Information on EC 3.4.14.4 - dipeptidyl-peptidase III

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The enzyme appears in viruses and cellular organisms

EC NUMBER
COMMENTARY hide
3.4.14.4
-
RECOMMENDED NAME
GeneOntology No.
dipeptidyl-peptidase III
REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
release of an N-terminal dipeptide from a peptide comprising four or more residues, with broad specificity. Also acts on dipeptidyl 2-naphthylamides.
show the reaction diagram
-
-
-
-
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
hydrolysis of peptide bond
CAS REGISTRY NUMBER
COMMENTARY hide
77464-87-0
-
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
Ala-Ala-2-naphthylamide + H2O
Ala-Ala + 2-naphthylamine
show the reaction diagram
Ala-Ala-2-naphthylamide + H2O
Ala-Ala + 2-naphtylamine
show the reaction diagram
-
assay at 37°C, pH 8.0
-
-
?
Ala-Ala-Ala-Ala + H2O
Ala-Ala + Ala-Ala
show the reaction diagram
-
action of goat brain DPP-III on the peptide is investigated, substrate is hydrolyzed
-
-
?
Ala-Ala-beta-naphthylamide + H2O
Ala-Ala + beta-naphthylamine
show the reaction diagram
-
10.0% activity
-
-
?
Ala-Arg-2-naphthylamide + H2O
Ala-Arg + 2-naphthylamine
show the reaction diagram
Ala-Phe-2-naphthylamide + H2O
Ala-Phe + 2-naphthylamine
show the reaction diagram
-
-
-
?
Ala-Phe-2-naphthylamide + H2O
Ala-Phe + 2-naphtylamine
show the reaction diagram
-
assay at 37°C, pH 8.0
-
-
?
angiotensin II + H2O
Asp-Arg + Val-Tyr + Ile-His + Pro-Phe
show the reaction diagram
Arg-Arg-2-naphthylamide + H2O
Arg-Arg + 2-naphthylamine
show the reaction diagram
Arg-Arg-4-methoxy-2-naphthylamide + H2O
Arg-Arg + 4-methoxy-2-naphthylamine
show the reaction diagram
Arg-Arg-4-methoxy-beta-naphthylamide + H2O
Arg-Arg + 4-methoxy-beta-naphthylamine
show the reaction diagram
-
activity assay, 100% activity
-
-
?
Arg-Arg-7-amido-4 methylcoumarin + H2O
?
show the reaction diagram
-
-
-
-
?
Arg-Arg-7-amido-4-methylcoumarin + H2O
Arg-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
assay at 37°C
-
-
?
Arg-Arg-naphthylamide + H2O
?
show the reaction diagram
-
substrate used in the activity assay
-
-
?
Arg-Tyr-Leu-Pro-Thr + H2O
Arg-Tyr + Leu-Pro-Thr
show the reaction diagram
Arg-Val-Tyr-Ile-His-Pro-Phe-His-Leu + H2O
?
show the reaction diagram
-
angiotensin III, action of goat brain DPP-III on the peptide is investigated, substrate is hydrolyzed
-
-
?
arginyl-arginyl-4-methoxy-beta-naphthylamide + H2O
Arg-Arg + 4-methoxy-beta-naphthylamine
show the reaction diagram
-
substrate used in the activity assay
-
-
?
Asp-Ala-beta-naphthylamide + H2O
Asp-Ala + beta-naphthylamine
show the reaction diagram
-
0% activity
-
-
?
Asp-Arg-beta-naphthylamide + H2O
Asp-Arg + beta-naphthylamine
show the reaction diagram
-
1.5% activity
-
-
?
Asp-Arg-Val-Tyr-Ile-His-Pro-Phe + H2O
?
show the reaction diagram
-
angiotensin II, action of goat brain DPP-III on the peptide is investigated, substrate is hydrolyzed
-
-
?
enkephalin + H2O
?
show the reaction diagram
-
-
-
-
?
Gly-Ala-beta-naphthylamide + H2O
Gly-Ala + beta-naphthylamine
show the reaction diagram
-
3.2% activity
-
-
?
