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Literature summary for 3.1.1.7 extracted from

  • Mohammed, A.; Sneathen, J.; Frojen, S.G.; Kuo, L.; Dupureur, C.M.
    Stereospecific cholinesterase inhibition by O,S-diethylphenylphosphonothioate (2017), Bioorg. Med. Chem., 25, 3053-3058 .
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
cyclophostin
-
Electrophorus electricus
cyclophostin
-
Homo sapiens
leptophos
-
Electrophorus electricus
leptophos
-
Homo sapiens
methamidophos
-
Electrophorus electricus
methamidophos
-
Homo sapiens
O-ethyl-S-[2-(diisopropylamino)-ethyl]-methylphosphonothioate nerve agent VX Electrophorus electricus
O-ethyl-S-[2-(diisopropylamino)-ethyl]-methylphosphonothioate nerve agent VX Homo sapiens
paraoxon
-
Electrophorus electricus
paraoxon
-
Homo sapiens
R-DEPP O,S-diethylphenylphosphonothioate, both S- and R-DEPP are poor inhibitors of eel AChE, stereospecific inhibition kinetics and stereospecificity of the chiral nerve agent derivative. Kinetic analysis of S-DEPP with cholinesterases Electrophorus electricus
R-DEPP O,S-diethylphenylphosphonothioate, stereospecific inhibition kinetics and stereospecificity of the chiral nerve agent derivative O,S-diethylphenylphosphonothioate. Chemical modification by DEPP, a measurable amount of the enzyme-phosphonate adduct does not undergo aging Homo sapiens
S-DEPP O,S-diethylphenylphosphonothioate, both S- and R-DEPP are poor inhibitors of eel AChE, stereospecific inhibition kinetics and stereospecificity of the chiral nerve agent derivative Electrophorus electricus
S-DEPP O,S-diethylphenylphosphonothioate, stereospecific inhibition kinetics and stereospecificity of the chiral nerve agent derivative O,S-diethylphenylphosphonothioate. Chemical modification by DEPP, a measurable amount of the enzyme-phosphonate adduct does not undergo aging. Pralidoxime, a common rescue agent, affects a modest recovery of eqBChE from treatment with S-DEPP. S-DEPP inhibition is practically irreversible. Kinetic analysis of S-DEPP with cholinesterases Homo sapiens
sarin
-
Electrophorus electricus
sarin
-
Homo sapiens
soman
-
Electrophorus electricus
soman
-
Homo sapiens
Tabun
-
Electrophorus electricus
Tabun
-
Homo sapiens
thiomethylcyclosarin
-
Electrophorus electricus
thiomethylcyclosarin
-
Homo sapiens
thiomethylsarin
-
Electrophorus electricus
thiomethylsarin
-
Homo sapiens
thiomethylsoman
-
Electrophorus electricus
thiomethylsoman
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Electrophorus electricus O42275
-
-
Homo sapiens P22303
-
-

Source Tissue

Source Tissue Comment Organism Textmining
commercial preparation
-
Homo sapiens
-
commercial preparation
-
Electrophorus electricus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
acetylthiocholine + H2O
-
Homo sapiens thiocholine + acetate
-
?
acetylthiocholine + H2O
-
Electrophorus electricus thiocholine + acetate
-
?

Synonyms

Synonyms Comment Organism
AChE
-
Electrophorus electricus
eeAChE
-
Electrophorus electricus
hAChE
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
25
-
assay at Homo sapiens
25
-
assay at Electrophorus electricus

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
8
-
assay at Homo sapiens
8
-
assay at Electrophorus electricus

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.008
-
S-DEPP pH 8.0, 25°C Homo sapiens
0.15
-
R-DEPP pH 8.0, 25°C Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.145
-
pH 8.0, 25°C Electrophorus electricus S-DEPP
0.165
-
pH 8.0, 25°C Electrophorus electricus R-DEPP