Synaptic plasticity, a symphony in GEF.

abstract：:1-Methyl-4-phenylpyridinium (MPP+) induces microglial activation and degeneration of dopaminergic (DAergic) neurons. Donepezil is a well-known acetylcholinesterase inhibitor used clinically to treat cognitive dysfunction in Alzheimer's disease (AD). In the present study, we tested the hypothesis that MPP+ promotes mic...

journal_title：ACS chemical neuroscience

authors： Chen T,Hou R,Xu S,Wu C

更新日期：2015-10-21 00:00:00

abstract：:Lithium has been used for the treatment of mood disorders for decades though the molecular mechanism of its therapeutic action and intracellular targets remain furtive. We report that neurotropic agent Li+ binds to the neuronal calcium sensor, Downstream Regulatory Element Antagonist Modulator (DREAM), with an equilib...

journal_title：ACS chemical neuroscience

authors： Azam S,Bhattarai N,Riveron A,Rodriguez S,Chapagain PP,Miksovska J

更新日期：2020-09-02 00:00:00

abstract：:Glutamate is the major excitatory transmitter in the mammalian CNS, exerting its effects through both ionotropic and metabotropic glutamate receptors. The metabotropic glutamate receptors (mGlus) belong to family C of the G-protein-coupled receptors (GPCRs). The eight mGlus identified to date are classified into three...

journal_title：ACS chemical neuroscience

authors： Lindsley CW,Bates BS,Menon UN,Jadhav SB,Kane AS,Jones CK,Rodriguez AL,Conn PJ,Olsen CM,Winder DG,Emmitte KA

更新日期：2011-08-17 00:00:00

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

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

abstract：:Several pharmacophore models have been proposed for 5-HT2A serotonin receptor antagonists. These typically consist of two aromatic/hydrophobic moieties separated by a given distance from each other, and from a basic amine. Although specified distances might vary, the models are relatively similar in their general cons...

journal_title：ACS chemical neuroscience

authors： Younkin J,Gaitonde SA,Ellaithy A,Vekariya R,Baki L,Moreno JL,Shah S,Drossopoulos P,Hideshima KS,Eltit JM,González-Maeso J,Logothetis DE,Dukat M,Glennon RA

更新日期：2016-09-21 00:00:00

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

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

abstract：:The permeation of the potassium ion (K+) through the selectivity filter (SF) of the large conductance Ca2+-activated potassium (Slo1) channel remains an interesting question to study. Although the mode of K+ entering and leaving the SF has been revealed, the mechanism of K+ passing through the SF is still not clear. I...

journal_title：ACS chemical neuroscience

authors： Guo J,Tan Z,Ji Y

更新日期：2019-08-21 00:00:00

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

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

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

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

abstract：:The discovery of haloperidol catalyzed a breakthrough in our understanding of the biochemical basis of schizophrenia, improved the treatment of psychosis, and facilitated deinstitutionalization. In doing so, it solidified the role for chemical neuroscience as a means to elucidate the molecular underpinnings of complex...

journal_title：ACS chemical neuroscience

authors： Tyler MW,Zaldivar-Diez J,Haggarty SJ

更新日期：2017-03-15 00:00:00

abstract：:Accumulating evidence suggested that soluble oligomeric β-amyloid protein (Aβ) exerts diverse roles in neuronal cell death, neuroinflammation, oxidative stress, and the eventual dementia associated with Alzheimer's disease (AD). Developing an agent with multiple properties may be a reasonable strategy for the treatmen...

journal_title：ACS chemical neuroscience

authors： Yang S,Liu W,Lu S,Tian YZ,Wang WY,Ling TJ,Liu RT

更新日期：2016-04-20 00:00:00

abstract：:Abnormally aggregated tau is the hallmark pathology of tauopathy neurodegenerative disorders and is a target for development of both diagnostic tools and therapeutic strategies across the tauopathy disease spectrum. Development of carbon-11- or fluorine-18-labeled radiotracers with appropriate affinity and specificity...

journal_title：ACS chemical neuroscience

authors： Fawaz MV,Brooks AF,Rodnick ME,Carpenter GM,Shao X,Desmond TJ,Sherman P,Quesada CA,Hockley BG,Kilbourn MR,Albin RL,Frey KA,Scott PJ

