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3.4.11.6: aminopeptidase B

This is an abbreviated version!
For detailed information about aminopeptidase B, go to the full flat file.

Word Map on EC 3.4.11.6

Reaction

release of N-terminal Arg and Lys from oligopeptides when P1' is not Pro. Also acts on arylamides of Arg and Lys =

Synonyms

AAP, ACE2, Aminopeptidase, aminopeptidase B, aminopeptidase, arginine, aminopeptidase-B, Ap-B, APB, Arg-AP, Arg/Lys aminopeptidase, ArgAP, arginine aminopeptidase, arginine-aminopeptidase, arginyl aminopeptidase, arginyl peptidase, arylamidase, arylamidase II, BSAP, chloride-dependent-basic aminopeptidase, Cl--activated arginine aminopeptidase, Cl--activated arinine aminopeptidase, Co(II)-Ap-B, ColAP, cold-active aminopeptidase, Cu(II)-Ap-B, cytosol aminopeptidase, cytosol aminopeptidase IV, DAP BII, dipeptidyl aminopeptidase BII, double-zinc aminopeptidase, EC 3.4.13.6, KAP, L-arginine aminopeptidase, L-RAP, LAPase, leukocyte-derived arginine aminopeptidase, LRAP, lysine-specific aminopeptidase, minopeptidase, More, protease IV, pumAPE, RAP

ECTree

     3 Hydrolases
         3.4 Acting on peptide bonds (peptidases)
             3.4.11 Aminopeptidases
                3.4.11.6 aminopeptidase B

