Development of a new photochromic ion channel blocker via azologization of fomocaine.

abstract：:The melanocortin system regulates an array of diverse physiological functions including pigmentation, feeding behavior, energy homeostasis, cardiovascular regulation, sexual function, and steroidogenesis. Endogenous melanocortin agonist ligands all possess the minimal messaging tetrapeptide sequence His-Phe-Arg-Trp. B...

journal_title：ACS chemical neuroscience

authors： Todorovic A,Lensing CJ,Holder JR,Scott JW,Sorensen NB,Haskell-Luevano C

更新日期：2018-11-21 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：:The nicotinic acetylcholine receptor (nAChR) family, the archetype member of the pentameric ligand-gated ion channels, is ubiquitously distributed in the central and peripheral nervous systems, and its members are the targets for both genetic and acquired forms of neurological disorders. In the central nervous system,...

journal_title：ACS chemical neuroscience

authors： Paz ML,Barrantes FJ

更新日期：2019-05-15 00:00:00

abstract：:The melanocortin-3 (MC3R) and melanocortin-4 (MC4R) receptors are expressed in the brain and are implicated in the regulation of food intake and energy homeostasis. The endogenous agonist ligands for these receptors (α-, β-, γ-MSH and ACTH) are linear peptides with limited receptor subtype selectivity and metabolic st...

journal_title：ACS chemical neuroscience

authors： Singh A,Dirain ML,Wilczynski A,Chen C,Gosnell BA,Levine AS,Edison AS,Haskell-Luevano C

更新日期：2014-10-15 00:00:00

abstract：:Ionic zinc is found at a high concentration in some glutamatergic vesicles of the mammalian brain. Ionic zinc is also found chelated to macromolecules in the extracellular space, constituting what has been called the "zinc veneer". In this communication we show that the zinc ionophore, pyrithione, can be used to demon...

journal_title：ACS chemical neuroscience

authors： Nydegger I,Rumschik SM,Zhao J,Kay AR

更新日期：2012-10-17 00:00:00

abstract：:Cognitive dysfunctions, including impaired attention, learning, memory, and problem solving, occur in psychiatric diseases, such as depression, and are a hallmark of aging. Altered GABAergic signaling is similarly reported across these conditions, but therapeutic approaches are limited by pan-receptor activities of be...

journal_title：ACS chemical neuroscience

authors： Prevot TD,Li G,Cook JM,Sibille E

更新日期：2019-05-15 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：: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：:The effect of the bis-sulfonated iron(III) corrole (1-Fe), a potent decomposition catalyst of reactive oxygen species, on rescuing SN4741 cells that were damaged by 6-hydroxydopamine (6-OHDA) was investigated as an in vitro model system for studying cell death of dopaminergic neurons in the substantia nigra. Important...

journal_title：ACS chemical neuroscience

authors： Soll M,Bar Am O,Mahammed A,Saltsman I,Mandel S,Youdim MB,Gross Z

更新日期：2016-10-19 00:00:00

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

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

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

abstract：:The blood-brain barrier (BBB) is an important barrier that separates brain tissue from peripheral blood. The permeability of the BBB can be destroyed by external harmful factors, such as lipopolysaccharide (LPS), which contributes to neuroinflammation and central nervous system diseases. The present study aims to inve...

journal_title：ACS chemical neuroscience

authors： Du H,Wang S

更新日期：2020-12-16 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：: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：:Exploration of dendrimers for effective drug delivery is giving promising results. The present study was designed and performed to explore the dendrimeric (polyamidoamine-lactoferrin; PAMAM-Lf) formulations for the effective rivastigmine (RIV) delivery against the Alzheimer's induced animal model using lactoferrin as ...

journal_title：ACS chemical neuroscience

authors： Gothwal A,Singh H,Jain SK,Dutta A,Borah A,Gupta U

更新日期：2019-08-21 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：:Alzheimer's disease (AD) is the most common neurodegenerative disease, and its main hallmark is the deposition of amyloid beta (Aβ) peptides. However, several clinical trials focusing on Aβ-targeting agents have failed recently, and thus new therapeutic leads are focusing on alternate targets such as tau protein patho...

journal_title：ACS chemical neuroscience

authors： Cho HJ,Sharma AK,Zhang Y,Gross ML,Mirica LM

更新日期：2020-05-20 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：: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 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：: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：: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

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

abstract：:Recreational consumption of synthetic cannabinoid receptor agonists (SCRAs) is a growing crisis in public health in many parts of the world. AMB-FUBINACA is a member of this class of drugs and is responsible for a large proportion of SCRA-related toxicity both in New Zealand and internationally. Strikingly, little is ...

journal_title：ACS chemical neuroscience

authors： Finlay DB,Manning JJ,Ibsen MS,Macdonald CE,Patel M,Javitch JA,Banister SD,Glass M

更新日期：2019-10-16 00:00:00

abstract：:Single-cell mass spectrometry has become an established technique to study specific molecular properties such as the neuropeptide complement of identified neurons. Here, we describe a strategy to characterize, by MALDI-TOF mass spectrometry, neurochemical composition of neurons that were identified by their electrophy...

journal_title：ACS chemical neuroscience

authors： Neupert S,Fusca D,Kloppenburg P,Predel R

更新日期：2018-08-15 00:00:00

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

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

abstract：:Essential hypertension is a major risk factor for cardiovascular disease that can lead eventually to structural and functional alterations in the brain. Accumulating evidence has suggested that the increased activities in renin-angiotensin system and sympathetic nerve participated in the pathogenesis of hypertension t...

journal_title：ACS chemical neuroscience

authors： Li Y,Yu R,Zhang D,Yang W,Hou Q,Li Y,Jiang H

更新日期：2020-06-03 00:00:00

abstract：:Serotonin (5-HT) is a key player in many physiological processes in both the adult organism and developing embryo. One of the mechanisms for 5-HT-mediated effects is covalent binding of 5-HT to the target proteins catalyzed by transglutaminases (serotonylation). Despite the implication in a variety of physiological pr...

journal_title：ACS chemical neuroscience

authors： Ivashkin E,Melnikova V,Kurtova A,Brun NR,Obukhova A,Khabarova MY,Yakusheff A,Adameyko I,Gribble KE,Voronezhskaya EE

更新日期：2019-08-21 00:00:00

abstract：:Zinc binding to β-amyloid structure could promote amyloid-β aggregation, as well as reactive oxygen species (ROS) production, as suggested in many experimental and theoretical studies. Therefore, the introduction of multifunctional drugs capable of chelating zinc metal ion and inhibiting Aβ aggregation is a promising ...

journal_title：ACS chemical neuroscience

authors： Asadbegi M,Shamloo A

更新日期：2019-11-20 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：: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