In developing antidotes to poisoning by cholinesterase (ChE) inhibitors, several potential target sites at the cholinergic synapse have been studied, including the postsynaptic receptor and acetylcholinesterase (AchE) itself. Muscarinic receptor blocking ...

... The signal sequences for these modifications were identified by site-directed mutagenesis: Asn-265, Asn-350 and Asn-464 appear to be targets for ...

of acetylcholinesterase (AChE) is the termination of nerve impulse transmission at cholinergic synapses by rapid of acetic acid (3) (see Scheme 1). In accordance with its function, AChE is an extremely rapid enzyme (3). Being an essential enzyme, AChE is the target of a variety of potent natural and synthetic toxic

The accepted target for oganophosphorus agent (OP) binding to enzymes is the active site serine in the consensus sequence GlyXSerXGly of acetylcholinesterase. By using mass spectrometry to fragment OP-labeled peptides, we have found that OP can make coval...

... Title : CONFORMATIONAL STUDIES ON THE ACTIVE SITE OF ACETYLCHOLINESTERASE BY ELECTRON PARAMAGNETIC RESONANCE,. ...

By targeting the dual active sites of acetylcholinesterase (AChE), a new series of berberine derivatives was designed, synthesized, and evaluated as AChE inhibitors. Most of the derivatives inhibited AChE in the sub-micromolar range. Compound 8c, berberine linked with phenol by a 4-carbon spacer, showed the most potent inhibition of ...

Examination of the enzyme structure for acetylcholinesterase (AChE) reveals two sites of ligand interaction: The peripheral site (P-site) located at the entrance of the gorge, and the acylation site (A-site) at the base of the gorge. Our goal is to develo...

Examination of the enzyme structure for acetylcholinesterase (AChE) reveals two sites of ligand interaction: The peripheral site (P-site) located at the entrance of the gorge, and the acylation site (A-site) at the base of the gorge. Our goal is to develo...

Examination of the enzyme structure for acetylcholinesterase (AChE) reveals two sites of ligand interaction: The peripheral site (P-site) located at the entrance of the gorge, and the acylation site (A-site) at the base of the gorge. Our goal is to develo...

The organothiophosphate diazinon inhibits the target site acetylcholinesterase only after activation to its metabolite diazoxon. Commonly, the toxicity of xenobiotics toward aquatic organisms is expressed as a function of the external concentration and the resulting effect on the individual level after fixed exposure times. This ...

... Accession Number : AD0745227. Title : Relative Binding Sites of Pharmacologically Active Ligands on Bovine Erythrocyte Acetylcholinesterase,. ...

The feasibility of using the fluorescent lanthanide terbium as a probe of the peripheral anionic sites on mammalian brain acetylcholinesterase (AChE) was studied. Terbium has been used as a fluorescence probe of Ca2+ binding sites in many enzyme proteins ...

Radiation inactivation is a method to determine the apparent target size of molecules. In this report we examined whether radiation inactivation of various enzymes and brain receptors is influenced by the preparation of samples preceding irradiation. The apparent target sizes of endogenous acetylcholinesterase and pyruvate kinase from ...

... Inhibitory Potencies of Chlorpyrifos Oxon, Chlorpyrifos Methyl Oxon, and Mipafox for Acetylcholinesterase Versus Neuropathy Target Esterase. ...

... Abstract : Studies on the structural of acetylcholinesterase (AChE) as a target of organophosphate toxicity continue and have yielded several leads ...

Tissue distribution of human acetyicholinesterase and butyryicholinesterase messenger RNA. 1 Cholinesterase inhibitors occur naturally in the calabar bean (eserine), green potatoes (solanine), insect-resistant crab apples, the coca plant (cocaine) and snake venom (fasciculin). There are also synthetic cholinesterase inhibitors, for example man-made insecticides. These inhibitors inactivate ...

By targeting multi-active sites of acetylcholinesterase (AChE), a series of huperzine A (Hup A) derivatives with various aromatic ring groups were designed and synthesized by Schiff reaction. They were evaluated as AChE and butyrylcholinesterase (BChE) inhibitors. Results showed very significant specificity that the group of imine ...

of the binding sites of huperzine A in acetylcholinesterase by docking studies. J. Comput- Aided Mol. Des. 1994

.P. Prediction of the binding sites of huperzine A in acetylcholinesterase by docking studies. J Comput Aided Mol

.P. Prediction of the binding sites of huperzine A in acetylcholinesterase by docking studies. J. Comput. Aided

... may lead to useful water and oil ... of the active site with acetate substrates containing ... Sodium dodecyl sulfate (SDS) polyacrylamide gel equipment ...

