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

abstract：:Protein function depends on both protein structure and amino acid (aa) sequence. Here we show that modular features of both structure and function can be quantified economically from the aa sequences alone for the small (40,42 aa) plaque-forming (aggregative) amyloid beta fragments. Some edge and center features of th...

journal_title：ACS chemical neuroscience

authors： Phillips JC

更新日期：2015-05-20 00:00:00

abstract：:Gangliosides are biologically important glycolipids widely distributed in vertebrate cells. An important member of the ganglioside family is the monosialylganglioside GM1, which has been suggested as a potential therapeutic for Parkinson's disease. In the current study, a late-stage radiofluorination protocol was deve...

journal_title：ACS chemical neuroscience

authors： Revunov E,Johnström P,Arakawa R,Malmquist J,Jucaite A,Defay T,Takano A,Schou M

更新日期：2020-05-06 00:00:00

abstract：:Amyloid-beta (Aβ) peptide misfolds into fibrillary aggregates (β-sheet) and is deposited as amyloid plaques in the cellular environment, which severely damages intraneuronal connections leading to Alzheimer's disease (AD) pathogenesis. Furthermore, neurons are rich in tubulin/microtubules, and the intracellular networ...

journal_title：ACS chemical neuroscience

authors： Mondal P,Das G,Khan J,Pradhan K,Mallesh R,Saha A,Jana B,Ghosh S

更新日期：2019-05-15 00:00:00

abstract：:Alzheimer's disease (AD) is a complex neurodegenerative disorder characterized by multiple hallmarks including extracellular amyloid (Aβ) plaques, neurofibrillary tangles, dysfunctional blood-brain barrier (BBB), neuroinflammation, and impaired autophagy. Thus, novel strategies that target multiple disease pathways wo...

journal_title：ACS chemical neuroscience

authors： Al Rihani SB,Darakjian LI,Kaddoumi A

更新日期：2019-08-21 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：: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

authors： Lee C,Robinson M,Willerth SM

更新日期：2018-12-19 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：: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：:The metabotropic glutamate receptor 2 (mGlu2) is a transmembrane-spanning class C G protein-coupled receptor that is an attractive therapeutic target for multiple psychiatric and neurological disorders. A key challenge has been deciphering the contribution of mGlu2 relative to other closely related mGlu receptors in m...

journal_title：ACS chemical neuroscience

authors： Hellyer SD,Aggarwal S,Chen ANY,Leach K,Lapinsky DJ,Gregory KJ

更新日期：2020-06-03 00:00:00

abstract：:The gut is the largest producer of serotonin or 5-hydroxytryptamine (5-HT) in the human body, and 5-HT has been recognized as an important signaling molecule in the gut for decades. There are two distinct sources of enteric 5-HT. Mucosal 5-HT is predominantly produced by enterochromaffin (EC) cells of the gastrointest...

journal_title：ACS chemical neuroscience

authors： Shajib MS,Baranov A,Khan WI

更新日期：2017-05-17 00:00:00

abstract：:Central norepinephrine (NE) and dopamine (DA) are involved in a variety of physiological functions and behaviors. Accumulating evidence suggests that NE neurons originating from the locus coeruleus (LC) innervate DA neurons of the ventral tegmental area (VTA) and influence VTA-DA neural activity. However, the underlyi...

journal_title：ACS chemical neuroscience

authors： Park JW,Bhimani RV,Park J

更新日期：2017-09-20 00:00:00

abstract：:This Review describes recent activity in the advancement of ligands for the metabotropic glutamate 4 receptor subtype and their potential utility as central nervous system (CNS) therapeutics. Until recently, there was a paucity of compounds with suitable selectivity and druglike properties to elucidate the value of th...

journal_title：ACS chemical neuroscience

authors： Robichaud AJ,Engers DW,Lindsley CW,Hopkins CR

更新日期：2011-08-17 00:00:00

abstract：:Previous work has established that D-serine (D-Ser) plays important roles in certain neurological processes. Study on its uptake/storage and release by neuronal cells is highly significant for elucidating relevant mechanisms. In this work, PC-12 cells were incubated with racemic Ser (100 μM each enantiomer). After inc...

journal_title：ACS chemical neuroscience

authors： Li X,McCullum C,Zhao S,Hu H,Liu YM

更新日期：2015-04-15 00:00:00

abstract：:Vesicular acetylcholine transporter (VAChT) is a member of the major facilitator superfamily (MFS). It contains conserved sequence motifs originally defined in the bacterial multidrug resistance transporter family of the MFS. Motif C (GSLV(227) A(228)PPFGGIL) is located at the C-terminal end of transmembrane helix 5 (...

