当前位置： SCI文献检索 > ACS Chemical Neuroscience期刊下所有文献 > Rethinking Glioblastoma Therapy: MDA-9/Syntenin Targeted Small Molecule.

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 pharmacokinetic properties, passes through the blood-brain barrier and is effective in preclinical animal models of GBM, particularly when combined with radiation therapy.

journal_name

ACS Chem Neurosci

journal_title

ACS chemical neuroscience

authors

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

doi

10.1021/acschemneuro.9b00016

subject

Has Abstract

pub_date

2019-03-20 00:00:00

pages

1121-1123

issue

3

issn

1948-7193

journal_volume

10

pub_type

杂志文章,评审

相关文献

ACS Chemical Neuroscience文献大全
  • 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

  • Targeting Chondroitin Sulfate Proteoglycans: An Emerging Therapeutic Strategy to Treat CNS Injury.

    abstract：:Chondroitin sulfate proteoglycans (CSPGs) are the most abundant components of glial scar formed after severe traumatic brain injury as well as spinal cord injury and play a crucial inhibitory role in axonal regeneration by selective contraction of filopodia of the growth cone of sprouting neurites. Healing of central ...

    journal_title：ACS chemical neuroscience

    pub_type： 杂志文章

    doi：10.1021/acschemneuro.0c00004

    authors： Mukherjee N,Nandi S,Garg S,Ghosh S,Ghosh S,Samat R,Ghosh S

    更新日期：2020-02-05 00:00:00

  • Olive Oil Lignan (+)-Acetoxypinoresinol Peripheral Motor and Neuronal Protection against the Tremorgenic Mycotoxin Penitrem A Toxicity via STAT1 Pathway.

    abstract：:Penitrem A, PA, is an indole diterpene alkaloid produced by several fungal species. PA acts as a selective Ca2+-dependent K-channels (Maxi-K, BK) antagonist in brain, causing motor system dysfunctions including tremors and seizures. However, its molecular mechanism at the peripheral nervous system (PNS) is still ambig...

    journal_title：ACS chemical neuroscience

    pub_type： 杂志文章

    doi：10.1021/acschemneuro.0c00458

    authors： Qusa MH,Abdelwahed KS,Meyer SA,El Sayed KA

    更新日期：2020-11-04 00:00:00

  • Discovery of Small Molecule Kappa Opioid Receptor Agonist and Antagonist Chemotypes through a HTS and Hit Refinement Strategy.

    abstract：:Herein we present the outcome of a high throughput screening (HTS) campaign-based strategy for the rapid identification and optimization of selective and general chemotypes for both kappa (κ) opioid receptor (KOR) activation and inhibition. In this program, we have developed potent antagonists (IC(50) < 120 nM) or ago...

    journal_title：ACS chemical neuroscience

    pub_type： 杂志文章

    doi：10.1021/cn200128x

    authors： Frankowski KJ,Hedrick MP,Gosalia P,Li K,Shi S,Whipple D,Ghosh P,Prisinzano TE,Schoenen FJ,Su Y,Vasile S,Sergienko E,Gray W,Hariharan S,Milan L,Heynen-Genel S,Mangravita-Novo A,Vicchiarelli M,Smith LH,Streicher JM,

    更新日期：2012-03-21 00:00:00

  • Direct Reprogramming of Glioblastoma Cells into Neurons Using Small Molecules.

    abstract：:Glioblastoma multiforme, a type of deadly brain cancer, originates most commonly from astrocytes found in the brain. Current multimodal treatments for glioblastoma minimally increase life expectancy, but significant advancements in prognosis have not been made in the past few decades. Here we investigate cellular repr...

    journal_title：ACS chemical neuroscience

    pub_type： 杂志文章

    doi：10.1021/acschemneuro.8b00365

    authors： Lee C,Robinson M,Willerth SM

    更新日期：2018-12-19 00:00:00

  • Phospho-Tau Impairs Nuclear-Cytoplasmic Transport.

    abstract：:Aggregation of hyperphosphorylated tau is the hallmark of several tauopathies, including Alzheimer's disease (AD). Although the mechanism underlying tau-associated neuronal damage remains unclear, it is believed that tau hyperphosphorylation is one of the key features in disease progression. A recent study demonstrate...

    journal_title：ACS chemical neuroscience

    pub_type： 杂志文章,评审

    doi：10.1021/acschemneuro.8b00632

    authors： Tripathi T,Prakash J,Shav-Tal Y

    更新日期：2019-01-16 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

  • Investigation of a calcium-responsive contrast agent in cellular model systems: feasibility for use as a smart molecular probe in functional MRI.