... agonist site and the lipid bilaver canl not be obtained. ... Upon dlealkylation this conjugate loses the ionic strength dependence for binding after aging ...

Acetylcholinesterase (ACHE) is an enzyme long noted for its essential role in the termination of neurotransmission at cholinergic synapses and neuromuscular junctions. Because acetylcholinesterase is the target protein for a variety of neurotoxic compound...

Though acetylcholinesterase is the primary target of organophosphorus toxicants, our finding that acetylcholinesterase knockout mice are supersensitive to the lethal effects of VX, DFP, chlorpyrifos oxon, and iso-OMPA demonstrates that other important tar...

Though acetylcholinesterase is the primary target of organophosphorus toxicants, our finding that acetylcholinesterase knockout mice are supersensitive to the lethal effects of VX, DFP, chlorpyrifos oxon, and iso-OMPA demonstrates that other important tar...

Molecular changes in acetylcholinesterase (AChE) leading to target-site resistance to carbamate and organophosphate insecticides have recently been identified. Of particular interest is the S431F mutation in ace2 and its orthologue ace1 of Myzus persicae Sulzer and Aphis gossypii Glover, respectively. This mutation has been correlated with resistance to ...

By rapid hydrolysis of the neurotransmitter, acetylcholine, acetylcholinesterase terminates neurotransmission at cholinergic synapses. Acetylcholinesterase is a very fast enzyme, functioning at a rate approaching that of a diffusion-controlled reaction. The powerful toxicity of organophosphate poisons is attributed primarily to their potent inhibition of ...

By rapid hydrolysis of the neurotransmitter, acetylcholine, acetylcholinesterase terminates neurotransmission at cholinergic synapses. Acetylcholinesterase is a very fast enzyme, functioning at a rate approaching that of a diffusion-controlled reaction. The powerful toxicity of organophosphate poisons is attributed primarily to their potent inhibition of ...

The objective of this project is the determination of the three-dimensional structure of acetylcholinesterase (AChE) from electric organ tissue of Torpedo californica, with the intention of elucidating the detailed topography of its catalytic site. In the...

The objective of this project is the crystallization of the enzyme acetylcholinesterase (AChE), with the long-term objective of determining its three-dimensional structure and, thereby, the detailed topography of its active site. Torpedo electric organ wa...

The goal of this research during the first year of the contract was to develop a method for the purification of human erythrocyte acetylcholinesterase and to initiate the preparation and analysis of monoclonal antibodies. This was accomplished by the prep...

We are studying the properties of the active site, and the region peripheral to it, of acetylcholinesterase (AcChE), the enzyme which hydrolyzes and thus terminates the action of the important neurotransmitter acetylcholine (AcCh). We have studied the res...

This report describes continued studies on organophosphorus (OP) inhibitors of acetylcholinesterase (AChE) in the mammalian spinal cord. The mechanism and site of action of the potentiation and/or depression of synaptic transmission by the OPs are being r...

This report describes studies on organophosphorus (OP) inhibitors of acetylcholinesterase (AChE) in the mammalian spinal cord in which the mechanism and site of action of the OPs on synaptic transmission were studied with selective agonists and antagonist...

The dissociation constants have been determined and compared for a series of reversible (noncovalent) inhibitors of eel acetylcholinesterase that are structurally related to the very potent inhibitor, 1,2,3,4-tetrahydro-9-aminoacridine (THA). It is conclu...

... in BChE. Modeling designated it as part of the peripheral anionic site, which is lacking in BChE. Site-directed mutagenesis ...

Acetylcholinesterase (AChE) inhibitors played an important role in developing a cure for Alzheimer' s disease. In order to study on the influence of modifications at different groups and side chains on the AChE inhibitory ability and the active sites of 7H-thiazolo[3,2-b][1,2,4]triazin-7-one derivatives, fourteen ...

