An enzyme that catalyzes the hydrolysis of ACETYLCHOLINE to CHOLINE and acetate. In the CNS, this enzyme plays a role in the function of peripheral neuromuscular junctions. EC 3.1.1.7.
Drugs that inhibit cholinesterases. The neurotransmitter ACETYLCHOLINE is rapidly hydrolyzed, and thereby inactivated, by cholinesterases. When cholinesterases are inhibited, the action of endogenously released acetylcholine at cholinergic synapses is potentiated. Cholinesterase inhibitors are widely used clinically for their potentiation of cholinergic inputs to the gastrointestinal tract and urinary bladder, the eye, and skeletal muscles; they are also used for their effects on the heart and the central nervous system.
An aspect of cholinesterase (EC 3.1.1.8).
An agent used as a substrate in assays for cholinesterases, especially to discriminate among enzyme types.
Drugs used to reverse the inactivation of cholinesterase caused by organophosphates or sulfonates. They are an important component of therapy in agricultural, industrial, and military poisonings by organophosphates and sulfonates.
A genus of fish, in the family GYMNOTIFORMES, capable of producing an electric shock that immobilizes fish and other prey. The species Electrophorus electricus is also known as the electric eel, though it is not a true eel.
A cholinesterase inhibitor that crosses the blood-brain barrier. Tacrine has been used to counter the effects of muscle relaxants, as a respiratory stimulant, and in the treatment of Alzheimer's disease and other central nervous system disorders.
An organophosphate cholinesterase inhibitor that is used as a pesticide.
A cholinesterase inhibitor that is rapidly absorbed through membranes. It can be applied topically to the conjunctiva. It also can cross the blood-brain barrier and is used when central nervous system effects are desired, as in the treatment of severe anticholinergic toxicity.
A genus of the Torpedinidae family consisting of several species. Members of this family have powerful electric organs and are commonly called electric rays.
A benzazepine derived from norbelladine. It is found in GALANTHUS and other AMARYLLIDACEAE. It is a cholinesterase inhibitor that has been used to reverse the muscular effects of GALLAMINE TRIETHIODIDE and TUBOCURARINE and has been studied as a treatment for ALZHEIMER DISEASE and other central nervous system disorders.
Various salts of a quaternary ammonium oxime that reconstitute inactivated acetylcholinesterase, especially at the neuromuscular junction, and may cause neuromuscular blockade. They are used as antidotes to organophosphorus poisoning as chlorides, iodides, methanesulfonates (mesylates), or other salts.
An organophosphorus ester compound that produces potent and irreversible inhibition of cholinesterase. It is toxic to the nervous system and is a chemical warfare agent.
A di-isopropyl-fluorophosphate which is an irreversible cholinesterase inhibitor used to investigate the NERVOUS SYSTEM.
A mercaptocholine used as a reagent for the determination of CHOLINESTERASES. It also serves as a highly selective nerve stain.
Aryl CYCLOPENTANES that are a reduced (protonated) form of INDENES.
An aspect of cholinesterases.
A rapid-onset, short-acting cholinesterase inhibitor used in cardiac arrhythmias and in the diagnosis of myasthenia gravis. It has also been used as an antidote to curare principles.
In about 250 species of electric fishes, modified muscle fibers forming disklike multinucleate plates arranged in stacks like batteries in series and embedded in a gelatinous matrix. A large torpedo ray may have half a million plates. Muscles in different parts of the body may be modified, i.e., the trunk and tail in the electric eel, the hyobranchial apparatus in the electric ray, and extrinsic eye muscles in the stargazers. Powerful electric organs emit pulses in brief bursts several times a second. They serve to stun prey and ward off predators. A large torpedo ray can produce of shock of more than 200 volts, capable of stunning a human. (Storer et al., General Zoology, 6th ed, p672)
Compounds containing carbon-phosphorus bonds in which the phosphorus component is also bonded to one or more sulfur atoms. Many of these compounds function as CHOLINERGIC AGENTS and as INSECTICIDES.
An organothiophosphate cholinesterase inhibitor that is used as an insecticide and as an acaricide.
Pesticides designed to control insects that are harmful to man. The insects may be directly harmful, as those acting as disease vectors, or indirectly harmful, as destroyers of crops, food products, or textile fabrics.
A cholinesterase inhibitor with a slightly longer duration of action than NEOSTIGMINE. It is used in the treatment of myasthenia gravis and to reverse the actions of muscle relaxants.
An organophosphorus compound that inhibits cholinesterase. It causes seizures and has been used as a chemical warfare agent.
A genus of poisonous snakes of the subfamily Elapinae of the family ELAPIDAE. They comprise the kraits. Twelve species are recognized and all inhabit southeast Asia. They are considered extremely dangerous. (Moore: Poisonous Snakes of the World, 1980, p120)
A cholinesterase inhibitor used in the treatment of myasthenia gravis and to reverse the effects of muscle relaxants such as gallamine and tubocurarine. Neostigmine, unlike PHYSOSTIGMINE, does not cross the blood-brain barrier.
Derivatives of carbamic acid, H2NC(=O)OH. Included under this heading are N-substituted and O-substituted carbamic acids. In general carbamate esters are referred to as urethanes, and polymers that include repeating units of carbamate are referred to as POLYURETHANES. Note however that polyurethanes are derived from the polymerization of ISOCYANATES and the singular term URETHANE refers to the ethyl ester of carbamic acid.
An organophosphorus insecticide that inhibits ACETYLCHOLINESTERASE.
Phenyl esters of carbamic acid or of N-substituted carbamic acids. Structures are similar to PHENYLUREA COMPOUNDS with a carbamate in place of the urea.
Carbon-containing phosphoric acid derivatives. Included under this heading are compounds that have CARBON atoms bound to one or more OXYGEN atoms of the P(=O)(O)3 structure. Note that several specific classes of endogenous phosphorus-containing compounds such as NUCLEOTIDES; PHOSPHOLIPIDS; and PHOSPHOPROTEINS are listed elsewhere.
A potent, long-acting cholinesterase inhibitor used as a miotic in the treatment of glaucoma.
N,N',N'',N'''-Tetraisopropylpyrophosphamide. A specific inhibitor of pseudocholinesterases. It is commonly used experimentally to determine whether pseudo- or acetylcholinesterases are involved in an enzymatic process.
Venoms from snakes of the family Elapidae, including cobras, kraits, mambas, coral, tiger, and Australian snakes. The venoms contain polypeptide toxins of various kinds, cytolytic, hemolytic, and neurotoxic factors, but fewer enzymes than viper or crotalid venoms. Many of the toxins have been characterized.
Compounds that contain the radical R2C=N.OH derived from condensation of ALDEHYDES or KETONES with HYDROXYLAMINE. Members of this group are CHOLINESTERASE REACTIVATORS.
Common name for an order (Anguilliformes) of voracious, elongate, snakelike teleost fishes.
Poisoning due to exposure to ORGANOPHOSPHORUS COMPOUNDS, such as ORGANOPHOSPHATES; ORGANOTHIOPHOSPHATES; and ORGANOTHIOPHOSPHONATES.
A wide spectrum aliphatic organophosphate insecticide widely used for both domestic and commercial agricultural purposes.
Organic compounds that contain phosphorus as an integral part of the molecule. Included under this heading is broad array of synthetic compounds that are used as PESTICIDES and DRUGS.
Chemicals that are used to cause the disturbance, disease, or death of humans during WARFARE.
Cholinesterase reactivator occurring in two interchangeable isomeric forms, syn and anti.
The synapse between a neuron and a muscle.
A sulfur-containing analog of butyrylcholine which is hydrolyzed by butyrylcholinesterase to butyrate and thiocholine. It is used as a reagent in the determination of butyrylcholinesterase activity.
An enzyme that catalyzes the formation of acetylcholine from acetyl-CoA and choline. EC 2.3.1.6.
A neurotransmitter found at neuromuscular junctions, autonomic ganglia, parasympathetic effector junctions, a subset of sympathetic effector junctions, and at many sites in the central nervous system.
An organochlorophosphate cholinesterase inhibitor that is used as an insecticide for the control of flies and roaches. It is also used in anthelmintic compositions for animals. (From Merck, 11th ed)
Cholinesterase reactivator used as an antidote in alkyl phosphate poisoning.
A carbamate insecticide.
Study of intracellular distribution of chemicals, reaction sites, enzymes, etc., by means of staining reactions, radioactive isotope uptake, selective metal distribution in electron microscopy, or other methods.
The development by insects of resistance to insecticides.
Carbon-containing thiophosphoric acid derivatives. Included under this heading are compounds that have carbon bound to either SULFUR atom, or the OXYGEN atom of the SPO3 core structure.
The rate dynamics in chemical or physical systems.
A highly toxic cholinesterase inhibitor that is used as an acaricide and as an insecticide.
The specialized postsynaptic region of a muscle cell. The motor endplate is immediately across the synaptic cleft from the presynaptic axon terminal. Among its anatomical specializations are junctional folds which harbor a high density of cholinergic receptors.
Carbamate derivative used as an insecticide, acaricide, and nematocide.
Agents counteracting or neutralizing the action of POISONS.
The part of CENTRAL NERVOUS SYSTEM that is contained within the skull (CRANIUM). Arising from the NEURAL TUBE, the embryonic brain is comprised of three major parts including PROSENCEPHALON (the forebrain); MESENCEPHALON (the midbrain); and RHOMBENCEPHALON (the hindbrain). The developed brain consists of CEREBRUM; CEREBELLUM; and other structures in the BRAIN STEM.
A family of hexahydropyridines.
Cell surface proteins that bind acetylcholine with high affinity and trigger intracellular changes influencing the behavior of cells. Cholinergic receptors are divided into two major classes, muscarinic and nicotinic, based originally on their affinity for nicotine and muscarine. Each group is further subdivided based on pharmacology, location, mode of action, and/or molecular biology.
Nerve fibers liberating acetylcholine at the synapse after an impulse.
Chemicals used to destroy pests of any sort. The concept includes fungicides (FUNGICIDES, INDUSTRIAL); INSECTICIDES; RODENTICIDES; etc.
Contractile tissue that produces movement in animals.
A cholinesterase inhibitor that is used as an organothiophosphorus insecticide.
The parts of a macromolecule that directly participate in its specific combination with another molecule.
Red blood cells. Mature erythrocytes are non-nucleated, biconcave disks containing HEMOGLOBIN whose function is to transport OXYGEN.
Drugs used to specifically facilitate learning or memory, particularly to prevent the cognitive deficits associated with dementias. These drugs act by a variety of mechanisms. While no potent nootropic drugs have yet been accepted for general use, several are being actively investigated.
An organothiophosphorus cholinesterase inhibitor that is used as a systemic and contact insecticide.
Compounds that contain the decamethylenebis(trimethyl)ammonium radical. These compounds frequently act as neuromuscular depolarizing agents.
A degenerative disease of the BRAIN characterized by the insidious onset of DEMENTIA. Impairment of MEMORY, judgment, attention span, and problem solving skills are followed by severe APRAXIAS and a global loss of cognitive abilities. The condition primarily occurs after age 60, and is marked pathologically by severe cortical atrophy and the triad of SENILE PLAQUES; NEUROFIBRILLARY TANGLES; and NEUROPIL THREADS. (From Adams et al., Principles of Neurology, 6th ed, pp1049-57)
Quaternary ammonium analog of ethidium; an intercalating dye with a specific affinity to certain forms of DNA and, used as diiodide, to separate them in density gradients; also forms fluorescent complexes with cholinesterase which it inhibits.

Why are there so few resistance-associated mutations in insecticide target genes? (1/2082)

The genes encoding the three major targets of conventional insecticides are: Rdl, which encodes a gamma-aminobutyric acid receptor subunit (RDL); para, which encodes a voltage-gated sodium channel (PARA); and Ace, which encodes insect acetylcholinesterase (AChE). Interestingly, despite the complexity of the encoded receptors or enzymes, very few amino acid residues are replaced in different resistant insects: one within RDL, two within PARA and three or more within AChE. Here we examine the possible reasons underlying this extreme conservation by looking at the aspects of receptor and/or enzyme function that may constrain replacements to such a limited number of residues.  (+info)

Calcitonin gene-related peptide decreases expression of acetylcholinesterase in mammalian myotubes. (2/2082)

Nerve-derived trophic factors are known to modulate expression of acetylcholinesterase (AChE) in skeletal muscle fibers, yet the precise identity of these factors remains elusive. In the present study, we treated mouse C2 myotubes with calcitonin gene-related peptide (CGRP). Compared to non-treated myotubes, cell-associated AChE activity levels were decreased by approximately 60% after 48 h of treatment. A parallel reduction in AChE total protein levels was also observed as determined by Western blot analysis. The reduction in AChE activity was due to a decrease in the levels of the G1 molecular form and to an elimination of G1. By contrast, levels of secreted AChE remained unchanged following CGRP treatment. Finally, the overall decrease in AChE activity was accompanied by a reduction in AChE transcripts which could not be attributed to changes in the transcriptional rate of the ACHE gene.  (+info)

Monoclonal antibody 3F3 against conformational epitope of Torpedo acetylcholinesterase. (3/2082)

AIM: To study the type of epitope of native Torpedo acetylcholinesterase (AChE) directed by its monoclonal antibody (McAb) 3F3. METHODS: Enzyme-linked immunosorbent assay (ELISA) was used for the assay of the reaction between antigen and antibody. RESULTS: McAb 3F3 immunoreacted well with the native AChE, but not with the reduced- and alkylated-AChE (RA-AChE) at all. Soman did not interfere the binding of 3F3 with AChE molecule. The synthesized 24-peptide containing the active serine residue of the AChE active center did not react with McAb 3F3. CONCLUSION: 3F3 is a monoclonal antibody against the conformational epitope of Torpedo AChE active center, but dose not occupy the active serine residue of the enzyme.  (+info)

Establishment and characterization of human neuroblastoma cell lines. (4/2082)

Three new tissue culture cell lines, CHP-100, CHP-126, and CHP-134, have been established from explant cultures of human neuroblastoma. The cell lines have been characterized with respect to morphology, chromosomes constitution, growth, neural enzyme content, and their ability to grow in nude mice. The cells grow as dense masses comprised of fibroblast-or neuroblast-like cells with small processes. The cell lines differ in their neural enzyme acitivity. The chromosomal content of the 3 cell lines is near diploid, and all are capable of forming tumors in nude mice. The morphological findings indicate that the cells in culture resemble those found in the tumor, and the enzyme activities are consistent with those of nervous tissue. This the morphological, biochemical, and tumorigenic properties confirm that the 3 cell lines are neoplastic cells of neural origin.  (+info)

Electron paramagnetic resonance reveals altered topography of the active center gorge of acetylcholinesterase after binding of fasciculin to the peripheral site. (5/2082)

Fasciculin, a peptidic toxin from snake venom, inhibits mammalian and fish acetylcholinesterases (AChE) by binding to the peripheral site of the enzyme. This site is located at the rim of a narrow, deep gorge which leads to the active center triad, located at its base. The proposed mechanisms for AChE inhibition by fasciculin include allosteric events resulting in altered conformation of the AChE active center gorge. However, a fasciculin-induced altered topography of the active center gorge has not been directly demonstrated. Using electron paramagnetic resonance with the spin-labeled organophosphate 1-oxyl-2,2,6, 6-tetramethyl-4-piperidinylethylphosphorofluoridate (EtOSL) specifically bound to the catalytic serine of mouse AChE (mAChE), we show that bound fasciculin on mAChE slows down, but does not prevent phosphorylation of the active site serine by EtOSL and protects the gorge conformation against thermal denaturation. Most importantly, a restricted freedom of motion of the spin label bound to the fasciculin-associated mAChE, compared to mAChE, is evidenced. Molecular models of mAChE and fasciculin-associated mAChE with tethered EtOSL enantiomers indicate that this restricted motion is due to greater proximity of the S-EtOSL nitroxide radical to the W86 residue in the fasciculin-associated enzyme. Our results demonstrate a topographical alteration indicative of a restricted conformation of the active center gorge of mAChE with bound fasciculin at its rim.  (+info)

