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Cholinesterase inhibitors

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https://www.readbyqxmd.com/read/28929747/the-structure-of-an-insecticide-sequestering-carboxylesterase-from-the-disease-vector-culex-quinquefasciatus-what-makes-an-enzyme-a-good-insecticide-sponge
#1
Davis Henry Hopkins, Nicholas J Fraser, Peter D Mabbitt, Paul D Carr, John G Oakeshott, Colin J Jackson
Carboxylesterase (CBE)-mediated metabolic resistance to organophosphate and carbamate insecticides is a major problem for the control of insect disease vectors, such as the mosquito. The most common mechanism involves overexpression of CBEs that bind to the insecticide with high affinity, thereby sequestering them before they can interact with their target. However, the absence of any structure for an insecticide-sequestering CBE limits our understanding of the molecular basis for this process. We present the first structure of a CBE involved in sequestration, Cqestβ21, from the mosquito disease vector, Culex quinquefasciatus...
September 20, 2017: Biochemistry
https://www.readbyqxmd.com/read/28925729/advances-toward-multifunctional-cholinesterase-and-%C3%AE-amyloid-aggregation-inhibitors
#2
Dawid Panek, Tomasz Wichur, Justyna Godyń, Anna Pasieka, Barbara Malawska
The emergence of a multitarget design approach in the development of new potential anti-Alzheimer's disease agents has resulted in the discovery of many multifunctional compounds focusing on various targets. Among them the largest group comprises inhibitors of both cholinesterases, with additional anti-β-amyloid aggregation activity. This review describes recent advances in this research area and presents the most interesting compounds reported over a 2-year span (2015-2016). The majority of hybrids possess heterodimeric structures obtained by linking structurally active fragments interacting with different targets...
September 19, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28922160/memantine-for-alzheimer-s-disease-an%C3%A2-updated-systematic-review-and%C3%A2-meta-analysis
#3
Taro Kishi, Shinji Matsunaga, Kazuto Oya, Ikuo Nomura, Toshikazu Ikuta, Nakao Iwata
BACKGROUND: The clinical benefit of memantine for Alzheimer's disease (AD) remains inconclusive. OBJECTIVE: We performed an updated systematic review and meta-analysis of the efficacy/safety of memantine in AD. METHODS: We included randomized trials of memantine for AD patients. Cognitive function scores (CF), behavioral disturbances scores (BD), and all-cause discontinuation were used as primary measures. Effect size based on a random-effects model was evaluated in the meta-analyses...
September 11, 2017: Journal of Alzheimer's Disease: JAD
https://www.readbyqxmd.com/read/28917965/the-development-of-a-butyrylcholinesterase-porous-pellet-for-innovative-detection-of-cholinesterase-inhibitors
#4
Jiří Zeman, David Vetchý, Aleš Franc, Sylvie Pavloková, Vladimír Pitschmann, Lukáš Matějovský
The aim of the presented research was the preparation of an innovative carrier with significantly improved properties for the fast and sensitive detection of cholinesterase inhibitors such as nerve agents. This innovative carrier was in the form of spherical pellets containing different amounts of Neusilin. Neusilin is a synthetic and amorphous form of magnesium aluminometasilicate with a high specific surface area, and the immobilized enzyme butyrylcholinesterase with an activity of 50nkat·g(-1). Pellets were prepared by the extrusion-spheronization method and dried in a hot air oven under two conditions - at 30°C for 72h and at 60°C for 24h...
September 13, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28901528/beyond-symptomatic-effects-donepezil-s-potential-for-neuroprotection-and-disease-modification-in-alzheimer-s-disease
#5
REVIEW
Seung Hyun Kim, Nagaendran Kandiah, Jung-Lung Hsu, Chuthamanee Suthisisang, Chesda Udommongkol, Amitabh Dash
Alzheimer's disease (AD) is associated with neurodegenerative changes resulting clinically in progressive cognitive and functional deficits. The only therapies are the cholinesterase inhibitors (ChEIs) donepezil, galantamine, and rivastigmine and the N-methyl-D-aspartate-receptor antagonist memantine. Donepezil acts primarily on the cholinergic system as symptomatic treatment, but it also has potential for disease modification and may reduce the rate of progression of AD. This review explores the potential for a disease modifying effect of donepezil...
