Kainic Acid-Based Agonists of Glutamate Receptors: SAR Analysis and Guidelines for Analog Design.

abstract：:Artesunate is a safe noncytotoxic drug with low side effects which is used in the treatment of chloroquine-resistant malaria. In addition to being an antimalarial drug, artesunate also has immunomodulatory, anticarcinogenic, and antiviral activity. There are in vivo and in vitro studies reporting that artesunate may h...

journal_title：ACS chemical neuroscience

authors： Uzun T,Toptaş O,Aydın Türkoğlu Ş

更新日期：2020-12-16 00:00:00

abstract：:Alzheimer's disease is characterized by pathological aggregation of protein tau and amyloid-β peptides, both of which are considered to be toxic to neurons. Naturally occurring dietary flavonoids have received considerable attention as alternative candidates for Alzheimer's therapy taking into account their antiamyloi...

journal_title：ACS chemical neuroscience

authors： Baptista FI,Henriques AG,Silva AM,Wiltfang J,da Cruz e Silva OA

更新日期：2014-02-19 00:00:00

abstract：:The l-enantiomer is the predominant type of amino acid in all living systems. However, d-amino acids, once thought to be "unnatural", have been found to be indigenous even in mammalian systems and increasingly appear to be functioning in essential biological and neurological roles. Both d- and l-amino acid levels in t...

journal_title：ACS chemical neuroscience

authors： Weatherly CA,Du S,Parpia C,Santos PT,Hartman AL,Armstrong DW

更新日期：2017-06-21 00:00:00

abstract：:Neuronal cytotoxicity observed in Alzheimer's disease (AD) is linked to the aggregation of β-amyloid peptide (Aβ) into toxic forms. Increasing evidence points to oligomeric materials as the neurotoxic species, not Aβ fibrils; disruption or inhibition of Aβ self-assembly into oligomeric or fibrillar forms remains a via...

journal_title：ACS chemical neuroscience

authors： Bett CK,Ngunjiri JN,Serem WK,Fontenot KR,Hammer RP,McCarley RL,Garno JC

更新日期：2010-09-15 00:00:00

abstract：:The present study was performed to investigate the possible role of protein kinase C (PKC) in morphine tolerance at spinal levels of rats. Intrathecal injection of 10 μg of morphine induced increases in the hindpaw withdrawal latency (HWL) to noxious thermal and mechanical stimulation in rats. After intrathecal inject...

journal_title：ACS chemical neuroscience

authors： Jin WY,Yu LC

更新日期：2010-02-17 00:00:00

abstract：:Quaternary ammonium analogues of atropine that are unable to cross the blood-brain barrier are used to alleviate peripheral muscarinic toxicity in animal models of epilepsy produced by systemic administration of pilocarpine or diisopropylfluorophosphate (DFP). Currently, methylatropine is the most popular and potent o...

journal_title：ACS chemical neuroscience

authors： Rojas A,Ganesh T,Walker A,Dingledine R

更新日期：2017-04-19 00:00:00

abstract：:Bromoalkaloids are secondary metabolites with a demonstrated high activity in several therapeutic areas. In this research, we probe the neuroprotective and antioxidant activities of hymenialdisine and hymenin. Both structures were tested in an oxidative stress cellular model, consisting of cortical neurons that are in...

journal_title：ACS chemical neuroscience

authors： Leirós M,Alonso E,Rateb ME,Houssen WE,Ebel R,Jaspars M,Alfonso A,Botana LM

更新日期：2015-02-18 00:00:00

abstract：:Reversion of protein or peptide aggregation is a formidable task, important in various domains of research at the interface of chemistry, medicine, and nanoscience. A novel class of dipeptides, termed as β-breaker dipeptides (BBDPs), is identified, which can be incorporated into the self-recognizing sequences to gener...

