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2.3.1.87: aralkylamine N-acetyltransferase

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

Word Map on EC 2.3.1.87

Reaction

acetyl-CoA
+
a 2-arylethylamine
=
CoA
 +
an N-acetyl-2-arylethylamine

Synonyms

AA-NAT, AANAT, AANAT1, AANAT2, AANAT3, AANATL7, AATNATL2, acetyl-CoA:aralkylamine N-acetyltransferase, acetyltransferase, arylalkylamine N-, arylalkylamine N-acetyltransferase, arylalkylamine N-acetyltransferase 1, arylalkylamine N-acetyltransferase 1a, arylalkylamine N-acetyltransferase 1b, arylalkylamine N-acetyltransferase 2, arylalkylamine N-acetyltransferase like 7, arylalkylamine N-acetyltransferase-2, Bm-iAANAT, Eis, hAANAT, More, MSMEG_3513, N-acetyltransferase, NAT, oAANAT, PA4534, PaaNAT, Rv2416c, serotonin acetylase, serotonin acetyltransferase, serotonin N-acetyltransferase, serotonin-N-acetyltransferase, SNA, SNAT, SNAT1, SNAT2

ECTree

     2 Transferases
         2.3 Acyltransferases
             2.3.1 Transferring groups other than aminoacyl groups
                2.3.1.87 aralkylamine N-acetyltransferase

Inhibitors

Inhibitors on EC 2.3.1.87 - aralkylamine N-acetyltransferase

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INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
2-bromo-N-[2-(5-fluoro-1-benzothien-3-yl)ethyl]acetamide
-
IC50: 0.00039 mM
9-carboxy-11-nor-delta-9-tetrahydrocannabinol
significantly reduces norepinephrine-induced arylalkylamine N-acetyltransferase activity
acetyl-CoA-tryptamine
alpha-trifluoromethyltryptamine
-
modest, competitive
bromoacetyltryptamine
cannabidiol
significantly reduces norepinephrine-induced arylalkylamine N-acetyltransferase activity
cannabinoid
cannabinoids inhibit AANAT activity and attenuate melatonin biosynthesis through intracellular actions without involvement of classical cannabinoid receptor-dependent signaling cascades
cannabinol
significantly reduces norepinephrine-induced arylalkylamine N-acetyltransferase activity
catechin
-
poorest inhibitor tested, 0.1 mM, 1.6fold inhibition of isoform SNAT1 at 0.1 mM
CoA-S-N-acetyl-7-hydroxynaphthylethylamine
fluorescent variant of CoA-T, a bisubstrate inhibitor, synthesis and enzyme binding structure, molecular modelling, overview
CoA-S-N-acetyltryptamine
total inhibition of N-acetyldopamine synthesis in presence of acetyl coenzyme-A and dopamine occurs in the presence of CoA-S-N-acetyltryptamine in liver
desulfo-CoA
-
dead end inhibitor analog, competitive versus CoA
Disulfides
fisetin
-
-
glutathione
reversible, acetyl-CoA protects
kaempferol
-
-
luteolin
-
-
Melatonin
methyl 3-[2-[(bromoacetyl)amino]ethyl]-1-benzothiophene-5-carboxylate
-
IC50: 0.00225 mM
morin
myricetin
N-acetylserotonin
IC50: 0.68 mM; very slightly
N-ethylmaleimide
irreversible, acetyl-CoA protects
N-[2-(2-benzyl-5-methoxy-benzofuran-3-yl)ethyl]iodoacetamide
-
IC50: 0.0087 mM
N-[2-(2-phenyl-benzo [b]thiophen-3-yl)ethyl]bromoacetamide
-
IC50: 0.001 mM
N-[2-(3-ethyl-7-methoxy-napht-1-yl)ethyl]iodoacetamide
-
IC50: 0.0006 mM
N-[2-(5-bromo-benzo[b]thiophen-3-yl)ethyl]bromoacetamide
-
IC50: 0.00378 mM
N-[2-(5-chloro-benzo[b]thiophen-3-yl)ethyl]bromoacetamide
-
IC50: 0.00018 mM
N-[2-(5-ethyl-1-benzothien-3-yl)ethyl]-2-iodoacetamide
-
IC50: 0.002 mM
N-[2-(5-ethyl-benzo[b]thiophen-3-yl)ethyl]bromoacetamide
-
IC50: 0.00071 mM
N-[2-(5-fluoro-1H-indol-3-yl)ethyl]bromoacetamide
-
IC50: 0.0056 mM
N-[2-(5-hydroxy-benzo[b]thiophen-3-yl)ethyl]bromoacetamide
-
IC50: 0.00018 mM
N-[2-(7-ethyl-1,2,3,4-tetrahydronapht-1-yl)ethyl]iodooacetamide
-
IC50: above 0.1 mM
N-[2-(7-ethyl-napht-1-yl)ethyl]-bromoacetamide
-
IC50: 0.00177 mM
N-[2-(7-hydroxy-naphth-1-yl)ethyl]bromoacetamide
-
IC50: 0.00072 mM
N-[2-(7-methoxy-3-(3-trifluoromethylphenyl)-napht-1-yl)ethyl]iodoacetamide
-
IC50: 0.045 mM
N-[2-(7-methoxy-8-propenyl-napht-1-yl)ethyl]-iodoacetamide
-
IC50: above 0.1 mM
N-[2-(7-methoxy-napht-1-yl)ethyl]bromoacetamide
-
IC50: 0.002 mM
N-[2-(7-propoxy-napht-1-yl)ethyl]iodoacetamide
-
IC50: 0.0042 mM
oxygen
reversible, acetyl-CoA protects
p-chloro-mercuribenzoate
-
-
Peptides containing a disulfide bond
-
quercetin
S 20251
S 23823
-
S 27244
S 27481
S 28036
serotonin
tryptamine
tryptamine-coenzyme A
a bisubstrate inhibitor, enzyme binding structure, molecular modelling, overview
tryptophol
-
dead end inhibitor analog, competitive versus tryptamine
UV light
-
NAT activity and melatonin content are suppressed by blue light of 450 nm wavelength, no effects of red light at 650 nm.UV radiation has intensity-dependent dual effects on the NAT activity and melatonin content: it is supressing at low intensity and activating at high intensity irradiation, overview
-
additional information
-