Inhibitors

Inhibitors on EC 3.4.11.6 - aminopeptidase B

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INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(S)-2-((2S,3R)-3-amino-2-hydroxy-4-phenylbutanamido)-4-methylpentanoic acid
-
1,10-phenanthroline
1-methyl cyclohexan bestatin
-
i.e. BE15, strong inhibition
2,2'-dipyridyl
-
-
2,4-dinitrofluorobenzene
-
-
2,6-pyridinedicarboxylate
-
-
2-Chloroethylphosphonic acid
-
-
2-mercaptoethanol
3,4-dichloroisocoumarin
3-[methyl[3-[4-(phenylmethyl)phenoxy]propyl]amino]-propanoic acid
-
4-(dimethylamino)-N-[7-(hydroxyamino)-7-oxoheptyl]benzamide
enzyme binding structure, overview
4-chloromercuribenzoate
-
-
5,5 dithiobis(2-nitrobenzoic acid)
-
1 mM, 74.89% enzyme inhibition
5,5'-dithiobis(2-nitrobenzoate)
8-hydroxyquinoline
-
-
abexinostat
-
Acetate buffer
-
-
actinonin
Ag+
-
complete inhibition at 0.1 mM
amastatin
amino acids
antipain
-
-
Aprotinin
-
34% residual activity at 0.25 mg/ml
apstatin
0.1 mM, 50% inhibition
arginine derivatives
-
with carboxyl or alpha-amino group blocked
arphamemine B
-
-
arphamenine A
Arphamenine B
belinostat
-
bestatin
beta-mercaptoethanol
bipyridine
-
-
Borax-pyruvic acid buffer
-
-
cementoin
-
-
-
citric acid-sodium citrate buffer
-
-
curcumin
-
non-competitive inhibitor
Cyclopeptide OF49-II
-
from Penicillium regulosum, total synthesis
-
cysteine
D,L-Homolysine
-
-
D-Arg
-
-
D-penicillamine
-
-
DFP
5 mM, 25% inhibition. 10 mM, 44% inhibition
dithiothreitol
DX600
-
only blocks human ACE2 activity but not mouse
E-64
-
99% residual activity at 0.1 mM
entinostat
-
ethanol
-
-
ethyliodoacetate
-
-
givinostat
-
Glu-pyrrolidide
0.1 mM, 98% inhibition
glutathione
-
high concentration
Gly-Gly
5 mM, 8% inhibition
HgCl2
-
complete inhibition at 1 mM
iodoacetamide
iodoacetate
-
0.1 mM, complete inactivation
iodobenzoate
-
-
JNJ-26481585
-
kallidin
-
human peptide hormone, 10 microM, Arg 4-methylcoumarin 7-amide hydrolysis: 73.7% (wild-type enzyme)
L-1-tosylamido-2-phenylethylchloromethylketone
-
-
L-Arg
5 mM, 70% inhibition
L-Arg-2-naphthylamide
-
competitive inhibition of hydrolysis of L-Ala-2-naphthylamide, no inhibition vice versa
L-Lys
5 mM, 28% inhibition
L-lysinethiol
-
-
L-Penicillamine
-
-
Leucine hydroxamate
-
-
leucinthiol
-
-
leuhistin
-
40% inhibition at 0.0003 mM, independent on TGF-beta1 activation
leupeptin
mangiferin
-
mixed non-competitive inhibitor
methyl bestatin
-
-
Mg2+
-
slight inhibition at 1 mM
MgCl2
-
0.1 mM MgCl2, 22% inhibition
MLN-4760
mocetinostat
-
N-(6-(2-aminophenylamino)-6-oxyhexyl)-4-methylbenzamide
-
N-alpha-p-Tosyl-L-lysine
-
-
N-alpha-p-tosyl-L-lysine-chloromethyl ketone
-
specific and irreversible inhibitor
N-ethylmaleimide
N-[(2S,3R)-3-amino-2-hydroxy-5-methylhexanoyl]-L-valyl-L-valyl-L-aspartic acid
-
-
N-[1-(R,S)-carboxy-3-phenyl propyl] Ala-Ala-Phe-p-aminobenzoate
-
-
Na+
