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2.3.1.6: choline O-acetyltransferase

This is an abbreviated version!
For detailed information about choline O-acetyltransferase, go to the full flat file.

Word Map on EC 2.3.1.6

Reaction

acetyl-CoA
+
choline
=
CoA
 +
O-acetylcholine

Synonyms

acetyl CoA:choline-O-acetyltransferase, acetyl-CoA:choline-O-acetyltransferase, acetyltransferase, choline, cChAT, chAcT, ChAT, choline acetyl transferase, choline acetylase, choline acetyltransferase, choline-acetyltransferase, pChAT, peripheral type of choline acetyltransferase

ECTree

     2 Transferases
         2.3 Acyltransferases
             2.3.1 Transferring groups other than aminoacyl groups
                2.3.1.6 choline O-acetyltransferase

Inhibitors

Inhibitors on EC 2.3.1.6 - choline O-acetyltransferase

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INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
1-(azepan-1-yl)-3-[(8-ethyl-4a,5-dihydro-4H-[1,2,4]triazino[5,6-b]indol-3-yl)sulfanyl]propan-1-one
the amide carbonyl of the compound forms a hydrogen bond with the Ser540 amino acid residue of ChAT with a distance of 2.15 A. The 5H-[1,2,4]triazino[5,6-b]indole nucleus forms a hydrogen bond with the Gly329 amino acid residue of ChAT active site
1-[2-[(naphthalen-1-yl)amino]-1,3-thiazole-4-carbonyl]-N-(propan-2-yl)piperidine-4-carboxamide
the terminal amide carbonyl forms a hydrogen bond with Ser438 at a distance of 1.88 A, while the thiazole nucleus forms pi_pi interactions with the Tyr436 amino acid residue of the active site of ChAT
2-(alpha-naphthoyl) ethyltrimethylammonium iodide
i.e. alpha-NETA, commercially available inhibitor. The naphthyl group forms pi-pi interaction with residue Tyr552, while the quaternary trimethyl ammonium moiety is closely surrounded by His324, Pro98, Asp328 residues. The naphthyl moiety is accommodated in a pocket consisting of Asn95, Pro554, Gly553, Thr539, and Ser538 residues. The determined IC50 values are 34.18 microM for acetylcholinesterase and 33.30 microM for butanoylcholinesterase
2-[[5-(furan-2-yl)-1H-1,2,4-triazol-3-yl]sulfanyl]-1-[4-(propan-2-yl)phenyl]ethan-1-one
compound makes the His324 residue inaccessible for the catalysis
3-Bromoacetonyltrimethylammonium bromide
-
-
3-Bromoacetonyltrimethylammonium ion
3-Chloro-4-stilbazole
3-trimethylammoniomethylcatechol
-
-
4-(1-Naphthylvinyl)pyridine
5,5'-dithiobis(2-nitrobenzoate)
Acetylaminocholine
-
-
Acetylcholine
Acyloylcholine
amyloid beta peptide
-
the aggregated form of A-beta 25-35 decreased significantly enzyme activity only in the aged striatum
-
arachidonic acid
-
-
beta-amyloid
-
-
bromo-acetylcholine
bromoacetyl-S-CoA
-
-
bromoacetylcholine
Catecholine
-
-
CdCl2
-
-
Chloroacetylcholine
Chlorocholine
-
-
choline
-
-
Choline mustard aziridinium salt
coenzyme A
CuSO4
-
-
dexamethasone
-
-
Diethylaminoethanol
-
-
diethyldicarbonate
Drosophila sp. (in: flies)
-
-
domoic acid
-
-
ethylenimine
-
-
Flubenzimine
-
i.e. N-[3-phenyl-4,5-bis[(trifluoromethyl)immino]-2-thiazolidinylidene]benzenamine
glutamate
-
-
Hg2+
-
noncompetitive with respect to choline, IC50: 0.0004 mM, mixed type inhibition with respect to acetyl-CoA, IC50: 0.0025 mM, activity can be recovered using 2,3-dimercapto-propanol
HgCl2
-
-
iodoacetamide
-
-
iodoacetate
kainate
-
-
N,N-Dimethylaminoethyl acrylate
-
-
N,N-Dimethylaminoethyl bromoacetate
-
-
N,N-Dimethylaminoethyl chloroacetate
-
-
N-ethylmaleimide
N-Methyl-4-(1-naphthylvinyl)pyridine
nerve growth factor
-
nerve growth factor, under specific development conditions, leads to a paradoxical down-regulation of the enzyme
-
ocadaic acid
p-chloromercuribenzoate
phenylacetate
-
-
phenylacetyl-CoA
-
-
phenylbutyrate
-
-
Phenylmethanesulfonylfluoride
pilocarpine
quisqualate
-
-
Reactive blue 2
Styrylpyridinium salts
thioctic acid
-
it is proposed that dihydrolipoic acid serves an essential role in the regulation of the activity of the the enzyme and that the ratio of reduced to oxidized lipoic acid in the cell may play an important role in the regulation of the activity of the enzyme
veratridine
-
-
Zinc acetate
-
-
[2-[3-(2-Ammonioethoxy)-benzoyl]ethyl]trimethylammonium bromide
-
-
additional information
-