

    pub_type: 杂志文章

    doi:10.1016/0014-5793(84)80558-x

    authors: Geelen MJ,Hindriks GA

    更新日期:1984-09-17 00:00:00

  • Heparin promotes fibril formation by the N-terminal fragment of amyloidogenic apolipoprotein A-I.

    abstract::Glycosaminoglycans are known to be associated with extracellular amyloid deposits of various amyloidogenic proteins. In this study, we found that the glycosaminoglycan heparin greatly accelerates the elongation step in fibril formation by the N-terminal 1-83 fragment of human apolipoprotein A-I (apoA-I), especially in...

    journal_title:FEBS letters

    pub_type: 信件

    doi:10.1002/1873-3468.12426

    authors: Mikawa S,Mizuguchi C,Nishitsuji K,Baba T,Shigenaga A,Shimanouchi T,Sakashita N,Otaka A,Akaji K,Saito H

    更新日期:2016-10-01 00:00:00

  • Differential expression of the protein kinase A regulatory subunit (RIalpha) in pancreatic endocrine cells.

    abstract::A PCR-based subtractive cloning procedure was used to identify genes expressed at higher levels in the pancreatic beta cell line betaTC1, as compared to the pancreatic alpha cell line alphaTC1. One of the clones isolated by this procedure corresponded to the regulatory subunit (RIalpha) of protein kinase A (PKA). Usin...

    journal_title:FEBS letters

    pub_type: 杂志文章

    doi:10.1016/s0014-5793(98)00186-0

    authors: Arava Y,Adamsky K,Belleli A,Shaltiel S,Walker MD

    更新日期:1998-03-20 00:00:00

  • Structure of the large ribosomal subunit RNA of Phytophthora megasperma, and phylogeny of the oomycetes.

    abstract::The 5.8S and 28S rRNA sequences of the oomycete Phytophthora megasperma were determined in order to study the secondary structure of these molecules and to assess the phylogenetic position of the oomycetes among the eukaryotes. Preliminary results point to an affiliation between the oomycetes, dinoflagellates and cili...

    journal_title:FEBS letters

    pub_type: 杂志文章

    doi:10.1016/0014-5793(94)80350-1

    authors: Van der Auwera G,Chapelle S,De Wachter R

    更新日期:1994-01-31 00:00:00