September 13, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28880354/-pimavanserin-a-new-treatment-for-the-parkinson-s-disease-psychosis
#6
J H Duits, M S Ongering, H J M Martens, P F J Schulte
Clozapine is an effective drug for treating psychosis in Parkinson's disease (PDP) and is registered as such in the Netherlands. However, clozapine can have adverse effects, including agranulocytosis. The new drug pimavanserin was recently registered in the United States for the treatment of PDP.<br/> AIM: To review the literature on pimavanserin and discuss the position it currently occupies in the Netherlands as a potential treatment for PDP.<br/> METHOD: Systematic search of the literature.<br/> RESULTS: We found reports on four randomised controlled trials (RCTs), one review and six articles about the pharmacokinetics and pharmacodynamics of pimavanserin...
2017: Tijdschrift Voor Psychiatrie
https://www.readbyqxmd.com/read/28874829/plant-expressed-cocaine-hydrolase-variants-of-butyrylcholinesterase-exhibit-altered-allosteric-effects-of-cholinesterase-activity-and-increased-inhibitor-sensitivity
#7
Katherine E Larrimore, I Can Kazan, Latha Kannan, R Player Kendle, Tameem Jamal, Matthew Barcus, Ashini Bolia, Stephen Brimijoin, Chang-Guo Zhan, S Banu Ozkan, Tsafrir S Mor
Butyrylcholinesterase (BChE) is an enzyme with broad substrate and ligand specificities and may function as a generalized bioscavenger by binding and/or hydrolyzing various xenobiotic agents and toxicants, many of which target the central and peripheral nervous systems. Variants of BChE were rationally designed to increase the enzyme's ability to hydrolyze the psychoactive enantiomer of cocaine. These variants were cloned, and then expressed using the magnICON transient expression system in plants and their enzymatic properties were investigated...
September 5, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28868119/coumarin-derivatives-bearing-benzoheterocycle-moiety-synthesis-cholinesterase-inhibitory-and-docking-simulation-study
#8
Kimia Hirbod, Leili Jalili-Baleh, Hamid Nadri, Seyed Esmaeil Sadat Ebrahimi, Alireza Moradi, Bahar Pakseresht, Alireza Foroumadi, Abbas Shafiee, Mehdi Khoobi
OBJECTIVES: To investigate the efficiency of a novel series of coumarin derivatives bearing benzoheterocycle moiety as novel cholinesterase inhibitors. MATERIALS AND METHODS: Different 7-hydroxycoumarin derivatives were synthesized via Pechmann or Knoevenagel condensation and conjugated to different benzoheterocycle (8-hydroxyquinoline, 2-mercaptobenzoxazole or 2-mercaptobenzimidazole) using dibromoalkanes 3a-m: Final compounds were evaluated against acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) by Ellman's method...
June 2017: Iranian Journal of Basic Medical Sciences
https://www.readbyqxmd.com/read/28859660/early-versus-late-onset-alzheimer-s-disease-in-clinical-practice-cognitive-and-global-outcomes-over-3%C3%A2-years
#9
Carina Wattmo, Åsa K Wallin
BACKGROUND: Whether age at onset influences Alzheimer's disease (AD) progression and the effectiveness of cholinesterase inhibitor (ChEI) therapy is not clear. We aimed to compare longitudinal cognitive and global outcomes in ChEI-treated patients with early-onset Alzheimer's disease (EOAD) versus late-onset Alzheimer's disease (LOAD) in clinical practice. METHODS: This 3-year, prospective, observational, multicentre study included 1017 participants with mild to moderate AD; 143 had EOAD (age at onset < 65 years) and 874 had LOAD (age at onset ≥ 65 years)...
August 31, 2017: Alzheimer's Research & Therapy
https://www.readbyqxmd.com/read/28832937/systematic-review-of-sex-specific-reporting-of-data-cholinesterase-inhibitor-example
#10
Nishila Mehta, Craig Rodrigues, Manpreet Lamba, Wei Wu, Susan E Bronskill, Nathan Herrmann, Sudeep S Gill, An-Wen Chan, Robin Mason, Suzanne Day, Jerry H Gurwitz, Paula A Rochon
OBJECTIVES: To improve the value of research for older adults, we examine sex-specific reporting of data from drug trials for the management of dementia. These data are important because they may influence considerations ranging from the health of populations to shared decision-making by individual patient and caregiver about the risk and benefit of a drug therapy. METHODS: Randomized controlled trials of cholinesterase inhibitors (i.e., donepezil, rivastigmine, or galantamine) with clinical outcomes were identified from searches of MEDLINE, EMBASE, and the Cochrane Library...
