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AcetylcholinesteraseCholinesterase InhibitorsButyrylcholinesteraseAcetylthiocholineCholinesterasesCholinesterase ReactivatorsElectrophorusTacrineParaoxonPhysostigmineTorpedoGalantaminePralidoxime CompoundsSarinIsoflurophateThiocholineIndansPseudocholinesteraseEdrophoniumElectric OrganOrganothiophosphorus CompoundsChlorpyrifosInsecticidesPyridostigmine BromideSomanBungarusNeostigmineCarbamatesDichlorvosPhenylcarbamatesOrganophosphatesEchothiophate IodideTetraisopropylpyrophosphamideElapid VenomsOximesEelsOrganophosphate PoisoningMalathionOrganophosphorus CompoundsChemical Warfare AgentsObidoxime ChlorideNeuromuscular JunctionButyrylthiocholineCholine O-AcetyltransferaseAcetylcholineTrichlorfonTrimedoximePropoxurHistocytochemistryInsecticide ResistanceOrganothiophosphatesKineticsParathionMotor EndplateAldicarbAntidotesBrainPiperidinesReceptors, CholinergicCholinergic FibersBenzyl CompoundsPyridinium CompoundsPesticidesMusclesDiazinonBinding SitesErythrocytesNootropic AgentsDimethoateDecamethonium CompoundsAlzheimer DiseasePropidiumDiazonium Compounds
AChEInhibitorsInhibitorInhibitionEnzyme acetylcholinesteraseTherapeutic strategy for the treatmentButyrylcholinesteraseReactivationKineticsPolymerase chain reOrganophosphateTriazolesActivity1997InactivationBindsAcetylthiocholinePrecursorsEnzymes workInsecticidesProteinBoundSubstratesChemical reactionHydrolysisNeuromuscularSubstancesStructuresMoleculeChain reactionsAdverse reactionsMolecularStudyOccurMoleculesSpeciesIrreversibleChronicSynthesisQuantitativeImprovesCompoundsSubstrateCatalyzeReactantsTimeActiveAtomPresentRate
AChE13
  • Ligand binding sites on acetylcholinesterase (AChE) comprise an active center, at the base of a deep and narrow gorge lined by aromatic residues, and a peripheral site at the gorge entry. (nih.gov)
  • These features launched AChE as a reaction vessel for in situ click-chemistry synthesis of high-affinity TZ2PA6 and TZ2PA5 inhibitors, forming a syn-triazole upon cycloaddition within the gorge from alkyne and azide reactants bound at the two sites, respectively. (nih.gov)
  • Acetylcholinesterase (AChE) is an enzyme that catalyzes the breakdown of the neurotransmitter acetylcholine that is essential for cognition and memory. (peerj.com)
  • The cytoarchitecture of nuclei in the diencephalon and the distribution of acetylcholinesterase (AChE) in the diencephalon and optic tectum were analyzed in the longnose gar, Lepisosteus osseus, a non-teleost actinopterygian fish. (karger.com)
  • METHODS: 120 MDMA abusers (MA) and 120 healthy volunteers (HV) were enrolled in an independent sample control design, in which the levels of lipoperoxide (LPO) in plasma and erythrocytes as well as the activities of superoxide dismutase (SOD), catalase (CAT), glutathione peroxidase (GPX) and acetylcholinesterase (AChE) in erythrocytes were determined by spectrophotometric methods. (mdma.net)
  • Acetylcholinesterase (AChE) activity levels can be used as an indicator for AChE inhibition due to pesticide poisoning in bird species. (scielo.br)
  • Organophosphorus pesticides (OPs) are a chemically diverse class of insecticides that inhibit acetylcholinesterase (AChE). (bvsalud.org)
  • The most successful therapeutic strategy in the treatment of Alzheimer's disease (AD) is directed toward increasing levels of the neurotransmitter acetylcholine (ACh) by inhibition of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), the enzymes responsible for its hydrolysis. (inra.fr)
  • Considering that acetylcholinesterase (AChE) inhibition is the most important mode of action expected of a potential drug used for the treatment of symptoms of Alzheimer's disease (AD), our previous pilot study of 4-aminoquinolines as potential human cholinesterase inhibitors was extended to twenty-two new structurally distinct 4-aminoquinolines bearing an adamantane moiety. (inra.fr)