journal_title：ACS chemical neuroscience

authors： Nadimpally KC,Paul A,Mandal B

更新日期：2014-05-21 00:00:00

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

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

更新日期：2010-05-19 00:00:00

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

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

更新日期：2021-01-19 00:00:00

abstract：:Metal-ion misregulation and oxidative stress continue to be components of the continually evolving hypothesis describing the molecular origins of Alzheimer's disease. Therefore, these features are viable targets for synthetic chemists to explore through hybridizations of metal-binding ligands and antioxidant units. To...

journal_title：ACS chemical neuroscience

authors： Gonzalez P,Pota K,Turan LS,da Costa VCP,Akkaraju G,Green KN

更新日期：2017-11-15 00:00:00

abstract：:Intra- and extraneuronal deposition of amyloid β (Aβ) peptides have been linked to Alzheimer's disease (AD). While both intra- and extraneuronal Aβ deposits affect neuronal cell viability, the molecular mechanism by which these Aβ structures, especially when intraneuronal, do so is still not entirely understood. This ...

journal_title：ACS chemical neuroscience

authors： Banerjee V,Oren O,Dagan B,Taube R,Engel S,Papo N

更新日期：2019-03-20 00:00:00

abstract：:The abnormal aggregation of α-synuclein (α-Syn) is closely associated with Parkinson's disease. Different post-translational modifications of α-Syn have been identified and contribute distinctly in α-Syn aggregation and cytotoxicity. Recently, α-Syn was reported to be N-terminally acetylated in cells, yet the function...

journal_title：ACS chemical neuroscience

authors： Bu B,Tong X,Li D,Hu Y,He W,Zhao C,Hu R,Li X,Shao Y,Liu C,Zhao Q,Ji B,Diao J

更新日期：2017-10-18 00:00:00

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

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

更新日期：2015-09-16 00:00:00

abstract：:Large aggregates of misfolded α-synuclein inside neuronal cells are the hallmarks of Parkinson's disease. The protein's natural function and its supposed toxicity, however, are believed to be closely related to its interaction with cell and vesicle membranes. Upon this interaction, the protein folds into an α-helical ...

journal_title：ACS chemical neuroscience

authors： Hähl H,Möller I,Kiesel I,Campioni S,Riek R,Verdes D,Seeger S

更新日期：2015-03-18 00:00:00

abstract：:We previously reported on the synthesis of substituted phenyl-4-hydroxy-1-piperidyl indole analogues with nanomolar affinity at D2 dopamine receptors, ranging from 10- to 100-fold selective for D2 compared to the D3 dopamine receptor subtype. More recently, we evaluated a panel of aripiprazole analogues, identifying s...

journal_title：ACS chemical neuroscience

authors： Luedtke RR,Mishra Y,Wang Q,Griffin SA,Bell-Horner C,Taylor M,Vangveravong S,Dillon GH,Huang RQ,Reichert DE,Mach RH

更新日期：2012-12-19 00:00:00

abstract：:Brain-eating amoebae (Acanthamoeba spp., Balamuthia mandrillaris, and Naegleria fowleri) can cause opportunistic infections involving the central nervous system. It is troubling that the mortality rate is more than 90% despite advances in antimicrobial chemotherapy over the last few decades. Here, we describe urgent k...

journal_title：ACS chemical neuroscience

authors： Khan NA,Anwar A,Siddiqui R

更新日期：2017-11-15 00:00:00

abstract：:Alcohol abuse is a chronic disease characterized by the consumption of alcohol at a level that interferes with physical and mental health and causes serious and persistent changes in the brain. Lipid metabolism is of particular interest due to its high concentration in the brain. Lipids are the main component of cell ...

journal_title：ACS chemical neuroscience

authors： Roux A,Jackson SN,Muller L,Barbacci D,O'Rourke J,Thanos PK,Volkow ND,Balaban C,Schultz JA,Woods AS

更新日期：2016-08-17 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：: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：:No selective drugs exist, and we have been designing, synthesizing, and evaluating multitarget-directed ligands since the beginning of modern medicinal chemistry, without knowing it, most possibly. The challenge to discover the efficient Multi-Target Small Molecules (MTSMs) for Alzheimer's disease (AD) therapy implies...

