当前位置： SCI文献检索 > ACS Chemical Neuroscience期刊下所有文献 > Benzothiophene Selective Estrogen Receptor Modulators Provide Neuroprotection by a novel GPR30-dependent Mechanism.

Benzothiophene Selective Estrogen Receptor Modulators Provide Neuroprotection by a novel GPR30-dependent Mechanism.

Abstract：

:The clinical benzothiophene SERM (BT-SERM), raloxifene, was compared with estrogens in protection of primary rat neurons against oxygen-glucose deprivation (OGD). Structure-activity relationships for neuroprotection were determined for a family of BT-SERMs displaying a spectrum of ERα and ERβ binding affinity and agonist/antagonist activity, leading to discovery of a neuroprotective pharmacophore, present in the clinically relevant SERMS, raloxifene and desmethylarzoxifene (DMA), for which submicromolar potency was observed for neuroprotection. BT-SERM neuroprotection did not correlate with binding to ER nor classical ER activity, however, both the neuroprotective SERMs and estrogens were shown, using pharmacological probes, to activate the same kinase signaling cascades. The antiestrogen ICI 182,780 inhibited the actions of estrogens, but not those of BT-SERMs, whereas antagonism of the G-protein coupled receptor, GPR30, was effective for both SERMs and estrogens. Since SERMs have antioxidant activity, ER-independent mechanisms were studied using the classical phenolic antioxidants, BHT and Trolox, and the Nrf2-dependent cytoprotective electrophile, sulforaphane. However, neuroprotection by these agents was not sensitive to GPR30 antagonism. Collectively, these data indicate that the activity of neuroprotective BT-SERMs is GPR30-dependent and ER-independent and not mediated by antioxidant effects. Comparison of novel BT-SERM derivatives and analogs identified a neuroprotective pharmacophore of potential use in design of novel neuroprotective agents with a spectrum of ER activity.

journal_name

ACS Chem Neurosci

journal_title

ACS chemical neuroscience

authors

Abdelhamid R,Luo J,Vandevrede L,Kundu I,Michalsen B,Litosh VA,Schiefer IT,Gherezghiher T,Yao P,Qin Z,Thatcher GR

doi

10.1021/cn100106a

subject

Has Abstract

pub_date

2011-05-18 00:00:00

pages

256-268

issue

5

issn

1948-7193

journal_volume

2

pub_type

杂志文章

相关文献

ACS Chemical Neuroscience文献大全
  • Imaging Fast-Acting Drug Effects in Humans Using 1H-MRS.

    abstract：:Proton magnetic spectroscopy (1H-MRS) is a noninvasive imaging technique that allows for the quantification of neurometabolic compounds at millimolar concentrations in the living human brain. This technique has been most often used to assess long-term changes in human brain metabolism in psychiatric disorders, pharmac...

    journal_title：ACS chemical neuroscience

    pub_type： 杂志文章

    doi：10.1021/acschemneuro.0c00474

    authors： White TL,Gonsalves MA

    更新日期：2020-09-02 00:00:00

  • Brain glucose-6-phosphate dehydrogenase protects against endogenous oxidative DNA damage and neurodegeneration in aged mice.

    abstract：:Glucose-6-phosphate dehydrogenase (G6PD) protects the embryo from endogenous and xenobiotic-enhanced oxidative DNA damage and embryopathies. Here we show in aged mice that G6PD similarly protects against endogenous reactive oxygen species (ROS)-mediated neurodegeneration. In G6PD-normal (G6PD(+/+)) and heterozygous (G...

    journal_title：ACS chemical neuroscience

    pub_type： 杂志文章

    doi：10.1021/cn400079y

    authors： Jeng W,Loniewska MM,Wells PG

    更新日期：2013-07-17 00:00:00

  • Brain Targeting by Liposome-Biomolecular Corona Boosts Anticancer Efficacy of Temozolomide in Glioblastoma Cells.

    abstract：:Temozolomide (TMZ) is the current first-line chemotherapy for treatment of glioblastoma multiforme (GBM). However, similar to other brain therapeutic compounds, access of TMZ to brain tumors is impaired by the blood-brain barrier (BBB) leading to poor response for GBM patients. To overcome this major hurdle, we have s...