Organophosphorylation of acetylcholinesterase in the presence of peripheral site ligands. Distinct effects of propidium and fasciculin. (6/2082)

Structural analysis of acetylcholinesterase (AChE) has revealed two sites of ligand interaction in the active site gorge: an acylation site at the base of the gorge and a peripheral site at its mouth. A goal of our studies is to understand how ligand binding to the peripheral site alters the reactivity of substrates and organophosphates at the acylation site. Kinetic rate constants were determined for the phosphorylation of AChE by two fluorogenic organophosphates, 7-[(diethoxyphosphoryl)oxy]-1-methylquinolinium iodide (DEPQ) and 7-[(methylethoxyphosphonyl)oxy]-4-methylcoumarin (EMPC), by monitoring release of the fluorescent leaving group. Rate constants obtained with human erythrocyte AChE were in good agreement with those obtained for recombinant human AChE produced from a high level Drosophila S2 cell expression system. First-order rate constants kOP were 1,600 +/- 300 min-1 for DEPQ and 150 +/- 11 min-1 for EMPC, and second-order rate constants kOP/KOP were 193 +/- 13 microM-1 min-1 for DEPQ and 0.7-1.0 +/- 0.1 microM-1 min-1 for EMPC. Binding of the small ligand propidium to the AChE peripheral site decreased kOP/KOP by factors of 2-20 for these organophosphates. Such modest inhibitory effects are consistent with our recently proposed steric blockade model (Szegletes, T., Mallender, W. D., and Rosenberry, T. L. (1998) Biochemistry 37, 4206-4216). Moreover, the binding of propidium resulted in a clear increase in kOP for EMPC, suggesting that molecular or electronic strain caused by the proximity of propidium to EMPC in the ternary complex may promote phosphorylation. In contrast, the binding of the polypeptide neurotoxin fasciculin to the peripheral site of AChE dramatically decreased phosphorylation rate constants. Values of kOP/KOP were decreased by factors of 10(3) to 10(5), and kOP was decreased by factors of 300-4,000. Such pronounced inhibition suggested a conformational change in the acylation site induced by fasciculin binding. As a note of caution to other investigators, measurements of phosphorylation of the fasciculin-AChE complex by AChE inactivation gave misleading rate constants because a small fraction of the AChE was resistant to inhibition by fasciculin.  (+info)

Genetic analysis of collagen Q: roles in acetylcholinesterase and butyrylcholinesterase assembly and in synaptic structure and function. (7/2082)

Acetylcholinesterase (AChE) occurs in both asymmetric forms, covalently associated with a collagenous subunit called Q (ColQ), and globular forms that may be either soluble or membrane associated. At the skeletal neuromuscular junction, asymmetric AChE is anchored to the basal lamina of the synaptic cleft, where it hydrolyzes acetylcholine to terminate synaptic transmission. AChE has also been hypothesized to play developmental roles in the nervous system, and ColQ is also expressed in some AChE-poor tissues. To seek roles of ColQ and AChE at synapses and elsewhere, we generated ColQ-deficient mutant mice. ColQ-/- mice completely lacked asymmetric AChE in skeletal and cardiac muscles and brain; they also lacked asymmetric forms of the AChE homologue, butyrylcholinesterase. Thus, products of the ColQ gene are required for assembly of all detectable asymmetric AChE and butyrylcholinesterase. Surprisingly, globular AChE tetramers were also absent from neonatal ColQ-/- muscles, suggesting a role for the ColQ gene in assembly or stabilization of AChE forms that do not themselves contain a collagenous subunit. Histochemical, immunohistochemical, toxicological, and electrophysiological assays all indicated absence of AChE at ColQ-/- neuromuscular junctions. Nonetheless, neuromuscular function was initially robust, demonstrating that AChE and ColQ do not play obligatory roles in early phases of synaptogenesis. Moreover, because acute inhibition of synaptic AChE is fatal to normal animals, there must be compensatory mechanisms in the mutant that allow the synapse to function in the chronic absence of AChE. One structural mechanism appears to be a partial ensheathment of nerve terminals by Schwann cells. Compensation was incomplete, however, as animals lacking ColQ and synaptic AChE failed to thrive and most died before they reached maturity.  (+info)

Cloning, expression, and properties of a nonneuronal secreted acetylcholinesterase from the parasitic nematode Nippostrongylus brasiliensis. (8/2082)

We have isolated a full-length cDNA encoding an acetylcholinesterase secreted by the nematode parasite Nippostrongylus brasiliensis. The predicted protein is truncated in comparison with acetylcholinesterases from other organisms such that the carboxyl terminus aligns closely to the end of the catalytic domain of the vertebrate enzymes. The residues in the catalytic triad are conserved, as are the six cysteines which form the three intramolecular disulfide bonds. Three of the fourteen aromatic residues which line the active site gorge in the Torpedo enzyme are substituted by nonaromatic residues, corresponding to Tyr-70 (Thr), Trp-279 (Asn), and Phe-288 (Met). High level expression was obtained via secretion from Pichia pastoris. The purified enzyme behaved as a monomeric hydrophilic species. Although of invertebrate origin and possessing the above substitutions in the active site gorge residues, the enzyme efficiently hydrolyzed acetylthiocholine and showed minimal activity against butyrylthiocholine. It displayed excess substrate inhibition with acetylthiocholine at concentrations over 2. 5 mM and was highly sensitive to both active site and "peripheral" site inhibitors. Northern blot analysis indicated a progressive increase in mRNA for AChE B in parasites isolated from 6 days postinfection.  (+info)

