Crystal structures of human cholinesterases in complex with huprine W and tacrine: elements of specificity for anti-Alzheimer's drugs targeting acetyl-and butyryl …

F Nachon, E Carletti, C Ronco, M Trovaslet… - Biochemical …, 2013 - portlandpress.com
The multifunctional nature of Alzheimer's disease calls for MTDLs (multitarget-directed
ligands) to act on different components of the pathology, like the cholinergic dysfunction and …

Acetylcholinesterase: a multifaceted target for structure-based drug design of anticholinesterase agents for the treatment of Alzheimer's disease

HM Greenblatt, H Dvir, I Silman, JL Sussman - Journal of Molecular …, 2003 - Springer
The structure of Torpedo californica acetylcholinesterase is examined in complex with
several inhibitors that are either in use or under development for treating Alzheimer's …

Structures of human acetylcholinesterase in complex with pharmacologically important ligands

J Cheung, MJ Rudolph, F Burshteyn… - Journal of medicinal …, 2012 - ACS Publications
Human acetylcholinesterase (AChE) is a significant target for therapeutic drugs. Here we
present high resolution crystal structures of human AChE, alone and in complexes with drug …

[HTML][HTML] Comparison of the binding of reversible inhibitors to human butyrylcholinesterase and acetylcholinesterase: A crystallographic, kinetic and calorimetric study

TL Rosenberry, X Brazzolotto, IR Macdonald… - Molecules, 2017 - mdpi.com
Acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) hydrolyze the
neurotransmitter acetylcholine and, thereby, function as coregulators of cholinergic …

3D Structure of Torpedo californica Acetylcholinesterase Complexed with Huprine X at 2.1 Å Resolution:  Kinetic and Molecular Dynamic Correlates,

H Dvir, DM Wong, M Harel, X Barril, M Orozco… - Biochemistry, 2002 - ACS Publications
Huprine X is a novel acetylcholinesterase (AChE) inhibitor, with one of the highest affinities
reported for a reversible inhibitor. It is a synthetic hybrid that contains the 4-aminoquinoline …

Huprine X is a novel high-affinity inhibitor of acetylcholinesterase that is of interest for treatment of Alzheimer's disease

P Camps, B Cusack, WD Mallender, R El Achab… - Molecular …, 2000 - ASPET
Inhibitors of the enzyme acetylcholinesterase (AChE) slow and sometimes reverse the
cognitive decline experienced by individuals with Alzheimer's disease. Huperzine A, a …

Structures of human acetylcholinesterase bound to dihydrotanshinone I and territrem B show peripheral site flexibility

J Cheung, EN Gary, K Shiomi… - ACS medicinal …, 2013 - ACS Publications
Acetylcholinesterase is a critical enzyme that regulates neurotransmission by degrading the
neurotransmitter acetylcholine in synapses of the nervous system. It is an important target for …

Huprine–tacrine heterodimers as anti-amyloidogenic compounds of potential interest against Alzheimer's and prion diseases

C Galdeano, E Viayna, I Sola, X Formosa… - Journal of medicinal …, 2012 - ACS Publications
A family of huprine–tacrine heterodimers has been developed to simultaneously block the
active and peripheral sites of acetylcholinesterase (AChE). Their dual site binding for AChE …

Specific targeting of acetylcholinesterase and butyrylcholinesterase recognition sites. Rational design of novel, selective, and highly potent cholinesterase inhibitors

L Savini, A Gaeta, C Fattorusso… - Journal of Medicinal …, 2003 - ACS Publications
Tacrine-based AChE and BuChE inhibitors were designed by investigating the topology of
the active site gorge of the two enzymes. The homobivalent ligands characterized by a …

[PDF][PDF] Peripheral and dual binding site acetylcholinesterase inhibitors: implications in treatment of Alzheimer's disease

A Castro, A Martinez - Mini reviews in medicinal chemistry, 2001 - researchgate.net
Recently advances in understanding the molecular basis of Alzheimer's disease have led to
the consideration of the relationship between cholinergic inhibitors and amyloid deposition …