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...

Resistance to temephos, an organophosphorous insecticide (OP), was found to be low (2-fold) in 2 Culex pipiens populations collected in Sayada (mid-eastern Tunisia). This resistance was synergized by an esterase inhibitor (DEF). Two sets of over-produced esterases (A2-B2 and A4-B4), known to be involved in resistance, were identified in almost 50% of the examined insects. In addition, 3% of ins...

The transient opening of a backdoor in the active-site wall of acetylcholinesterase, one of nature's most rapid enzymes, has been suggested to contribute to the efficient traffic of substrates and products. A crystal structure of Torpedo californica acetylcholinesterase in complex with the peripheral-site inhibitor aflatoxin is now presented, in which a tyrosine at the bottom of the active-site...

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...

Introduction: Hyperphosphorylation of tau is an important event in Alzheimer’s disease (AD) pathogenesis, leading to the generation “neurofibrillary tangles,” a histopathological hallmark associated with onset AD and related tauopathies. Microtubule-affinity regulating kinase 4 (MARK4) evolutionarily conserved Ser-Thr (S/T) that phosphorylates microtubule-associated proteins, thus playing criti...

Levels of acetylcholinesterase activity can be made to vary in response to the presence or absence of sunlight in a system that can be considered as a model for photoperiodic processes found in nature. The enzyme is rendered photosensitive by the presence of a photochromic inhibitor, N-p-phenylazophenylcarbamyl choline, which changes from a trans to a cis isomer under the influence of the light...

The Amaryllidaceae family is well known for its pharmacologically active alkaloids. An important approach to treat Alzheimer’s disease involves the inhibition of the enzyme acetylcholinesterase (AChE). Galanthamine, an Amaryllidaceae alkaloid, is an effective, selective, reversible, and competitive AchE inhibitor. This work was aimed at studying the alkaloid composition of four wild Argentinian...

ligand because the smaller molecular forms, which would be better able to penetrate the agarose gel, are not bound, whereas the larger form does bind. The gel can also discriminate between acetylcholinesterase and cholinesterase. This is unexpected because edrophonium is a competitive inhibitor of both enzymes. This suggests that the coupling of a side chain to the meta-hydroxy group of edropho...

The X-ray crystallographic structure of Torpedo californica acetylcholinesterase (TcAChE) in complex with the bifunctional inhibitor NF595, a potentially new anti-Alzheimer drug, has been solved. For the first time in TcAChE, a major conformational change in the peripheral-site tryptophan residue is observed upon complexation. The observed conformational flexibility highlights the dynamic natur...