-
NaCl (0.1-100 mM) has an opposite effect on the EGTA-treated KAP apo-enzyme, it inhibits 13% at 0.1 mM and 100% at 100 mM
NEM
-
13% inhibition at 1 mM
nitrobestatin
-
92.3% inhibition at 0.133 mM
o-phenanthroline
-
the native enzyme is inhibited by 76% at 0.5 mM, the recombinant enzyme is inhibited by 80% at 0.5 mM
p-aminophenylmercuric acetate
-
1 mM, 41.27% enzyme inhibition
p-chloromercuribenzene sulfonic acid
-
-
p-chloromercuribenzoate
p-hydroxymercuriphenyl sulfonic acid
-
1 mM, 72.22% enzyme inhibition
p-Hydroxymercuriphenylsulfonic acid
-
-
panobinostat
-
PCMB
2 mM, complete inactivation
pefabloc
pepstatin
Phe
-
noncompetitive
Phenylmethanesulfonylfluoride
phosphate
-
-
Porphyrindine
-
-
pracinostat
-
pre-elafin
-
-
-
puromycin
resminostat
-
rocilinostat
-
scriptaid
-
suberanilohydroxamic acid
enzyme binding structure, overview
-
Substance P
-
human peptide hormone, 100 microM, Arg 4-methylcoumarin 7-amide hydrolysis: 63.8% (wild-type enzyme); human peptide hormone, 10 microM, Arg 4-methylcoumarin 7-amide hydrolysis: 78% (wild-type enzyme)
tert-butyl bestatin
-
i.e. BE17, the BE15 derivative has a dual inhibitory effect of invasion and motility on tumor and endothelial cells
thioglycolic acid
-
-
trichostatin A
-
Valproate
-
ZnCl2
[(2Z)-3-[(7-chloro-4-oxo-1,2,3-benzotriazin-3(4H)-yl)methyl]-4-oxo-1,3-thiazolidin-2-ylidene]cyanamide
11.7% inhibition at 0.01 mM
[(2Z)-3-[2-(6-methyl-4-oxo-1,2,3-benzotriazin-3(4H)-yl)ethyl]-4-oxo-1,3-thiazolidin-2-ylidene]cyanamide
54.8% inhibition at 0.01 mM
[(2Z)-3-[2-(6-nitro-4-oxo-1,2,3-benzotriazin-3(4H)-yl)ethyl]-4-oxo-1,3-thiazolidin-2-ylidene]cyanamide
32.8% inhibition at 0.01 mM
[(2Z)-3-[2-(7-bromo-4-oxo-1,2,3-benzotriazin-3(4H)-yl)ethyl]-4-oxo-1,3-thiazolidin-2-ylidene]cyanamide
53.5% inhibition at 0.01 mM
[(2Z)-3-[2-(7-chloro-4-oxo-1,2,3-benzotriazin-3(4H)-yl)ethyl]-4-oxo-1,3-thiazolidin-2-ylidene]cyanamide
65.2% inhibition at 0.01 mM
[(2Z)-3-[2-(7-fluoro-4-oxo-1,2,3-benzotriazin-3(4H)-yl)ethyl]-4-oxo-1,3-thiazolidin-2-ylidene]cyanamide
36.4% inhibition at 0.01 mM
[(2Z)-3-[4-(6-methyl-4-oxo-1,2,3-benzotriazin-3(4H)-yl)butyl]-4-oxo-1,3-thiazolidin-2-ylidene]cyanamide
26.0% inhibition at 0.01 mM
[(2Z)-3-[4-(6-nitro-4-oxo-1,2,3-benzotriazin-3(4H)-yl)butyl]-4-oxo-1,3-thiazolidin-2-ylidene]cyanamide
22.2% inhibition at 0.01 mM
[(2Z)-3-[4-(7-bromo-4-oxo-1,2,3-benzotriazin-3(4H)-yl)butyl]-4-oxo-1,3-thiazolidin-2-ylidene]cyanamide
26.8% inhibition at 0.01 mM
[(2Z)-3-[4-(7-chloro-4-oxo-1,2,3-benzotriazin-3(4H)-yl)butyl]-4-oxo-1,3-thiazolidin-2-ylidene]cyanamide
33.7% inhibition at 0.01 mM
[(2Z)-3-[4-(7-fluoro-4-oxo-1,2,3-benzotriazin-3(4H)-yl)butyl]-4-oxo-1,3-thiazolidin-2-ylidene]cyanamide
26.0% inhibition at 0.01 mM
[(2Z)-3-[5-(6-methyl-4-oxo-1,2,3-benzotriazin-3(4H)-yl)pentyl]-4-oxo-1,3-thiazolidin-2-ylidene]cyanamide
52.6% inhibition at 0.01 mM