  • The formation of plaque in the brain (and the associated dendritic loss) is from neuron death caused by reactions with acetylcholinesterase (AChE). (thrivous.com)
  • In normal neurotransmission, an the AChE enzyme, (acetylcholinesterase) creates a reaction which breakdown acetylcholine (ACh) and revents overstimulation and blockage of receptors. (basf.com.au)
  • Muscle acetylcholinesterase (AChE) activity determines the impairment of muscle force generation, and red blood cell (RBC) AChE has been regarded as a surrogate for muscle AChE in organophosphate poisoning. (rcjournal.com)
  • Organophosphates interfere with the elimination of acetylcholine by inhibiting acetylcholinesterase (AChE), resulting in accumulation of acetylcholine at nerve terminals. (rcjournal.com)
Inhibitors5
Inhibitor5
Inhibition7
  • As discussed in the previous section, the accumulation of acetylcholine due to acetylcholinesterase inhibition by nerve gas causes overactivation of acetylcholine receptors all over the body. (duke.edu)
  • There are other examples of acetylcholinesterase inhibition that play a role in our lives. (duke.edu)
  • The inhibition of acetylcholinesterase causes the accumulation of acetylcholine in all areas of the nervous system, causing excessive muscle contraction followed by paralysis, secretions, seizures and death by respiratory failure. (duke.edu)
  • Pharmacological effects of anti-cholinesterase drugs are due to inhibition of acetylcholinesterase. (pharmacology2000.com)
  • Possible screening candidates must fulfill two fundamental requirements: They must (i) show an affinity to acetylcholinesterase well balanced between sufficient binding and competitive inhibition and (ii) facilitate the nucleophilic cleavage of the phosphorylated catalytic serine residue. (irb.hr)
  • Evaluation of their inhibition and reactivation potential in vitro showed some activity with respect to acetylcholinesterase inhibited by cyclosarin. (irb.hr)
  • Therefore, physiological or toxicological relevance of the hysteretic behavior and damped oscillations in ChE-catalyzed reactions and inhibition cannot be ruled out. (msu.ru)
Enzyme acetylcholinesterase2
  • The two precursor molecules at left bind to neighboring subsites in the enzyme acetylcholinesterase. (rcsb.org)
  • In their classic experiment, they added many pairs of precursors with azide or alkyne groups to the enzyme acetylcholinesterase , and found that the enzyme connected only the best one. (rcsb.org)
Therapeutic strategy for the treatment1
Butyrylcholinesterase2
Reactivation1
Kinetics3
  • Enzyme kinetics is the study of the rates of enzyme-catalysed chemical reactions . (wikipedia.org)
  • In enzyme kinetics, the reaction rate is measured and the effects of varying the conditions of the reaction are investigated. (wikipedia.org)
  • Ribozymes also perform a more limited set of reactions, although their reaction mechanisms and kinetics can be analysed and classified by the same methods. (wikipedia.org)
Polymerase chain re1
  • Species composition and allele frequencies for knock-down resistance (kdr-L1014F and L1014S) and acetylcholinesterase (ace-1 G119S) mutations were further characterized using polymerase chain reaction (PCR). (cdc.gov)
Organophosphate1
  • Acetylcholinesterase activity of one hundred and sixty one school children in the age group 15-16 years, belong to two districts, Kurunegala and Kegalle where Organophosphate and Carbamate pesticides are widely used, were studied. (who.int)
Triazoles1
  • Click chemistry between azide and alkyne precursors can generate two slightly different triazoles, anti and syn , depending on how they line up next to each other during the reaction. (rcsb.org)
Activity8
  • They contain phosphorus groups and bind avidly to acetylcholinesterase to inhibit its activity. (duke.edu)
  • O BJECTIVE: To investigate whether 3,4-methylenedioxymethamphetamine (MDMA) abuse produces another neurotoxicity which may significantly inhibit the acetylcholinesterase activity and result in severe oxidative damage and liperoxidative damage to MDMA abusers. (mdma.net)