    journal_title：ACS chemical neuroscience

    pub_type： 杂志文章

    doi：10.1021/acschemneuro.8b00339

    authors： Arcella A,Palchetti S,Digiacomo L,Pozzi D,Capriotti AL,Frati L,Oliva MA,Tsaouli G,Rota R,Screpanti I,Mahmoudi M,Caracciolo G

    更新日期：2018-12-19 00:00:00

  • Protective Effect of a Mitochondria-Targeted Peptide against the Development of Chemotherapy-Induced Peripheral Neuropathy in Mice.

    abstract：:Several chemotherapeutic agents used for cancer treatment induce dose-limiting peripheral neuropathy that compromises patients' quality of life and limits cancer treatment. Recently, mitochondrial dysfunction has been shown to be involved in the mechanism of chemotherapy-induced peripheral neuropathy. SS-20 is a mitoc...

    journal_title：ACS chemical neuroscience

    pub_type： 杂志文章

    doi：10.1021/acschemneuro.8b00013

    authors： Toyama S,Shimoyama N,Szeto HH,Schiller PW,Shimoyama M

    更新日期：2018-07-18 00:00:00

  • Amyloid-β Peptide Targeting Peptidomimetics for Prevention of Neurotoxicity.

    abstract：:A new generation of ligands designed to interact with the α-helix/β-strand discordant region of the amyloid-β peptide (Aβ) and to counteract its oligomerization is presented. These ligands are designed to interact with and stabilize the Aβ central helix (residues 13-26) in an α-helical conformation with increased inte...

    journal_title：ACS chemical neuroscience

    pub_type： 杂志文章

    doi：10.1021/acschemneuro.8b00485

    authors： Honcharenko D,Juneja A,Roshan F,Maity J,Galán-Acosta L,Biverstål H,Hjorth E,Johansson J,Fisahn A,Nilsson L,Strömberg R

    更新日期：2019-03-20 00:00:00

  • Water-soluble mmp-9 inhibitor prodrug generates active metabolites that cross the blood-brain barrier.

    abstract：:MMP-9 plays a detrimental role in the pathology of several neurological diseases and, thus, represents an important target for intervention. The water-soluble prodrug ND-478 is hydrolyzed to the active MMP-9 inhibitor ND-322, which in turn is N-acetylated to the even more potent metabolite ND-364. We used a sensitive ...

    journal_title：ACS chemical neuroscience

    pub_type： 杂志文章

    doi：10.1021/cn400077d

    authors： Song W,Peng Z,Gooyit M,Suckow MA,Schroeder VA,Wolter WR,Lee M,Ikejiri M,Cui J,Gu Z,Chang M

    更新日期：2013-08-21 00:00:00

  • Interrogating the Molecular Basis for Substrate Recognition in Serotonin and Dopamine Transporters with High-Affinity Substrate-Based Bivalent Ligands.

    abstract：:The transporters for the neurotransmitters serotonin and dopamine (SERT and DAT, respectively) are targets for drugs used in the treatment of mental disorders and widely used drugs of abuse. Studies of prokaryotic homologues have advanced our structural understanding of SERT and DAT, but it still remains enigmatic whe...

    journal_title：ACS chemical neuroscience

    pub_type： 杂志文章

    doi：10.1021/acschemneuro.6b00164

    authors： Andersen J,Ladefoged LK,Kristensen TN,Munro L,Grouleff J,Stuhr-Hansen N,Kristensen AS,Schiøtt B,Strømgaard K

    更新日期：2016-10-19 00:00:00

  • A small linear peptide encompassing the NGF N-terminus partly mimics the biological activities of the entire neurotrophin in PC12 cells.

    abstract：:Ever since the discovery of its neurite growth promoting activity in sympathetic and sensory ganglia, nerve growth factor (NGF) became the prototype of the large family of neurotrophins. The use of primary cultures and clonal cell lines has revealed several distinct actions of NGF and other neurotrophins. Among severa...