    abstract：:Responsive or smart contrast agents (SCAs) represent a promising direction for development of novel functional MRI (fMRI) methods for the eventual noninvasive assessment of brain function. In particular, SCAs that respond to Ca(2+) may allow tracking neuronal activity independent of brain vasculature, thus avoiding th...

    journal_title：ACS chemical neuroscience

    pub_type： 杂志文章

    doi：10.1021/cn500049n

    authors： Angelovski G,Gottschalk S,Milošević M,Engelmann J,Hagberg GE,Kadjane P,Andjus P,Logothetis NK

    更新日期：2014-05-21 00:00:00

  • An Orally Active Phenylaminotetralin-Chemotype Serotonin 5-HT7 and 5-HT1A Receptor Partial Agonist that Corrects Motor Stereotypy in Mouse Models.

    abstract：:Stereotypy (e.g., repetitive hand waving) is a key phenotype of autism spectrum disorder, Fragile X and Rett syndromes, and other neuropsychiatric disorders, and its severity correlates with cognitive and attention deficits. There are no effective treatments, however, for stereotypy. Perturbation of serotonin (5-HT) n...

    journal_title：ACS chemical neuroscience

    pub_type： 杂志文章

    doi：10.1021/acschemneuro.5b00099

    authors： Canal CE,Felsing DE,Liu Y,Zhu W,Wood JT,Perry CK,Vemula R,Booth RG

    更新日期：2015-07-15 00:00:00

  • Identification of Novel 1-O-Substituted Aporphine Analogues as Potent 5-HT2C Receptor Agonists.

    abstract：:The 5-HT2C receptor has emerged as a promising target in the treatment of a variety of central nervous system disorders. We have first identified aporphines as a new class of 5-HT2C receptor agonists. Structure-activity relationship results indicate that the aporphine core may be required for 5-HT2C receptor activity,...

    journal_title：ACS chemical neuroscience

    pub_type： 杂志文章

    doi：10.1021/acschemneuro.9b00563

    authors： Mao Q,Zhang B,Li W,Tian S,Shui W,Ye N

    更新日期：2020-02-19 00:00:00

  • A Novel Negative Allosteric Modulator Selective for GluN2C/2D-Containing NMDA Receptors Inhibits Synaptic Transmission in Hippocampal Interneurons.

    abstract：:N-Methyl-d-aspartate receptors (NMDARs) are ionotropic glutamate receptors that mediate excitatory synaptic transmission and have been implicated in numerous neurological disorders. NMDARs typically comprise two GluN1 and two GluN2 subunits. The four GluN2 subtypes (GluN2A-GluN2D) have distinct functional properties a...

    journal_title：ACS chemical neuroscience

    pub_type： 杂志文章

    doi：10.1021/acschemneuro.7b00329

    authors： Swanger SA,Vance KM,Acker TM,Zimmerman SS,DiRaddo JO,Myers SJ,Bundgaard C,Mosley CA,Summer SL,Menaldino DS,Jensen HS,Liotta DC,Traynelis SF

    更新日期：2018-02-21 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

  • 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

  • AMPA Receptor Noncompetitive Inhibitors Occupy a Promiscuous Binding Site.

    abstract：:Noncompetitive inhibitors of AMPA receptors have attracted interest in recent years as antiepileptic drugs. However, their development is hindered by a lack of detailed understanding of the protein-inhibitor interaction mechanisms. Recently, structures of AMPA receptor complexes with the structurally dissimilar, nonco...

    journal_title：ACS chemical neuroscience

    pub_type： 杂志文章

    doi：10.1021/acschemneuro.9b00344

    authors： Narangoda C,Sakipov SN,Kurnikova MG

    更新日期：2019-11-20 00:00:00

  • Neuron Activity Dependent Redox Compartmentation Revealed with a Second Generation Red-Shifted Ratiometric Sensor.

    abstract：:Oxidative stress is a hallmark of several aging and trauma related neurological disorders, but the precise details of how altered neuronal activity elicits subcellular redox changes have remained difficult to resolve. Current redox sensitive dyes and fluorescent proteins can quantify spatially distinct changes in reac...

    journal_title：ACS chemical neuroscience

    pub_type： 杂志文章

    doi：10.1021/acschemneuro.0c00342

    authors： Radhakrishnan S,Norley J,Wendt S,LeRoy N,Hall H,Norcross S,Doan S,Snaider J,MacVicar BA,Weake VM,Huang L,Tantama M

    更新日期：2020-09-02 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

  • Delivery of Dual Drug Loaded Lipid Based Nanoparticles across the Blood-Brain Barrier Impart Enhanced Neuroprotection in a Rotenone Induced Mouse Model of Parkinson's Disease.