  • CONCLUSION: The findings in the present study suggest that MDMA abuse can induce another neurotoxicity that significantly inhibits acetylcholinesterase activity and aggravates a series of free radical chain reactions and oxidative stress in the bodies of MDMA abusers, thereby resulting in severe neural, oxidative and lipoperoxidative damages in MDMA abusers. (mdma.net)
  • Enzymes are essential to sustain life because most chemical reactions in biological cells , such as the digestion of food, would occur too slowly or would lead to different products without the activity of enzymes. (newworldencyclopedia.org)
  • 1. To determine activity of acetylcholinesterase activity. (journalmedicalthesis.com)
  • 2. To evaluate the inhibitory effects of various neurotoxic contaminants on acetylcholinesterase activity. (journalmedicalthesis.com)
  • Improvement of butyryl- and acetylcholinesterase activity suggests that maybe TQ supplement could be beneficial as pre-exposure prophylaxis among farm workers spraying pesticides. (bvsalud.org)
  • Recovery from soman-induced hypothermia is due to an increase in acetylcholinesterase activity but not new protein synthesis. (bmc-rm.org)
19971
Inactivation3
Binds3
  • Nerve gas 1 also binds to the acetylcholinesterase 2 enzyme 3 , but only at 1 site. (duke.edu)
  • It binds to one of the reactants (a substrate) to cause a change in the reactant's structure, facilitating the reaction. (duke.edu)
  • This antidote must be given fast enough (within a few minutes) before the nerve gas irreversibly binds to the acetylcholinesterase. (duke.edu)
Acetylthiocholine1
Precursors3
  • Acetylcholine is synthesized from the immediate precursors acetyl coenzyme A and choline in a reaction catalyzed by choline acetyltransferase (choline acetylase). (pharmacology2000.com)
  • However, in the acetylcholinesterase-catalyzed reaction described above, the precursors mostly align side-by-side to form the syn triazole (PDB ID 1q83) . (rcsb.org)
  • You can see alkyne and azide precursors bound to acetylcholinesterase in PDB ID 5eih . (rcsb.org)
Enzymes work1
  • Like all catalysts, enzymes work to lower the activation energy of a reaction, or the initial energy input necessary for most chemical reactions to occur. (newworldencyclopedia.org)
Insecticides1
Protein2
  • 3 a protein that catalyzes the rate at which a reaction occurs. (duke.edu)
  • The two molecules both bind to the protein, bringing the azide and alkyne groups in close proximity and promoting reaction. (rcsb.org)
Bound3
  • Virtually all the open channels are confined to the initial reaction space, although acetylcholine-bound receptor sites can be much more widely distributed. (elsevierpure.com)
  • There are some antidotes (called oxides 6 ) that could work if given fast enough, before the nerve gas becomes irreversibly bound to the acetylcholinesterase. (duke.edu)
  • in such cases, it is helpful to determine the enzyme structure with and without bound substrate analogues that do not undergo the enzymatic reaction. (wikipedia.org)
Substrates5
  • Like any catalyst, the enzyme remains unaltered by the completed reaction and can therefore continue to interact with substrates. (newworldencyclopedia.org)
  • Enzymes are usually specific, or unique, to the reactions they catalyze and the substrates that are involved in these reactions. (newworldencyclopedia.org)
  • Reactions with three or four substrates or products are less common, but they exist. (wikipedia.org)
  • This rate-determining step may be a chemical reaction or a conformational change of the enzyme or substrates, such as those involved in the release of product(s) from the enzyme. (wikipedia.org)
  • A newer model, the induced-fit model, helps to account for reactions between substrates and active sites that are not exact fits. (medicalnewstoday.com)
Chemical reaction4
