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

Pub. Date : 2000 Feb

PMID : 10648652






5 Functional Relationships(s)
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Compound Name
Protein Name
Organism
1 Huprine X is a novel high-affinity inhibitor of acetylcholinesterase that is of interest for treatment of Alzheimer"s disease. huprine acetylcholinesterase (Cartwright blood group) Homo sapiens
2 Huprine X inhibited human AChE with an inhibition constant K(I) of 26 pM, indicating that it binds to this enzyme with one of the highest affinities yet reported. huprine acetylcholinesterase (Cartwright blood group) Homo sapiens
3 The association and dissociation rate constants for huprine X with AChE were determined, and the location of its binding site on the enzyme was probed in competition studies with the peripheral site inhibitor propidium and the acylation site inhibitor edrophonium. huprine acetylcholinesterase (Cartwright blood group) Homo sapiens
4 In contrast, huprine X did form a ternary complex with propidium and AChE, although its affinity for the free enzyme was found to be 17 times its affinity for the propidium-AChE complex. huprine acetylcholinesterase (Cartwright blood group) Homo sapiens
5 In contrast, huprine X did form a ternary complex with propidium and AChE, although its affinity for the free enzyme was found to be 17 times its affinity for the propidium-AChE complex. huprine acetylcholinesterase (Cartwright blood group) Homo sapiens