Acetylcholinesterase Antisense Oligonucleotides (EN101) as a Novel Treatment Strategy for ALS: A Mouse Model Study Marc Gotkine, Gladis Gilinski, Leah Rozenstein, Oded Abramsky, Zohar Argov, Hanna Rosenmann, Jerusalem, Israel The study investigated the effect of EN101 on a transgenic mouse model of ALS. Previous evidence indicated that acetylcholinesterase (AChE) is involved in ALS. However, AC...

The reversible inhibition of acetylcholinesterase (AChE) by 4,4'-bipyridine (BP) was measured with acetylthiocholine as substrate. The enzyme/inhibitor dissociation constant for binding of BP to the catalytic site was Ka = 1.0 mM and the non-competitive dissociation constant for binding to an allosteric site was K, = = 9.0 mM. BP protected AChE against phosphylation by sarin, soman, tabun and V...

A wide range of evidence shows that acetylcholinesterase (AChE) inhibitors can interfere with the progression of Alzheimer's disease (AD). The successful development of these compounds was based on a well-accepted theory that the decline in cognitive and mental functions associated with AD is related to the loss of cortical cholinergic neurotransmission. The earliest known AChE inhibitors, name...

Acetylcholinesterase (AChE) enzyme which catalyses the hydrolysis of choline esters, such as acetylcholine, is very important in nerve function. Previous structural studies showed the possible amyloid fibril formation on the AChE. Therefore it is important to understand interaction of ligands to prevent the formation of  amyloid fibrils. The purpose of the present study was to  char...

A common feature in the Alzheimer's disease (AD) brain is the presence of acetylcholinesterase (AChE) which is commonly associated with β-amyloid plaques and neurofibrillary tangles (NFT). Although our understanding of the relationship between AChE and the pathological features of AD is incomplete, increasing evidence suggests that both β-amyloid protein (Aβ) and abnormally hyperphosphorylated ...

A wide range of evidence show that acetylcholinesterase (AChE) inhibitors can interfere with the progression of Alzheimer's Disease (AD). The successful development of these compounds was based on a well-accepted theory that the decline in cognitive and mental functions associated with AD is related to the loss of cortical cholinergic neurotransmission. The earliest known AChE inhibitors, namel...

Nerve agents are highly toxic organophosphorus compounds with strong inhibition potency against acetylcholinesterase (AChE). Herein, we describe two first extremely promising uncharged reactivators for poisoned human AChE with a superior or similar in vitro ability to reactivate the enzyme as compared to that of HI-6, obidoxime, TMB-4 and HLö-7.

A highly sensitive, selective, and dual-readout (colorimetric and fluorometric) assay for acetylcholinesterase (AChE) based on Rhodamine B-modified gold nanoparticle is reported. Due to its good sensitivity and selectivity, the assay can be used for monitoring AChE levels in the cerebrospinal fluid of transgenic mice with Alzheimer's disease.

In the course of our screening of microbial metabolites that inhibit the activity of acetylcholinesterase (AchE), we isolated potent and selective inhibitors of AchE, arisugacin A (1) and B (2) from the culture broth of Penicillium sp. FO-42591~4^ together with the structurally related known compound, territrem B (3) (Fig. 1)5'6). Interestingly, structures 1-3 resemble the pyripyropene A (4), w...

In the present study we describe the synthesis and biological assessment of new tacrine analogs in the course of inhibition of acetylcholinesterase. The obtained molecules were synthesized in a condensation reaction between activated 6-BOC-hydrazinopyridine-3-carboxylic acid and 8-aminoalkyl derivatives of 2,3-dihydro-1H-cyclopenta[b]quinoline. Activities of the newly synthesized compounds were...