  • The simulations indicate that the amplitudes and time-courses are primarily determined by the chemical reaction rates that characterize acetylcholine interactions with receptor and esterase and that these interactions occur under nonequilibrium conditions. (elsevierpure.com)
  • An enzyme is a biological catalyst that regulates the rate of a chemical reaction in a living organism. (newworldencyclopedia.org)
  • Yet, a denatured enzyme can refold within fractions of a second and then precisely react in a chemical reaction. (newworldencyclopedia.org)
  • Heat cannot be added to a living system, so enzymes provide an alternate pathway: they bond with a substrate (the substance involved in the chemical reaction) to form a "transition state," an unstable intermediate complex that requires less energy for the reaction to proceed. (newworldencyclopedia.org)
Hydrolysis1
  • The hydrolysis reaction of the carboxyl ester leads to the formation of an acyl-enzyme and free choline. (wikipedia.org)
Neuromuscular3
  • Two kinetic models are introduced which predict amplitudes and time-courses of endplate currents and miniature endplate currents at neuromuscular junctions, at both normal and acetylcholinesterase-inhibited endplates. (elsevierpure.com)
  • Rosenberry, TL 1979, ' Quantitative simulation of endplate currents at neuromuscular junctions based on the reaction of acetylcholine with acetylcholine receptor and acetylcholinesterase ', Biophysical Journal , vol. 26, no. 2, pp. 263-289. (elsevierpure.com)
  • Acetylcholinesterase is present at ganglia, visceral neuroeffector junctions, and neuromuscular junctional endplates. (pharmacology2000.com)
Substances1
  • Although drugs like obidoxime or pralidoxime have been used with considerable success, there is a need for new substances capable of reactivating acetylcholinesterase with a broader scope and increased efficacy. (irb.hr)
Structures1
  • The NMDAR1 immunoreaction was usually confined to acetylcholinesterase-positive structures, implying that the reaction is present in nerves. (nih.gov)
Molecule1
  • 55 It was found that the solventfree reaction of ETFAA 1a, benzaldehyde, and ammonium acetate at 100 C proceeded with the loss of the water molecule to aff ord partially dehydrated 2-hydroxy-2,6-bis(trifl uoromethyl)-1,2,3,4-tetrahydropyridine-3,5-dicarboxylate 6. (researchgate.net)
Chain reactions1
  • Antioxidant compounds are molecules that can inhibit or delay the oxidation of lipids or other biomolecules by inhibiting the initiation and propagation of oxidative chain reactions [ 29 ]. (ijpsonline.com)
Adverse reactions2
  • Gradually reduce the dose in 2.5-mg decrements if severe adverse reactions occur. (medscape.com)
  • Most common adverse reactions are transient hypotension and hypertension. (ncats.io)
Molecular1
  • The Bertozzi lab has developed a collection of cell-friendly click reactions, for example, by removing the need for toxic copper catalysts by embedding the alkyne inside a strained molecular ring. (rcsb.org)
Study4
  • The recent advances in the study of the Hantzsch and Biginelli reactions involving polyfluoroalkyl-3-oxo esters are analyzed. (researchgate.net)
  • Current sets of observations show that the study of Acetylcholinesterase enzyme can help the Eco-toxicologists to assess the impacts of various lethal & sub-lethal pollution in the marine environment. (journalmedicalthesis.com)
  • Regarding treatment, this study also found that there might be different reactions to medicine for each gender. (enhanceyourmemory.co)
  • Spectrophotometric and electrochemical study of protolytic equilibria of some oximes-acetylcholinesterase reactivators. (bmc-rm.org)
Occur1
  • This region, where the binding of the substrate(s) and the reaction occur, is known as the active site of the enzyme. (newworldencyclopedia.org)
Molecules2
  • The body must synthesize new enzyme molecules to overcome the loss of acetylcholinesterase. (duke.edu)