TY - JOUR. T1 - Correlation of Red Blood Cell Acetylcholinesterase Enzyme Activity with Various RBC Indices. AU - Gupta, Shalvika. AU - Belle, Vijetha Shenoy. AU - Kumbarakeri Rajashekhar, Ramya. AU - Jogi, Sushma. AU - Prabhu, RV Krishnananda. PY - 2018/9/4. Y1 - 2018/9/4. N2 - Cholinesterases belongs to class hydrolases. There are two types acetylcholinesterase and butyryl cholinesterase. Acetylcholinesterase present in nerve endings and also in the RBC membrane. It helps to maintain the shape and size of RBCs. Any change in shape and size of RBCs may affect the activity of Acetylcholinesterase. Thus this study aimed to estimate RBCs Acetylcholinesterase enzyme activity in various types of anemias and correlate the RBCs Acetylcholinesterase enzyme activity with various hematological indices such as Erythrocyte Sedimentation Rate (ESR), Mean Corpuscular Hemoglobin (MCH), Mean Corpuscular Hemoglobin Concentration (MCHC), Mean Corpuscular Volume (MCV), Red cell Distribution Width (RDW) etc. After ...
Cholinesterases belongs to class hydrolases.There are two types acetylcholinesterase and butyryl cholinesterase. Acetylcholinesterase present in nerve endings and also in the RBC membrane. It helps to maintain the shape and size of RBCs. Any change in shape and size of RBCs may affect the activity of Acetylcholinesterase. Thus this study aimed to estimate RBCs Acetylcholinesterase enzyme activity in various types of anemias and correlate the RBCs Acetylcholinesterase enzyme activity with various hematological indices such as Erythrocyte Sedimentation Rate (ESR), Mean Corpuscular Hemoglobin (MCH),Mean Corpuscular Hemoglobin Concentration (MCHC), Mean Corpuscular Volume (MCV), Red cell Distribution Width (RDW) etc. After obtaining ethical approval from Institutional ethics committee total of 100 samples were collected from Clinical Biochemistry laboratory, Kasturba Medical College, Manipal, Manipal University. 25 were having normal RBC indices, 12 with hemolytic anemia, 26 with microcytic anemia ...
This gene encodes the subunit of a collagen-like molecule associated with acetylcholinesterase in skeletal muscle. Each molecule is composed of three identical subunits. Each subunit contains a proline-rich attachment domain (PRAD) that binds an acetylcholinesterase tetramer to anchor the catalytic subunit of the enzyme to the basal lamina. Mutations in this gene are associated with endplate acetylcholinesterase deficiency. Multiple transcript variants encoding different isoforms have been found for this gene. [provided by RefSeq, Jul 2008 ...
Free Online Library: AhR-mediated effects of dioxin on neuronal acetylcholinesterase expression in vitro.(Research, Report) by Environmental Health Perspectives; Health, general Environmental issues Acetylcholinesterase Chlorocarbons Analysis Dibenzofurans Dichloropropane Dioxin Health aspects Dioxins Enzymes Neurons
TY - JOUR. T1 - Stabilization of collagen-tailed acetylcholinesterase in muscle cells through extracellular anchorage by transglutaminase-catalyzed cross-linking. AU - Hand, D. AU - Dias, D. AU - Haynes, LW. PY - 2000. Y1 - 2000. M3 - Article (Academic Journal). VL - 204. SP - 65. EP - 76. JO - Molecular and Cellular Biochemistry. JF - Molecular and Cellular Biochemistry. SN - 0300-8177. ER - ...
Organophosphate and carbamate insecticides irreversibly inhibit acetylcholinesterase causing death of insects. Resistance-modified acetylcholinesterases(AChEs) have been described in many insect species and sequencing of their genes allowed several point mutations to be described. However, their relative frequency and their cartography had not yet been addressed. To analyze the most frequent mutations providing insecticide resistance in Drosophila melanogaster acetylcholinesterase, the Ace gene was cloned and sequenced in several strains harvested from different parts of the world. Sequence comparison revealed four widespread mutations, I161V, G265A, F330Y and G368A. We confirm here that mutations are found either isolated or in combination in the same protein and we show that most natural populations are heterogeneous, composed of a mixture of different alleles. In vitro expression of mutated proteins showed that combining mutations in the same protein has two consequences: it increases resistance
Define acetylcholinesterase. acetylcholinesterase synonyms, acetylcholinesterase pronunciation, acetylcholinesterase translation, English dictionary definition of acetylcholinesterase. n. An enzyme in the blood and in certain tissues that catalyzes the hydrolysis of acetylcholine. n an enzyme in nerve cells that is responsible for the...
Objective:To investigate the effect of YiShenJiangZhuo decoction on intracerebral AchE activity of ischemia reperfusion rat.Methods:After preparing a model of ischemia-reperfusion based on hypotension,we observed the praxiology of rat by using water labyrinth test and AchE activity of hippocampus by colorimetric method.Results:The model rat had distinct disturbances of learning and remembrance the Ache activity increased.The result of learning and remembrance in YiShenJiangZhuo decoction group improved significantly (P0.01)compared with the model rat;And AchE activity in YiShenJiangZhuo decoction group significaitly decreased(P0.05).Conclusion:It is suggested that the YiShenJiangZhuo decoction can improve the learning and remembrance by decreasing the AchE activity of ischemia reperfusion
TY - JOUR. T1 - Reaction pathway and free-energy barrier for reactivation of dimethylphosphoryl-inhibited human acetylcholinesterase. AU - Liu, Junjun. AU - Zhang, Yingkai. AU - Zhan, Chang Guo. PY - 2009/12/17. Y1 - 2009/12/17. N2 - The dephosphorylation/reactivation mechanism and the corresponding free-energy profile of the dimethylphosphoryl-inhibited conjugate of human acetylcholinesterase (AChE) has been studied by performing firstprinciples quantum mechanical/molecular mechanical free-energy (QM/MM-FE) calculations. On the basis of the QM/MM-FE results, for the favorable reaction pathway, the entire dephosphorylation/reactivation process consists of three reaction steps, including the nucleophilic water attack on the P atom, the spatial reorganization of the dimethylphosphoryl group, and the dissociation between the dimethylphosphoryl group and Ser203 of AChE. The overall free-energy barrier for the entire dephosphorylation/reactivation reaction is found to be the free-energy change from ...
In non-neuronal contexts, ACh (acetylcholine) is thought to be involved in the regulation of vital cell functions, such as proliferation, differentiation, apoptosis and cell-cell interaction. In airways, most cells express the non-neuronal cholinergic system, each containing a specific set of components required for synthesis, signal transduction and ACh hydrolysis. The aim of the present study was determine the expression of cholinergic system components in bronchial aspirates from control subjects and patients with lung cancer. We conducted an analysis of cholinergic components in the stored soluble and cellular fraction of bronchial aspirates from non-cancerous patients and patients diagnosed with lung cancer. The results show that the fluid secreted by human lung cells contains enough AChE (acetylcholinesterase) activity to control ACh levels. Thus these findings demonstrate that: (i) AChE activity is significantly lower in aspirates from squamous cell carcinomas; (ii) the molecular ...
A rabbit antiserum against commercially available Electrophorus electricus acetylcholinesterase has been prepared. Five precipitation bands were distinguished by immunoelectrophoresis, but only three of these contained demonstrable enzyme activity. In an in vitro system, activity of the commercial enzyme or of highly purified acetylcholinesterase was inhibited by 70-82 per cent after incubation with antiserum. Antibody specificity was demonstrated by the absence of serological cross reactions or enzyme inhibition with bovine erythrocyte acetylcholinesterase or horse serum cholinesterase. ...
Irreversible inhibition of the essential nervous system enzyme acetylcholinesterase by organophosphate nerve agents and pesticides may quickly lead to death. Oxime reactivators currently used as antidotes are generally less effective against pesticide exposure than nerve agent exposure, and pesticide exposure constitutes the majority of cases of organophosphate poisoning in the world. The current lack of published structural data specific to human acetylcholinesterase organophosphate-inhibited and oxime-bound states hinders development of effective medical treatments. We have solved structures of human acetylcholinesterase in different states in complex with the organophosphate insecticide, paraoxon, and oximes. Reaction with paraoxon results in a highly perturbed acyl loop that causes a narrowing of the gorge in the peripheral site that may impede entry of reactivators. This appears characteristic of acetylcholinesterase inhibition by organophosphate insecticides but not nerve agents. ...
Molecular isoform distribution and glycosylation of acetylcholinesterase are altered in brain and cerebrospinal fluid of patients with Alzheimers disease
An acetylcholinesterase has been purified from Torpedo californica by mild proteolysis of electroplax membranes with trypsin (5 µg/ml for 5 min) to solubilize the enzyme, followed by affinity chromatography of the soluble enzyme. The procedure yields an apparently homogeneous enzyme whose molecular weight (approximately 335,000), frictional coefficient (1.65), and amino acid composition all distinguished the Torpedo acetylcholinesterase from that which has been prepared by lytic procedures from Electrophorus. The enzyme is composed of four similar, if not identical, subunits, each of which possesses a catalytic and inhibitor binding site. Torpedo acetylcholinesterase contains 7.9% carbohydrate present as hexoses, hexosamines, and sialic acid, and at least some of these residues are exposed on the outer surface of the molecule. Concanavalin A, a plant lectin with specificity toward mannose residues at nonreducing positions, forms a sedimentable complex with the purified acetylcholinesterase ...
The X-ray crystal structures were solved for complexes with Torpedo californica acetylcholinesterase of two bivalent tacrine derivative compounds in which the two tacrine rings were separated by 5- and 7-carbon spacers. The derivative with the 7-carbon spacer spans the length of the active-site gorge, making sandwich interactions with aromatic residues both in the catalytic anionic site (Trp84 and Phe330) at the bottom of the gorge and at the peripheral anionic site near its mouth (Tyr70 and Trp279). The derivative with the 5-carbon spacer interacts in a similar manner at the bottom of the gorge, but the shorter tether precludes a sandwich interaction at the peripheral anionic site. Although the upper tacrine group does interact with Trp279, it displaces the phenyl residue of Phe331, thus causing a major rearrangement in the Trp279-Ser291 loop. The ability of this inhibitor to induce large-scale structural changes in the active-site gorge of acetylcholinesterase has significant implications for ...
TY - JOUR. T1 - COOH-terminal collagen Q (COLQ) mutants causing human deficiency of endplate acetylcholinesterase impair the interaction of ColQ with proteins of the basal lamina. AU - Arredondo, Juan. AU - Lara, Marian. AU - Ng, Fiona. AU - Gochez, Danielle A.. AU - Lee, Diana C.. AU - Logia, Stephanie P.. AU - Nguyen, Joanna. AU - Maselli, Ricardo A. PY - 2014. Y1 - 2014. N2 - Collagen Q (ColQ) is a key multidomain functional protein of the neuromuscular junction (NMJ), crucial for anchoring acetylcholinesterase (AChE) to the basal lamina (BL) and accumulating AChE at the NMJ. The attachment of AChE to the BL is primarily accomplished by the binding of the ColQ collagen domain to the heparan sulfate proteoglycan perlecan and the COOH-terminus to the muscle-specific receptor tyrosine kinase (MuSK), which in turn plays a fundamental role in the development and maintenance of the NMJ. Yet, the precise mechanism by which ColQ anchors AChE at the NMJ remains unknown. We identified five novel ...
A cholinesterase inhibitor (or anticholinesterase) suppresses the action of the enzyme. Because of its essential function, chemicals that interfere with the action of cholinesterase are potent neurotoxins, causing excessive salivation and eye-watering in low doses, followed by muscle spasms and ultimately death (examples are some snake venoms, and the nerve gases sarin and VX). One counteracting medication is pralidoxime. The so-called nerve gases and many substances used in insecticides have been shown to act by combining with a residue of serine in the active site of acetylcholine esterase, inhibiting the enzyme completely. The enzyme acetylcholine esterase breaks down the neurotransmitter acetylcholine, which is released at nerve and muscle junctions, in order to allow the muscle or organ to relax. The result of acetylcholine esterase inhibition is that acetylcholine builds up and continues to act so that any nerve impulses are continually transmitted and muscle contractions do not stop. ...
Acetylcholinesterase (AChE, EC.3.1.1.7.) is an enzyme located in the postsynaptic membrane and in the muscle endplates, where it hydrolyses the neurotransmitter acetylcholin. AChE from brain is a tetramer (G4-AChE) with a molecular mass of 320 kDa, AChE from erythrocytes is a dimer (G2-AChE) with a molecular mass of 170 kDa. Detection of higher levels of AChE in amniotic fluid can indicate fetal malformations such as neural tube defects. This antibody is specific for brain AChE and does not recognize AChE from erythrocytes. The antibody can thus distinguish between mammalian brain AChE and erythrocyte AChE. There is a weak cross-reactivity with Torpedo marmorata AChE but none with AChE from electric eel or human BtChE ...
Clean Seas Environment Monitoring Programme (CSEMP) accessment of acetylcholine esterase activity in biota (common dab muscle) at station Severn_SeInter_fi01 (Camarthen Bay) from the Marine Environment Monitoring and Assessment National database (MERMAN).
Background: Neuropsychological studies have extensively described the presence of cognitive dysfunction in MS patients. One possible pharmacological treatment of the impairment could be based on acetylcholinesterase inhibitors (AChEIs), which have sh
A new approach toward acetylcholinesterase (AChE) detection has been demonstrated based on the electrostatic interactions between anionic alkynylplatinum(II) complex molecules and cationic coordination polymer, together with the spectroscopic and emission characteristics of alkynylplatinum(II) complexes upon supramolecular selfassembly. This process involves strengthening of distinct noncovalent Pt(II)···Pt(II) and π-π stacking interactions, which is evidenced by UVvis absorption, emission, and resonance light scattering results. Such a method has been applied to AChE inhibitor screening, which is important as the demand for AChE inhibitor assays arises along with the drug development for Alzheimers disease. It affords an emission turn-on response and operates in a continuous and label-free fashion. The low-energy red emission and large Stokes shift of alkynylplatinum(II) complexes are advantageous to biological applications. Reference: Law A. S.-Y.; Yeung M. C.-L.; Yam V. W.-W. ACS ...
2HA4: Substrate and product trafficking through the active center gorge of acetylcholinesterase analyzed by crystallography and equilibrium binding
The bovine acetylcholinesterase (BoAChE) gene was cloned from genomic DNA and its structure was determined. Five exons coding for the AChE T-subunit and the alternative H-subunit were identified and their organization suggests high conservation of structure in mammalian AChE genes. The deduced amino acid sequence of the bovine T-subunit is highly similar to the human sequence, showing differences at 34 positions only. However, the cloned BoAChE sequence differs from the published amino acid sequence of AChE isolated from fetal bovine serum (FBS) by: (1) 13 amino acids, 12 of which are conserved between BoAChE and human AChE, and (2) the presence of four rather than five potential N-glycosylation sites. The full coding sequence of the mature BoAChE T-subunit was expressed in human embryonal kidney 293 cells (HEK-293). The catalytic properties of recombinant BoAChE and its reactivity towards various inhibitors were similar to those of the native bovine enzyme. Soluble recombinant BoAChE is ...
Acetylcholinesterase (AChE) is a tetrameric serine hydrolase that rapidly catalyzes the hydrolysis of acetylcholine to acetate and choline. The breakdown of acetylcholine is critical for the termination of impulse transmissions at cholinergic synapses within the nervous system. Progressive loss of cholinergic neurons in Alzheimers disease (AD) patients results in severe memory loss and impairment of cognitive function. AChE inhibitors are a strategic approach to symptomatic treatment for AD, since AChE inhibitors increase the levels of acetylcholine in the synapse, thereby enhancing cholinergic activity in the affected regions of the brain. AChE also plays an important role in agriculture since modifications in AChE can confer resistance to pesticides. AChE is a key component in many snake venoms, and AChE staining is routinely used for the initial diagnosis of Hirschsprungs disease, a congenital disorder caused by the absence of ganglion cells in the distal colon ...
Recombinant Acetylcholinesterase (AChE) Protein. Species: Mouse (Murine). Source: Escherichia coli (E. coli). Order product ABIN6301593.
The long article for discussion on the August 31, 2018 #GeriMedJC will take a look at Acetylcholinesterase inhibitors and risk of stroke and death in people with dementia.. Remember during the live hour, you can view the presentation live via Zoom https://zoom.us/j/102282147 . Have you missed our previous sessions? The 2018 presentations are all available on YouTube (click the Subscribe button!): https://www.youtube.com/channel/UC0lfYRt-7pBKFG_81JHUyWg. Acetylcholinesterase inhibitors and risk of stroke and death in people with dementia. Alzheimers Dement. 2018 Jul;14(7):944-951. INTRODUCTION ...