    journal_title：ACS chemical neuroscience

    pub_type： 杂志文章

    doi：10.1021/acschemneuro.5b00069

    authors： Travaglia A,Pietropaolo A,Di Martino R,Nicoletti VG,La Mendola D,Calissano P,Rizzarelli E

    更新日期：2015-08-19 00:00:00

  • Epigallocatechin Gallate Destabilizes α-Synuclein Fibril by Disrupting the E46-K80 Salt-Bridge and Inter-protofibril Interface.

    abstract：:The accumulation and deposition of fibrillar aggregates of α-synuclein (α-syn) into Lewy bodies are the major hallmarks of Parkinson's disease (PD) for which there is no cure yet. Disrupting preformed α-syn fibrils is considered one of the rational therapeutic strategies to combat PD. Experimental studies reported tha...

    journal_title：ACS chemical neuroscience

    pub_type： 杂志文章

    doi：10.1021/acschemneuro.0c00598

    authors： Yao Y,Tang Y,Wei G

    更新日期：2020-12-16 00:00:00

  • Facile Installation of Post-translational Modifications on the Tau Protein via Chemical Mutagenesis.

    abstract：:Post-translational modifications of proteins are ubiquitous in living organisms, as they enable an accurate control of the interactions of these macromolecules. For mechanistic studies, it would be highly advantageous to be able to produce in vitro post-translationally modified proteins with site-specificity. Here, we...

    journal_title：ACS chemical neuroscience

    pub_type： 杂志文章

    doi：10.1021/acschemneuro.0c00761

    authors： Lindstedt PR,Taylor RJ,Bernardes GJL,Vendruscolo M

    更新日期：2021-01-19 00:00:00

  • Pair of Residue Substitutions at the Outer Mouth of the Channel Pore Act as Inputs for a Boolean Logic "OR" Gate Based on the Glycine Receptor.

    abstract：:The glycine receptor (GlyR) is a ligand-activated chloride channel, whose mutations are the major cause of hereditary hyperekplexia. The hyperekplexia-causing R271Q mutation, which is located at the extracellular outer mouth of the channel pore, dramatically impairs the GlyR function manifesting a reduced sensitivity ...

    journal_title：ACS chemical neuroscience

    pub_type： 杂志文章

    doi：10.1021/acschemneuro.0c00522

    authors： Han L,Shan Q

    更新日期：2020-10-21 00:00:00

  • We know very little about the subjective effects of drugs in females.

    abstract：:Pharmaceutical companies assessing the nervous system effects of candidate therapeutics often use a behavioral assay in rodents that assesses the drug's subjective (internal stimulus) effects. Variants of this so-called "drug discrimination task" have also been widely used by basic scientist for more than 50 years to ...

    journal_title：ACS chemical neuroscience

    pub_type： 杂志文章

    doi：10.1021/acschemneuro.5b00018

    authors： Bevins RA,Charntikov S

    更新日期：2015-03-18 00:00:00

  • Preference for Glucose over Inositol Headgroup during Lysolipid Activation of G Protein-Coupled Receptor 55.

    abstract：:G protein-coupled receptor 55 (GPR55) is highly expressed in brain and peripheral nervous system. Originally deorphanized as a cannabinoid receptor, recently GPR55 has been described as a lysophospholipid-responsive receptor, specifically toward lysophosphatidylinositol and lysophosphatidyl-β-d-glucoside (LysoPtdGlc)....

    journal_title：ACS chemical neuroscience

    pub_type： 杂志文章

    doi：10.1021/acschemneuro.8b00505

    authors： Guy AT,Kano K,Ohyama J,Kamiguchi H,Hirabayashi Y,Ito Y,Matsuo I,Greimel P

    更新日期：2019-01-16 00:00:00

  • Eckmaxol, a Phlorotannin Extracted from Ecklonia maxima, Produces Anti-β-amyloid Oligomer Neuroprotective Effects Possibly via Directly Acting on Glycogen Synthase Kinase 3β.