  • the citric acid cycle glycolysis the electron transport system the preparatory reaction, Complete oxidative breakdown of glucose results in _____ ATP molecules. (craftwithmagic.nl)
Species2
  • and non-free radical species such as hydrogen peroxide (H 2 O 2 ) are diverse kinds of activated oxygen and mostly produced by exogenous factors or oxidation product of biological reactions [ 1 - 3 ]. (ijpsonline.com)
  • In a heterogeneous catalysis configuration, this reaction could generate long-lived Fe(IV) species with the correct additives. (lu.se)
Irreversible1
  • Benzenemethane Sulfonylfluoride (329-98-6) is an irreversible inactivator of many esterases including mammalian acetylcholinesterases. (elsevierpure.com)
Chronic1
  • As an example, acute inhalation MRLs may not be protective for health effects that are delayed in development or are acquired following repeated acute insults, such as hypersensitivity reactions, asthma, or chronic bronchitis. (cdc.gov)
Synthesis1
  • These are cofactors that are needed in metabolic reactions and that are essential for normal deoxyribonucleic acid (DNA) synthesis, with some vitamins providing antioxidant effects. (medscape.com)
Quantitative1
  • The increased interfacial area of the biphasic reaction mixture and the lack of headspace enabled almost quantitative conversions within ca. 30 minutes at 120 °C and 20 bar even for unpolar starting materials. (thieme-connect.com)
Improves2
  • Alpha GPC (50 mg): Improves reaction time while improving memory. (naspcenter.org)
  • A relaxed mind improves mental performance and reaction time, especially for highly anxious people. (thrivous.com)
Compounds2
  • 6 compounds that bind to the phosphorus group on the nerve gas to pull it off of the acetylcholinesterase. (duke.edu)
  • The review is summarized and systematized the published data on the multicomponent reactions of ethyl trifluoroacetoacetate, carbonyl compounds (aldehydes and ketones), and nucleophilic reagents. (researchgate.net)
Substrate5
  • This example assumes the simplest case of a reaction with one substrate and one product. (wikipedia.org)
  • Such cases exist: for example, a mutase such as phosphoglucomutase catalyses the transfer of a phospho group from one position to another, and isomerase is a more general term for an enzyme that catalyses any one-substrate one-product reaction, such as triosephosphate isomerase . (wikipedia.org)
  • Beyond this limit the enzyme is saturated with substrate and the reaction rate ceases to increase. (wikipedia.org)
  • Hysteresis in ChE-catalyzed reactions can be interpreted in terms of slow transitions between two enzyme conformers E and E′. Substrate can bind to E and/or E′, both Michaelian complexes ES and Ε′S can be catalytically competent, or only one of them can make products. (msu.ru)
  • The formal reaction pathway depends on both the chemical structure of the substrate and the type of enzyme. (msu.ru)
Catalyze1
Reactants1
  • The reaction catalysed by an enzyme uses exactly the same reactants and produces exactly the same products as the uncatalysed reaction. (wikipedia.org)
Time4
  • The simpler homogeneous reaction space model accurately predicts decay phase time constants are inaccurate. (elsevierpure.com)
  • The two-reaction space model predicts amplitudes and time constants within a factor of two of those observed experimentally. (elsevierpure.com)
  • The present approach shows the significant outcomes such as yield up to 94%, catalyst‐free reaction, easy workup procedure and shorter period of reaction time. (researchgate.net)
  • The reaction time was reduced to half an hour. (who.int)
Active1
Atom1
  • The spherical cryptophane at the top, which has the alkyne half of the click reaction, traps a xenon atom that may be useful as a contrast agent for MRI. (rcsb.org)
Present1
  • Acetylcholinesterase is present in some of the fibers in the optic tracts and in most retinorecipient nuclei, as well as in some other nuclei and tracts. (karger.com)
Rate1