Apple orchards are highly manipulated crops in which large amounts of pesticides are used. Some of these pesticides lack target specificity and can cause adverse effects in non-target organisms. In order to evaluate the environmental risk of these products, the use of transplanted sentinel organisms avoids side-effects from past events and facilitate ...

data are presented on the interaction with Torpedo californica acetylcholinesterase (TcAChE acetylcholine (ACh). The enzyme acetylcholinesterase (AChE; EC 3.1.1.7) functions in cholinergic synapses for AD using AChE inhibitors as drugs (5-7). The inhibitors approved so far include synthetic compounds

The purpose of the work done was to prepare derivatives of 2-PAM that are substituted in the 3-position by groups capable of bonding to, or liganding with, the oxygen on the phosphorus of aged, poisoned (by phosphonylation or phosphorylation) acetylcholinesterase. The derivatives suggested for preparation were designed to facilitate cleavage of the bond between phosphorus and ...

How Does Huperzine A Enter and Leave the Binding Gorge of Acetylcholinesterase? Steered Molecular of Huperzine A (HupA) binding with the long active-site gorge of Torpedo californica acetylcholinesterase (Tc and Huperzine A (HupA), is much larger than the size of bottleneck, large-amplitude fluctuations are necessary

... Acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and neuropathy target esterase catalytic domain (NEST) were reacted with ...

Monoclonal antibodies have been raised against acetyicholinesterase isolated from a variety of sources and species. Although none of these antibodies bind to the esteratic site, some of them appear to interact with the region of the catalytic subunit referred to as the peripheral anionic site. We describe here the production and characterization of six ...

Acetyicholinesterase (AChE) is one of the most efficient enzymes known. The AChE active site consists of a narrow gorge with two separate ligand binding sites: an acylation site at the bottom of the gorge where substrate hydrolysis occurs and a peripheral...

Acetylcholinesterase and paraoxonase are important targets for treatment of degenerative diseases, Alzheimer's disease and atherosclerosis, respectively, both of which impose major burdens on the health care systems in Western society. Acetylcholinesterase is the target of lethal nerve agents, and paraoxonase is ...

Aphids, among the most destructive insects to world agriculture, are mainly controlled by organophosphate insecticides that disable the catalytic serine residue of acetylcholinesterase (AChE). Because these agents also affect vertebrate AChEs, they are toxic to non-target species including humans and birds. We previously reported that a cysteine residue ...

... using the CHARMm module of QUANTA96 (conjugate k-st >> ak2; k-- >> k3; km >> bk3; 32; 33; see ref 22). This gradient). ...

Previously we used site-directed mutagenesis, in vitro expression, and molecular modeling to investigate the inactivation of an invertebrate acetylcholinesterase, cholinesterase 2 from amphioxus, by the sulfhydryl reagents 5,5�-dithiobis(2-nitrobenzoic acid) (DTNB) and N-ethylmaleimide (NEM). We created the mutants C310A, C466A, C310A/C466A and ...

The relative inhibitory potency (RIP) of an organophosphorus (OP) inhibitor against acetylcholinesterase(AChE) versus neuropathy target esterase (NTE) is ki(AChE)/ki(NTE), where ki is the bimolecular rate constant of inhibition. RIPs>1 correlate with the ...

Inhibition of neuropathy target esterase (NTE, neurotoxic esterase) and acetylcholinesterase (AME) activities was compared in brain and spinal cords of adult. hile Leghorn hens and adult male Long Evans rats 4-48 hr after administration of tri-ortho-tolyl phosphate (TOTP po, 50-5...

Current anticholinesterase pesticides were developed during World War II and are toxic to mammals because they target a catalytic serine residue of acetylcholinesterases (AChEs) in insects and in mammals. A sequence analysis of AChEs from 73 species and a three-dimensional model of a malaria-carrying mosquito (Anopheles gambiae) AChE (AgAChE) reported here ...

Current anticholinesterase pesticides were developed during World War II and are toxic to mammals because they target a catalytic serine residue of acetylcholinesterases (AChEs) in insects and in mammals. A sequence analysis of AChEs from 73 species and a three-dimensional model of a malaria-carrying mosquito (Anopheles gambiae) AChE (AgAChE) reported here ...

The photosensitizer, methylene blue (MB), is a strong reversible inhibitor of Torpedo californica acetylcholinesterase (AChE) in the dark. Under illumination it causes irreversible inactivation. Loss of fluorescence of the singlet oxygen ((1)O(2)) trap, 9,10-dimethylanthracene, was retarded in the presence of AChE, and the rate of photo-inactivation was increased in the ...

