In Alzheimer's disease, both acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) colocalize with brain fibrils of amyloid-beta (Abeta) peptides, and synaptic AChE-S facilitates fibril formation by association with insoluble Abeta fibrils. Here, we report that human BChE and BSP41, a synthetic peptide derived from the BChE C terminus, inversely associate with the soluble Abeta conformer...

Brain-Mind Project and University of Miami School of Medicine, Miami, FL, Departments of Medicine, Anatomy and Neurobiology, Dalhousie University, Halifax, Nova Scotia, Canada, Drug Design & Development Section, Laboratory of Neurosciences, Intramural Research Program, National Institute on Aging, Baltimore, MD, and Laboratory for Neurodegenerative and Aging Research, Harvard Medical School, Be...

Acetylcholinesterase (AChE) inhibitors are widely used for the symptomatic treatment of Alzheimer's disease and other dementias. More recent use is for myasthenia gravis. Many of these inhibitors interact with the second known cholinesterase, butyrylcholinesterase (BChE). Further, evidence shows that acetylcholine plays a role in suppression of cytokine release through a "cholinergic anti-infla...

A new tacrine based cholinesterase inhibitor, N-(bromobut-3-en-2-yl)-7-methoxy-1,2,3,4-tetrahydroacridin-9-amine (1), was designed and synthesized to interact with specific regions of human acetylcholinesterase and human butyrylcholinesterase. Its inhibitory ability towards cholinesterases was determined and compared to tacrine (THA) and 9-amino-7-methoxy-1,2,3,4-tetrahydroacridine (7-MEOTA). T...

Approximately, two-thirds patients with Alzheimer’s disease (AD) are reported to have homozygous wild-type butyrylcholinesterase (BuChE) gene expression. It is associated with a higher rate of hydrolysis of acetylcholine, which ultimately leads to increase in the levels of BuChE in advanced stages of the disease. Rivastigmine, a dual inhibitor of acetylcholinesterase (AChE) and BuChE, might be ...

In 1986, Whittaker wrote ‘Churchill-Davidson’s editorial entitled “The succinylcholine story” in 1963, highlighted probably for the first time in the UK, the role of serum protein polymorphism in drug sensitivity’ [1]. Following a series of detailed family studies, in 1959 Kalow [2] concluded that individuals who had prolonged apnoea following succinylcholine administration were homozygous for ...

Enzymes acetylcholinesterase (AChE; E.C. 3.1.1.7) and butyrylcholinesterase (BChE; E.C. 3.1.1.8) have intensively been investigated in biomedicine and toxicology due to important role in organisms. Even if structurally homologous, they differ in catalytic activity, specificity, for substrates, and selectivity in binding to many ligands. This paper compiles the results of research on cholinester...