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Literature summary for 3.1.1.7 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 3.1.1.7

Protein Variants

Protein Variants Comment Organism
D74N altered Ki for E2020 Mus musculus
F295L altered Ki for E2020 Mus musculus
F297I altered Ki for E2020 Mus musculus
W286A altered Ki for E2020 Mus musculus
W86A altered Ki for E2020 Mus musculus
Y124Q altered Ki for E2020 Mus musculus
Y337A altered Ki for E2020 Mus musculus
Y337F altered Ki for E2020 Mus musculus
Y72N altered Ki for E2020 Mus musculus
Y72N/Y124N/W286R altered Ki for E2020 Mus musculus

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 diaease, inhibition kinetics Mus musculus
(R,S)-1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride E2020, acetylcholinesterase inhibitor used in treatment of Alzheimer's diaease, interacts with the active site and the peripheral anionic site of the enzyme Tetronarce californica

Organism

Organism UniProt Comment Textmining
Mus musculus
-
-
-
Tetronarce californica
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
acetylthiocholine + H2O
-
 Tetronarce californica thiocholine + acetate
-
 ?
butyrylthiocholine + H2O
-
 Mus musculus thiocholine + butyrate
-
 ?

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0000004
-
 (R,S)-1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride pH 8, 25°C, Y337A mutant Mus musculus
0.0000005
-
 (R,S)-1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride pH 8, 25°C, Y337F mutant Mus musculus
0.0000022
-
 (R,S)-1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride pH 8, 25°C, wild-type enzyme Mus musculus
0.0000031
-
 (R,S)-1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride pH 8, 25°C Tetronarce californica
0.00002
-
 (R,S)-1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride pH 8, 25°C, Y124Q mutant Mus musculus
0.00002
-
 (R,S)-1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride pH 8, 25°C, Y72N mutant Mus musculus
0.000027
-
 (R,S)-1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride pH 8, 25°C, F295L mutant Mus musculus
0.00007
-
 (R,S)-1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride pH 8, 25°C, F297I mutant Mus musculus
0.00069
-
 (R,S)-1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride pH 8, 25°C, W86A mutant Mus musculus
0.0032
-
 (R,S)-1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride pH 8, 25°C, W286A mutant Mus musculus
0.0051
-
 (R,S)-1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride pH 8, 25°C, D74N mutant Mus musculus
0.0087
-
 (R,S)-1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride pH 8, 25°C, Y72N/Y124N/W286R mutant Mus musculus