Date Published: May 31, 2019. Publisher: Public Library of Science. Author(s): Devashree N. Patil, Sushama A. Patil, Srinivas Sistla, Jyoti P. Jadhav, David A. Lightfoot.. http://doi.org/10.1371/journal.pone.0215291. Abstract. Among neurodegenerative diseases, Alzheimers disease (AD) is one of the most grievous disease. The oldest cholinergic hypothesis is used to elevate the level of cognitive impairment and acetylcholinesterase (AChE) comprises the major targeted enzyme in AD. Thus, acetylcholinesterase inhibitors (AChEI) constitutes the essential remedy for the treatment of AD. The study aims to evaluate the interactions between natural molecules and AChE by Surface Plasmon Resonance (SPR). The molecules like alkaloids, polyphenols and substrates of AChE have been considered for the study with a major emphasis on affinity and kinetics. To better understand the activity of small molecules, the investigation is supported by both experimental and theoretical approach such as fluorescence, ...
In this study, acetylcholinesterase (AChE; EC 3.1.1.7) was purified from plasma and erythrocytes in the Lake Van fish (Chalcalburnus tarichii P. 1811) by affinity chromatography. Enzymatic activity was spectrophotometrically measured according to Ellmans method, at 412 nm. Then, the optimal pH and temperature of the enzyme was determined. According to the results, the optimal pH and the optimum temperature were 8.0 and 25degreesC, respectively. In order to control the purification of the enzyme, sodium dodecyl-sulfate-polyacrylamide gel electrophoresis (SDS-PAGE) was done. SDS-PAGE showed a single band for enzyme. The purification rates for plasma AChE and erythrocyte AChE are 3251.6 and 8500, respectively. ...
Procedures for the preparative purification of human acetylcholinesterase (AChE; EC 3.1.1.7) have been examined. Chromatofocussing showed caudate nucleus and cerebrospinal fluid (CSF) AChE eluting between isoelectric points (pi) of 5.2 - 5.57, whilst isoelectric focussing (IEF) revealed
2JGJ: Crystal Structures of Acetylcholinesterase in Complex with Organophosphorus Compounds Suggest that the Acyl Pocket Modulates the Aging Reaction by Precluding the Formation of the Trigonal Bipyramidal Transition State.
TY - JOUR. T1 - Prediction of the binding site of 1-benzyl-4-[(5,6-dimethoxy-1-indanon-2-yl)methyl]piperidine in acetylcholinesterase by docking studies with the SYSDOC program. AU - Pang, Yuan-Ping. AU - Kozikowski, Alan P.. PY - 1994/12. Y1 - 1994/12. N2 - In the preceding paper we reported on a docking study with the SYSDOC program for predicting the binding sites of huperzine A in acetylcholinesterase (AChE) [Pang, Y.-P. and Kozikowski, A.P., J. Comput.-Aided Mol. Design, 8 (1994) 669]. Here we present a prediction of the binding sites of 1-benzyl-4-[(5,6-dimethoxy-1-indanon-2-yl)methyl]piperidine (E2020) in AChE by the same method. E2020 is one of the most potent and selective reversible inhibitors of AChE, and this molecule has puzzled researchers, partly due to its flexible structure, in understanding how it binds to AChE. Based on the results of docking 1320 different conformers of E2020 into 69 different conformers of AChE and on the pharmacological data reported for E2020 and its ...
Two novel families of dual binding site acetylcholinesterase (AChE) inhibitors have been developed, consisting of a tacrine or 6-chlorotacrine unit as the active site interacting moiety, either the 5,6-dimethoxy-2-[(4-piperidinyl)methyl]-1-indanone fragment of donepezil (or the indane derivative thereof) or a 5-phenylpyrano[3,2-c]quinoline system, reminiscent to the tryciclic core of propidium, as the peripheral site interacting unit, and a linker of suitable length as to allow the simultaneous binding at both sites. These hybrid compounds are all potent and selective inhibitors of human AChE, and more interestingly, are able to interfere in vitro both formation and aggregation of the beta-amyloid peptide, the latter effects endowing these compounds with the potential to modify Alzheimers disease progression ...
Due to the diversity of biological activities that can be found in aquatic ecosystems, marine metabolites have been an active area of drug discovery for the last 30 years. Marine metabolites have been found to inhibit a number of enzymes important in the treatment of human disease. Here, we focus on marine metabolites that inhibit the enzyme acetylcholinesterase, which is the cellular target for treatment of early-stage Alzheimers disease. Currently, development of anticholinesterase drugs with improved potency, and drugs that act as dual acetylcholinesterase and amyloid-β aggregation inhibitors, are being sought to treat Alzheimers disease. Seven classes of marine metabolites are reported to possess anti-cholinesterase activity. We compared these metabolites to clinically-used acetylcholinesterase inhibitors having known mechanisms of inhibition. We performed a docking simulation and compared them to published experimental data for each metabolite to determine the most likely mechanism of
Complete information for COLQ gene (Protein Coding), Collagen Like Tail Subunit Of Asymmetric Acetylcholinesterase, including: function, proteins, disorders, pathways, orthologs, and expression. GeneCards - The Human Gene Compendium
Vol 14: Acetylcholinesterase overexpression mediated by oncolytic adenovirus exhibited potent anti-tumor effect.. This article is from BMC Cancer, volume 14.AbstractBackground: Acetylcholinesterase (AChE) mainly functions as an effici. Biblioteca virtual para leer y descargar libros, documentos, trabajos y tesis universitarias en PDF. Material universiario, documentación y tareas realizadas por universitarios en nuestra biblioteca. Para descargar gratis y para leer online.
In the fetal and neonatal monkey, periodically organized regions of high activity of acetylcholinesterase were found in the visual cortical area V2 (Area 18). The acetylcholinesterase bands, like the thin and thick stripes of cytochrome oxidase, were found to run orthogonal to the area 17/18 border. During neonatal development these bands progressively narrow and finally disappear shortly after four months of age.
Small numbers of postganglionic cells persist in sympathetic ganglia after the treatment of newborn animals with the nerve growth factor antiserum. In the present study the possibiity was explored whether the cells which survive the immunosympathectomy may be predominantly those which have been designated, in the cat, as cholinergic sympathetic cells. The acetylcholinesterase activity of sympathetic ganglia (superior cervical, stellate, thoracic chain, superior mesenteric, celiac and cardiac) from immunosympathectomized and control rats was visualized by the histochemical method of Koelle. As in the cat, the sympathetic ganglia of rats contain postganglionic cell bodies with either marked, moderate or slight acetylcholinestrase activity. Contrary to cat sympathetic ganglia, the cells with marked and moderate acetylcholinesterase activity predominate in the sympathetic ganglia of control rats. In the various sympathetic ganglia studied in this investigation, cells with slight acetylcholinesterase ...
Excess expression of acetylcholinesterase (AChE) in the cortex and hippocampus causes a decrease in the number of glutamatergic synapses and alters the expression of neurexin and neuroligin, trans-synaptic proteins that control synaptic stability. The molecular sequence and three-dimensional structure of AChE are homologous to the corresponding aspects of the ectodomain of neuroligin. This study investigated whether excess AChE interacts physically with neurexin to destabilize glutamatergic synapses. The results showed that AChE clusters colocalized with neurexin assemblies in the neurites of hippocampal neurons and that AChE co-immunoprecipitated with neurexin from the lysate of these neurons. Moreover, when expressed in human embryonic kidney 293 cells, N-glycosylated AChE co-immunoprecipitated with non-O-glycosylated neurexin-1β, with N-glycosylation of the AChE being required for this co-precipitation to occur. Increasing extracellular AChE decreased the association of neurexin with neuroligin and
Acetylcholinesterase小鼠单克隆抗体[HR2](ab2803)可与小鼠, 兔, 豚鼠, 牛, 猫, 人, 猕猴样本反应并经IP, ELISA, IHC, Flow Cyt, ICC/IF实验严格验证,被3篇文献引用。
inproceedings{BUT7539, author=Lukáš {Fujcik} and Radimír {Vrba} and Jan {Krejčí} and Jiří {Háze} and Michal {Skočdopole} and Ondřej {Sajdl}, title=INPUT CONTROL OF SENSOR PARAMETERS AND REPRODUCIBILITY OF SENSOR MEASUREMENT, annote=Fast detection of pesticide toxicity in the field conditions is very important in many aspects (longtime influence of low concentrations on man´s health, pesticide storage, price of one test etc.). The pesticide concentration measurements are performed on a biosensor with acetylcholinesterase (AChE). The AChE is a very sensitive compound. The measurement uses principle of an artificial synapse (AS) and inhibition of an enzyme Acetylcholinesterase (AChE). The AS is a very effective detector of the pesticide toxicity. Therefore properties of the sensor have to be measured without AChE at first. This process is called input control of the sensor. The reproducibility of electrochemical detector is studied first using hydrogen peroxide and second ...
Acetylcholinesterase (HGNC symbol ACHE), also known as AChE or acetylhydrolase, is the primary cholinesterase in the body. It is an enzyme that catalyzes the breakdown of acetylcholine and of some other choline esters that function as neurotransmitters. AChE is found at mainly neuromuscular junctions and in chemical synapses of the cholinergic type, where its activity serves to terminate synaptic transmission. It belongs to carboxylesterase family of enzymes. It is the primary target of inhibition by organophosphorus compounds such as nerve agents and pesticides. AChE is a hydrolase that hydrolyzes choline esters. It has a very high catalytic activity - each molecule of AChE degrades about 25000 molecules of acetylcholine (ACh) per second, approaching the limit allowed by diffusion of the substrate. The active site of AChE comprises 2 subsites - the anionic site and the esteratic subsite. The structure and mechanism of action of AChE have been elucidated from the crystal structure of the enzyme. ...
The researchers) demonstrate that the active component of marijuana, Delta9-tetrahydrocannabinol (THC), competitively inhibits the enzyme acetylcholinesterase (AChE) as well as prevents AChE-induced amyloid beta-peptide (Abeta) aggregation, the key pathological marker of Alzheimers disease. Computational modeling of the THC-AChE interaction revealed that THC binds in the peripheral anionic site of AChE, the critical region involved in amyloidgenesis. Compared to currently approved drugs prescribed for the treatment of Alzheimers disease, THC is a considerably superior inhibitor of Abeta aggregation, and this study provides a previously unrecognized molecular mechanism through which cannabinoid molecules may directly impact the progression of this debilitating disease. ...
Acetylcholinesterase inhibitor: | | ||| | |Acetylcholine| | | | | ... World Heritage Encyclopedia, the aggregation of the largest online encyclopedias available, and the most definitive collection ever assembled.
Has anyone had any luck using acetylcholinesterase inhibitors like razadyne/ aricept to improve cognitive function? My Doc prescribed razadyne, but insurance wont cover it unless I get a DX of Alzheimers. Im not willing to do that. I saw and ...
Characterization and gene cloning of acetylecholinesterase (AChE) in the insecticide-resistant (R) and -susceptible (S) insects have been reported in the past. However, the studies focused mostly on herbivorous pests, rather than predacious species, such as ladybird beetles. Using R and S Propylaea japonica (thunberg), a full-length cDNA sequence (2928 bp) of the ace1-type AChE gene was determined for the first time. The ace1 encoding a protein of 645 amino acids contained typical conserved motifs, such as FGESAG domains, catalytic triad, acyl pocket, oxyanino hole, choline binding site, peripheral anionic site, omega loop and conserved aromatic residues. R P. japonica displayed 50-times greater resistance to chlorpyrifos or mathamidophos with a significantly lower AChE sensitivity to paraoxon, malaoxon, chlorpyrifos or methamidophos than its S counterpart. Five amino acids in the ace1 of R P. japonica differed from those found in S P. japonica. One of them, F358S, located in the acyl-binding ...
The combined effect of Vitashield 40EC (chlorpyrifos ethyl-CPF) and Bassa 50EC (fenobucarb-F) was compared with the effects from exposure to the two pesticides separately, by measuring the brain acetylcholinesterase (AChE) activity in climbing perch fingerlings (Anabas testudineus). The experiment was conducted under controlled laboratory conditions and included three treatments containing 0.173 mg/L of CPF, 1.137 mg/L of F, 0.173 mg/L of CPF + 1.137 mg/L of F (M), and a control. The inhibition of the brain AChE activity in fish exposed to F was weaker and shorter than in fish exposed to CPF. The inhibition by the mixture of CPF and F was significantly lower and less prolonged than the inhibition by only CPF but significantly higher than the inhibition by only F.. ...
Some embryos of Ciona intestinalis which were permanently cleavage-arrested with cytochalasin B at the 1-cell, 4-cell, or 8-cell stages produced, after 12 or 16 h of development time (18 °C), a level of muscle acetylcholinesterase activity equal to that found in normal early and later larval stage embryos of the same age. Enzyme activity was measured quantitatively in single whole embryos by a colorimetric procedure using microdensitometry. Quantitative regulation of a differentiation end product indicated that the usual transcriptional and translational control mechanisms for that histospecific protein continued to operate normally in the cleavage-arrested embryos. Acetylcholinesterase expression was apparently regulated independently of the usual cell cytoplasmic volume in the muscle lineage cells and possibly also independently of the normal nuclear number in the lineage. There is an egg cytoplasmic determinant that is segregated into the muscle lineage cells during cleavage and which ...
But after this step the cholinesterase is irreversibly inhibited. The irreversible phosphorylation of the cholinesterase occurs in two steps. This results in continuous activation of acetylcholine receptors, which leads to the acute symptoms of TEPP poisoning. … Acetylcholinesterase inhibitors (AchEI), like donepezil, galantamine and rivastigmine are the only drugs - together with memantine (glutamate receptor antagonist) - which obtained the indication for the symptomatic treatment of Alzheimer disease, but are also used for … Then the second step takes place. More than 7100 monographs are provided for prescription and over-the-counter drugs, as well as for corresponding brand-name drugs… Acetylcholinesterase Inhibitors Acetylcholinesterase inhibitors (AChEI) bind to acetylcholinesterase (Achase) so it will prevent the enzyme from breaking down ACh. [6], The time dependent irreversible inhibition of the cholinesterase can be described by the following equation.[6]. This increases levels ...
In this study, we have employed in silico methodology combining double pharmacophore based screening, molecular docking, and ADME/T filtering to identify dual binding site acetylcholinesterase inhibitors that can preferentially inhibit acetylcholinesterase and simultaneously inhibit the butyrylcholinesterase also but in the lesser extent than acetylcholinesterase. 3D-pharmacophore models of AChE and BuChE enzyme inhibitors have been developed from xanthostigmine derivatives through HypoGen and validated using test set, Fischers randomization technique. The best acetylcholinesterase and butyrylcholinesterase inhibitors pharmacophore hypotheses Hypo1_A and Hypo1_B, with high correlation coefficient of 0.96 and 0.94, respectively, were used as 3D query for screening the Zinc database. The screened hits were then subjected to the ADME/T and molecular docking study to prioritise the compounds. Finally, 18 compounds were identified as potential leads against AChE enzyme, showing good predicted ...
Humans in modern society are exposed to an ever-increasing number of electromagneticfields (EMFs) and some studies have demonstrated that these waves can alter brain function but the mechanism still remains unclear. Hence, this study sought to investigate the effect of 2.5 Ghz band radio-frequency electromagnetic waves (RFEMF) exposure on cerebral cortex acetylcholinesterase (AChE) activity and their mRNA expression level as well as locomotor function and anxiety-linked behaviour in male rats. Animals were divided into four groups namely; group 1 was control (without exposure), group 2-4 were exposed to 2.5 Ghz radiofrequency waves from an installed WI-FI device for a period of 4, 6 and 8 weeks respectively. The results revealed that WiFi exposure caused a significant increase in anxiety level and affect locomotor function. Furthermore, there was a significant decrease in AChE activity with a concomitant increase in AChE mRNA expression level in WiFi exposed rats when compared with control. In ...
TY - JOUR. T1 - Treatment of Alzheimers disease with acetylcholinesterase inhibitors. T2 - Bridging the gap between evidence and practice. AU - Frisoni, Giovanni B.. PY - 2001. Y1 - 2001. N2 - Views on drug therapy with acetylcholinesterase inhibitors of the cognitive symptoms of Alzheimers disease are not uniform, varying from excitement at the possibility of significantly improving the personal and social burden of the disease to skeptical and nihilistic attitudes. Clinical practice from generous prescription to evidence-based guidelines and advising much stricter rules, mirror these attitudes. The epidemiological and clinical relevance of the issue requires understanding of the factors responsible for such discrepancies. Randomized clinical trials have only been able to address a few of the many variables that can affect the response to acetylcholinesterase inhibitors. The effect on behavioral symptoms, severe Alzheimers dementia, and non-Alzheimers forms of degenerative dementia need to ...
TY - JOUR AU - Bosak, Anita AU - Opsenica, Dejan AU - Šinko, Goran AU - Zlatar, Matija AU - Kovarik, Zrinka PY - 2019 UR - http://cer.ihtm.bg.ac.rs/handle/123456789/2905 AB - Eight derivatives of 4-aminoquinolines differing in the substituents attached to the C(4)-amino group and C(7)were synthesised and tested as inhibitors of human acetylcholinesterase (AChE)and butyrylcholinesterase (BChE). Both enzymes were inhibited by all of the compounds with inhibition constants (K i )ranging from 0.50 to 50 μM exhibiting slight selectivity toward AChE over BChE. The most potent inhibitors of AChE were compounds with an n-octylamino chain or adamantyl group. The shortening of the chain length resulted in a decrease in AChE inhibition by 5-20 times. Docking studies revealed that the quinoline group within the AChE active site was positioned in the choline binding site, while the C(4)-amino group substituents, depending on their lipophilicity, could establish hydrogen bonds or π-interactions with ...