更新日期：2014-08-20 00:00:00

abstract：:In our efforts to develop hybrid compounds of curcumin and melatonin as potential disease-modifying agents for Alzheimer's disease (AD), a potent lead hybrid compound, Z-CM-I-1, has been recently identified and biologically characterized in vitro. In this work, we report the in vivo effects of Z-CM-I-1 on AD pathologi...

journal_title：ACS chemical neuroscience

authors： Gerenu G,Liu K,Chojnacki JE,Saathoff JM,Martínez-Martín P,Perry G,Zhu X,Lee HG,Zhang S

更新日期：2015-08-19 00:00:00

abstract：:γ-Secretase is a multiprotein complex that catalyzes intramembrane proteolysis associated with Alzheimer's disease and cancer. Here, we have developed potent sulfonamide clickable photoaffinity probes that target γ-secretase in vitro and in cells by incorporating various photoreactive groups and walking the clickable ...

journal_title：ACS chemical neuroscience

authors： Crump CJ,Murrey HE,Ballard TE,Am Ende CW,Wu X,Gertsik N,Johnson DS,Li YM

更新日期：2016-08-17 00:00:00

abstract：:Exosomes, which are lipid bilayer membrane vesicles, have been implicated as carriers of biological macromolecules. In recent years, the functions of exosomes in the spreading of pathological conversion of proteins among neurons have drawn particular attention in Parkinson's disease research. Extracellular α-synuclein...

journal_title：ACS chemical neuroscience

authors： Yuan L,Li JY

更新日期：2019-02-20 00:00:00

abstract：:Early diagnosis in Alzheimer's disease (AD), prior to the appearance of marked clinical symptoms, is critical to prevent irreversible neuronal damage and neural malfunction that lead to dementia and death. Therefore, there is an urgent need to generate new contrast agents which reveal by a noninvasive method the prese...

journal_title：ACS chemical neuroscience

authors： Fernández T,Martínez-Serrano A,Cussó L,Desco M,Ramos-Gómez M

更新日期：2018-05-16 00:00:00

abstract：:The intramembrane aspartyl protease γ-secretase (GSEC) cleaves single-span transmembrane helices including the C-terminal fragment of the amyloid precursor protein (APP). This substrate is initially cleaved at the ϵ-site followed by successive processing (trimming) events mostly in steps of three amino acids. GSEC is ...

journal_title：ACS chemical neuroscience

authors： Hitzenberger M,Zacharias M

更新日期：2019-03-20 00:00:00

abstract：:Neurons choose growth pathways with half hearted reluctance, behavior that may be appropriate to maintain fixed long lasting connections but not to regenerate them. We now recognize that intrinsic brakes on regrowth are widely expressed in these hesitant neurons and include classical tumor suppressor molecules. Here, ...

journal_title：ACS chemical neuroscience

authors： Zochodne DW

更新日期：2014-08-20 00:00:00

abstract：:α-Synuclein (α-syn) is a 140-amino acid protein that plays a central role in the pathogenesis of Parkinson's disease (PD) and other synucleinopathies. However, the molecular determinants that are responsible for triggering and/or propagating α-syn aggregation and toxicity remain poorly understood. Several studies have...

journal_title：ACS chemical neuroscience

authors： Lu Y,Prudent M,Fauvet B,Lashuel HA,Girault HH

更新日期：2011-11-16 00:00:00

abstract：:Several antidepressants increase adult hippocampal neurogenesis (ahNG) in rodents, primates, and, potentially, humans. This effect may at least partially account for their therapeutic activity. The availability of antidepressants whose mechanism of action involves different neurotransmitter receptors represents an opp...

journal_title：ACS chemical neuroscience

authors： Bortolotto V,Mancini F,Mangano G,Salem R,Xia E,Del Grosso E,Bianchi M,Canonico PL,Polenzani L,Grilli M

更新日期：2017-09-20 00:00:00

abstract：:Promotion of neurite outgrowth and synapse formation is a key step for nervous tissue regeneration. It is important for finding a new biomaterial to guide neuron growth to target neurons. Aminated graphene oxide (NH2-GO) displays electrical properties and dispersibility, which may change the surface charge of neurons ...