Gly-Arg-beta-naphthylamide + H2O
Gly-Arg + beta-naphthylamine
show the reaction diagram
-
11.8% activity
-
-
?
Gly-Gly-Phe-Leu + H2O
?
show the reaction diagram
-
-
-
-
?
Gly-Phe-2-naphthylamide + H2O
Gly-Phe + 2-naphthylamine
show the reaction diagram
-
assay at 37°C, pH 8.0
-
-
?
Gly-Phe-beta-naphthylamide + H2O
Gly-Phe + beta-naphthylamine
show the reaction diagram
-
2.4% activity
-
-
?
Gly-Pro-4-methoxy-beta-naphthylamide + H2O
Gly-Pro + 4-methoxy-beta-naphthylamine
show the reaction diagram
-
0% activity
-
-
?
His-Phe-beta-naphthylamide + H2O
His-Phe + beta-naphthylamine
show the reaction diagram
-
0% activity
-
-
?
His-Ser-2-naphthylamide + H2O
His-Ser + 2-naphthylamine
show the reaction diagram
-
-
-
?
His-Ser-beta-naphthylamide + H2O
His-Ser + beta-naphthylamine
show the reaction diagram
-
0% activity
-
-
?
L-Ala-L-Ala 2-naphthylamide + H2O
L-Ala-L-Ala + 2-naphthylamine
show the reaction diagram
-
-
-
-
?
L-Ala-L-Ala-2-naphthylamide + H2O
L-Ala-L-Ala + 2-naphthylamine
show the reaction diagram
-
36.64% of the activiy with L-Arg-L-Arg-4-methoxy-2-naphthylamide
-
-
?
L-Arg-L-Arg 2-naphthylamide + H2O
L-Arg-L-Arg + 2-naphthylamine
show the reaction diagram
-
-
-
-
?
L-Arg-L-Arg-2-naphthylamide + H2O
L-Arg-L-Arg + 2-naphthylamine
show the reaction diagram
L-Arg-L-Arg-4-methoxy-2-naphthylamide + H2O
L-Arg-L-Arg + 4-methoxy-2-naphthylamine
show the reaction diagram
L-Asp-L-Ala-2-naphthylamide + H2O
L-Asp-L-Ala + 2-naphthylamine
show the reaction diagram
-
8.67% of the activiy with L-Arg-L-Arg-4-methoxy-2-naphthylamide
-
-
?
L-Asp-L-Arg-2-naphthylamide + H2O
L-Asp-L-Arg + 2-naphthylamine
show the reaction diagram
-
9.8% of the activiy with L-Arg-L-Arg-4-methoxy-2-naphthylamide
-
-
?
L-His-L-Ser-4-methoxy-2-naphthylamide + H2O
L-His-L-Ser + 4-methoxy-2-naphthylamine
show the reaction diagram
-
58.46% of the activiy with L-Arg-L-Arg-4-methoxy-2-naphthylamide
-
-
?
L-Lys-L-Ala-2-naphthylamide + H2O
L-Lys-L-Ala + 2-naphthylamine
show the reaction diagram
-
activity of the cupric derivative for Lys-Ala-beta-naphthylamide is about 30% of that of the wild-type enzyme
-
-
?
L-Ser-L-Tyr-2-naphthylamide + H2O
L-Ser-L-Tyr + 2-naphthylamine
show the reaction diagram
-
7.35% of the activiy with L-Arg-L-Arg-4-methoxy-2-naphthylamide
-
-
?
Leu-Ala-beta-naphthylamide + H2O
Leu-Ala + beta-naphthylamine
show the reaction diagram
-
5.0% activity
-
-
?