SUMMARY: Adult female Wistar rats were treated daily for 60 days with sodium fluoride (500 ppm NaF = 226 ppm fluoride ion) in drinking water, alone or in combination with vitamin D (200 IU/kg by oral intubation). Throughout the period, food intake was measured daily. Body weight gain, exploratory motor activity (EMA) rota-rod motor coordination, dental structure, brain acetylcholinesterase (AchE) activity, and serum fluoride and serum calcium concentration were determined 24 hr after the last treatment. Serum fluoride concentration increased markedly in the NaF-treated animals and was accompanied by decreased food intake, reduced body weight gain, impairment of EMA and motor coordination, dental lesions, inhibition of brain AchE activity, and hypocalcemia. Administration of vitamin D along with NaF prevented hypocalcemia. However, the toxic action fluoride on motor coordination, brain AchE activity, and the teeth was not prevented in these animals, probably because vitamin D is not able to ...
Galantamine Hydrobromide is the hydrobromide salt form of galantamine, a tertiary alkaloid with anticholinesterase and neurocognitive-enhancing activities. It is an alkaloid acetylcholinesterase inhibitor. Galantamine competitively and reversibly inhibits acetylcholinesterase, thereby increasing the concentration and enhancing the action of acetylcholine (Ach). This agent may improve neurocognitive function in mild and moderate Alzheimer s disease and may reduce abstinence-induced cognitive symptoms that promote smoking relapse.
TY - JOUR. T1 - Acetylcholinesterase Choline-Based Ionic Liquid Inhibitors: In Vitro and in Silico Molecular Docking Studies. AU - Siopa, Filipa. AU - Frade, Raquel F. M.. AU - Diniz, Ana. AU - Andrade, Joana M.. AU - Nicolai, Marisa. AU - Meirinhos, Ana. AU - Lucas, Susana D.. AU - Marcelo, Filipa. AU - Afonso, Carlos A. M.. AU - Rijo, Patrícia. N1 - info:eu-repo/grantAgreement/FCT/SFRH/SFRH%2FBPD%2F73822%2F2010/PT# info:eu-repo/grantAgreement/FCT/SFRH/SFRH%2FBPD%2F88666%2F2012/PT# info:eu-repo/grantAgreement/FCT/5876/147348/PT# COMPETE Programme: SAICTPAC/0019/2015 IF/00780/2015 Project no. 022161. PY - 2018/12/12. Y1 - 2018/12/12. N2 - Monocationic and dicationic cholinium ionic liquids (ILs) were synthesized and evaluated as acetylcholinesterase (AChE) inhibitors with in vitro and in silico models, and their cytotoxicity was assessed using human cell lines from skin (CRL-1502) and colon cancer (CaCo-2). The ILs with a longer alkyl chain were stronger AChE inhibitors, the dicationic ILs ...
Butyrylcholinesterase [BuChE (acylcholine acyl hydrolase); EC 3.1.1.8] limits the access of drugs, including tacrine, to other proteins. The atypical BuChE variant, in which Asp70 at the rim of the active site gorge is substituted by glycine, displayed a more drastically weakened interaction with tacrine than with cocaine, dibucaine, succinylcholine, BW284c51 [1,5-bis(4-allyldimethylammoniumphenyl)pentan-3-one dibromide], or alpha-solanine. To delineate the protein domains that are responsible for this phenomenon, we mutated residues within the rim of the active site gorge, the region parallel to the peripheral site in the homologous enzyme acetylcholinesterase [AChE (acetylcholine acetyl hydrolase); EC 3.1.1.7], the oxyanion hole, and the choline-binding site. When expressed in microinjected Xenopus laevis oocytes, all mutant DNAs yielded comparable amounts of immunoreactive protein products. Most mutants retained catalytic activity close to that of wild-type BuChE and were capable of binding ligands
Pralidoxime reactivates acetylcholinesterase only if irreversible binding to the OP has not already occurred (ageing). The acetylcholinesterase enzyme has two parts to it. In organophosphate poisoning, an organophosphate binds to just one end of the acetylcholinesterase enzyme (the esteric site), blocking its activity.
TY - JOUR. T1 - Simple general acid-base catalysis of physiological acetylcholinesterase reactions. AU - Pryor, Alton N.. AU - Selwood, Trevor. AU - Leu, Lee Shan. AU - Andracki, Mark A.. AU - Lee, Bong Ho. AU - Rao, Muralikrishna. AU - Rosenberry, Terrone. AU - Doctor, Bhupendra P.. AU - Silman, Israel. AU - Quinn, Daniel M.. PY - 1992/5/6. Y1 - 1992/5/6. N2 - Elements of transition-state stabilization by proton bridging have been characterized by measuring solvent isotope effects and proton inventories for hydrolyses of (acetylthio)choline (ATCh), (propionylthio)choline (PrTCh), and (butyrylthio)choline (BuTCh) catalyzed by acetylcholinesterases (AChEs) from Electrophorus electricus, fetal bovine serum, human erythrocytes, and Torpedo californica. For the Electrophorus enzyme, the acylation rate constant, kcat/Km {= (V/K)/[E]T}, decreases in the order ATCh , PrTCh ≫ BuTCh. Solvent isotope effects for V/K of ATCh hydrolysis are usually within experimental error of unity, which is consistent ...
Huperzine A. The severity of the cognitive and functional symptoms of various neurodegenerative diseases, including Alzheimers disease (AD), are strongly correlated to decreased levels of the neurotransmitter acetylcholine (ACh). Consequently, inhibition of acetylcholine esterase (AChE) is an established strategy to alleviate these symptoms, and several AChE inhibitors are currently in clinical use. (-)-Huperzine A (6) is a potent and reversible AChE inhibitor that is well-tolerated in humans. Natural (-)-huperzine A (6) has been employed for over a decade to treatment mild-to-moderate AD in China. In addition to relieving the symptoms associated with acetylcholinesterase deficiencies, there is evidence that huperzine may modify the progression of AD. Furthermore, a large body of evidence also suggests that (-)-huperzine A (6) may be useful as a prophylaxis against organophosphate-based nerve agents. Although several syntheses of huperzine have been reported, a practical and scalable route to ...
Data & statistics on mean acetylcholinesterase levels in the lungs of guinea pigs: Mean acetylcholinesterase (AChE) levels in the lungs of guinea pigs, 1 mg or 3 mg vitamin C/animal/day Bax and Bcl-2 of the lung extracts of guinea pigs exposed to air or CS supplemented with A, Immunoblots of caspase 3, PARP, A, Immunoblots of caspase 3, PARP, Bax and Bcl-2 of the lung extracts of guinea pigs exposed to air or CS supplemented with 1 mg or 15 mg vitamin C/animal/day. Vit C means vitamin C. Air + vit C means exposed to air and fed 1 mg or 15 mg vitamin ..., 8-iso-PGF2α levels in perfusate samples taken during the allergen-induced early asthmatic response of isolated guinea pig lungs. OVA challenge increased 8-isoPGF2α formation in lungs from OVA-sensitized animals (black bars) as compared to saline-sensitized controls (white bars), and UWPC feeding tended to further increase these levels. Bars indicate mean ± SEM; * P | 0.05....
Background: Acetylcholinesterase inhibitors (AChEIs) are widely used to delay cognitive decline in Alzheimers disease. Observational studies in routine clinical practice have shown cognitive improvement in some groups of patients receiving these agents but longitudinal trajectories before and after AChEI initiation have not previously been considered. Objectives: To compare trajectories of cognitive function before and after AChEI initiation and investigate predictors of these differences. Method: A retrospective longitudinal study was constructed using data from 2460 patients who received AChEIs and who had routine data on cognitive function (Mini-Mental State Examination; MMSE) before and after AChEI initiation. Longitudinal MMSE change was modelled using three-piece linear mixed models with the following segments: 0-12 months prior to AChEI initiation, 0-6 months and 6-36 months after initiation. Results: MMSE decline was reversed (in that the slope was improved by an average 4.2 units per ...
Heavy metals and organophosphorus insecticide is known to act as disruptors for the enzyme system, leading to physiologic disorders. The present study was conducted to investigate the potential use of these enzymes as biomarkers in assessment of contaminated sediments on tropical chironomid species. Acetylcholinesterase (AChE), glutathione-S-transferase (GST) and metallothionein (MT) activity was measured in the fourth-instar chironomid larvae, Chironomus javanus, Kieffer, after either 48-hr or 96-hr exposure to organophosphorus insecticide, chlorpyrifos (0.01- 0.25 mg kg-1) or heavy metal cadmium (0.1-25 mg kg-1). Exposure to chlorpyrifos (0.01 mg kg-1) at 48 and 96 hr significantly of AChE activity (64.2 % -85.9%) and induced GST activity (33.9 - 63.8 %) when compared with control (P,0.05). Moreover, exposure to cadmium (0.1mg kg-1) at 48 and 96 hr also showed significant increas GST activity (11.7 - 40 %) and MT level (9.0 % - 70.5 %) when compared with control (P,0.05). The results indicated ...
We are happy to share a great write-up by colorimeter user (and kickstarter backer) Steve Maxwell Detecting Pesticides in Organic and Conventional Raspberries. Steve has used a modified colorimeter along with a acetylcholinesterase inhibition assay to determine whether there was any detectable difference in the levels of pesticides found in store-bought organic versus conventional raspberries.. The acetylcholinesterase (AChE) inhibition assay works as follows: Activity of AChE produces thiocholine which reacts with Ellmans Reagent (DNTB: 5,5-dithio-bis-[2-nitrobenzoic acid) to produce a 412nm absorbing product. The product is measured with a colorimeter or spectrophotometer at 412nm to determine AChE activity. Pesticides in food (mainly Carbamate and Organophosphate) inhibit AChE activity thereby also inhibiting the production of the 412nm product in the assay tube.. For this pesticide assay, Steve used a commercially available kit, the Rapid Pesticide Detection Test Kit from RenekaBio, Cat ...
Authors: DURRE SHAHWAR, MUHAMMAD ASAM RAZA, TANIA KHAN Abstract: This study was designed to synthesize and evaluate derivatives of scopolamine (1) as acetylcholine esterase and protease inhibitors. Scopolamine (1) was extracted from the aerial parts of Datura innoxia through bioassay guided fractionation. Five different derivatives of scopolamine (1) were synthesized, and identified through spectroscopic studies. Their acetylcholine esterase (AChE) and trypsin inhibitory potentials were determined through standard protocols and evaluated from the perspective of structure-activity relationship. The synthesized scopolamine derivatives (2-6) showed remarkable AChE inhibitory activity, except for scopoline (6). The results showed higher enzyme inhibition potential of the synthesized compounds (2-5) as compared to scopolamine (1). Maximum inhibition was exhibited by scopolamine N-oxide (89.9 \pm 1.2%, IC_{50} = 37.4 \pm 1.1 \mu M)), followed by scopolamine sulfonic acid (70.3 \pm 0.8%, IC_{50} = 46.9 ...
The present study was focused upon the assessment of acetyl-cholinesterase (AChE) activity in the digestive gland (main metabolic center) and foot (highly innervated organ) of the green garden snail, Cantareus apertus (Born, 1778), exposed to different nominal dietary concentrations of Pb (25 and 2500 mg Pb/Kg), Cd (10 and 100 mg Cd/Kg) and their combination (25 mg Pb + 10 mg Cd/Kg and 2500 mg Pb + 100 mg Cd/ Kg) for 60 days. AChE activity was lower in the foot than in the digestive gland (~50%) and decreased with experimental time in both tissues. In metal treated snails, AChE activity was significantly decreased in both tissues to a 50-60% of the values recorded in control snails. This decrease followed a dose depending trend at each exposure time, albeit the response was attenuated at the long-term (60 d) in comparison with the short-term (7 d). Besides, the combination of both metals provoked interactive effects not seemingly related with the tissue levels of the metals. Thus, it was concluded that
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By analogy with the natural product chelerythrine, which has been identified as an inhibitor of both acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), we prepared a small series of 8-hydroxy-2,7-naphthyridin-2-ium salts. Spectroscopic analyses allowed us to elucidate the zwitterionic nature of 2,
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Alzheimers disease is the most common cause of dementia in our older Americans. The disease is named after the psychiatrist and neuropathologist Dr. Alois Alzheimer. He discovered unique changes in the brain of a patient with severe dementia who had died - deposits of amyloid plaques and neurofibrillary tangles. Today the presence of these plaques and tangles is considered characteristic of Alzheimers disease. The brain shrinks due to loss of brain cells and there is decreased transmission of the chemical messages in the brain (neurotransmission). Currently, medicine cannot remove the plaques and tangles, and we cannot replace the lost tissue in the brain. All of the prescription drugs on the market for Alzheimers disease are aimed at improving neurotransmission. Tacrine has several proposed mechanisms of action, but primarily it strongly inhibits the enzyme acetylcholinesterase. We want to inhibit acetylcholinesterase because it breaks down acetylcholine, which is a neurotransmitter that has ...
Background Phlebotomus papatasi vectors zoonotic cutaneous leishmaniasis. Previous expression of recombinant P. papatasi acetylcholinesterase (PpAChE1) revealed 85% amino acid sequence identity to mosquito AChE and identified synthetic carbamates that effectively inhibited PpAChE1 with improved specificity for arthropod AChEs compared to mammalian AChEs. We hypothesized that the G119S mutation causing high level resistance to organophosphate insecticides in mosquitoes may occur in PpAChE1 and may reduce sensitivity to inhibition. We report construction, expression, and biochemical properties of rPpAChE1 containing the G119S orthologous mutation. Methods Targeted mutagenesis introduced the G119S orthologous substitution in PpAChE1 cDNA. Recombinant PpAChE1 enzymes containing or lacking the G119S mutation were expressed in the baculoviral system. Biochemical assays were conducted to determine altered catalytic properties and inhibitor sensitivity resulting from the G119S substitution. A molecular ...
Beyond Pesticides, September 4, 2020) When pesticide drift is investigated, it is most often drift from agricultural fields that is examined. A new study shows that off-target drift of pesticides from greenhouses is also a reality. This research deduced such drift of organophosphate and carbamate pesticides from crop applications done in Ecuadoran floriculture greenhouses by evaluating the acetylcholinesterase enzyme (AChE) activity, necessary to the transmission of nerve impulses, in children residing nearby. The team finds that children living in homes near greenhouses in which these insecticides (widely recognized as cholinesterase inhibitors) are used exhibit reduced activity of this enzyme and abnormal functioning of the nervous system. Beyond Pesticides has monitored the pesticide drift issue intensively, and has long advocated for far better protections for farmworkers. This new information connects those issues, and expands the drift concerns to include risks to people working in ...
Altered glycosylation of acetylcholinesterase in the Alzheimer disease brain: involvement of alfa7 nicotinic acetylcholine receptors Chapter 2005 ...
This work presents the development of bioassays and biosensors for the detection of insecticides widely used in the treatment of olive trees. The systems are based on the covalent immobilisation of acetylcholinesterase on magnetic microbeads using either colorimetry or amperometry as detection technique. The magnetic beads were immobilised on screen-printed electrodes or microtitration plates and tested using standard solutions and real samples. The developed devices showed good analytical performances with limits of detection much lower than the maximum residue limit tolerated by international regulations, as well as a good reproducibility and stability.
SILVA, Joyce Izidoro da; MORAES, Marcela Cristina de; VIEIRA, Lucas Campos Curcino; et al. Acetylcholinesterase capillary enzyme reactor for screening and characterization of selective inhibitors. Journal of Pharmaceutical and Biomedical Analysis, Amsterdam, v. 73, p. 44-52, 2013. Disponível em: < http://dx.doi.org/10.1016/j.jpba.2012.01.026 > DOI: 10.1016/j.jpba.2012.01.026 ...
Pre-invasion history and demography shape the genetic variation in the insecticide resistance-related acetylcholinesterase 2 gene in the invasive Colorado potato beetle. . Biblioteca virtual para leer y descargar libros, documentos, trabajos y tesis universitarias en PDF. Material universiario, documentación y tareas realizadas por universitarios en nuestra biblioteca. Para descargar gratis y para leer online.
Sorption isotherms were estimated for two model organophosphorus pesticides - methamidophos and paraoxon-ethyl - and four typical Central European soils endangered by these pesticides: haplic Chernozems, Cambisols, Luvisols, and Fluvisols. A photometric microplate assay based on the recognition capability of the enzyme acetylcholinesterase toward organophosphorous pesticides was used for the construction of sorption isotherms. The sorption capacity of each soil was then determined and it was found that the soils with the highest content of humic acid (haplic Chernozems and haplic Luvisols) sorbed pesticides most. Pesticides in concentrations over the sorption capacity were easily removed from soil by water ...
Nerve agents are compounds that have the capacity to inactivate the enzyme acetylcholinesterase (AChE). The first compounds to be synthesized were known as the G-series agents (
Adult male albino rats were fed on stored wheat grains (Triticum aestivum L.) treated with malathion and spinosad at both 8 and 16 ppm for 90 consecutive days to evaluate their hepatic and renal toxicity. The activity of serum acetylcholinesterase (AChE) was decreased in rats treated with the higher concentration of both tested pesticides. Biochemical parameters of liver functions [i.e., aspartate aminotransferase (AST), alanine aminotransferase (ALT), alkaline phosphatase (ALP), acid phosphatase (ACP) activity, as well as total protein, albumin, bilirubin and cholesterol levels] were severely affected especially at higher concentration. Malathion and spinosad elevated the activity of ALT, AST, ALP and ACP in rats treated with the higher concentration. Also, total and direct bilirubin levels increased in rats treated with the higher concentration of both pesticides. On the contrary, both pesticides decreased total protein and albumin levels in treated rats in a concentration-dependent manner. ...