August 18, 2017: Journal of the American Geriatrics Society
https://www.readbyqxmd.com/read/28820005/inhibition-of-endocannabinoid-metabolizing-enzymes-in-peripheral-tissues-following-developmental-chlorpyrifos-exposure-in-rats
#11
Robert W Buntyn, Navatha Alugubelly, Rachel L Hybart, Afzaal N Mohammed, Carole A Nail, Greta C Parker, Matthew K Ross, Russell L Carr
Repeated developmental exposure to the organophosphate (OP) insecticide chlorpyrifos (CPF) inhibits brain fatty acid amide hydrolase (FAAH) activity at low levels, whereas at higher levels, it inhibits brain monoacylglycerol lipase (MAGL) activity. FAAH and MAGL hydrolyze the endocannabinoids anandamide (AEA) and 2-arachidonylglycerol (2-AG), respectively. Peripherally, AEA and 2-AG have physiological roles in the regulation of lipid metabolism and immune function, and altering the normal levels of these lipid mediators can negatively affect these processes...
January 1, 2017: International Journal of Toxicology
https://www.readbyqxmd.com/read/28801274/mannich-base-approach-to-5-methoxyisatin-3-4-isopropylphenyl-hydrazone-a-water-soluble-prodrug-for-a-multitarget-inhibition-of-cholinesterases-beta-amyloid-fibrillization-and-oligomer-induced-cytotoxicity
#12
Leonardo Pisani, Annalisa De Palma, Nicola Giangregorio, Daniela V Miniero, Paolo Pesce, Orazio Nicolotti, Francesco Campagna, Cosimo D Altomare, Marco Catto
Targeting protein aggregation for the therapy of neurodegenerative diseases remains elusive for medicinal chemists, despite a number of small molecules known to interfere in amyloidogenesis, particularly of amyloid beta (Aβ) protein. Starting from previous findings in the antiaggregating activity of a class of indolin-2-ones inhibiting Aβ fibrillization, 5-methoxyisatin 3-(4-isopropylphenyl)hydrazone 1 was identified as a multitarget inhibitor of Aβ aggregation and cholinesterases with IC50s in the low μM range...
August 9, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28790827/the-effects-of-memantine-on-behavioral-disturbances-in-patients-with-alzheimer-s-disease-a-meta-analysis
#13
Taro Kishi, Shinji Matsunaga, Nakao Iwata
BACKGROUND: Memantine is effective in the treatment of behavioral disturbances in patients with Alzheimer's disease. It has not yet been fully determined which behavioral disturbances respond best to memantine. METHODS: We conducted a meta-analysis of memantine vs control (placebo or usual care) for the treatment of individual behavioral disturbances (delusion, hallucination, agitation/aggression, dysphoria, anxiety/phobia, euphoria, apathy, disinhibition, irritability/lability, aberrant motor activity/activity disturbances, nighttime disturbance/diurnal rhythm disturbances, and eating disturbances)...
2017: Neuropsychiatric Disease and Treatment
https://www.readbyqxmd.com/read/28782481/rational-approaches-design-strategies-structure-activity-relationship-and-mechanistic-insights-for-esterase-inhibitors
#14
Harbinder Singh, Jatinder Vir Singh, Navdeep Kaur, Mohit Sanduja, Gurpreet Singh, Preet Mohinder Singh Bedi, Sahil Sharma
BACKGROUND: Esterase is an enzyme that splits esters into an acid and alcohol. Varieties of esterases are present in human body to control diverse set of cellular processes and execute their specific functions. It can be seen that any increase in metabolites produced by these enzymes lead to severe pathological conditions like Alzheimer disease, hypercholesterolemia etc. OBJECTIVE: Numerous esterase inhibitors have been developed and reported by the researchers around the globe, but not systematically summarized yet...
August 7, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28770024/metformin-and-its-sulfenamide-prodrugs-inhibit-human-cholinesterase-activity
#15
Magdalena Markowicz-Piasecka, Joanna Sikora, Łukasz Mateusiak, Elżbieta Mikiciuk-Olasik, Kristiina M Huttunen
The results of epidemiological and pathophysiological studies suggest that type 2 diabetes mellitus (T2DM) may predispose to Alzheimer's disease (AD). The two conditions present similar glucose levels, insulin resistance, and biochemical etiologies such as inflammation and oxidative stress. The diabetic state also contributes to increased acetylcholinesterase (AChE) activity, which is one of the factors leading to neurodegeneration in AD. The aim of this study was to assess in vitro the effects of metformin, phenformin, and metformin sulfenamide prodrugs on the activity of human AChE and butyrylcholinesterase (BuChE) and establish the type of inhibition...