[(2Z)-3-[5-(6-nitro-4-oxo-1,2,3-benzotriazin-3(4H)-yl)pentyl]-4-oxo-1,3-thiazolidin-2-ylidene]cyanamide
34.1% inhibition at 0.01 mM
[(2Z)-3-[5-(7-bromo-4-oxo-1,2,3-benzotriazin-3(4H)-yl)pentyl]-4-oxo-1,3-thiazolidin-2-ylidene]cyanamide
78.8% inhibition at 0.01 mM
[(2Z)-3-[5-(7-chloro-4-oxo-1,2,3-benzotriazin-3(4H)-yl)pentyl]-4-oxo-1,3-thiazolidin-2-ylidene]cyanamide
76.1% inhibition at 0.01 mM
[(2Z)-3-[5-(7-fluoro-4-oxo-1,2,3-benzotriazin-3(4H)-yl)pentyl]-4-oxo-1,3-thiazolidin-2-ylidene]cyanamide
54.0% inhibition at 0.01 mM
[(2Z)-3-[6-(5-chloro-4-oxo-1,2,3-benzotriazin-3(4H)-yl)hexyl]-4-oxo-1,3-thiazolidin-2-ylidene]cyanamide
37.8% inhibition at 0.01 mM
[(2Z)-3-[6-(6-chloro-4-oxo-1,2,3-benzotriazin-3(4H)-yl)hexyl]-4-oxo-1,3-thiazolidin-2-ylidene]cyanamide
68.8% inhibition at 0.01 mM
[(2Z)-3-[6-(6-methyl-4-oxo-1,2,3-benzotriazin-3(4H)-yl)hexyl]-4-oxo-1,3-thiazolidin-2-ylidene]cyanamide
62.5% inhibition at 0.01 mM
[(2Z)-3-[6-(6-nitro-4-oxo-1,2,3-benzotriazin-3(4H)-yl)hexyl]-4-oxo-1,3-thiazolidin-2-ylidene]cyanamide
36.9% inhibition at 0.01 mM
[(2Z)-3-[6-(7-bromo-4-oxo-1,2,3-benzotriazin-3(4H)-yl)hexyl]-4-oxo-1,3-thiazolidin-2-ylidene]cyanamide
70.6% inhibition at 0.01 mM
[(2Z)-3-[6-(7-chloro-4-oxo-1,2,3-benzotriazin-3(4H)-yl)hexyl]-4-oxo-1,3-thiazolidin-2-ylidene]cyanamide
80.6% inhibition at 0.01 mM
[(2Z)-3-[6-(7-fluoro-4-oxo-1,2,3-benzotriazin-3(4H)-yl)hexyl]-4-oxo-1,3-thiazolidin-2-ylidene]cyanamide
51.7% inhibition at 0.01 mM
[(2Z)-3-[6-(7-methoxy-4-oxo-1,2,3-benzotriazin-3(4H)-yl)hexyl]-4-oxo-1,3-thiazolidin-2-ylidene]cyanamide
50.3% inhibition at 0.01 mM
[(2Z)-3-[6-(7-nitro-4-oxo-1,2,3-benzotriazin-3(4H)-yl)hexyl]-4-oxo-1,3-thiazolidin-2-ylidene]cyanamide
34.6% inhibition at 0.01 mM
[(2Z)-3-[6-(8-chloro-4-oxo-1,2,3-benzotriazin-3(4H)-yl)hexyl]-4-oxo-1,3-thiazolidin-2-ylidene]cyanamide
37.9% inhibition at 0.01 mM
[(2Z)-4-oxo-3-[(4-oxo-1,2,3-benzotriazin-3(4H)-yl)methyl]-1,3-thiazolidin-2-ylidene]cyanamide
over 10.0% inhibition at 0.01 mM
[(2Z)-4-oxo-3-[2-(4-oxo-1,2,3-benzotriazin-3(4H)-yl)ethyl]-1,3-thiazolidin-2-ylidene]cyanamide
30.2% inhibition at 0.01 mM
[(2Z)-4-oxo-3-[2-[4-oxo-6-(trifluoromethyl)-1,2,3-benzotriazin-3(4H)-yl]ethyl]-1,3-thiazolidin-2-ylidene]cyanamide
55.6% inhibition at 0.01 mM
[(2Z)-4-oxo-3-[4-[4-oxo-6-(trifluoromethyl)-1,2,3-benzotriazin-3(4H)-yl]butyl]-1,3-thiazolidin-2-ylidene]cyanamide
41.6% inhibition at 0.01 mM
[(2Z)-4-oxo-3-[5-[4-oxo-6-(trifluoromethyl)-1,2,3-benzotriazin-3(4H)-yl]pentyl]-1,3-thiazolidin-2-ylidene]cyanamide
50.1% inhibition at 0.01 mM
[(2Z)-4-oxo-3-[6-[4-oxo-6-(trifluoromethyl)-1,2,3-benzotriazin-3(4H)-yl]hexyl]-1,3-thiazolidin-2-ylidene]cyanamide
60.1% inhibition at 0.01 mM
[(2Z)-4-oxo-3-[[4-oxo-6-(trifluoromethyl)-1,2,3-benzotriazin-3(4H)-yl]methyl]-1,3-thiazolidin-2-ylidene]cyanamide
15.8% inhibition at 0.01 mM
additional information
-