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Literature summary for 3.1.1.7 extracted from

  • Bar-On, P.; Millard, C.B.; Harel, M.; Dvir, H.; Enz, A.; Sussman, J.L.; Silman, I.
    Kinetic and structural studies on the interaction of cholinesterases with the anti-Alzheimer drug Rivastigmine (2002), Biochemistry, 41, 3555-3564.
    View publication on PubMed

Crystallization (Commentary)

Crystallization (Comment) Organism
complex with rivastigmine or (-)-S-3-[1-(dimethylamino)ethyl]phenol, hanging drop vapor diffusion method Tetronarce californica

Inhibitors

Inhibitors Comment Organism Structure
(-)-S-3-[1-(dimethylamino)ethyl]phenol competitive reversible inhibitor Tetronarce californica
rivastigmine trade name: Exelon, carbamylates the enzyme, enzyme reactivates spontaneous at a slow rate Drosophila melanogaster
rivastigmine trade name: Exelon, carbamylates the enzyme, enzyme reactivates spontaneously at a slow rate Homo sapiens
rivastigmine trade name: Exelon, carbamylates the enzyme, 10% spontaneous reactivation after 48 h Tetronarce californica
SDZ 212-712 optical isomer of rivastigmine Drosophila melanogaster

Organism

Organism UniProt Comment Textmining
Drosophila melanogaster
-
-
-
Homo sapiens
-
-
-
Tetronarce californica P04058
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
acetylthiocholine + H2O
-
Drosophila melanogaster thiocholine + acetate
-
?
acetylthiocholine + H2O
-
Homo sapiens thiocholine + acetate
-
?
acetylthiocholine + H2O
-
Tetronarce californica thiocholine + acetate
-
?

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0005
-
(-)-S-3-[1-(dimethylamino)ethyl]phenol pH 7.5, 25°C Tetronarce californica