Acetylcholinesterase (AcChE, EC 3.1.1.7) was isolated from the electric organ of T. nobiliana and treated with the active-site-directed alkylating agent 1-bromo-2-(14C)pinacolone or with BrPin, which acts initially as a competitive inhibitor, and then ina...

Our previous molecular dynamics simulation (10 ns) of mouse acetylcholinesterase (EC 3.1.1.7) revealed complex fluctuation of the enzyme active site gorge. Now we report a 5-ns simulation of acetylcholinesterase complexed with fasciculin 2. Fasciculin 2 binds to the gorge entrance of acetylcholinesterase with ...

MicroRNAs (miRNAs) contribute to both neuronal and immune cell fate, but their involvement in intertissue communication remained unexplored. The brain, via vagal secretion of acetylcholine (ACh), suppresses peripheral inflammation by intercepting cytokine production; therefore, we predicted that microRNAs targeting acetylcholinesterase (AChE) can attenuate ...

Therapeutically valuable proteins are often rare and/or unstable in their natural context, calling for production solutions in heterologous systems. A relevant example is that of the stress-induced, normally rare, and naturally unstable �read-through� human acetylcholinesterase variant, AChE-R. AChE-R shares its active site with the synaptic AChE-S ...

Objectives? Inhibition of acetylcholinesterase (AChE) is a common treatment for early stages of the most general form of dementia, Alzheimer's disease. In this study selected components of essential oils, which carry a variety of important functional groups, were tested for their in-vitro anti-acetylcholinesterase activity. Methods? In-vitro ...

: Acetylcholinesterase (AChE) Target Category: Substrate for enzymatic hydrolysis Method of detection: PET Source), but not in vascular dementia. Acetylcholinesterase (AChE) is the enzyme that terminates cholinergic actions through the rapid hydrolysis of acetylcholine to choline and acetate. AChE is localized on both cholinergic

Acetylcholinesterase (AChE) is a key neural enzyme of both vertebrates and invertebrates, and is the biochemical target of organophosphate and carbamate pesticides for invertebrates, as well as vertebrate nerve agents, e.g., soman, tabun, VX, and others. AChE inhibitors are also key drugs among thos...

Representing receptors as ensembles of protein conformations during docking is a powerful method to approximate protein flexibility and increase the accuracy of the resulting ranked list of compounds. Unfortunately, docking compounds against a large number of ensemble members can increase computational cost and time investment. In this article, we present an efficient method to evaluate and select ...

BackgroundN,N-Diethyl-3-methylbenzamide (deet) remains the gold standard for insect repellents. About 200 million people use it every year and over 8 billion doses have been applied over the past 50 years. Despite the widespread and increased interest in the use of deet in public health programmes, controversies remain concerning both the identification of its target ...

Pharmacological studies from our group [Lima et al. Pharmacol Biochem Behav 92:508, (2009)] revealed that geissospermine (GSP), the major alkaloid of the bark extract of Brazilian Geissospermum vellosii, inhibits acetylcholinesterases (AChEs) in the brains of rats and electric eels (Electrophorus electricus). However, the binding mode (i.e., conformation and orientation) of ...

Radiation inactivation was used to measure the target sizes for binding of disulfonic stilbene anion transport inhibitor 4,4'-dibenzamido-2,2'-disulfonic stilbene (DBDS) and mercurial water transport inhibitor p-chloromercuribenzene sulfonate (pCMBS) to human erythrocytes. The measured target size for erythrocyte ghost ...

Insecticides directed against acetylcholinesterase (AChE) are facing increased resistance among target species as well as increasing concerns for human toxicity. The result has been a resurgence of disease vectors, insects destructive to agriculture, and residential pests. We previously reported a free cysteine (Cys) residue at the entrance to the AChE ...

Hartree-Fock and density functional methods were used to analyze electronic and structural properties of known drugs to evaluate the influence of these data on acetylcholinesterase inhibition. The energies of the frontier orbitals and the distances between the more acidic hydrogen species were investigated to determine their contributions to the activity of a group of ...

Molecular dynamics simulations are leading to a deeper understanding of the activity of the enzyme acetylcholinesterase. Simulations have shown how breathing motions in the enzyme facilitate the displacement of substrate from the surface of the enzyme to the buried active site. The most recent work points to the complex and spatially extensive nature of ...

