Reversal of aggregation using β-breaker dipeptide containing peptides: Application to Aβ(1-40) self-assembly and its inhibition.

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：:Alzheimer's disease (AD) is the most common form of dementia affecting 35 million individuals worldwide. Current AD treatments provide only brief symptomatic relief. It is therefore urgent to replace this symptomatic approach with a curative one. Increasing serotonin signaling as well as developing molecules that enha...

journal_title：ACS chemical neuroscience

authors： Claeysen S,Bockaert J,Giannoni P

更新日期：2015-07-15 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：: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

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

abstract：:The finding that acetylcholinesterase (AChE) colocalizes with β-amyloid (Aβ) and promotes and accelerates Aβ aggregation has renewed an intense interest in developing new multifunctional AChE inhibitors as potential disease-modifying drugs for Alzheimer's therapy. To this end, we have developed a new class of selectiv...

journal_title：ACS chemical neuroscience

authors： Zheng H,Youdim MB,Fridkin M

更新日期：2010-11-17 00:00:00

abstract：:Metabolic adaptation to stress is a crucial yet poorly understood phenomenon, particularly in the central nervous system (CNS). The ability to identify essential metabolic events which predict neuronal fate in response to injury is critical to developing predictive markers of outcome, for interpreting CNS spectroscopi...

journal_title：ACS chemical neuroscience

authors： McKenzie JR,Palubinsky AM,Brown JE,McLaughlin B,Cliffel DE

更新日期：2012-07-18 00:00:00

abstract：:Glucose-6-phosphate dehydrogenase (G6PD) protects the embryo from endogenous and xenobiotic-enhanced oxidative DNA damage and embryopathies. Here we show in aged mice that G6PD similarly protects against endogenous reactive oxygen species (ROS)-mediated neurodegeneration. In G6PD-normal (G6PD(+/+)) and heterozygous (G...

journal_title：ACS chemical neuroscience

authors： Jeng W,Loniewska MM,Wells PG

更新日期：2013-07-17 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：:The understanding of the interaction between the membrane of neurons and amyloid-β peptides is of crucial importance to shed light on the mechanism of toxicity in Alzheimer's disease. This paper describes how supercritical angle fluorescence spectroscopy was applied to monitor in real-time the interaction between a su...

journal_title：ACS chemical neuroscience

authors： Dubois V,Serrano D,Seeger S

更新日期：2019-12-18 00:00:00

abstract：:NLRP3-PYD inflammasome activates an inflammatory pathway in response to a wide variety of cell damage or infections. Dysregulated NLRP3 inflammatory signaling has many chronic inflammatory and autoimmune disorders. NLRP3 and ASC have a PYD, a superfamily member of the Death Domain, which plays a key role in inflammato...

journal_title：ACS chemical neuroscience

authors： Riaz M,Rehman AU,Shah SA,Rafiq H,Lu S,Qiu Y,Wadood A

更新日期：2021-01-27 00:00:00

abstract：:Depression, a major cause of disability worldwide, is characterized by a complex and heterogeneous symptomatology. With this respect, cognitive deterioration represents a major problem that has a strong impact on a patient's function. Thus, within the context of a depressive phenotype, it is important to characterize ...

journal_title：ACS chemical neuroscience

authors： Calabrese F,Brivio P,Gruca P,Lason-Tyburkiewicz M,Papp M,Riva MA

更新日期：2017-04-19 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：:A new generation of ligands designed to interact with the α-helix/β-strand discordant region of the amyloid-β peptide (Aβ) and to counteract its oligomerization is presented. These ligands are designed to interact with and stabilize the Aβ central helix (residues 13-26) in an α-helical conformation with increased inte...

journal_title：ACS chemical neuroscience

authors： Honcharenko D,Juneja A,Roshan F,Maity J,Galán-Acosta L,Biverstål H,Hjorth E,Johansson J,Fisahn A,Nilsson L,Strömberg R

更新日期：2019-03-20 00:00:00

abstract：:While selective-serotonin reuptake inhibitor (SSRI) antidepressants are commonly prescribed in the treatment of depression, their use during pregnancy leads to fetal drug exposures. According to recent reports, such exposures could affect fetal development and long-term offspring health. A central question is how preg...