    abstract：:Alzheimer's disease is a progressive neurodegenerative disorder that mainly affects the elderly. Soluble β-amyloid oligomer, which can induce neurotoxicity, is generally regarded as the main neurotoxin in Alzheimer's disease. Here we report that eckmaxol, a phlorotannin extracted from the brown alga Ecklonia maxima, c...

    journal_title：ACS chemical neuroscience

    pub_type： 杂志文章

    doi：10.1021/acschemneuro.7b00527

    authors： Wang J,Zheng J,Huang C,Zhao J,Lin J,Zhou X,Naman CB,Wang N,Gerwick WH,Wang Q,Yan X,Cui W,He S

    更新日期：2018-06-20 00:00:00

  • Different Inhibitors of Aβ42-Induced Toxicity Have Distinct Metal-Ion Dependency.

    abstract：:Oligomers of amyloid β-protein (Aβ) are thought to be the proximal toxic agents initiating the neuropathologic process in Alzheimer's disease (AD). Therefore, targeting the self-assembly and oligomerization of Aβ has been an important strategy for designing AD therapeutics. In parallel, research into the metallobiolog...

    journal_title：ACS chemical neuroscience

    pub_type： 杂志文章

    doi：10.1021/acschemneuro.0c00192

    authors： Mason AJ,Hurst I,Malik R,Siddique I,Solomonov I,Sagi I,Klärner FG,Schrader T,Bitan G

    更新日期：2020-08-05 00:00:00

  • Design and Synthesis of 2,3- trans-Proline Analogues as Ligands for Ionotropic Glutamate Receptors and Excitatory Amino Acid Transporters.

    abstract：:Development of pharmacological tools for the ionotropic glutamate receptors (iGluRs) is imperative for the study and understanding of the role and function of these receptors in the central nervous system. We report the synthesis of 18 analogues of (2 S,3 R)-2-carboxy-3-pyrrolidine acetic acid (3a), which explores the...

    journal_title：ACS chemical neuroscience

    pub_type： 杂志文章

    doi：10.1021/acschemneuro.9b00205

    authors： Poulie CBM,Alcaide A,Krell-Jørgensen M,Larsen Y,Astier E,Bjørn-Yoshimoto WE,Yi F,Syrenne JT,Storgaard M,Nielsen B,Frydenvang KA,Jensen AA,Hansen KB,Pickering DS,Bunch L

    更新日期：2019-06-19 00:00:00

  • Assembly of protein-based hollow spheres encapsulating a therapeutic factor.

    abstract：:Neurotrophins, as important regulators of neural development, function, and survival, have a therapeutic potential to repair damaged neurons. However, a controlled delivery of therapeutic molecules to injured tissue remains one of the greatest challenges facing the translation of novel drug therapeutics field. This st...

    journal_title：ACS chemical neuroscience

    pub_type： 杂志文章

    doi：10.1021/cn400080h

    authors： Kraskiewicz H,Breen B,Sargeant T,McMahon S,Pandit A

    更新日期：2013-09-18 00:00:00

  • DARK Classics in Chemical Neuroscience: Aminorex Analogues.

    abstract：:Aminorex (5-phenyl-4,5-dihydro-1,3-oxazol-2-amine) and 4-methylaminorex (4-methyl-5-phenyl-4,5-dihydro-1,3-oxazol-2-amine) are psychostimulants that have long been listed in Schedules IV and I of the UN Convention on Psychotropic Substances of 1971. However, a range of psychoactive analogues exist that are not interna...

    journal_title：ACS chemical neuroscience

    pub_type： 历史文章,杂志文章,评审

    doi：10.1021/acschemneuro.8b00415

    authors： Maier J,Mayer FP,Brandt SD,Sitte HH

    更新日期：2018-10-17 00:00:00

  • Improved Calibration of Voltammetric Sensors for Studying Pharmacological Effects on Dopamine Transporter Kinetics in Vivo.

    abstract：:The distribution and density of neurons within the brain poses many challenges when making quantitative measurements of neurotransmission in the extracellular space. A volume neurotransmitter is released into the synapse during chemical communication and must diffuse through the extracellular space to an implanted sen...