Jose Raul Tormos Melendez, Ph.D., received his bachelors in Chemistry from the University of Sacred Heart in San Juan, Puerto Rico. During his years as an undergraduate he worked as a REU (Research Experience for Undergraduates) student in the Department of Chemistry at the University of Puerto Rico - Rio Piedras isolating and analyzing soil samples that contain novel fatty acids with potential medicinal applications. After graduation he worked in the Chemical Technology Division at Argonne National Laboratories in Chicago, IL.. Dr. Tormos obtained his masters and doctorate from research laboratory of Dr. Dan Quinn from the Department of Chemistry at the University of Iowa. His research involved using enzyme kinetics and isotope effects with UV-Vis spectrophotometry to demonstrate the accumulation of a tetrahedral intermediate in the active site of the enzymes acetylcholinesterase, an enzyme found in the neuromuscular junction; and butyrylcholinesterase, an enzyme that has been the target of ...
BioMed Research International is a peer-reviewed, Open Access journal that publishes original research articles, review articles, and clinical studies covering a wide range of subjects in life sciences and medicine. The journal is divided into 55 subject areas.
VX nerve gas. Molecular model of the nerve gas VX, or ethyl S-[2-diisopropylaminoethyl]- methylphosphonothioate. It has the formula (C11.H26.N.O2.P.S). The atoms are shown as sticks and are colour-coded: carbon (magenta), hydrogen (white), oxygen (red), nitrogen (blue), phosphorus (green) and sulphur (yellow). VX is a synthetic compound used in chemical weapons. It belongs to a class of drugs called cholinesterase inhibitors, which block the enzyme acetylcholinesterase. They cause muscle spasms and death through respiratory failure. VX can be absorbed through the skin, and may remain active for weeks after deployment. - Stock Image A700/0123
Avoiding TragedyMy heart aches at the tragedy of John Richard Gregory and his adoptive parents.Johns parents are suing the state because they were not told that his biological mother had used drugs
Among organophosphorothioate (OPT) pesticides, malathion is considered relatively safe for use in mammals. Its rapid degradation by carboxylesterases competes with the cytochrome P450 (P450)-catalyzed formation of malaoxon, the toxic metabolite. However, impurities in commercial formulations are potent inhibitors of carboxylesterase, allowing a dramatic increase in malaoxon formation. Malathion desulfuration has been characterized in human liver microsomes (HLMs) with a method based on acetylcholinesterase inhibition that is able to detect nanomolar levels of oxon. The active P450 isoforms have been identified by means of a multifaceted strategy, including the use of cDNA-expressed human P450s and correlation, immunoinhibition, and chemical inhibition studies in a panel of phenotyped HLMs. HLMs catalyzed malaoxon formation with a high level of variability (,200-fold). One or two components (Kmapp1 = 53-67 μM; Kmapp2 = 427-1721 μM) were evidenced, depending on the relative specific P450 ...
VX is a liquid that cannot be smelled or tasted. It is a thick liquid with the texture of motor oil. As a weapon, it can be used as a liquid or an aerosol. It could be spread by air, through water, or through food.[5] Making VX is difficult and very dangerous. Many toxic and dangerous chemicals are used in the process.[2] VX works the same way other nerve agents do. It blocks nerve signals from getting from the brain to the body. Normally, a neurotransmitter (chemical messenger) called acetylcholine tells the bodys muscles to tighten up when they need to. When it is time for the muscles to relax, an enzyme called acetylcholinesterase destroys acetylcholine, so the muscles stop getting the signal to relax.[6] VX blocks acetylcholinesterase. Acetylcholine builds up, because it is not getting destroyed by acetylcholinesterase. The muscles get tighter and tighter, because the extra acetylcholine keeps telling them to. The extra acetylcholine also signals the parasympathetic nervous system to work ...
A laboratory study on the sublethal effects of malathion on the net-spinning behavior of the caddisfly larvae Hydropsycheslossonae was conducted in order to assess the potential of net anomalies as an indicator of chronic exposure to organophosphorus insecticides. Two anomalies were identified after chronic exposure to 0.01, 0.05, 0.1, 0.5 and 1.0 μg l−1 malathion. The first was a distortion of the midline meshes where the normal diamond shape structure was disrupted and the meshes were separated by extra strands (called midline anomaly). The second aberration observed was a significant decrease in net symmetry. Both anomalies were highly correlated to the toxic action of malathion, i.e. inhibition of the acetylcholinesterase enzyme (AChE). Sodium dodecyl sulfate-polyacrylamide gel electrophoresis analyses of capture nets did not show any modification of silk polypeptides after exposure to malathion, indicating that net distortions were not related to silk composition. Both anomalies seem ...
In human cell biology globules of fat are the individual pieces of intracellular fat inside other cell types than adipocytes (fat cells). Intracellular fat is bound in the globular form by phospholipid membranes, which are hydrophobic. This means that fat globules are insoluble in water. In simpler terms: a vacuole or droplet of triglyceride or some other blood lipid, which is located inside a cell that is not an adipocyte (fat cell), as opposed to fat cells in between other cells in an organ. Lipids and any lipid digestive derivatives must be transported in the globular form within the cell, blood and tissue spaces due to its insolubility. Globules of fat are emulsified in the stomach into small droplets by bile salts during food digestion, speeding up the rate of digestion by the enzyme lipase later on. Bile salts possess detergent properties that allow them to emulsify fat globules into smaller emulsion droplets, and then into even smaller micelles. This increases the surface area for ...
IQ Brain Function supplement was formulated for individuals that need to maintain over all brain function in terms of memory. This supplement is good for students, professionals as well as the elderly who are experiencing some cognitive loss or have Alzheimers disease. If you need some assistance with remembering names, addresses and phone numbers, this supplement is for you. IQ Brain combines Huperzine A, Phosphatidylcholine, Folic acid and amino acids to support memory and learning function. Huperzine A is an acetylcholinesterase inhibitor which allows the neurotransmitter acetylcholine to linger in the synaptic cleft longer promoting short term memory. Phosphatidylcholine is an important phospholipid that is found in neuronal cell membranes and important for maintaining proper membrane function. It can also be used to supply choline for the neurotransmitter acetylcholine.. ...
HUP 13 is an analogue of huperzine A with comparable inhibitory action on acetylcholinesterase, but less inhibitory effect on butyrylcholinesterase. HUP 13 is
TY - JOUR. T1 - Acetylcholine and its enzymes in some brain areas of the rat under stress. AU - Fatranská, M.. AU - Budai, D.. AU - Opršalová, Z.. AU - Kvetňanský, R.. PY - 1987/10/20. Y1 - 1987/10/20. N2 - A period of 1 or 24 h of cold stress (5 °C) resulted in a significant decrease of acetylcholine (ACh) concentration in the hypothalamus and hippocampus in rats. In the hippocampus the activity of the choline acetyltransferase (ChAT) was significantly increased after 24 h and that of acetylcholinesterase (AChE) after 1 and 24 h exposure to cold, whereas in the hypothalamus, AChE activity was found to be decreased, albeit only after 24 h exposure. Separate investigation of the dorsal and ventral hippocampus under 24 h of cold revealed that the ACh decreased in the dorsal hippocampus only, where no change in ChAT activity was observed. On the other hand, ACh showed no change in the ventral hippocampus where andincrease of ChAT activity was found. Forced swimming for 20 min also induced a ...
"Acetylcholinesterase". Proteopedia. "Hemoglobin". Proteopedia. "Photosystem II". Proteopedia. Luiggi C (September 2010). "Web ... as well as pages that are more descriptive of protein structures in general such as acetylcholinesterase, hemoglobin, and the ...
Leuzinger W, Baker AL, Cauvin E (1968). "Acetylcholinesterase. II. Crystallization, absorption spectra, isoionic point". Proc. ...
Acetylcholinesterase (AChE) inhibitors. AChE is an enzyme associated with nerve synapses that it's designed to regulate nerve ... see Acetylcholinesterase inhibitors). Irritants. These are chemicals that cause an inflammatory effect on living tissue by ...
MSH6 Endplate acetylcholinesterase deficiency; 603034; COLQ Enhanced S-cone syndrome; 268100; NR2E3 Enlarged vestibular ...
In a study it has also been found to weakly inhibit acetylcholinesterase in rat brain (striatum) homogenates. Fung M, Thornton ... Contreras JM, Rival YM, Chayer S, Bourguignon JJ, Wermuth CG (February 1999). "Aminopyridazines as acetylcholinesterase ...
English, Brett A.; Webster, Andrew A. (2012). "Acetylcholinesterase and its Inhibitors". Primer on the Autonomic Nervous System ... This group of inhibitors is divided into two subgroups, acetylcholinesterase inhibitors (AChEIs) and butyrylcholinesterase ... Paraoxon and rivastigmine are both acetylcholinesterase inhibitors and butyrylcholinesterase inhibitors. In 2015, the United ... "Acetylcholinesterase Inhibitors: Pharmacology and Toxicology". Current Neuropharmacology. Bentham Science Publishers Ltd. 11 (3 ...
Acetylcholinesterase inhibitor Weise, C; Kreienkamp, HJ; Raba, R; Pedak, A; Aaviksaar, A; Hucho, F (December 1990). "Anionic ... N,N-Dimethyl-2-chloro-2-phenylethylamine is chemical compound that irreversibly inhibits the acetylcholinesterase. This ... "Anionic subsites of the catalytic center of acetylcholinesterase from Torpedo and from cobra venom". Proceedings of the ... DPA binds to the anionic site of acetylcholinesterase, where it alkylates and irreversibly inhibits the enzyme. ...
Singh, J; Kour, K; Jayaram, MB (January 2012). "Acetylcholinesterase inhibitors for schizophrenia". Cochrane Database of ...
Acetylcholinesterase (AChE) is an enzyme found in animals, from insects to humans. It is essential to nerve cell function ... Other artificial enzyme inhibitors block acetylcholinesterase, an enzyme which breaks down acetylcholine, and are used as nerve ... Hostettmann K, Borloz A, Urbain A, Marston A (2006). "Natural Product Inhibitors of Acetylcholinesterase". Current Organic ... The organophosphate pesticides such as malathion, parathion, and chlorpyrifos irreversibly inhibit acetylcholinesterase. The ...
"Acetylcholinesterase Inhibitors: Pharmacology and Toxicology". Current Neuropharmacology. 11 (3): 315-335. doi:10.2174/ ...
Other carbamate based acetylcholinesterase inhibitors are known with even higher toxicity to humans, and some such as T-1123 ... Besides inhibiting human acetylcholinesterase (although to a lesser degree than the insect enzyme), carbamate insecticides also ... These insecticides kill insects by reversibly inactivating the enzyme acetylcholinesterase (IRAC mode of action 1a). The ... The insect repellent icaridin is a substituted carbamate.[citation needed] While the carbamate acetylcholinesterase inhibitors ...
They affect the nervous system of target pests (and non-target organisms) by disrupting acetylcholinesterase activity, the ... Colović MB, Krstić DZ, Lazarević-Pašti TD, Bondžić AM, Vasić VM (May 2013). "Acetylcholinesterase inhibitors: pharmacology and ... Studies show that farm workers in Ethiopia, Kenya, and Zimbabwe have decreased concentrations of plasma acetylcholinesterase, ... For example, many studies investigating exposure to pesticides often involve the quantification of the acetylcholinesterase ...
... is an acetylcholinesterase inhibitor isolated from Corydalis yanhusuo. Xiao, Hai-Tao; Peng, Jiao; Liang, Yan; Yang, ... Jie; Bai, Xue; Hao, Xiao-Yan; Yang, Fu-Mei; Sun, Qian-Yun (September 2011). "Acetylcholinesterase inhibitors from Corydalis ...
It also contains the acetylcholinesterase inhibitor corydaline. N-Methyltetrahydroprotoberberines have been isolated from C. ... "Acetylcholinesterase inhibitors from Corydalis yanhusuo". Natural Product Research. Taylor and Francis. 25 (15): 1418-1422. doi ...
... is an acetylcholinesterase inhibitor. It acts by covalently binding to acetylcholinesterase. Diisopropyl- ...
Colović MB, Krstić DZ, Lazarević-Pašti TD, Bondžić AM, Vasić VM (May 2013). "Acetylcholinesterase inhibitors: pharmacology and ... It is lethal because it inhibits acetylcholinesterase. Inhibition causes an overly high accumulation of acetylcholine between ...
... is an acetylcholinesterase inhibitor, a diverse family of chemicals. Upon uptake into the target organism, it binds ... Malathion is an organophosphate insecticide which acts as an acetylcholinesterase inhibitor. In the USSR, it was known as ... Its metabolite malaoxon is 61x more toxic, being a more potent inhibitor of acetylcholinesterase. According to the United ... "Acetylcholinesterase Inhibitors: Pharmacology and Toxicology". Current Neuropharmacology. 11 (3): 315-335. doi:10.2174/ ...
VX is an acetylcholinesterase inhibitor. It works by blocking the function of acetylcholinesterase (AChE). Normally, when a ... The reaction products of acetylcholinesterase with VX before and after the "aging" reaction were solved near atomic resolution ... of acetylcholinesterase. VX has a very high "on-rate" to react with the target enzyme and form a stable P-O-C bond ( ... "Reaction Products of Acetylcholinesterase and VX Reveal a Mobile Histidine in the Catalytic Triad". Journal of the American ...
... by inhibiting acetylcholinesterase (AChE). The function of acetylcholinesterase is to break down the neurotransmitter ... Organophosphorus compounds inhibit acetylcholinesterase by forming a covalent bond between the compound and the active site of ... By inhibiting acetylcholinesterase, acetylcholine accumulates in the synaptic cleft, reaching toxic levels. Loss of AChE ... Colović MB, Krstić DZ, Lazarević-Pašti TD, Bondžić AM, Vasić VM (May 2013). "Acetylcholinesterase inhibitors: pharmacology and ...
Physostigmine is an acetylcholinesterase inhibitor; it is a drug that inhibits the breakdown of the inhibitory neurotransmitter ... 0.6 words when participants were given the acetylcholinesterase inhibitor. Conversely, neither speed nor accuracy declined in ...
This leads to the formation of an enzyme-sorption complex with the anionic portion of the acetylcholinesterase located on the ... Studies on the hydrochloride of lupinine have shown it to be a reversible inhibitor of acetylcholinesterases. Lupinine, a ... At physiological pH, the amine of lupinine is protonated which leads to ion-ion interaction with the acetylcholinesterase ... Studies have shown that lupinine hydrochloride is a mildly toxic acetylcholinesterase inhibitor and that lupinine has an ...
Acetylcholinesterase inhibition in plasma happened at a dose of 100 mg/kg/day. For short-term inhalation, a study was done with ... The results showed a NOAEL of 0.025 mg/kg/day and the acetylcholinesterase inhibition in plasma occurred at a dose of 0.075 mg/ ... It is used as an insecticide and nematicide and it is an acetylcholinesterase inhibitor. Ethoprop can be synthesised by ... Another target of ethoprophos is erythrocyte acetylcholinesterase. The only known location of this enzyme is on the outside of ...
AChE (acetylcholinesterase) inhibitors or anti-cholinesterases inhibit the enzyme cholinesterase from breaking down ACh, ... Acetylcholinesterase and butyrylcholinesterase inhibitory compounds from Chelidonium majus (Papaveraceae). ... Journal of Molecular Structure, 734(1-3), 1-6. Colovic, M. B. (2013). Acetylcholinesterase Inhibitors: Pharmacology and ... Chelidonine is an isolate of Papaveraceae with acetylcholinesterase and butyrylcholinesterase inhibitory activity. Chelidonine ...
It inhibits acetylcholinesterase and butyrylcholinesterase. Phorate is most commonly applied in granular form. It is non- ...
Acetylcholinesterase inhibitors are currently prescribed to those with neurodegenerative disorders, as research suggests that ... dos Santos, Thaiane Coelho; Gomes, Thaís Mota (2018). "Naturally Occurring Acetylcholinesterase Inhibitors and Their Potential ... Čolović, Mirjana B; Krstić, Danijela Z (May 2013). "Acetylcholinesterase Inhibitors: Pharmacology and Toxicology". Current ... researchers found that these compounds exhibited high levels of acetylcholinesterase inhibitory activity. Being inhibitors of ...
inhibitor of acetylcholinesterase Quinidine antiarrhythmic Quinine antipyretic, antimalarial Reserpine antihypertensive ...
It is a reversible inhibitor of acetylcholinesterase, the enzyme responsible for the breakdown of acetylcholine in the synaptic ... Physostigmine's poor tolerability led to it being abandoned in favor of later acetylcholinesterase inhibitors, three of which ... Its mechanism is to prevent the hydrolysis of acetylcholine by acetylcholinesterase at the transmitted sites of acetylcholine. ... Mehta M, Adem A, Sabbagh M (2012). "New acetylcholinesterase inhibitors for Alzheimer's disease". International Journal of ...
Physostigmine is a reversible acetylcholinesterase inhibitor. Plants and fungi that contain indole alkaloids have a long ... Physostigmine - an inhibitor of acetylcholinesterase - and its synthetic analogs are used in the treatment of glaucoma, ...
Golomb BA (March 2008). "Acetylcholinesterase inhibitors and Gulf War illnesses". Proc. Natl. Acad. Sci. U.S.A. 105 (11): 4295- ...
... also affects the cholinergic system where it is a moderate inhibitor of the enzyme acetylcholinesterase. Caffeine from ... Karadsheh, Naif; Kussie, Paul; Linthicum, D.Scott (March 1991). "Inhibition of acetylcholinesterase by caffeine, anabasine, ... Pohanka, Miroslav; Dobes, Petr (8 May 2013). "Caffeine Inhibits Acetylcholinesterase, But Not Butyrylcholinesterase". ...
An acetylcholinesterase inhibitor (often abbreviated AChEI) or anti-cholinesterase is a chemical or a drug that inhibits the ... Comparison of reversible acetylcholinesterase inhibitors Inhibitor Duration Main site of action Clinical use Adverse effects ... Acetylcholinesterase+inhibitors at the US National Library of Medicine Medical Subject Headings (MeSH) ... Wang, BS; Wang, H; Wei, ZH; Song, YY; Zhang, L; Chen, HZ (2009). "Efficacy and safety of natural acetylcholinesterase inhibitor ...