journal_title：ACS chemical neuroscience

authors： Oset-Gasque MJ,Marco-Contelles J

更新日期：2018-03-21 00:00:00

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

authors： Elsayed Y,Khan NA

更新日期：2020-06-17 00:00:00

abstract：:Oligomers of amyloid-β (AβO) are deemed key in synaptotoxicity and amyloid seeding of Alzheimer's disease (AD). However, the heterogeneous and dynamic nature of AβO and inadequate markers for AβO subtypes have stymied effective AβO identification and therapeutic targeting in vivo. We identified an AβO-subclass epitope...

journal_title：ACS chemical neuroscience

authors： Silverman JM,Gibbs E,Peng X,Martens KM,Balducci C,Wang J,Yousefi M,Cowan CM,Lamour G,Louadi S,Ban Y,Robert J,Stukas S,Forloni G,Hsiung GR,Plotkin SS,Wellington CL,Cashman NR

更新日期：2018-07-18 00:00:00

abstract：:Amyloid fibrils are the most distinct components of the plaques associated with various neurodegenerative diseases. Kinetic studies of amyloid fibril formation shed light on the microscopic mechanisms that underlie this process as well as the contributions of internal and external factors to the interplay between diff...

journal_title：ACS chemical neuroscience

authors： Nasir I,Linse S,Cabaleiro-Lago C

更新日期：2015-08-19 00:00:00

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

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

abstract：:Amyloid-β (Aβ), the main constituent in senile plaques found in the brain of patients with Alzheimer's disease (AD), is considered as a causative factor in AD pathogenesis. The clinical examination of the brains of patients with AD has demonstrated that caspase-3 colocalizes with senile plaques. Cellular studies have ...

journal_title：ACS chemical neuroscience

authors： Chang YJ,Linh NH,Shih YH,Yu HM,Li MS,Chen YR

更新日期：2016-08-17 00:00:00

abstract：:We propose a tripartite mechanism to describe the processing of cognitive information (cog-info), comprising the (1) neuron, (2) surrounding neural extracellular matrix (nECM), and (3) numerous "trace" metals distributed therein. The neuron is encased in a polyanionic nECM lattice doped with metals (>10), wherein it p...

journal_title：ACS chemical neuroscience

authors： Marx G,Gilon C

更新日期：2013-06-19 00:00:00

abstract：:Relapse to cocaine dependence, even after extended abstinence, involves a number of liability factors including impulsivity (predisposition toward rapid, unplanned reactions to stimuli without regard to negative consequences) and cue reactivity (sensitivity to cues associated with cocaine-taking which can promote coca...

journal_title：ACS chemical neuroscience

authors： Cunningham KA,Anastasio NC,Fox RG,Stutz SJ,Bubar MJ,Swinford SE,Watson CS,Gilbertson SR,Rice KC,Rosenzweig-Lipson S,Moeller FG

更新日期：2013-01-16 00:00:00

abstract：:CBD-2115 was selected from a library of 148 compounds based on a pyridinyl-indole scaffold as a first-in-class 4R-tau radiotracer. In vitro binding assays showed [3H]CBD-2115 had a KD value of 6.9 nM and a nominal Bmax of 500 nM in 4R-tau expressing P301L transgenic mouse tissue. In binding assays with human brain tis...

journal_title：ACS chemical neuroscience

authors： Lindberg A,Knight AC,Sohn D,Rakos L,Tong J,Radelet A,Mason NS,Stehouwer JS,Lopresti BJ,Klunk WE,Sandell J,Sandberg A,Hammarström P,Svensson S,Mathis CA,Vasdev N

更新日期：2021-01-26 00:00:00

abstract：:As the intrinsic origin of the hypothesis for β-amyloid (Aβ) from Alzheimer's disease, histidine behaviors were found to play a crucial role in Aβ aggregation. To investigate the histidine behaviors during the early stage of aggregation, Aβ40/42 pentamers with different histidine isomer states were simulated at the at...

journal_title：ACS chemical neuroscience

authors： Xing X,Zhao W,Hu D,Kang B,Shi H,Lee JY,Ai H

更新日期：2019-05-15 00:00:00