    journal_title：ACS chemical neuroscience

    pub_type： 杂志文章

    doi：10.1021/cn500020s

    authors： Atcherley CW,Laude ND,Monroe EB,Wood KM,Hashemi P,Heien ML

    更新日期：2015-09-16 00:00:00

  • (-)-Hardwickiic Acid and Hautriwaic Acid Induce Antinociception via Blockade of Tetrodotoxin-Sensitive Voltage-Dependent Sodium Channels.

    abstract：:For an affliction that debilitates an estimated 50 million adults in the United States, the current chronic pain management approaches are inadequate. The Centers for Disease Control and Prevention have called for a minimization in opioid prescription and use for chronic pain conditions, and thus, it is imperative to ...

    journal_title：ACS chemical neuroscience

    pub_type： 杂志文章

    doi：10.1021/acschemneuro.8b00617

    authors： Cai S,Bellampalli SS,Yu J,Li W,Ji Y,Wijeratne EMK,Dorame A,Luo S,Shan Z,Khanna M,Moutal A,Streicher JM,Gunatilaka AAL,Khanna R

    更新日期：2019-03-20 00:00:00

  • Akt-dependent and isoform-specific regulation of dopamine transporter cell surface expression.

    abstract：:Dopamine (DA) is a neurotransmitter implicated in multiple functions, including movement, cognition, motivation, and reward. The DA transporter (DAT) is responsible for clearing extracellular DA, thereby terminating DA neurotransmission. Previously, it has been shown that insulin signaling through protein kinase B/Akt...

    journal_title：ACS chemical neuroscience

    pub_type： 信件

    doi：10.1021/cn100031t

    authors： Speed NK,Matthies HJ,Kennedy JP,Vaughan RA,Javitch JA,Russo SJ,Lindsley CW,Niswender K,Galli A

    更新日期：2010-07-21 00:00:00

  • Tau-derived-hexapeptide 306VQIVYK311 aggregation inhibitors: nitrocatechol moiety as a pharmacophore in drug design.

    abstract：:The nitrocatechol derivatives tolcapone (1) and entacapone (2), used as adjunctive therapy in the treatment of Parkinson's disease, were investigated for their potential to inhibit the tau-derived-hexapeptide 306VQIVYK311. They were compared to small molecules that contain similar pharmacophores including the catechol...

    journal_title：ACS chemical neuroscience

    pub_type： 杂志文章

    doi：10.1021/cn400151a

    authors： Mohamed T,Hoang T,Jelokhani-Niaraki M,Rao PP

    更新日期：2013-12-18 00:00:00

  • Selective acetylcholinesterase inhibitor activated by acetylcholinesterase releases an active chelator with neurorescuing and anti-amyloid activities.

    abstract：:The finding that acetylcholinesterase (AChE) colocalizes with β-amyloid (Aβ) and promotes and accelerates Aβ aggregation has renewed an intense interest in developing new multifunctional AChE inhibitors as potential disease-modifying drugs for Alzheimer's therapy. To this end, we have developed a new class of selectiv...

    journal_title：ACS chemical neuroscience

    pub_type： 杂志文章

    doi：10.1021/cn100069c

    authors： Zheng H,Youdim MB,Fridkin M

    更新日期：2010-11-17 00:00:00

  • Identifying New AMP-Activated Protein Kinase Inhibitors That Protect against Ischemic Brain Injury.

    abstract：:We recently reported that AMP-activated protein kinase (AMPK) contributes to zinc-induced neuronal death by inducing Bim, a pro-apoptotic Bcl-2 homology domain 3-only protein, in a liver kinase B1 (LKB1)-dependent manner. Current data suggest AMPK plays key roles in excitotoxicity and ischemic brain injury, with zinc ...

    journal_title：ACS chemical neuroscience

    pub_type： 杂志文章

    doi：10.1021/acschemneuro.8b00654

    authors： Eom JW,Kim TY,Seo BR,Park H,Koh JY,Kim YH

    更新日期：2019-05-15 00:00:00

  • Detection of orexin A neuropeptide in biological fluids using a zinc oxide field effect transistor.