    abstract：:Parkinson's disease (PD) is the most widespread form of dementia where there is an age related degeneration of dopaminergic neurons in the substantia nigra region of the brain. Accumulation of α-synuclein (αS) protein aggregate, mitochondrial dysfunction, oxidative stress, and neuronal cell death are the pathological ...

    journal_title：ACS chemical neuroscience

    pub_type： 杂志文章

    doi：10.1021/acschemneuro.6b00207

    authors： Kundu P,Das M,Tripathy K,Sahoo SK

    更新日期：2016-12-21 00:00:00

  • Syntheses and evaluation of carbon-11- and fluorine-18-radiolabeled pan-tropomyosin receptor kinase (Trk) inhibitors: exploration of the 4-aza-2-oxindole scaffold as Trk PET imaging agents.

    abstract：:Tropomyosin receptor kinases (TrkA/B/C) are critically involved in the development of the nervous system, in neurological disorders as well as in multiple neoplasms of both neural and non-neural origins. The development of Trk radiopharmaceuticals would offer unique opportunities toward a more complete understanding o...

    journal_title：ACS chemical neuroscience

    pub_type： 杂志文章

    doi：10.1021/cn500193f

    authors： Bernard-Gauthier V,Aliaga A,Aliaga A,Boudjemeline M,Hopewell R,Kostikov A,Rosa-Neto P,Thiel A,Schirrmacher R

    更新日期：2015-02-18 00:00:00

  • Investigation of the Role of Chirality in the Interaction with σ Receptors and Effect on Binge Eating Episode of a Potent σ1 Antagonist Analogue of Spipethiane.

    abstract：:The enantiomers of the potent σ1 receptor antagonist (±)-1 were synthesized and evaluated for their affinity at σ1, σ2 receptors and dopamine transporter (DAT). Analogously to (±)-1, both of the enantiomers showed very high affinity for the σ1 receptor and unprecedented selectivity over both the σ2 receptor and DAT. T...

    journal_title：ACS chemical neuroscience

    pub_type： 杂志文章

    doi：10.1021/acschemneuro.9b00261

    authors： Del Bello F,Micioni Di Bonaventura MV,Bonifazi A,Wünsch B,Schepmann D,Giancola JB,Micioni Di Bonaventura E,Vistoli G,Giorgioni G,Quaglia W,Piergentili A,Cifani C

    更新日期：2019-08-21 00:00:00

  • Recent Advances in Virtual Screening for Cholinesterase Inhibitors.

    abstract：:Alzheimer's disease (AD) is a significant health crisis, and current treatments provide only limited benefits to cognition at the cost of serious side effects. Recently, virtual screening techniques such as ligand-based virtual screening (LBVS) and structure-based virtual screening (SBVS) have emerged as powerful drug...

    journal_title：ACS chemical neuroscience

    pub_type： 杂志文章

    doi：10.1021/acschemneuro.0c00627

    authors： Miles JA,Ross BP

    更新日期：2021-01-06 00:00:00

  • DARK Classics in Chemical Neuroscience: Opium, a Historical Perspective.

    abstract：:Opium is the latex from the opium poppy Papaver somniferum L., which humankind has utilized since ancient Mesopotamia all the way to modern times. Opium used to be surrounded in divine mystery or magic-like abilities and was given to cure a wide variety of diseases until its analgesic, antitussive, and antidiarrheal p...

    journal_title：ACS chemical neuroscience

    pub_type： 历史文章,杂志文章,评审

    doi：10.1021/acschemneuro.8b00459

    authors： Presley CC,Lindsley CW

    更新日期：2018-10-17 00:00:00

  • Neurotensin Analogues Containing Cyclic Surrogates of Tyrosine at Position 11 Improve NTS2 Selectivity Leading to Analgesia without Hypotension and Hypothermia.

    abstract：:Neurotensin (NT) exerts its analgesic effects through activation of the G protein-coupled receptors NTS1 and NTS2. This opioid-independent antinociception represents a potential alternative for pain management. While activation of NTS1 also induces a drop in blood pressure and body temperature, NTS2 appears to be an a...

    journal_title：ACS chemical neuroscience

    pub_type： 杂志文章

    doi：10.1021/acschemneuro.9b00390

    authors： Eiselt E,Gonzalez S,Martin C,Chartier M,Betti C,Longpré JM,Cavelier F,Tourwé D,Gendron L,Ballet S,Sarret P

    更新日期：2019-11-20 00:00:00

  • Pharmacology of Valinate and tert-Leucinate Synthetic Cannabinoids 5F-AMBICA, 5F-AMB, 5F-ADB, AMB-FUBINACA, MDMB-FUBINACA, MDMB-CHMICA, and Their Analogues.