In an in vitro system, activity of the commercial enzyme or of highly purified acetylcholinesterase was inhibited by 70-82 per ... A rabbit antiserum against commercially available Electrophorus electricus acetylcholinesterase has been prepared. Five ... ANTIBODIES TO ACETYLCHOLINESTERASE. R. Michael Williams. PNAS April 1, 1969 62 (4) 1175-1180; https://doi.org/10.1073/pnas.62.4 ... demonstrated by the absence of serological cross reactions or enzyme inhibition with bovine erythrocyte acetylcholinesterase or ...
In mammals, acetylcholinesterase is encoded by a single AChE gene while some invertebrates have multiple acetylcholinesterase ... inhibitors AChE bivalent inhibitors Acetylcholinesterase: A gorge-ous enzyme-PDBe Acetylcholinesterase-RCSB PDB Human ACHE ... and secretion of recombinant human acetylcholinesterase. Expression of acetylcholinesterase Cys-580----Ala mutant". J. Biol. ... "Entrez Gene: ACHE acetylcholinesterase (Yt blood group)". Dori A, Ifergane G, Saar-Levy T, Bersudsky M, Mor I, Soreq H, Wirguin ...
Acetylcholinesterase inhibitors (AChEIs) also often called cholinesterase inhibitors, inhibit the enzyme acetylcholinesterase ... Acetylcholinesterase inhibitors: Occur naturally as venoms and poisons (e.g onchidal) Are used as weapons (nerve agents) Are ... Acetylcholinesterase inhibitors are one of two types of cholinesterase inhibitors; the other being butyryl-cholinesterase ... Wang BS, Wang H, Wei ZH, Song YY, Zhang L, Chen HZ (April 2009). "Efficacy and safety of natural acetylcholinesterase inhibitor ...
acetylcholinesterase synonyms, acetylcholinesterase pronunciation, acetylcholinesterase translation, English dictionary ... definition of acetylcholinesterase. n. An enzyme in the blood and in certain tissues that catalyzes the hydrolysis of ... Related to acetylcholinesterase: Acetylcholinesterase inhibitors. a·ce·tyl·cho·li·nes·ter·ase. (ə-sēt′l-kō′lə-nĕs′tə-rās′, -rāz ... acetylcholinesterase. Also found in: Thesaurus, Medical, Legal, Acronyms, Encyclopedia, Wikipedia. ...
Acetylcholinesterase (AChE) is histochemically demonstrable in capillary basement membranes of brain regions that contain ... Acetylcholinesterase (AChE) is histochemically demonstrable in capillary basement membranes of brain regions that contain ... AChE Activity Alzheimer Brain Sucrose Density Gradient Acetylcholinesterase Activity Sedimentation Coefficient These keywords ... Kreutzberg, G. W., Tóth L., and Kaiya, H., 1975, Acetylcholinesterase as a marker for dendritic transport and dendritic ...
Inhibition of mammalian acetylcholinesterase by phenylmethanesulfonyl fluoride.. Alid G, Orrego FG.. PMID:. 5013045. DOI:. ...
Various types of acetylcholinesterase (AChE) subunits are characterized by specific C-terminal peptides. In Torpedoand mammals ... Various types of acetylcholinesterase (AChE) subunits are characterized by specific C-terminal peptides. In Torpedo and mammals ... Bon S., Coussen F., Massoulié J. (1998) The Glycolipid-Addition Signal of Acetylcholinesterase. In: Doctor B.P., Taylor P., ... The Glycolipid-Addition Signal of Acetylcholinesterase. Cellular Compartmentation, Cleavage, GPI Addition and Secretion ...
... , Acetylcholinesterase Inhibitor, Cholinesterase Inhibitor, Anticholinesterase. ... Central Acetylcholinesterase Inhibitor. Aka: Central Acetylcholinesterase Inhibitor, Acetylcholinesterase Inhibitor, ... Central cholinesterase inhib, Central acetylcholinesterase inhibitor, Central acetylcholinesterase inhibitor (product), Central ... acetylcholinesterase inhibitor (substance). Spanish. inhibidor central de la acetilcolinesterasa (producto), inhibidor central ...
... acetylcholinesterase OTTHUMP00000211347 translation, English dictionary definition of acetylcholinesterase OTTHUMP00000211347. ... redirected from acetylcholinesterase OTTHUMP00000211347). Also found in: Thesaurus, Medical, Encyclopedia. ache. (āk). intr.v. ... Acetylcholinesterase OTTHUMP00000211347 - definition of acetylcholinesterase OTTHUMP00000211347 by The Free Dictionary https:// ... Define acetylcholinesterase OTTHUMP00000211347. acetylcholinesterase OTTHUMP00000211347 synonyms, acetylcholinesterase ...
Unbalanced acetylcholinesterase activity in larynx squamous cell carcinoma.. Castillo-González AC1, Pelegrín-Hernández JP2, ... pieces of larynx squamous cell carcinoma and adjacent non-cancerous tissue were compared in terms of their acetylcholinesterase ...
ACETYLCHOLINESTERASE. A. 537. Tetronarce californica. Mutation(s): 0 Gene Names: ache. EC: 3.1.1.7. ... Static Laue diffraction studies on acetylcholinesterase.. Ravelli, R.B., Raves, M.L., Ren, Z., Bourgeois, D., Roth, M., Kroon, ... Acetylcholinesterase (AChE) is one of natures fastest enzymes, despite the fact that its three-dimensional structure reveals ... Acetylcholinesterase (AChE) is one of natures fastest enzymes, despite the fact that its three-dimensional structure reveals ...
An acetylcholinesterase inhibitor or anti-cholinesterase is a chemical that inhibits the cholinesterase enzyme ... Comparison of reversible acetylcholinesterase inhibitors Inhibitor Duration[1] Main site of action[1] Clinical use[1] Adverse ... An acetylcholinesterase inhibitor or anti-cholinesterase is a chemical that inhibits the cholinesterase enzyme from breaking ... It uses material from the Wikipedia article "Acetylcholinesterase_inhibitor". A list of authors is available in Wikipedia. ...
Mouse monoclonal Acetylcholinesterase antibody [4E11] validated for WB, ELISA and tested in Human. Referenced in 1 publication ... Monoclonal antibodies against a C-terminal peptide of human brain acetylcholinesterase distinguish between erythrocyte and ... Synthetic peptide corresponding to Human Acetylcholinesterase aa 574-583.. Sequence: TDTLDEA ERQ ... brain acetylcholinesterases.. Clin Chem 42:19-23 (1996). Read more (PubMed: 8565226) » ...
Acetylcholinesterase. A. 581. Drosophila melanogaster. Mutation(s): 0 Gene Names: Ace, CG17907. EC: 3.1.1.7. ... Here, we present updated crystal structures of Drosophila melanogaster acetylcholinesterase ( Dm AChE) originally published in ... Three-dimensional structures of Drosophila melanogaster acetylcholinesterase and of its complexes with two potent inhibitors.. ...
Autorité publique indépendante à caractère scientifique, la Haute Autorité de santé (HAS) vise à développer la qualité dans le champ sanitaire, social et médico-social, au bénéfice des personnes. Elle travaille aux côtés des pouvoirs publics dont elle éclaire la décision, avec les professionnels pour optimiser leurs pratiques et organisations, et au bénéfice des usagers dont elle renforce la capacité à faire des choix., Insufficient clinical benefit: these medicinal products no longer have a role in the treatment of Alzheimers disease
The present invention relates to organophosphate-inhibited acetylcholinesterase (AChE) reactivators with central nervous system ... The present invention relates to organophosphate-inhibited acetylcholinesterase (AChE) reactivators with central nervous system ...
... with Reflex to Acetylcholinesterase,ARUP Laboratories is a national reference laboratory and a worldwide leader in innovative ...
References for Abcams Acetylcholinesterase peptide (601-614) (ab45700). Please let us know if you have used this product in ...
Alpha-Fetoprotein and Acetylcholinesterase. Estimation of maternal serum AFP has been used since the late 1970s. Blood samples ... as well as for the presence of acetylcholinesterase, a nerve-specific enzyme. Myelomeningocele can be detected in 99% of ...
AcetylcholinesteraseAdd BLAST. 583. Amino acid modifications. Feature key. Position(s). DescriptionActions. Graphical view. ... acetylcholinesterase activity Source: RGDInferred from direct assayi*. "Cholinesterase activity in the hypoglossal nucleus of ... "Differential localization of acetylcholinesterase in neuronal and non-neuronal cells.". Thullbery M.D., Cox H.D., Schule T., ... "Differential localization of acetylcholinesterase in neuronal and non-neuronal cells.". Thullbery M.D., Cox H.D., Schule T., ...
Adverse Pharmacological Actions : Acetylcholinesterase inhibitor (xenobiotic) : CK(6) : AC(3), Aquacidal : CK(18) : AC(9), ... The toxic effect of sublethal concentrations (1, 17.5 and 35 mg L(-1)) of pure glyphosate was evaluated on acetylcholinesterase ...
Acetylcholinesterase inhibitor treatment for myasthenia gravis. Review question We reviewed the evidence about the effect of ... An enzyme called acetylcholinesterase breaks down acetylcholine. Some drugs that are used to treat myasthenia gravis act on ... The response to acetylcholinesterase inhibitors in observational studies is so clear that a randomised controlled trial ... The trial compared neostigmine (an acetylcholinesterase inhibitor) given via the nose, with placebo. Each treatment was given ...
Stabilization of Torpedo californica acetylcholinesterase by reversible inhibitors.. [Lev Weiner, Valery L Shnyrov, Leonid ... Elucidation of the 3D structures of complexes of Torpedo californica acetylcholinesterase with a repertoire of reversible ... The effects of these three categories of reversible inhibitors on the stability of Torpedo californica acetylcholinesterase ... Stabilization of Torpedo californica acetylcholinesterase by both divalent cations and chemical chaperones was earlier shown to ...
We report here the in vitro selection of DNA aptamers for electric eel acetylcholinesterase (AChE). One selected aptamer ... High Efficiency Acetylcholinesterase Immobilization on DNA Aptamer Modified Surfaces. Orada Chumphukam, Thao T. Le and Anthony ... We report here the in vitro selection of DNA aptamers for electric eel acetylcholinesterase (AChE). One selected aptamer ... "High Efficiency Acetylcholinesterase Immobilization on DNA Aptamer Modified Surfaces." Molecules 19, no. 4: 4986-4996. ...
The free-radical scavenging, ferric reducing, and acetylcholinesterase inhibition effect of the flesh were higher as compared ... Phytochemicals Content, Antioxidant Activity and Acetylcholinesterase Inhibition Properties of Indigenous Garcinia parvifolia ... and antioxidant and acetylcholinesterase inhibition activity of the flesh and peel of G. parvifolia. All samples were freeze- ...
Phytochemicals Content, Antioxidant Activity and Acetylcholinesterase Inhibition Properties of Indigenous Garcinia parvifolia ... Antioxidant Activity and Acetylcholinesterase Inhibition Properties of Indigenous Garcinia parvifolia Fruit," BioMed Research ...
This reaction is called aging and produces an anionic phosphyl adduct with acetylcholinesterase that is refractory to ... Consequently, the evolutionary mechanisms that have led to transition state stabilization in acetylcholinesterase catalysis are ... discussed herein, as are the challenges that they present to reactivation of aged acetylcholinesterase. ... Organophosphorus agents are potent inhibitors of acetylcholinesterase. Inhibition involves successive chemical events. The ...
Browse our Acetylcholinesterase/ACHE product catalog backed by our Guarantee+. ... PTMs for Acetylcholinesterase/ACHE. Learn more about PTMs related to Acetylcholinesterase/ACHE.. Phosphorylation. Cleavage. ... Diseases related to Acetylcholinesterase/ACHE. Discover more about diseases related to Acetylcholinesterase/ACHE.. Alzheimers ... Bioinformatics Tool for Acetylcholinesterase/ACHE. Discover related pathways, diseases and genes to Acetylcholinesterase/ACHE. ...
Shop a large selection of products and learn more about Acetylcholinesterase/ACHE Mouse anti-Human, Bovine, Janelia Fluor 646, ... acetylcholinesterase, acetylcholinesterase (Yt blood group), AChE, apoptosis-related acetylcholinesterase, ARACHE, EC 3.1.1, EC ... Acetylcholinesterase/ACHE Monoclonal antibody specifically detects Acetylcholinesterase/ACHE in Human, Bovine samples. It is ... Acetylcholinesterase/ACHE Mouse anti-Human, Bovine, Janelia Fluor 646, Clone: 400000000000, Novus Biologicals ...
  • Although the etiology of Alzheimer's disease (AD) is not fully understood, nevertheless, inhibition of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) activity has been accepted as an effective treatment/management strategy against mild AD [6, 7]. (thefreedictionary.com)
  • Fingerman, "Inhibition of acetylcholinesterase activity in the central nervous system of the red swamp crayfish, Procambarus clarkii, by mercury, cadmium, and lead," Bulletin of Environmental Contamination and Toxicology, vol. (thefreedictionary.com)
  • The primary mechanism of action for organophosphorus (OP) insecticides involves the inhibition of acetylcholinesterase (AChE) by active oxon metabolites. (cdc.gov)
  • A dynamic combinatorial library composed of interconverting acylhydrazones has been generated and screened towards inhibition of acetylcholinesterase from the electric ray Torpedo marmorata. (diva-portal.org)
  • Inhibition of acetylcholinesterase (AChE) from head of honey bee (Apis mellifera L.) by organophosphate and carbamate insecticides was developed from Ellman reaction and analyzed by spectrophotometer at the wave length of 412 nm. (fao.org)
  • The inhibition of acetylcholinesterase (AChE) by organophosphorus compounds (OPs) causes acute toxicity or death of the intoxicated individual. (ovid.com)
  • Acetylcholinesterase inhibitors (AChEIs) also often called cholinesterase inhibitors, inhibit the enzyme acetylcholinesterase from breaking down the neurotransmitter acetylcholine into choline and acetate, thereby increasing both the level and duration of action of acetylcholine in the central nervous system, autonomic ganglia and neuromuscular junctions, which are rich in acetylcholine receptors. (wikipedia.org)
  • Here, we developed method for assay of neurotoxic pesticides via inhibition of enzyme acetylcholinesterase (AChE) and coloration measuring through an optical fiber. (omicsonline.org)
  • The effects of chlorpyrifos, an organophosphorus insecticide, were examined on the activity of the nervous system enzyme acetylcholinesterase (AChE) in the threeridge mussel Amblema plicata in a 24-day laboratory test. (usgs.gov)
  • An acetylcholinesterase inhibitor (often abbreviated AChEI ) or anti-cholinesterase is a chemical or a drug that inhibits the acetylcholinesterase enzyme from breaking down acetylcholine , thereby increasing both the level and duration of action of the neurotransmitter acetylcholine. (wikipedia.org)
  • An acetylcholinesterase inhibitor or anti-cholinesterase is a chemical that inhibits the cholinesterase enzyme from breaking down acetylcholine , so increasing both the level and duration of action of the neurotransmitter acetylcholine. (bionity.com)
  • An enzyme called acetylcholinesterase breaks down acetylcholine. (cochrane.org)
  • Some drugs that are used to treat myasthenia gravis act on acetylcholinesterase to stop the breakdown of acetylcholine. (cochrane.org)
  • These acetylcholinesterase inhibitors increase the amount of acetylcholine available and so help muscle activation and contraction. (cochrane.org)
  • Acetylcholinesterase hydrolyzes the neurotransmitter, acetylcholine at neuromuscular junctions and brain cholinergic synapses, and thus terminates signal transmission. (thermofisher.com)
  • Acetylcholinesterase (AChE) is an enzyme that breaks down and deactivates acetylcholine (ACh) after it is released by terminal buttons. (alleydog.com)
  • Acetylcholinesterase, or ACHE, hydrolyzes the neurotransmitter, acetylcholine at neuromuscular junctions and brain cholinergic synapses, and thus terminates signal transmission. (novusbio.com)
  • Acetylcholinesterase (AChE) catalyses the hydrolysis of the neurotransmitter acetylcholine and it has been implicated in several non-cholinergic actions, including neurite outgrowth and amyloid formation. (ovid.com)
  • Currently, the most widely prescribed treatment for AD is acetylcholinesterase inhibitor medications, which work by partially blocking the degradation of acetylcholine in the synapse and enabling more of the neurotransmitter to reach and activate cholinergic receptors. (eurekaselect.com)
  • Acetylcholinesterase inhibitors increase parasympathetic neurotransmission through inhibition of the enzymatic breakdown of acetylcholine at cholinergic receptor sites in the autonomic nervous system. (bmj.com)
  • The concentration dependence of activity towards the natural substrate acetylcholine is almost identical for the two enzymes, whereas substrate inhibition of chicken acetylcholinesterase is somewhat weaker than that of the Torpedo enzyme. (aspetjournals.org)
  • Acetylcholinesterase (AChE) is an essential enzyme with an evolutionary conserved function: to terminate nerve signaling by rapid hydrolysis of the neurotransmitter acetylcholine. (diva-portal.org)
  • Acetylcholinesterase Inhibitor Screening Kit (Colorimetric) from BIOVISION, INC. (linscottsdirectory.com)
  • Search, find, compare suppliers for Acetylcholinesterase Inhibitor Screening Kit (Colorimetric) products. (linscottsdirectory.com)
  • In this study, we have employed in silico methodology combining double pharmacophore based screening, molecular docking, and ADME/T filtering to identify dual binding site acetylcholinesterase inhibitors that can preferentially inhibit acetylcholinesterase and simultaneously inhibit the butyrylcholinesterase also but in the lesser extent than acetylcholinesterase. (amrita.edu)
  • In an in vitro system, activity of the commercial enzyme or of highly purified acetylcholinesterase was inhibited by 70-82 per cent after incubation with antiserum. (pnas.org)
  • Acetylcholinesterase (AChE) is histochemically demonstrable in capillary basement membranes of brain regions that contain relatively high AChE activity in their neuronal elements (Kreutzberg et al. (springer.com)
  • Unbalanced acetylcholinesterase activity in larynx squamous cell carcinoma. (nih.gov)
  • Fifty paired pieces of larynx squamous cell carcinoma and adjacent non-cancerous tissue were compared in terms of their acetylcholinesterase activity (AChE). (nih.gov)
  • Influence of estrogen on acetylcholinesterase activity in primary. (ingentaconnect.com)
  • To estimate the influence of estrogen on the functional development of the central nervous system during the neonatal period, several doses of estradiol-17β (E 2 ) were treated to cultured cells from the cerebral cortex of neonatal rats and the acetylcholinesterase (AChE) activity was examined. (ingentaconnect.com)
  • The toxic effect of sublethal concentrations (1, 17.5 and 35 mg L(-1)) of pure glyphosate was evaluated on acetylcholinesterase (AChE) activity in the fish species, Cnesterodon decemmaculatus. (greenmedinfo.com)
