3.5.1.13: aryl-acylamidase
This is an abbreviated version!
For detailed information about aryl-acylamidase, go to the full flat file.
Word Map on EC 3.5.1.13
-
3.5.1.13
-
acetylcholinesterase
-
aaa
-
cholinesterases
-
o-nitroacetanilide
-
buche
-
acetanilid
-
eserine
-
serotonin-sensitive
-
propanil
-
3.1.1.8
-
neostigmine
-
pharmacology
-
acylanilide
-
diagnostics
- 3.5.1.13
- acetylcholinesterase
- aaa
- cholinesterases
- o-nitroacetanilide
- buche
-
acetanilid
- eserine
-
serotonin-sensitive
- propanil
-
3.1.1.8
- neostigmine
- pharmacology
-
acylanilide
- diagnostics
Reaction
Synonyms
AAA, aryl acylamidase, aryl acylaminidase, Azl13, EC 3.5.1.13 AAA-2, EC 3.5.1.13, AAA-1, M-1 amidase, More, PamH, polyamidase, pseudocholinesterase
ECTree
3.5.1.13 aryl-acylamidaseAdvanced search results
results (
results (Inhibitors
Inhibitors on EC 3.5.1.13 - aryl-acylamidase
Please wait a moment until all data is loaded. This message will disappear when all data is loaded.
top
INHIBITOR 
ORGANISM
UNIPROT
COMMENTARY 
LITERATURE
IMAGE
1,5-bis(4-allyl-dimethylammonium-phenyl)pentan-3-one-dibromide
-
i.e. BW284c51, inhibition is more pronounced at older developmental stages
6-hydroxy-tetrahydroharman
-
slight inhibition of enzyme form AAA-1 and AAA-2
diisopropylfluorophosphate
-
complete inhibition of aryl acylacylamidase activity of fatty acid free human albumin at 2 mM, covalent binding to the catalytic site Tyr411
edrophonium
activity is reduced to 64.1% and 30.7% at 0.1 and 0.5 mM. Edrophonium inhibits esterase activity and aryl acylamidase activity of acetylcholinesterase
fatty acid
-
fatty acids block aryl acylamidase activity competing with amides for binding in the catalytic domain
N-Acetylimidazole
-
stimulation at low concentrations, inactivation at high concentration
N-benzyl-N-dodecyl-N,N-dimethylammonium chloride
-
inhibitor at low substrate concentrations
puromycin
-
competitive inhibition of hydrolysis L-Ala-4-nitroanilide
pyridoxal 5'-phosphate
-
inactivates aryl acylamidase activity and acetylcholinesterase activity in absence of acetylcholine or 1,5-bis[4-(allyl-dimethylammonium)phenyl]pentan-3-one. Presence of acetylcholine or 1,5-bis[4-(allyl-dimethylammonium)phenyl]pentan-3-one prevents loss of acetylcholinesterase activity but not of aryl acylamidase activity
Tetranitromethane
-
stimulation at low concentrations, inactivation at high concentration
1,2,3,4-tetrahydro-beta-carboline
-
competitive inhibition of AAA-1, slight inhibition of enzyme form AAA-2
2-bromo-lysergic acid diethylamide
-
marked inhibition of enzyme form AAA1 at pH 7.5, moderate inhibition of enzyme form AAA-1 at pH 5.5
2-Hydroxy-5-nitrobenzyl bromide
-
inactivates aryl acylamidase activity and acetylcholinesterase activity in absence of acetylcholine or 1,5-bis[4-(allyl-dimethylammonium)phenyl]pentan-3-one. Presence of acetylcholine or 1,5-bis[4-(allyl-dimethylammonium)phenyl]pentan-3-one prevents loss of acetylcholinesterase activity but not of aryl acylamidase activity
Acetic anhydride
-
stimulation at low concentrations, inactivation at high concentration
Acetic anhydride
-
inactivates aryl acylamidase activity and acetylcholinesterase activity in absence of acetylcholine or 1,5-bis[4-(allyl-dimethylammonium)phenyl]pentan-3-one. Presence of acetylcholine or 1,5-bis[4-(allyl-dimethylammonium)phenyl]pentan-3-one prevents loss of acetylcholinesterase activity but not of aryl acylamidase activity
Acetylcholine
-
serotonin-sensitive aryl acylamidase is inhibited, serotonin-insensitive aryl acylamidase is not inhibited
BW284c51
-
the specific AChE inhibitor inhibits the aryl amidase activity of acetylcholinesterase to a higher extent than the acetylcholinesterase activity
BW284c51