journal_title：ACS chemical neuroscience

authors： Liu M,Huang C,Jia Z,Zhao Z,Xiao X,Wang A,Li P,Guan X,Zhou G,Fan Y

更新日期：2020-02-19 00:00:00

abstract：:In this article, we have demonstrated the in vivo efficacy of D-512 and D-440 in a 6-OHDA-induced unilaterally lesioned rat model experiment, a Parkinson's disease animal model. D-512 is a novel highly potent D2/D3 agonist, and D-440 is a novel highly selective D3 agonist. We evaluated the neuroprotective properties o...

journal_title：ACS chemical neuroscience

authors： Santra S,Xu L,Shah M,Johnson M,Dutta A

更新日期：2013-10-16 00:00:00

abstract：:Of the free-living amoebae (FLA) Naegleria fowleri, Balamuthia mandrillaris, and Acanthamoeba spp. are known to cause encephalitis. Coined with the term "brain-eating amoebae" (BEA), infection of the central nervous system with FLA has a high mortality rate. A combination of diagnostic delay, lack of new drug developm...

journal_title：ACS chemical neuroscience

authors： Baig AM,Khaleeq A,Nazim F

更新日期：2020-08-19 00:00:00

abstract：:A hallmark of Alzheimer's disease (AD) is the formation of senile plaques comprised of the β-amyloid (Aβ) peptide. Aβ fibrillization is a complex nucleation-dependent process involving a variety of metastable intermediate aggregates and features the formation of inter- and intramolecular salt bridges involving lysine ...

journal_title：ACS chemical neuroscience

authors： Pilkington AW 4th,Schupp J,Nyman M,Valentine SJ,Smith DM,Legleiter J

更新日期：2020-01-15 00:00:00

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

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

abstract：:Selective potentiators of glutamate response at metabotropic glutamate receptor subtype 5 (mGluR5) have exciting potential for the development of novel treatment strategies for schizophrenia. A total of 1,382 compounds with positive allosteric modulation (PAM) of the mGluR5 glutamate response were identified through h...

journal_title：ACS chemical neuroscience

authors： Mueller R,Rodriguez AL,Dawson ES,Butkiewicz M,Nguyen TT,Oleszkiewicz S,Bleckmann A,Weaver CD,Lindsley CW,Conn PJ,Meiler J

更新日期：2010-04-21 00:00:00

abstract：:Pyramidal cells and astrocytes have differential susceptibility to oxygen-glucose deprivation and reperfusion (OGD-RP). It is known that excessive reactive oxygen species (ROS) in mitochondria initiates cell death, while glutathione (GSH) is one of the major defenses against ROS. Although it is known that astrocytes c...

journal_title：ACS chemical neuroscience

authors： Yin B,Barrionuevo G,Weber SG

更新日期：2018-04-18 00:00:00

abstract：:On the basis of the drug-repositioning and redeveloping strategy, first-generation dual-target inhibitors of acetylcholinesterase (AChE) and phosphodiesterase 5 (PDE5) have been recently reported as a potentially novel therapeutic method for the treatment of Alzheimer's disease (AD), and the lead compound 2 has proven...

journal_title：ACS chemical neuroscience

authors： Ni W,Wang H,Li X,Zheng X,Wang M,Zhang J,Gong Q,Ling D,Mao F,Zhang H,Li J

更新日期：2018-07-18 00:00:00

abstract：:Bipolar disorder is a complex neuropsychiatric disorder, characterized by intermittent episodes of mania and depression. Recent studies have indicated argyrophilic grains, composed of hyperphosphorylated tau, are observable in postmortem brains of bipolar patients. It remains uncertain how tau hyperphosphorylation res...

journal_title：ACS chemical neuroscience

authors： Naserkhaki R,Zamanzadeh S,Baharvand H,Nabavi SM,Pakdaman H,Shahbazi S,Vosough M,Ghaedi G,Barzegar A,Mirtorabi D,Hedayatshodeh M,Ehsani E,Falahati M,Hajipour MJ,Shahpasand K

更新日期：2019-03-20 00:00:00

abstract：:Natural environments contain numerous volatile compounds emanating from a large number of sources, and the survival of many animals depends on their ability to segregate odors of interest within complex odorous scenes. In a recent paper, we described how the ability of mice to detect odors within mixtures depends on t...

journal_title：ACS chemical neuroscience

authors： Rokni D,Murthy VN

更新日期：2014-10-15 00:00:00