journal_title：ACS chemical neuroscience

authors： Luo J,Parsons SM

更新日期：2010-05-19 00:00:00

abstract：:We review here recent discoveries in the exciting new field of neuromicrobiology. This field encompasses the interactions between the microbiome and the central nervous system. The microbiome has a tremendous impact on human health. In particular, the gut microbiota may play a key role in many essential processes in h...

journal_title：ACS chemical neuroscience

authors： de la Fuente-Nunez C,Meneguetti BT,Franco OL,Lu TK

更新日期：2018-02-21 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：:Interactions between superoxide dismutase-1 (SOD1) and lipid membranes might be directly involved in the toxicity and intercellular propagation of aggregated SOD1 in amyotrophic lateral sclerosis (ALS), but the chemical details of lipid-SOD1 interactions and their effects on SOD1 aggregation remain unclear. This paper...

journal_title：ACS chemical neuroscience

authors： Rasouli S,Abdolvahabi A,Croom CM,Plewman DL,Shi Y,Shaw BF

更新日期：2018-07-18 00:00:00

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

authors： Yao Y,Tang Y,Wei G

更新日期：2020-12-16 00:00:00

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

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

更新日期：2019-07-17 00:00:00

abstract：:Extensive experimental and computational studies have suggested that multiple Zn(2+) binding modes in amyloid β (Aβ) peptides could exist simultaneously. However, consistent results have not been obtained for the effects of Zn(2+) binding on Aβ structure, dynamics, and kinetics in particular. Some key questions such a...

journal_title：ACS chemical neuroscience

authors： Xu L,Wang X,Wang X

更新日期：2013-11-20 00:00:00

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

authors： White TL,Gonsalves MA

更新日期：2020-09-02 00:00:00

abstract：:We propose a tripartite biochemical mechanism for memory. Three physiologic components are involved, namely, the neuron (individual and circuit), the surrounding neural extracellular matrix, and the various trace metals distributed within the matrix. The binding of a metal cation affects a corresponding nanostructure ...

journal_title：ACS chemical neuroscience

authors： Marx G,Gilon C

更新日期：2012-08-15 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：: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：:Mutations in the SOD1 gene are associated with some forms of familial amyotrophic lateral sclerosis (fALS). There are more than 150 different mutations in the SOD1 gene that have various effects on the copper-zinc superoxide dismutase (SOD1) enzyme structure, including the loss of metal binding and a decrease in dimer...

journal_title：ACS chemical neuroscience

authors： Farrawell NE,Yerbury MR,Plotkin SS,McAlary L,Yerbury JJ

更新日期：2019-03-20 00:00:00

abstract：:Amyloid β (Abeta) peptides in their oligomeric form have been proposed as major toxic species in Alzheimer's disease (AD). There are a limited number of anti-Abeta antibodies specific to oligomeric forms of Abeta compared to the monomeric form, and accurate measurement of oligomeric forms in biological samples, cerebr...

journal_title：ACS chemical neuroscience

authors： Matveeva EG,Rudolph A,Moll JR,Thompson RB

更新日期：2012-11-21 00:00:00

abstract：:Savella (milnacipran), a selective serotonin and noradrenaline reuptake inhibitor, was approved by the FDA on January 14th, 2009, for the treatment of fibromyalgia. ...

journal_title：ACS chemical neuroscience

authors： Hopkins CR

更新日期：2010-05-19 00:00:00

abstract：:The Chinese mitten crab (Eriocheir sinensis) is a commercially important crab in China and is usually managed at high stocking densities. Agonistic behavior directly impacts crab integrity, survival, and growth and results in economic losses. In the present study, we evaluated the modulatory effects of serotonin (5-HT...

journal_title：ACS chemical neuroscience

authors： Pang YY,Song YM,Zhang L,Song XZ,Zhang C,Lv JH,He L,Cheng YX,Yang XZ

更新日期：2019-11-20 00:00:00

abstract：:Imidazo[2,1-b]benzothiazoles (IBTs) are a promising novel class of amyloid positron emission tomography (PET) radiopharmaceuticals for diagnosis of neurodegenerative disorders like Alzheimer's disease (AD). Their good in vivo imaging properties have previously been shown in preclinical studies. Among IBTs, fluorinated...

journal_title：ACS chemical neuroscience

authors： Yousefi BH,Manook A,Grimmer T,Arzberger T,von Reutern B,Henriksen G,Drzezga A,Förster S,Schwaiger M,Wester HJ

更新日期：2015-03-18 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