2017: Oxidative Medicine and Cellular Longevity
https://www.readbyqxmd.com/read/28760642/galantamine-administration-reduces-reactive-astrogliosis-and-upregulates-the-anti-oxidant-enzyme-catalase-in-rats-submitted-to-neonatal-hypoxia-ischemia
#16
F K Odorcyk, F Nicola, L E Duran-Carabali, F Figueiró, J Kolling, A Vizuete, E L Konrath, C A Gonçalves, A T S Wyse, C A Netto
Neonatal hypoxia ischemia (HI) plays a role in the etiology of several neurological pathologies and causes severe sequelae. Acetylcholine is a neurotransmitter in the central nervous system and cholinesterase inhibitors have demonstrated a positive action over HI induced deficits. In order to evaluate the effects of pre and post-hypoxia administrations of galantamine, a cholinesterase inhibitor, in a model of perinatal HI, Wistar rats in the post-natal day 7 (PND7) were subjected to a combination of unilateral occlusion of the right carotid artery with the exposure to a 1h hypoxia...
July 29, 2017: International Journal of Developmental Neuroscience
https://www.readbyqxmd.com/read/28756012/design-synthesis-and-pharmacological-evaluation-of-a-novel-series-of-hormone-sensitive-lipase-inhibitor
#17
Tomoko Ogiyama, Mitsuhiro Yamaguchi, Nobuya Kurikawa, Shoko Honzumi, Koji Terayama, Nobumi Nagaoka, Yuka Yamamoto, Takako Kimura, Daisuke Sugiyama, Shin-Ichi Inoue
HSL inhibition is a promising approach to the treatment of dyslipidemia. As a result of re-optimization of lead compound 2, we identified novel compound 25a exhibiting potent inhibitory activity against HSL enzyme and cell with high selectivity for cholinesterases (AChE and BuChE). Reflecting its potent in vitro activity, compound 25a exhibited antilipolytic effect in rats at 1mg/kg p.o., which indicated that this novel compound is the most potent orally active HSL inhibitor. Moreover, compound 25a did not show bioactivation liability...
July 17, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28752503/trends-in-drug-prescription-rates-for-dementia-an-observational-population-based-study-in-france-2006-2014
#18
Mathilde François, Jonathan Sicsic, Alexis Elbaz, Nathalie Pelletier Fleury
BACKGROUND: Since the 2011 French guidance updates, cholinesterase inhibitors and memantine are considered optional in the management of dementia and leave physicians free to prescribe based on their clinical expertise. OBJECTIVES: The aims of this study were to analyze the influence of these recent guidance updates on the prescription rates of these drugs and to quantify the impact of potential changes on healthcare expenditures. METHODS: Patients over 65 years old from a representative sample of a national administrative claims database, the French national health insurance database, were retrospectively included from 2006 to 2014...
July 27, 2017: Drugs & Aging
https://www.readbyqxmd.com/read/28751142/design-synthesis-and-biological-evaluation-of-dual-acetylcholinesterase-and-phosphodiesterase-5a-inhibitors-in-treatment-for-alzheimer-s-disease
#19
Li-Yun Zhou, Yao Zhu, Yu-Ren Jiang, Xiong-Jie Zhao, Dong Guo
With the recent research advances in molecular biology and technology, multiple credible hypotheses about the progress of Alzheimer's disease (AD) have been proposed; multi-target drugs have emerged as an innovative therapeutic approach for AD. Current clinical therapy for AD patients is mainly palliative treatment targeting acetylcholinesterase (AChE). Inhibition of phosphodiesterase 5A (PDE5A) has recently been validated as a potentially novel therapeutic approach for Alzheimer's disease (AD). In this work, series of new compounds were designed, synthesized and evaluated as dual cholinesterase and PDE5A inhibitor...
September 1, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28749013/physiological-versus-pharmacological-signalling-to-myosin-phosphorylation-in-airway-smooth-muscle
#20
Ning Gao, Ming-Ho Tsai, Audrey N Chang, Weiqi He, Cai-Ping Chen, Minsheng Zhu, Kristine E Kamm, James T Stull
Ca(2+) /calmodulin activation of myosin light chain kinase (MLCK) initiates myosin regulatory light chain (RLC) phosphorylation for smooth muscle contraction with subsequent dephosphorylation for relaxation by myosin light chain phosphatase (MLCP) containing regulatory (MYPT1) and catalytic (PP1cδ) subunits. RLC phosphorylation-dependent force development is regulated by distinct signalling modules involving protein phosphorylations. We investigated responses to cholinergic agonist treatment versus neurostimulation by electric field stimulation (EFS) in bovine tracheal smooth muscle...
July 27, 2017: Journal of Physiology
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