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Literature summary for 3.1.1.8 extracted from

  • Darvesh, S.; Darvesh, K.V.; McDonald, R.S.; Mataija, D.; Walsh, R.; Mothana, S.; Lockridge, O.; Martin, E.
    Carbamates with differential mechanism of inhibition toward acetylcholinesterase and butyrylcholinesterase (2008), J. Med. Chem., 51, 4200-4212.
    View publication on PubMed
Search for more literature for 3.1.1.8

Protein Variants

Protein Variants Comment Organism
A328F the mutant is more sensitive to aryl phenothiazine carbamate inhibitors and deactivation, i.e. 4-biphenyl phenothiazine carbamate, compared to the wild-type enzyme Homo sapiens
A328W the mutant is more sensitive to aryl phenothiazine carbamate inhibitors and deactivation, i.e. 4-biphenyl phenothiazine carbamate, compared to the wild-type enzyme Homo sapiens
A328Y the mutant is more sensitive to aryl phenothiazine carbamate inhibitors and deactivation, i.e. 4-biphenyl phenothiazine carbamate, compared to the wild-type enzyme Homo sapiens
A539T the mutant is more sensitive to aryl phenothiazine carbamate inhibitors and deactivation, i.e. 4-biphenyl phenothiazine carbamate, compared to the wild-type enzyme Homo sapiens
D70G the mutant is more sensitive to aryl phenothiazine carbamate inhibitors and deactivation, i.e. 4-biphenyl phenothiazine carbamate, compared to the wild-type enzyme Homo sapiens
F329A the mutant is more sensitive to aryl phenothiazine carbamate inhibitors and deactivation, i.e. 4-biphenyl phenothiazine carbamate, compared to the wild-type enzyme Homo sapiens
Y332A the mutant is more sensitive to aryl phenothiazine carbamate inhibitors and deactivation, i.e. 4-biphenyl phenothiazine carbamate, compared to the wild-type enzyme Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
1-naphthyl phenothiazine carbamate
-
 Homo sapiens
2-(1-piperidinyl)ethyl phenothiazine carbamate
-
 Homo sapiens
2-(1-pyrrolidinyl)ethyl phenothiazine carbamate
-
 Homo sapiens
2-(4-morpholino)ethyl phenothiazine carbamate
-
 Homo sapiens
2-(diethylamino)ethyl 10H-phenothiazine-10-carboxylate
-
 Homo sapiens
2-(dimethylamino)ethyl 10H-phenothiazine-10-carboxylate
-
 Homo sapiens
2-chlorophenyl phenothiazine carbamate
-
 Homo sapiens
2-methoxyphenyl phenothiazine carbamate
-
 Homo sapiens
2-methylphenyl phenothiazine carbamate
-
 Homo sapiens
2-naphthyl phenothiazine carbamate
-
 Homo sapiens
2-t-butylphenyl phenothiazine carbamate
-
 Homo sapiens
3-(diethylamino)propyl 10H-phenothiazine-10-carboxylate
-
 Homo sapiens
3-(N,N-dimethylamino) phenyl phenothiazine carbamate binding by residues F329 and Y332, structure, overview Homo sapiens
3-chlorophenyl phenothiazine carbamate
-
 Homo sapiens
3-methoxyphenyl phenothiazine carbamate
-
 Homo sapiens
3-methylphenyl phenothiazine carbamate
-
 Homo sapiens
4-biphenyl phenothiazine carbamate
-
 Homo sapiens
4-chlorophenyl phenothiazine carbamate
-
 Homo sapiens
4-methoxyphenyl phenothiazine carbamate
-
 Homo sapiens
4-methylphenyl phenothiazine carbamate
-
 Homo sapiens
4-t-butylphenyl phenothiazine carbamate
-
 Homo sapiens
butyl carbamate
-
 Homo sapiens
cyclopentyl phenothiazine carbamate
-
 Homo sapiens
donepezil
-
 Homo sapiens
ethyl carbamate
-
 Homo sapiens
galanthamine
-
 Homo sapiens
iso-propyl carbamate
-
 Homo sapiens
methyl carbamate
-
 Homo sapiens
additional information inhibitor molecular mechanics calculations, general mechanism of pseudoirreversible cholinesterase inhibition by carbamates. Enzyme deactivation is initiated by nucleophilic attack of the catalytic triad serine oxygen on the carbonyl group of the carbamate, structure-activity relationships of wild-type and mutant enzymes, overview Homo sapiens
phenyl phenothiazine carbamate
-
 Homo sapiens
propyl phenothiazine carbamate
-
 Homo sapiens
rivastigmine
-
 Homo sapiens
tert-butyl 10H-phenothiazine-10-carboxylate
-
 Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
extracellular
-
 Homo sapiens
-
-

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
plasma
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
butyrylthiocholine + H2O detection using 5,5'-dithiobis(2-nitrobenzoic acid) Homo sapiens butyrate + thiocholine
-
 ?

Synonyms

Synonyms Comment Organism
BuChE
-
 Homo sapiens
butyrylcholinesterase
-
 Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
23
-
 assay at Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
additional information
-
 additional information molecular mechanics calculations and inhibition kinetics, overview Homo sapiens
0.0006
-
 2-(diethylamino)ethyl 10H-phenothiazine-10-carboxylate 23°C Homo sapiens
0.00065
-
 2-(1-pyrrolidinyl)ethyl phenothiazine carbamate 23°C Homo sapiens
0.00074
-
 3-(diethylamino)propyl 10H-phenothiazine-10-carboxylate 23°C Homo sapiens
0.0024
-
 2-(4-morpholino)ethyl phenothiazine carbamate 23°C Homo sapiens
0.0025
-
 2-(dimethylamino)ethyl 10H-phenothiazine-10-carboxylate 23°C Homo sapiens
0.0032
-
 2-(1-piperidinyl)ethyl phenothiazine carbamate 23°C Homo sapiens
0.0032
-
 cyclopentyl phenothiazine carbamate 23°C Homo sapiens
0.0043
-
 tert-butyl 10H-phenothiazine-10-carboxylate 23°C Homo sapiens
0.0102
-
 methyl carbamate 23°C Homo sapiens
0.0134
-
 n-butyl carbamate 23°C Homo sapiens
0.0181
-
 iso-propyl carbamate 23°C Homo sapiens
0.0234
-
 ethyl carbamate 23°C Homo sapiens
0.26
-
 propyl phenothiazine carbamate 23°C Homo sapiens