    abstract：:Indole and indazole synthetic cannabinoids (SCs) featuring l-valinate or l-tert-leucinate pendant group have recently emerged as prevalent recreational drugs, and their use has been associated with serious adverse health effects. Due to the limited pharmacological data available for these compounds, 5F-AMBICA, 5F-AMB,...

    journal_title：ACS chemical neuroscience

    pub_type： 杂志文章

    doi：10.1021/acschemneuro.6b00137

    authors： Banister SD,Longworth M,Kevin R,Sachdev S,Santiago M,Stuart J,Mack JB,Glass M,McGregor IS,Connor M,Kassiou M

    更新日期：2016-09-21 00:00:00

  • The KDM5 Inhibitor KDM5-C70 Induces Astrocyte Differentiation in Rat Neural Stem Cells.

    abstract：:Members of the lysine-specific histone demethylase 5 (KDM5/JARID1) family are known to play important roles in stem cell fate determination. Here, using the KDM5 inhibitor C70 (KDM5-C70), we demonstrated that the histone demethylase activity of the KDM5 enzyme is essential for the repression of astrocytic differentiat...

    journal_title：ACS chemical neuroscience

    pub_type： 杂志文章

    doi：10.1021/acschemneuro.0c00613

    authors： Lee HR,Ann J,Kim YM,Lee J,Kim HJ

    更新日期：2021-01-22 00:00:00

  • Discovery and Optimization of Chromone Derivatives as Novel Selective Phosphodiesterase 10 Inhibitors.

    abstract：:Phosphodiesterase 10 (PDE10) inhibitors have received much attention as promising therapeutic agents for central nervous system (CNS) disorders such as schizophrenia and Huntington's disease. Recently, a hit compound 1 with a novel chromone scaffold has shown moderate inhibitory activity against PDE10A (IC50 = 500 nM)...

    journal_title：ACS chemical neuroscience

    pub_type： 杂志文章

    doi：10.1021/acschemneuro.0c00024

    authors： Yu YF,Zhang C,Huang YY,Zhang S,Zhou Q,Li X,Lai Z,Li Z,Gao Y,Wu Y,Guo L,Wu D,Luo HB

    更新日期：2020-04-01 00:00:00

  • A Review of Single-Nucleotide Polymorphisms in Orexigenic Neuropeptides Targeting G Protein-Coupled Receptors.

    abstract：:Many physiological pathways are involved in appetite, food intake, and the maintenance of energy homeostasis. In particular, neuropeptides within the central nervous system have been demonstrated to be critical signaling molecules for modulating appetite. Both anorexigenic (appetite-decreasing) and orexigenic (appetit...

    journal_title：ACS chemical neuroscience

    pub_type： 杂志文章,评审

    doi：10.1021/acschemneuro.8b00151

    authors： Ericson MD,Haskell-Luevano C

    更新日期：2018-06-20 00:00:00

  • Immunity-Boosting Spices and the Novel Coronavirus.

    abstract：:Although there is no reported genetic predisposition in contracting coronavirus disease 2019 (COVID-19), the mortality rate varies among different ethnic groups. Here we determined potential correlation between COVID-19 and spice consumption. The data from 163 countries including total cases, total deaths, and total r...

    journal_title：ACS chemical neuroscience

    pub_type： 杂志文章

    doi：10.1021/acschemneuro.0c00239

    authors： Elsayed Y,Khan NA

    更新日期：2020-06-17 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

  • DARK Classics in Chemical Neuroscience: Morphine.

    abstract：:As the major psychoactive agent in opium and direct precursor for heroin, morphine is a historically critical molecule in chemical neuroscience. A structurally complex phenanthrene alkaloid produced by Papaver somniferum, morphine has fascinated chemists seeking to disentangle pharmacologically beneficial analgesic ef...

    journal_title：ACS chemical neuroscience

    pub_type： 历史文章,杂志文章,评审

    doi：10.1021/acschemneuro.8b00150

    authors： Devereaux AL,Mercer SL,Cunningham CW

    更新日期：2018-10-17 00:00:00

  • Binding of Metal-Ion-Induced Tau Oligomers to Lipid Surfaces Is Enhanced by GSK-3β-Mediated Phosphorylation.

    abstract：:While fibrillar deposits of hyperphosphorylated protein tau are a key hallmark of several neurodegenerative diseases such as Alzheimer's disease, small oligomers have been speculated to be the key toxic aggregate species. Trivalent metal ions were shown to promote tau oligomer formation in vitro. However, little is kn...

    journal_title：ACS chemical neuroscience

    pub_type： 杂志文章

    doi：10.1021/acschemneuro.9b00459

    authors： Nuebling GS,Plesch E,Ruf VC,Högen T,Lorenzl S,Kamp F,Giese A,Levin J

    更新日期：2020-03-18 00:00:00