journal_title：ACS chemical neuroscience

authors： Velasquez JC,Goeden N,Herod SM,Bonnin A

更新日期：2016-03-16 00:00:00

abstract：:The propagation of pathological proteins throughout the brain is the primary physiological hallmark of the progression of Alzheimer's Disease (AD). A growing body of evidence indicates that hyperphosphorylated Tau proteins are spread transcellularly between neurons in a prionlike fashion, inducing misfolding and aggre...

journal_title：ACS chemical neuroscience

authors： Bell BJ,Malvankar MM,Tallon C,Slusher BS

更新日期：2020-11-04 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：: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

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

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：:Glioblastoma (GBM) is characterized by a poor response to conventional chemotherapeutic agents, attributed to the insurgence of drug resistance mechanisms and to the presence of a subpopulation of glioma stem cells (GSCs). GBM cells and GSCs present, among others, an overexpression of antiapoptotic proteins and an inh...

journal_title：ACS chemical neuroscience

authors： Daniele S,Pietrobono D,Costa B,Giustiniano M,La Pietra V,Giacomelli C,La Regina G,Silvestri R,Taliani S,Trincavelli ML,Da Settimo F,Novellino E,Martini C,Marinelli L

更新日期：2018-01-17 00:00:00

abstract：:The light emission chemistry of firefly luciferase can be harnessed to reveal otherwise invisible biological processes occurring in the brains of live animals. Though powerful, the need for the luciferase substrate D-luciferin to traverse the blood-brain barrier poses limitations on the sensitivity and interpretation ...

journal_title：ACS chemical neuroscience

authors： Mofford DM,Miller SC

更新日期：2015-08-19 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：:Using microdialysis in C57Bl6 mice, we monitored cholinergic activity in the hypothalamus. Food intake after an overnight fast caused a 3-fold increase of extracellular acetylcholine (ACh) concentrations in the hypothalamus. The effect lasted for about 30 min. Food containing no calories (kaolin pellets), or food that...

journal_title：ACS chemical neuroscience

authors： Thinnes A,Klein J

更新日期：2019-04-17 00:00:00

abstract：:Neuroinflammatory processes promote a constellation of neurochemical and hormonal changes resulting in profound effects on motivational states (anhedonia), mood (depression and anxiety disorders), and cognitive function (decrements in learning and memory). The enhancement of immunoregulatory processes, such as increas...

journal_title：ACS chemical neuroscience

authors： Frank MG,Fonken LK,Watkins LR,Maier SF,Lowry CA

更新日期：2019-01-16 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：:The aggregation of α-synuclein (α-Syn) has been implicated strongly in Parkinson's disease (PD). The intrinsically disordered nature of α-Syn makes this protein prone to self-association or heteroassociation with another protein or lipid. While conformational fluctuation and free radical chemistry have been shown to p...

journal_title：ACS chemical neuroscience

authors： Ghosh S,Mahapatra A,Chattopadhyay K

更新日期：2019-03-20 00:00:00

abstract：:3-Iodobenzoyl naltrexamine (IBNtxA) is a potent analgesic belonging to the pharmacologically diverse 6β-amidoepoxymorphinan group of opioids. We present the synthesis and pharmacological evaluation of five analogs of IBNtxA. The scaffold of IBNtxA was modified by removing the 14-hydroxy group, incorporating a 7,8 doub...

journal_title：ACS chemical neuroscience

authors： Váradi A,Marrone GF,Eans SO,Ganno ML,Subrath JJ,Le Rouzic V,Hunkele A,Pasternak GW,McLaughlin JP,Majumdar S

更新日期：2015-11-18 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

abstract：:Botulinum neurotoxin (BoNT), the etiological agent that causes the neuroparalytic disease botulism, has become a highly studied drug target in light of the potential abuse of this toxin as a weapon of bioterrorism. In particular, small molecule inhibitors of the light chain metalloprotease of BoNT serotype A have rece...

journal_title：ACS chemical neuroscience

authors： Capek P,Zhang Y,Barlow DJ,Houseknecht KL,Smith GR,Dickerson TJ

更新日期：2011-06-15 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：: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