-ray structures of complexes, e.g., of fasciculin/AChE (Harel et al., 1995) and of huperzine A/AChE (Raves et al of acetylcholinesterase complexed with the nootropic alkaloid, ( )- huperzine A. Nat Struct Biol 4:57�63. Richards FM

The authors have studied the binding properties and inhibitory activity of AE-2, a monoclonal antibody which binds to acetylcholinesterase(AChE) and inhibits its activity by up to 50%. This antibody was compared to C1B7, another inhibitory enzyme. It was ...

The principal role of acetylcholinesterase (AChE, acetylcholine hydrolase, EC 3.1.1.7) is termination of impulse). In keeping with this requirement, AChE possesses a remarkably high speci�c activity, especially for a serine). The three-dimensional structure of AChE from Tor- pedo californica (TcAChE) reveals that the catalytic triad

With the object of developing an alkylating type of active site reagent for acetylcholinesterase (AChE; acetylcholine acetylhydrolase, EC 3.1.1.7), (3-bromo-2-oxopropyl)trimethylammonium bromide (BAT). 1-(3-bromo-2-oxopropyl)pyridinium bromide, 3-(bromoac...

New insecticides are urgently needed because resistance to current insecticides allows resurgence of disease-transmitting mosquitoes while concerns for human toxicity from current compounds are growing. We previously reported the finding of a free cysteine (Cys) residue at the entrance of the active site of acetylcholinesterase (AChE) in some insects but ...

New insecticides are urgently needed because resistance to current insecticides allows resurgence of disease-transmitting mosquitoes while concerns for human toxicity from current compounds are growing. We previously reported the finding of a free cysteine (Cys) residue at the entrance of the active site of acetylcholinesterase (AChE) in some insects but ...

The overall goal was to study mechanisms of aging of serine esterases inhibited by organophosphorus compounds capable of producing acute and delayed neurotoxicity. Acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and neuropathy target esterase c...

Studies on the structure of acetylcholinesterase (AChE) as a target for organophosphate toxicity continue and have resulted in several leads of significance. First, we have completed the first phase of studies of the structural determinants on the enzyme ...

The active center of acetylcholinesterase (AChE), a target site for competitive inhibitors, resides centrosymmetric to the subunit at the base of a deep, narrow gorge lined by aromatic residues. At the gorge entry, a peripheral site encompasses overlapping binding loci for noncompetitive inhibitors, which alter ...

p-(trimethyl ammonium) benzene diazonium difluoroborate (TDF), an affinity-labeling reagent of the acetylcholine receptor site(s), which in the normal cell acts as an irreversible inhibitor becomes a reversible activator after in vivo exposure of the electroplax to dithiothreitol (DTT), a disulfide bond reducing agent. After in vitro exposure of ...

Metallothionein level (MT), and acetylcholinesterase (AChE), catalase (CAT) and glutathione-S-transferase (GST) enzyme activities in the bivalves Mytilus edulis and Macoma balthica were investigated for seasonal variations from an inshore and an offshore site in the northern Baltic Sea. All the biomarkers showed variability, following mostly a similar ...

A new series of tacrine-multialkoxybenzene hybrids (9a-9n) were designed, synthesized and evaluated as dual inhibitors of cholinesterases (ChEs) and self-induced ?-amyloid (A?) aggregation. All the synthesized compounds had high acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitory activity with IC?? values at the nanomolar range, which were much better than ...

BackgroundAlzheimer's disease (AD) is the most common cause of dementia characterized by progressive cognitive impairment in the elderly people. The most dramatic abnormalities are those of the cholinergic system. Acetylcholinesterase (AChE) plays a key role in the regulation of the cholinergic system, and hence, inhibition of AChE has emerged as one of the most promising ...

The peripheral anionic site of acetylcholinesterase, when occupied by a ligand, is known to modulate reaction rates at the active site of this important enzyme. The current report utilized the peripheral anionic site specific fluorogenic probe thioflavin t to determine if the organophosphates chlorpyrifos oxon and ...

The principal objectives of this contract are to better understand the mechanism of action of AChE, and to characterize its various ligand-binding sites. These objectives are being approached by the method of single crystal X- ray diffraction, together wi...

