An Engineered Variant of the B1 Domain of Protein G Suppresses the Aggregation and Toxicity of Intra- and Extracellular Aβ42.

abstract：:The aggregation of amyloid-β (Aβ) peptide induced by Cu(2+) is a key factor in development of Alzheimer's disease (AD), and metal ion chelation therapy enables treatment of AD. Three CQi (i = 1, 2, and 3 with R = H, Cl, and NO2, respectively) drugs had been verified experimentally to be much stronger inhibitors than t...

journal_title：ACS chemical neuroscience

authors： Dong M,Li H,Hu D,Zhao W,Zhu X,Ai H

更新日期：2016-05-18 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：:Azobenzenes are the most widely studied photoswitches, and have become popular optical probes for biological systems. The cis configuration is normally metastable, meaning the trans configuration is always thermodynamically favored. The unique exception to this rule is an azobenzene having a two-carbon bridge between ...

journal_title：ACS chemical neuroscience

authors： Thapaliya ER,Zhao J,Ellis-Davies GCR

更新日期：2019-05-15 00:00:00

abstract：:High levels of histamine H3 receptors (H3Rs) are found in the globus pallidus (GP), a neuronal nucleus in the basal ganglia involved in the control of motor behavior. By using rat GP isolated nerve terminals (synaptosomes), we studied whether H3R activation modified the previously reported enhancing action of adenosin...

journal_title：ACS chemical neuroscience

authors： Morales-Figueroa GE,Márquez-Gómez R,González-Pantoja R,Escamilla-Sánchez J,Arias-Montaño JA

更新日期：2014-08-20 00:00:00

abstract：:This work describes the use of fluorescence correlation spectroscopy (FCS) and a novel amyloid-binding fluorescent probe, ARCAM 1, to monitor the aggregation of the Alzheimer's disease-associated amyloid β-peptide (Aβ). ARCAM 1 exhibits a large increase in fluorescence emission upon binding to Aβ assemblies, making it...

journal_title：ACS chemical neuroscience

authors： Guan Y,Cao KJ,Cantlon A,Elbel K,Theodorakis EA,Walsh DM,Yang J,Shah JV

更新日期：2015-09-16 00:00:00

abstract：:The molecular mechanism of protein aggregation is of both fundamental and clinical importance as amyloid aggregates are linked to a number of neurodegenerative disorders. Such protein aggregates include macroscopic insoluble fibrils as well as small soluble oligomeric species. Time-dependent resolution of these specie...

journal_title：ACS chemical neuroscience

authors： Kjaergaard M,Dear AJ,Kundel F,Qamar S,Meisl G,Knowles TPJ,Klenerman D

更新日期：2018-12-19 00:00:00

abstract：:Baicalein, a flavonoid derived from the roots of Scutellariae baicalensis Georgi, has shown health benefits for an array of human diseases including dementia. The senescence-accelerated mouse prone 8 (SAMP8) strain is extensively used as a senile dementia model. To further investigate the effects of baicalein in SAMP8...

journal_title：ACS chemical neuroscience

authors： Gao L,Li J,Zhou Y,Huang X,Qin X,Du G

更新日期：2018-07-18 00:00:00

abstract：:Amyloid formation and neuroinflammation are major features of Alzheimer's disease pathology. Proinflammatory mediator S100A9 was shown to act as a link between the amyloid and neuroinflammatory cascades in Alzheimer's disease, leading together with Aβ to plaque formation, neuronal loss and memory impairment. In order ...

journal_title：ACS chemical neuroscience

authors： Iashchishyn IA,Gruden MA,Moskalenko RA,Davydova TV,Wang C,Sewell RDE,Morozova-Roche LA

更新日期：2018-06-20 00:00:00

abstract：:The nitrocatechol derivatives tolcapone (1) and entacapone (2), used as adjunctive therapy in the treatment of Parkinson's disease, were investigated for their potential to inhibit the tau-derived-hexapeptide 306VQIVYK311. They were compared to small molecules that contain similar pharmacophores including the catechol...

journal_title：ACS chemical neuroscience

authors： Mohamed T,Hoang T,Jelokhani-Niaraki M,Rao PP

更新日期：2013-12-18 00:00:00

abstract：:Sevoflurane, one of the most commonly used anesthetic agents, has been demonstrated to induce widespread neurodegeneration in the developing brain. We aimed to evaluate the protective effects of a PDE-7 inhibitor (BRL-50481) against the neurotoxic effects of sevoflurane on the developing nervous system. Spatial learni...

journal_title：ACS chemical neuroscience

authors： Chen Y,Li S,Zhong X,Kang Z,Chen R

更新日期：2020-05-06 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：: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：:Deltorphins are naturally occurring peptides produced by the skin of the giant monkey frog (Phyllomedusa bicolor). They are δ-opioid receptor-selective agonists. Herein, we report the design and synthesis of a peptide, Tyr-d-Ala-(pI)Phe-Glu-Ile-Ile-Gly-NH2 3 (GATE3-8), based on the [d-Ala(2)]deltorphin II template, wh...

