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Literature summary for 3.1.1.8 extracted from

  • Saxena, A.; Fedorko, J.M.; Vinayaka, C.R.; Medhekar, R.; Radic, Z.; Taylor, P.; Lockridge, O.; Doctor, B.P.
    Aromatic amino-acid residues at the active and peripheral anionic sites control the binding of E2020 (Aricept) to cholinesterases (2003), Eur. J. Biochem., 270, 4447-4458.
    View publication on PubMed
Search for more literature for 3.1.1.8

Protein Variants

Protein Variants Comment Organism
A277W mutation does not affect binding of E2020 Homo sapiens
A328F altered Ki for E2020 Homo sapiens
A328Y Ki for E2020 similar to wild-type enzyme Homo sapiens
D70G altered Ki for E2020 Homo sapiens
Q119Y altered Ki for E2020 Homo sapiens
Q119Y/V288F/A328Y altered Ki for E2020 Homo sapiens
V288F Ki for E2020 similar to wild-type enzyme Homo sapiens
W82A altered Ki for E2020 Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(R,S)-1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride E2020, acetylcholinesterase inhibitor used in treatment of Alzheimer's disease, interacts with the active site and the peripheral anionic site of the enzyme Equus caballus
(R,S)-1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride E2020, acetylcholinesterase inhibitor used in treatment of Alzheimer's diaease, inhibition kinetics Homo sapiens
7(R,S)-1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride
-
 Equus caballus

Organism

Organism UniProt Comment Textmining
Equus caballus
-
-
-
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
butyrylthiocholine + H2O
-
 Homo sapiens thiocholine + butyrate
-
 ?
butyrylthiocholine + H2O
-
 Equus caballus thiocholine + butyrate
-
 ?

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00064
-
 7(R,S)-1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride pH 8, 25°C Equus caballus
0.0008
-
 (R,S)-1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride pH 8, 25°C, Q119Y/V288F/A328Y mutant Homo sapiens
0.00111
-
 (R,S)-1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride pH 8, 25°C, wild-type enzyme Homo sapiens
0.0024
-
 (R,S)-1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride pH 8, 25°C, A277W mutant Homo sapiens
0.0035
-
 (R,S)-1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride pH 8, 25°C, V288F mutant Homo sapiens
0.0039
-
 (R,S)-1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride pH 8, 25°C, A328Y mutant Homo sapiens
0.0129
-
 (R,S)-1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride pH 8, 25°C, Q119Y mutant Homo sapiens
0.0228
-
 (R,S)-1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride pH 8, 25°C, A328F mutant Homo sapiens
0.03
-
 (R,S)-1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride pH 8, 25°C, D70G mutant Homo sapiens
0.12
-
 (R,S)-1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride pH 8, 25°C, W82A mutant Homo sapiens