Page 1. Page 2. Page 3. Page 4. Page 5. Page 6. Page 7. Page 8. Page 9. Page 10. Page 11. Page 12. Page 13. Page 14. Page 15. Page 16. Page ...

Page 1. Page 2. Page 3. Page 4. Page 5. Page 6. Page 7. Page 8. Page 9. Page 10. Page 11. Page 12. Page 13. Page 14. Page 15. Page 16. Page ...

Page 1. Page 2. Page 3. Page 4. Page 5. Page 6. Page 7. Page 8. Page 9. Page 10. Page 11. Page 12. Page 13. Page 14. Page 15. Page 16. Page ...

Page 1. Page 2. Page 3. Page 4. Page 5. Page 6. Page 7. Page 8. Page 9. Page 10. Page 11. Page 12. Page 13. Page 14. Page 15. Page 16. Page ...

The total cholinesterase activity in canine tracheal smooth muscle was found to consist of butyrylcholinesterase and acetylcholinesterase in a ratio of 3:1. Most of the acetyl- and butyrylcholinesterase sites were distributed on the muscle surface; the re...

were obtained. Different from the unbinding of other AChE inhibitors, such as Huperzine from other AChE inhibitors, such as Huperzine A (HupA), which binds to the acylation site, E2020

, decamethonium; GAL, (-)-galan- thamine; (-)-HupA, (-)-huperzine A; hupyridone or 2, 5-amino-5, including the alka- loids (-)-galanthamine (GAL, Reminyl)9 and (-)-huperzine A [(-)-HupA]10

Single and multiple site mutants of recombinant mouse acetyicholinesterase (rMoAChE) were inhibited with racemic 7-(methylethoxyphosphinyloxy) -1-methylquinolinium iodide (MEPO) and the resulting mixture.

... TITLE: Targeting Osteoblastic Bone Metastasis with a Novel Site ... 5. FUNDING NUMBERS Targeting Osteoblastic Bone Metastasis with a Novel Site ...

A computation docking study of the highly potent, non-nitrogen containing, acetylcholinesterase inhibitor (+)-Arisugacin A is presented. The model suggests that (+)-arisugacin A is a dual binding site covalent inhibitor of AChE. These findings are examined in the context of Alzheimer's disease-modifying therapeutic design. (+)-Arisugacin A's revealed mode ...

Alzheimer's disease (AD) is the most common neurodegenerative disease, affecting mainly elderly people. The reasons why AD occurs are complex and multifactorial and several biochemical targets are thought to play a key role in its progress and development. This fact has led to the development of a multitarget-directed ligand strategy as a logical approach for designing a ...

Structural and dynamic properties of water molecules around acetylcholinesterase are examined from a 10-nsec molecular dynamics simulation to help understand how the protein alters water properties. Water structure is broken down into hydration sites constructed from the water density <3.6 � from the protein surface. These sites ...

The interactions of substrates, inhibitors and antibodies with Torpedo and mammalian acetylcholinesterases and butyrylcholinesterases have been studied by enzyme kinetic analyses, site-specific mutagenesis, molecular modeling, and peptide and antibody titrations. The high yield expression systems we developed have enabled us to obtain sufficient wild-type ...

For some enzymes, virtually every substrate molecule that encounters the entrance to the active site proceeds to reaction, at low substrate concentrations. Such diffusion-limited enzymes display high apparent bimolecular rate constants ((kcat/KM)), which depend strongly upon solvent viscosity. Some experimental studies provide evidence that ...

Insecticide resistance in Anopheles gambiae threatens the success of malaria vector control programmes in sub-Saharan Africa. In order to manage insecticide resistance successfully, it is essential to assess continuously the target mosquito population. Here, we collected baseline information on the distribution and prevalence of insecticide resistance and its association with ...

For many decades it has been thought that oxygen analogs (oxons) of organophosphorus insecticides phosphorylate the catalytic site of acetylcholinesterase by a mechanism that follows simple Michaelis-Menten kinetics. More recently, the interactions of at least some oxons have been shown to be far more complex and likely involve binding of oxons to a second ...

In this laboratory experiment, college students are introduced to dynamic combinatorial chemistry (DCC) and apply it to determine the substrate selectivity of acetylcholinesterase (AChE). Initially, the students construct a chemical library of dynamically interchanging thioesters and thiols. Then, AChE is added and allowed to select and hydrolyze the best substrate, thereby ...