journal_title：ACS chemical neuroscience

authors： Pescatore R,Marrone GF,Sedberry S,Vinton D,Finkelstein N,Katlowitz YE,Pasternak GW,Wilson KR,Majumdar S

更新日期：2015-06-17 00:00:00

abstract：:Neurotensin (NT) exerts its analgesic effects through activation of the G protein-coupled receptors NTS1 and NTS2. This opioid-independent antinociception represents a potential alternative for pain management. While activation of NTS1 also induces a drop in blood pressure and body temperature, NTS2 appears to be an a...

journal_title：ACS chemical neuroscience

authors： Eiselt E,Gonzalez S,Martin C,Chartier M,Betti C,Longpré JM,Cavelier F,Tourwé D,Gendron L,Ballet S,Sarret P

更新日期：2019-11-20 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：:The 5-HT2C receptor has emerged as a promising target in the treatment of a variety of central nervous system disorders. We have first identified aporphines as a new class of 5-HT2C receptor agonists. Structure-activity relationship results indicate that the aporphine core may be required for 5-HT2C receptor activity,...

journal_title：ACS chemical neuroscience

authors： Mao Q,Zhang B,Li W,Tian S,Shui W,Ye N

更新日期：2020-02-19 00:00:00

abstract：:Responsive or smart contrast agents (SCAs) represent a promising direction for development of novel functional MRI (fMRI) methods for the eventual noninvasive assessment of brain function. In particular, SCAs that respond to Ca(2+) may allow tracking neuronal activity independent of brain vasculature, thus avoiding th...

journal_title：ACS chemical neuroscience

authors： Angelovski G,Gottschalk S,Milošević M,Engelmann J,Hagberg GE,Kadjane P,Andjus P,Logothetis NK

更新日期：2014-05-21 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：:Aminorex (5-phenyl-4,5-dihydro-1,3-oxazol-2-amine) and 4-methylaminorex (4-methyl-5-phenyl-4,5-dihydro-1,3-oxazol-2-amine) are psychostimulants that have long been listed in Schedules IV and I of the UN Convention on Psychotropic Substances of 1971. However, a range of psychoactive analogues exist that are not interna...

journal_title：ACS chemical neuroscience

authors： Maier J,Mayer FP,Brandt SD,Sitte HH

更新日期：2018-10-17 00:00:00

abstract：:The delivery of specific genes into neurons offers a potent approach for treatment of diseases as well as for the study of neuronal cell biology. Here we investigated the capabilities of cationic amino acid based lipid assemblies to act as nonviral gene delivery vectors in primary cultured neurons. An arginine-based l...

journal_title：ACS chemical neuroscience

authors： Aoshima Y,Hokama R,Sou K,Sarker SR,Iida K,Nakamura H,Inoue T,Takeoka S

更新日期：2013-12-18 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：:The fibrillogenesis of amyloid-β protein (Aβ) is considered a crucial factor in the pathogenesis of Alzheimer's disease (AD). Hence, inhibiting Aβ fibrillogenesis is regarded as the primary therapeutic strategy for the prevention and treatment of AD. However, the development of effective inhibitors against Aβ fibrillo...

journal_title：ACS chemical neuroscience

authors： Liu F,Wang W,Sang J,Jia L,Lu F

更新日期：2019-01-16 00:00:00

abstract：:Autoantibodies to Parkinson's disease (PD) amyloidogenic protein, α-synuclein, were recognized as a prospective biomarker for early disease diagnostics, yet there is inconsistency in previous reports, potentially related to PD status. Therefore, plasma and cerebrospinal fluid (CSF) of the cross-sectional cohort of 60 ...

journal_title：ACS chemical neuroscience

authors： Horvath I,Iashchishyn IA,Forsgren L,Morozova-Roche LA

更新日期：2017-06-21 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：: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：: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：: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：:No universally efficacious therapy exists for chronic pain, a disease affecting one-fifth of the global population. An overreliance on the prescription of opioids for chronic pain despite their poor ability to improve function has led to a national opioid crisis. In 2018, the NIH launched a Helping to End Addiction Lo...

journal_title：ACS chemical neuroscience

authors： Shan Z,Cai S,Yu J,Zhang Z,Vallecillo TGM,Serafini MJ,Thomas AM,Pham NYN,Bellampalli SS,Moutal A,Zhou Y,Xu GB,Xu YM,Luo S,Patek M,Streicher JM,Gunatilaka AAL,Khanna R

更新日期：2019-06-19 00:00:00

abstract：:The dorsal raphe nucleus contains one of the largest groups of serotonergic neurons in the mammalian brain and is the main site of origin of the serotonergic projection to the cerebral cortex. Early electrophysiological studies suggested that serotonergic neurons in this cell group formed a homogeneous cell class. Mor...

journal_title：ACS chemical neuroscience

authors： Andrade R,Haj-Dahmane S

更新日期：2013-01-16 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