    abstract：:Biomarkers which are indicative of acute physiological and emotional states are studied in a number of different areas in cognitive neuroscience. Currently, many cognitive studies are conducted based on programmed tasks followed by timed biofluid sampling, central laboratory processing, and followed by data analysis. ...

    journal_title：ACS chemical neuroscience

    pub_type： 杂志文章

    doi：10.1021/cn300159e

    authors： Hagen J,Lyon W,Chushak Y,Tomczak M,Naik R,Stone M,Kelley-Loughnane N

    更新日期：2013-03-20 00:00:00

  • Correlation between Cellular Uptake and Cytotoxicity of Fragmented α-Synuclein Amyloid Fibrils Suggests Intracellular Basis for Toxicity.

    abstract：:Aggregation and intracellular deposition of the protein α-synuclein is an underlying characteristic of Parkinson's disease. α-Synuclein assemblies also undergo cell-cell spreading, facilitating propagation of their cellular pathology. Understanding how cellular interactions and uptake of extracellular α-synuclein asse...

    journal_title：ACS chemical neuroscience

    pub_type： 杂志文章

    doi：10.1021/acschemneuro.9b00562

    authors： Zhang X,Wesén E,Kumar R,Bernson D,Gallud A,Paul A,Wittung-Stafshede P,Esbjörner EK

    更新日期：2020-02-05 00:00:00

  • Endogenous Serotonin 5-HT2A and 5-HT2C Receptors Associate in the Medial Prefrontal Cortex.

    abstract：:The 5-HT2A receptor (5-HT2AR) and 5-HT2CR are localized to the same neurons within the medial prefrontal cortex (mPFC), which regulates executive function, decision-making, and reward-guided learning and memory processes. The 5-HT2AR and 5-HT2CR coimmunoprecipitate in the mPFC of male Sprague-Dawley rats, while in vit...

    journal_title：ACS chemical neuroscience

    pub_type： 杂志文章

    doi：10.1021/acschemneuro.8b00669

    authors： Price AE,Sholler DJ,Stutz SJ,Anastasio NC,Cunningham KA

    更新日期：2019-07-17 00:00:00

  • Synaptic plasticity, a symphony in GEF.

    abstract：:Dendritic spines are the postsynaptic sites for the majority of excitatory synapses in the mammalian forebrain. While many spines display great stability, others change shape in a matter of seconds to minutes. These rapid alterations in dendritic spine number and size require tight control of the actin cytoskeleton, t...

    journal_title：ACS chemical neuroscience

    pub_type： 杂志文章

    doi：10.1021/cn100012x

    authors： Kiraly DD,Eipper-Mains JE,Mains RE,Eipper BA

    更新日期：2010-05-19 00:00:00

  • Rethinking Glioblastoma Therapy: MDA-9/Syntenin Targeted Small Molecule.

    abstract：:Effective therapies for glioblastoma multiforme (GBM) are not currently available. A small molecule has been identified using fragment-based drug-discovery guided by NMR that targets important protein-protein interactions controlling GBM invasion and pathogenicity. This first generation drug displays excellent pharmac...

    journal_title：ACS chemical neuroscience

    pub_type： 杂志文章,评审

    doi：10.1021/acschemneuro.9b00016

    authors： Das SK,Sarkar D,Cavenee WK,Emdad L,Fisher PB

    更新日期：2019-03-20 00:00:00

  • Histamine H3 receptor activation counteracts adenosine A2A receptor-mediated enhancement of depolarization-evoked [3H]-GABA release from rat globus pallidus synaptosomes.

    abstract：:High levels of histamine H3 receptors (H3Rs) are found in the globus pallidus (GP), a neuronal nucleus in the basal ganglia involved in the control of motor behavior. By using rat GP isolated nerve terminals (synaptosomes), we studied whether H3R activation modified the previously reported enhancing action of adenosin...

    journal_title：ACS chemical neuroscience

    pub_type： 杂志文章

    doi：10.1021/cn500001m

    authors： Morales-Figueroa GE,Márquez-Gómez R,González-Pantoja R,Escamilla-Sánchez J,Arias-Montaño JA

    更新日期：2014-08-20 00:00:00