dual site binder, interacts with PAS and the active site of acetylcholinesterase, thus inhibiting both the activities (esterase and aryl acylamidase)
d-lysergic acid diethylamide
-
marked inhibition of enzyme form AAA1 at pH 7.5, moderate inhibition of enzyme form AAA-1 at pH 5.5
diethyl dicarbonate
-
inactivates aryl acylamidase activity and acetylcholinesterase activity in absence of acetylcholine or 1,5-bis[4-(allyl-dimethylammonium)phenyl]pentan-3-one. Presence of acetylcholine or 1,5-bis[4-(allyl-dimethylammonium)phenyl]pentan-3-one prevents loss of acetylcholinesterase activity and of aryl acylamidase activity
diisopropylphosphofluoridate
-
complete inhibition at 1 mM , scarcely inhibited at 0.1 mM
eserine
-
0.001 mM, nearly complete inhibition of serum and erythrocyte enzyme, liver enzyme is unaffected
iso-ompa
-
i.e. tetra-isopropyl-pyrophosphoramide, specific inhibitor for BChE, inhibits also the aryl amidase activity
iso-ompa
-
inhibitor of butyrylcholinesterase (BChE), also inhibits aryl acylamidase activity
neostigmine
-
0.01 mM, nearly complete inhibition of serum and erythrocyte enzyme, liver enzyme is unaffected
neostigmine
-
inhibition of enzyme form AAA-2, no effect of enzyme form AAA-1
neostigmine bromide
-
i.e. 1,5-bis(4-allyldimethylammoniumphenyl)pentan-3-one dibromide or BW284C5
neostigmine bromide
-
i.e. 1,5-bis(4-allyldimethylammoniumphenyl)pentan-3-one dibromide or BW284C5
serotonin
-
inhibitor of butyrylcholinesterase (BChE), also inhibits aryl acylamidase activity
serotonin
serotonin inhibits aryl acylamidase while remaining ineffective against the esterase activity. It interacts with D74, N87, L76 and T83 residues of the side door
serotonin
-
serotonin-sensitive aryl acylamidase, serotonin-insensitive aryl acylamidase is not inhibited
serotonin
-
enzyme from brain is inhibited, liver enzyme is not inhibited; non-competitive
serotonin creatinine sulfate
-
moderate inhibition of enzyme form AAA-1 at pH 7.5, no inhibition of enzyme form AAA-2 at pH 5.5
Trinitrobenzenesulfonic acid
-
inactivates aryl acylamidase activity and acetylcholinesterase activity in absence of acetylcholine or 1,5-bis[4-(allyl-dimethylammonium)phenyl]pentan-3-one. Presence of acetylcholine or 1,5-bis[4-(allyl-dimethylammonium)phenyl]pentan-3-one prevents loss of acetylcholinesterase activity but not of aryl acylamidase activity
tryptamine
-
slight inhibition of enzyme form AAA-1 at pH 7.5, no inhibition of enzyme form AAA-2 at pH 5.5
additional information
-
the aryl acylamidase activity is associated with acetylcholinesterase in chicken embryonic brain, and is much more sensitive to Alzheimer drugs, huperzine and donepezil, especially at younger developmental stages, than the esterase activity of the acetylcholinesterase, whereas inhibition of esterase activity is sensitive to tacrine and DFP
-
additional information
by molecular docking studies the most favourable binding site of aryl acylamidase substrates and serotonin is identified as the side door of acetylcholinesterase. Propidium, a peripheral anionic site binder blocks the main door without affecting the side door, which explains its ineffectiveness in inhibiting aryl acylamidase
-
additional information
gallamine selectively inhibits the esterase activity to 63.6% (0.1 mM) and 45.4% (0.5 mM), whereas the aryl acylamidase activity remains significantly unaltered in the presence of gallamine (0.1 mM: 105.2%. 0.5 mM: 107%)
-
additional information
-
phosphatidylinositol-specific phospholipase C of Staphylococcus aureus or sodium deoxycholate-activated endogenous phospholipase C solubilizes serotonin-sensitive arylacylamidase , a loss of activity occurs which can be restored by externally added phosphatidylinositol
-
additional information
no effect by EDTA, 8-hydroxyquinoline, and 2-mercaptoethanol
-