  • Acetylcholinesterase activity and neurodevelopment in boys and girls. (sigmaaldrich.com)
  • The present study was conducted to determine the phytochemicals content (total phenolic, flavonoid, anthocyanin, and carotenoid content) and antioxidant and acetylcholinesterase inhibition activity of the flesh and peel of G. parvifolia . (hindawi.com)
  • Acetylcholinesterase/ACHE Activity. (novusbio.com)
  • Incubation of synaptosomal plasma membranes (SPM) with liposomes of phosphatidylserine (PS), phosphatidylinositol (PIN) or phosphatidylglycerol (PGL), led to an increase of acetylcholinesterase (AchE) activity at concentrations of 0.1-1 mumol phospholipids per mg SPM protein. (nih.gov)
  • They found that "TP administration dramatically inhibited AChE [acetylcholinesterase] activity (71% inhibition) as compared to the control. (life-enhancement.com)
  • What compounds increase acetylcholinesterase activity? (healthtap.com)
  • A drug to reduce the activity of acetylcholinesterase. (healthtap.com)
  • Result Among the numerous endophytic fungi, we identified two strains, L10Q37 and LQ2F02, that have anti-acetylcholinesterase activity, but the active compound was not huperzine A. The aim of this study was to investigate the anti-acetylcholinesterase activity of secondary metabolites isolated from the endophytic fungi of Huperzia serrata . (scielo.cl)
  • In conclusion, endophytic fungal strains were found in H. serrata that had the same anti-acetylcholinesterase activity. (scielo.cl)
  • After tested anti acetylcholinesterase activity, S5 has the best activity. (scielo.cl)
  • Other compounds' anti acetylcholinesterase activity was not better compared with huperzine A. (scielo.cl)
  • In the present study, the effects during 1.5, 6 and 9-month periods of chronic ingestion of uranyl nitrate (UN) in drinking water (40 mg of uranium per litre) on cholinergic acetylcholinesterase (AChE) activity and on dopaminergic and serotoninergicmetabolisms were investigated in several areas of male Sprague Dawley rat brains. (irsn.fr)
  • 1. The erythrocyte membrane acetylcholinesterase activity is significantly (P less than 0.001) decreased in insulin-dependent diabetes mellitus. (portlandpress.com)
  • Approximately 150/o of the total acetylcholinesterase (AChE) activity of pig brain cortex can be extracted in dilute buffer solution and the properties of this »soluble« form of the enzyme have been compared with the membrane bound enzyme which was brought into solution by extraction with 1-0/o Triton X-100 or 1 mM EDTA. (srce.hr)
  • 29 participants with clinical AD and 35 with non-AD diagnoses underwent positron emission tomography (PET) with the amyloid ligand [11C] PIB and plasma measurements of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) activity. (pubmedcentralcanada.ca)
  • Similar results were found for analyses with the actual level of acetylcholinesterase activity. (bmj.com)
  • CONCLUSION The results suggest the presence of a relation between exposure and acetylcholinesterase inhibition, acetylcholinesterase activity, and respiratory, eye, and central nervous system symptoms. (bmj.com)
  • The equilibrium constant for the reaction of diethylphosphofluoridate with acetylcholinesterase was evaluated by measuring the second-order rate constant for the inhibition of the enzyme and the second-order rate constant for the restoration of enzyme activity, starting with inhibited enzyme and using fluoride as a reactivator. (aspetjournals.org)
  • The synthesis and the biological activity of compounds 5-40 as inhibitors of acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE), as well as modulators of voltage-dependent Ca(2+) channels and nicotinic receptors, are described. (ub.edu)
  • s ( 1961 ) method was followed to estimate the activity of acetylcholinesterase of insects. (bioone.org)
  • Crude spider venom also significantly inhibited the estimated activity of acetylcholinesterase in M . domestica and Ae . (bioone.org)
  • It is concluded from the study that both plant extracts and spider venom inhibited the activity of acetylcholinesterase in M . domestica and Ae . (bioone.org)
  • The activity of acetylcholinesterase (AChE) and the density of muscarinic cholinergic binding receptors (mCBR) were measured in brains from normal Japanese quail ( Coturnix coturnix japonica ) and from quail after lethal intoxication with diazinon. (bioone.org)
  • The acetylcholinesterase activity of sympathetic ganglia (superior cervical, stellate, thoracic chain, superior mesenteric, celiac and cardiac) from immunosympathectomized and control rats was visualized by the histochemical method of Koelle. (aspetjournals.org)
  • Contrary to cat sympathetic ganglia, the cells with marked and moderate acetylcholinesterase activity predominate in the sympathetic ganglia of control rats. (aspetjournals.org)
  • In the various sympathetic ganglia studied in this investigation, cells with slight acetylcholinesterase activity made up only 3.8 to 10.3% of the total cell populations. (aspetjournals.org)
  • No predominant survival of cells with marked acetylcholinesterase activity took place after immunosympathectomy. (aspetjournals.org)
  • Nerve growth factor antiserum treatment destroyed cells with marked, moderate and slight acetylcholinesterase activity, and a small number of cells of each type persisted. (aspetjournals.org)
  • These experimental observations do not support our previous postulate that the small percentage of cells surviving antiserum treatment are those with marked acetylcholinesterase activity, which may be considered the cholinergic sympathetic cells. (aspetjournals.org)
  • However since these medications have limited effectiveness, alternate treatments that focus on augmenting the activity of the receptors themselves, independent of acetylcholinesterase inhibition, are being explored. (eurekaselect.com)
  • BioVision's Acetylcholinesterase Inhibitor Screening Kit can be used to screen for potential inhibitors of AChE activity. (linscottsdirectory.com)
  • The normal acetylcholinesterase activity from bee head was 33,645+-3,008 mUnit/g(protein) or 88.23 mUnit/bee head. (fao.org)
  • Firstly, they are inefficient in the restoration of brain acetylcholinesterase (AChE) activity due to a hard blood-brain barrier penetration. (eurekaselect.com)
  • Some embryos of Ciona intestinalis which were permanently cleavage-arrested with cytochalasin B at the 1-cell, 4-cell, or 8-cell stages produced, after 12 or 16 h of development time (18 °C), a level of muscle acetylcholinesterase activity equal to that found in normal early and later larval stage embryos of the same age. (biologists.org)
  • Antibody specificity was demonstrated by the absence of serological cross reactions or enzyme inhibition with bovine erythrocyte acetylcholinesterase or horse serum cholinesterase. (pnas.org)
  • the other being butyryl-cholinesterase inhibitors.Acetylcholinesterase is the primary member of the cholinesterase enzyme family. (wikipedia.org)
  • Walujo B. Prijono and Frederick A. Leighton "Parallel Measurement of Brain Acetylcholinesterase and the Muscarinic Cholinergic Receptor in the Diagnosis of Acute, Lethal Poisoning by Anti-Cholinesterase Pesticides," Journal of Wildlife Diseases 27(1), 110-115, (1 January 1991). (bioone.org)
  • This chapter discusses toxins from Mamba venoms that inhibit acetylcholinesterase. (strath.ac.uk)
  • In our quest to find new inhibitors able to inhibit acetylcholinesterase (AChE) and, at the same time, to protect neurons from beta amyloid toxicity, i.e., inhibitors interacting with the catalytic anionic subsite as well as with the peripherical anionic site of AChE, a virtual screening of the Centre d'Etudes et de Recherche sur le Mdicament de Normandie (CERMN) chemical library was carried out. (chemaxon.com)
  • C-terminal 10 residues (aa 574-583) of human brain acetylcholinesterase. (abcam.com)
  • Monoclonal antibodies against a C-terminal peptide of human brain acetylcholinesterase distinguish between erythrocyte and brain acetylcholinesterases. (abcam.com)
  • Acetylcholinesterase/ACHE Monoclonal antibody specifically detects Acetylcholinesterase/ACHE in Human, Bovine samples. (fishersci.com)
  • C-terminal 10 residues of brain acetylcholinesterase (human and bovine), absent from the erythrocyte enzyme. (fishersci.com)
  • The bovine acetylcholinesterase (BoAChE) gene was cloned from genomic DNA and its structure was determined. (biochemj.org)
  • These compounds are moderate acetylcholinesterase and butyrylcholinesterase inhibitors, the BuChE/AChE selectivity of the most active molecules ranges from 10.0 (compound 29) to 76.9 (compound 16). (ub.edu)
  • A series of berberine-thiophenyl hybrids were designed, synthesised, and evaluated as inhibitors of acetylcholinesterase (AChE), butyrylcholinesterase (BuChE) and β-amyloid (Aβ) aggregation and as antioxidants. (unboundmedicine.com)
  • The MA3-042 antigen is purified human cerebellar acetylcholinesterase. (thermofisher.com)
  • The present invention relates to organophosphate-inhibited acetylcholinesterase (AChE) reactivators with central nervous system (CNS) bioavailability and their associated methods of preparation including their use for treatment of exposure to AChE inhibitors such as an organophosphate (OP) insecticides and nerve agents. (swri.org)
  • The main goal of this study is the application of systematic strategies of characterization in order to optimize the biocomposite composition based on graphite-epoxy that incorporates acetylcholinesterase (AChE) on the matrix. (thefreedictionary.com)
  • Chemical and pharmacological characterization of galanthamine, and acetylcholinesterase inhibitor , and its derivates. (thefreedictionary.com)
  • Patients with a low UPSIT score who were assigned to donepezil showed a mean 10.4point improvement on the Selective Reminding Test, while those with an UPSIT score of 30 or more showed a 2.7-point improvement in response to the acetylcholinesterase inhibitor. (thefreedictionary.com)
  • In a study of 202 patients, those who continued treatment with the acetylcholinesterase inhibitor donepezil had significant improvements in their scores on the Neuropsychiatric Inventory, even when their scores on the Mini-Mental State Examination (MMSE) were stagnant or had declined. (thefreedictionary.com)
  • Sustained treatment with the acetylcholinesterase inhibitor donepezil significantly reduced health care costs for patients with Alzheimer's disease in a Medicare-managed care organization plan, Jerrold W. (thefreedictionary.com)
  • The double-blind, randomized trial is the first to examine the effect of the Nmethyl-D-aspartate (NMDA) receptor antagonist memantine and the acetylcholinesterase inhibitor donepezil against donepezil monotherapy, said Dr. (thefreedictionary.com)
  • The major form of acetylcholinesterase found in brain, muscle and other tissues is the hydrophilic species, which forms disulfide-linked oligomers with collagenous, or lipid-containing structural subunits. (thermofisher.com)
  • Increased latency in the treated animals, i.e., delayed entry into the dark compartment (as compared to nontreated animals) after previous shock, is a measure of the memory-enhancing effects of acetylcholinesterase inhibitors. (life-enhancement.com)
  • To characterise the effects of acetylcholinesterase inhibition with pyridostigmine on parasympathetic tone in patients with chronic heart failure (CHF). (bmj.com)
  • The following product was used in this experiment: Acetylcholinesterase Monoclonal Antibody (HR2) from Thermo Fisher Scientific, catalog # MA3-042, RRID AB_325478. (thermofisher.com)
  • Immunocytochemistry/ Immunofluorescence: Acetylcholinesterase/ACHE Antibody [NB100-1519] - Immunofluorescence analysis of paraformaldehyde fixed U2OS cells, permeabilized with 0.15% Triton. (novusbio.com)
  • Flow Cytometry: Acetylcholinesterase/ACHE Antibody [NB100-1519] - Flow cytometric analysis of paraformaldehyde fixed HeLa cells (blue line), permeabilized with 0.5% Triton. (novusbio.com)
  • This Acetylcholinesterase/ACHE antibody is validated for IHC-FrFl from a verified customer review. (novusbio.com)
  • it is suggested that the absence, in the chicken enzyme, of two aromatic residues, Tyr-70 and Trp-279, that contribute to the peripheral site of Torpedo acetylcholinesterase is responsible for the differential effects of peripheral site ligands on the two enzymes. (aspetjournals.org)
  • This feature makes acetylcholinesterase inhibitors (AChEi) the main class of drugs currently used for the treatment of AD dementia phase, among which galantamine is the only naturally occurring substance. (frontiersin.org)
  • We report here the in vitro selection of DNA aptamers for electric eel acetylcholinesterase (AChE). (mdpi.com)
  • AhR-mediated effects of dioxin on neuronal acetylcholinesterase expression in vitro. (thefreelibrary.com)
  • The June 2004 RCSB PDB Molecule of the Month feature on Acetylcholinesterase by David S. Goodsell is 10.2210/rcsb_pdb/mom_2004_6 . (proteopedia.org)
  • Erythrocyte acetylcholinesterase in Hirschsprung's disease. (bmj.com)
  • The best acetylcholinesterase and butyrylcholinesterase inhibitors pharmacophore hypotheses Hypo1_A and Hypo1_B, with high correlation coefficient of 0.96 and 0.94, respectively, were used as 3D query for screening the Zinc database. (amrita.edu)
  • Tsuji T., Mimori Y., Nakamura S. (1990) Acetylcholinesterase of Cerebral Microvessels Changes in Alzheimer's Disease. (springer.com)
  • A randomized trial evaluating the efficacy and safety of ENA 713 (rivastigmine tartrate), a new acetylcholinesterase inhibitor , in patients with mild to moderately severe Alzheimer's disease. (thefreedictionary.com)
  • Asante R. Kamkwalala and Paul A. Newhouse, "Beyond Acetylcholinesterase Inhibitors: Novel Cholinergic Treatments for Alzheimer's Disease", Current Alzheimer Research (2017) 14: 377. (eurekaselect.com)
  • The dimeric form of Torpedo californica acetylcholinesterase provides a valuable experimental system for studying transitions between native, partially unfolded, and unfolded states since long-lived partially unfolded states can be generated by chemical modification of a nonconserved buried cysteine residue, Cys 231, by denaturing agents, by oxidative stress, and by thermal inactivation. (sigmaaldrich.com)
  • Stabilization of Torpedo californica acetylcholinesterase by reversible inhibitors. (sigmaaldrich.com)
  • The effects of these three categories of reversible inhibitors on the stability of Torpedo californica acetylcholinesterase were investigated using spectroscopic techniques and differential scanning calorimetry. (sigmaaldrich.com)
  • Stabilization of Torpedo californica acetylcholinesterase by both divalent cations and chemical chaperones was earlier shown to be due to a shift in equilibrium between the native state and a partially unfolded state ( Millard et al. (sigmaaldrich.com)
  • Differential effects of "peripheral" site ligands on Torpedo and chicken acetylcholinesterase. (aspetjournals.org)
  • Two bisquaternary ligands, decamethonium and 1,5-bis(4-allydimethylammoniumphenyl)pentan-3-one dibromide, which are believed to bridge the anionic subsite of the active site and the "peripheral" anionic site, are much weaker inhibitors of the chicken enzyme than of Torpedo acetylcholinesterase, whereas the shorter bisquaternary ligand hexamethonium inhibits the two enzymes similarly. (aspetjournals.org)
  • Synthetic peptide corresponding to Human Acetylcholinesterase aa 574-583. (abcam.com)
  • Acetylcholinesterase (AChE) is one of nature's fastest enzymes, despite the fact that its three-dimensional structure reveals its active site to be deeply sequestered within the molecule. (rcsb.org)
  • 34 Acetylcholinesterase (AChE) ELISA Kits from 12 manufacturers are available on www.antibodies-online.com. (antibodies-online.com)
  • acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) has widely been used as biomarkers to evaluate the noxious effects of pesticides i.e. (thefreedictionary.com)
  • The predominant cholinesterases are acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). (pubmedcentralcanada.ca)
  • Acetylcholinesterase inhibitors: Occur naturally as venoms and poisons (e.g onchidal) Are used as weapons (nerve agents) Are used as insecticides (e.g malathion) Are used medicinally: To treat myasthenia gravis. (wikipedia.org)
  • Since many possible reasons exist for false-positive results, a presumptive diagnosis based on maternal serum AFP is confirmed with amniocentesis and assay of the amniotic fluid for AFP, as well as for the presence of acetylcholinesterase, a nerve-specific enzyme. (medscape.com)
  • Acetylcholinesterase (AChE) rapidly hydrolyzes ACh to acetate and choline, thereby inactivating it. (novusbio.com)
  • It is also believed that galantamine may be an acetylcholinesterase inhibitor , as well as an allosteric modulator of nicotinic receptors. (thefreedictionary.com)
  • In a 12-week, double-blind, placebo-controlled, randomized trial, the acetylcholinesterase inhibitor galantamine had an insignificant overall effect on a composite of neuropsychological outcomes among 44 patients who received it, compared with 42 who got placebo. (thefreedictionary.com)
  • Organophosphorous and carbamates kill honeybees through the inactivation of acetylcholinesterase (AChE), thereby interfering with nerve signaling and function. (biomedsearch.com)
  • A new magnetic electrochemical immunoassay has been developed as a tool for biomonitoring exposures to organophosphate (OP) compounds, e.g., insecticides and chemical nerve agents, by directly detecting organophosphorylated acetylcholinesterase (OP-AChE). (cdc.gov)
  • When the acetylcholinesterase (AChE) reaction was performed subsequently to the GIF reaction the following nerve types could be identified: 1. (biomedsearch.com)
  • Point-of-care monitoring of acetylcholinesterase (AChE) is of significant importance for pesticide poisoning and disease diagnosis because it plays a pivotal role in biological nerve conduction systems. (rsc.org)
  • D.T. Plummer, C.A. Reavill i C.H.S. McIntosh, "Properties of the Soluble and Membrane-Bound Forms of Acetylcholinesterase Present in Pig Brain", Croatica Chemica Acta , vol.47, br. (srce.hr)
  • Comparison of chlorpyrifos-oxon and paraoxon acetylcholinesterase inhibition dynamics: potential role of a peripheral binding site. (cdc.gov)
  • Three-dimensional structures of Drosophila melanogaster acetylcholinesterase and of its complexes with two potent inhibitors. (rcsb.org)
  • Organophosphorus agents are potent inhibitors of acetylcholinesterase. (mdpi.com)