Comparison of kinetic parameters for acetylthiocholine, soman, ketamine and fasciculin towards acetylcholinesterase in liposomes and in solution

Automated Docking with Protein Flexibility in the Design of Femtomolar “Click Chemistry” Inhibitors of Acetylcholinesterase

“…The dissociation constant, K d , of the compound 1,5-TZ2/PA6 was determined to be 77 fM with Tc AChE and 410 fM with mAChE. This made 1,5-TZ2/PA6 the most potent noncovalent AChE inhibitor by approximately 2 orders of magnitude . The 1,4-TZ2/PA6 isomer exhibited K d values of between 720 fM with Tc AChE and 14 pM with Ee AChE.…”

Swine models in the design of more effective medical countermeasures against organophosphorus poisoning

“…ChE activity was determined using a radiometric assay (Johnson and Russell, 1975). Ketamine is another anaesthetic known to inhibit acetylcholinesterase (AChE) and it was shown to protect the enzyme from the action of NA like sarin, soman, some OP pesticides and other inhibitors such as the carbamate physostigmine (Puu, 1988;Puu and Koch, 1990;Puu et al, 1991;Kounenis et al, 1994;Koutsoviti-Papadopoulou et al, 1994). During anaesthesia with ketamine, an inhibition of 32 ± 5.8% in ChE activity has been previously reported (Göransson-Nyberg et al, 1995b).…”

How to Catch a Membrane Protein in Action: A Review of Functional Membrane Protein Immobilization Strategies and Their Applications

“…Lipid rigidification can be minimized when proteoliposomes are immobilized by fusion with monolayers on glass surfaces to form bilayers without any chemical cross-linking. To demonstrate the approach, bacteriorhodopsin from purple membranes of Halobacterium halobium was added to a lipid, cholesterol, and octylglucoside mixture, and upon removal of octylglucoside during gel filtration, proteoliposomes were formed by the so-called detergent-depletion technique . Langmuir−Blodgett (LB) lipid monolayers were used to treat platinum/glass surfaces and subsequently converted into bilayers when fused with the bacteriorhodopsin proteoliposomes .…”

“…To demonstrate the approach, bacteriorhodopsin from purple membranes of Halobacterium halobium was added to a lipid, cholesterol, and octylglucoside mixture, and upon removal of octylglucoside during gel filtration, proteoliposomes were formed by the so-called detergentdepletion technique. 43 Langmuir-Blodgett (LB) lipid monolayers 44 were used to treat platinum/glass surfaces and subsequently converted into bilayers when fused with the bacteriorhodopsin proteoliposomes. 45 Bacteriorhodopsin photoactivity in the reconstituted bilayers, monitored by electrochemistry, was comparable to natural membrane fragments containing bacteriorhodpsin on platinum surfaces.…”