Leu-enkephalin + H2O
Tyr-Gly + Gly-Phe-Leu
show the reaction diagram
Leu-Gly-2-naphthylamide + H2O
Leu-Gly + 2-naphthylamine
show the reaction diagram
Lys-Ala-2-naphthylamide + H2O
Lys-Ala + 2-naphthylamine
show the reaction diagram
Lys-Ala-4-methoxy-2-naphthylamide + H2O
Lys-Ala + 4-methoxy-2-naphthylamine
show the reaction diagram
Lys-Ala-4-methoxy-beta-naphthylamide + H2O
Lys-Ala + 4-methoxy-beta-naphthylamine
show the reaction diagram
-
5.0% activity
-
-
?
Met-Arg-Phe-Ala + H2O
Met-Arg + Phe-Ala
show the reaction diagram
-
-
-
?
Phe-Arg-beta-naphthylamide + H2O
Phe-Arg + beta-naphthylamine
show the reaction diagram
-
17.6% activity
-
-
?
proctolin + H2O
Tyr-Leu + ?
show the reaction diagram
-
-
-
-
?
Ser-Met-beta-naphthylamide + H2O
Ser-Met + beta-naphthylamine
show the reaction diagram
-
0% activity
-
-
?
Ser-Tyr-beta-naphthylamide + H2O
Ser-Tyr + beta-naphthylamine
show the reaction diagram
-
0% activity
-
-
?
Ser-Tyr-Ser-Met-Glu-His-Phe-Arg-Trp-Gly + H2O
?
show the reaction diagram
-
ACTH, action of goat brain DPP-III on the peptide is investigated, substrate is hydrolyzed
-
-
?
Trp-Met-Asp-Phe-NH2 + H2O
?
show the reaction diagram
-
-
-
-
?
Trp-Met-Asp-Phe-NH2 + H2O
Trp-Met + Asp-Phe-NH2
show the reaction diagram
-
gastrin tetrapeptide amide, action of goat brain DPP-III on the peptide is investigated, substrate is hydrolyzed
-
-
?
Tyr-Gly-Gly-Phe + H2O
Tyr-Gly + Gly-Phe
show the reaction diagram
Tyr-Gly-Gly-Phe-Leu + H2O
Tyr-Gly + Gly-Phe-Leu
show the reaction diagram
Tyr-Gly-Gly-Phe-Met + H2O
?
show the reaction diagram
-
-
-
?
Tyr-Pro-Trp-Phe-NH2 + H2O
Tyr-Pro + Trp-Phe-NH2
show the reaction diagram
-
endomorphin-1
-
-
?
additional information
?
-
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
Ni2+
-
may substitue for Zn2+
additional information
-
spectral analysis of Zn2+-, Ni2+-, Cu2+-, Co2+-substituted enzyme
INHIBITORS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
1,10-phenanthroline
1,3-di-[5-(2-imidazolinyl)-2-benzimidazolyl]-2,4-di-o-chlorophenyl-cyclobutane dihydrochloride
-
-
1,3-di-[5-(2-imidazolinyl)-2-benzimidazolyl]-2,4-di-phenyl-cyclobutane dihydrochloride
-
-
1,3-di-[5-(2-imidazolinyl)-2-benzoimidazolyl]-2,4-di-(2-furyl)-cyclobutane dihydrochloride
-
-
1,3-di-[5-(2-imidazolinyl)-2-benzoimidazolyl]-2,4-di-(2-thienyl)-cyclobutane dihydrochloride
-
-
1,3-di-[5-(2-imidazolinyl)-2-benzoimidazolyl]-2,4-di-(2-thienyl)-cyclobutanedihydrochloride
-
-
1,3-di-[5-(N-amidino)-2-benzimidazolyl]-2,4-di-o-chlorophenyl-cyclobutane dihydrochloride
-
-
1,3-di-[5-(N-amidino)-2-benzimidazolyl]-2,4-di-phenyl-cyclobutane dihydrochloride
-
-
1,3-di-[5-(N-isopropylamidino)-2-benzimidazolyl]-2,4-di-o-chlorophenyl-cyclobutane dihydrochloride
-
-
1,3-di-[5-(N-isopropylamidino)-2-benzimidazolyl]-2,4-di-o-chlorophenylcyclobutane dihydrochloride
-
-
1,3-di-[5-(N-isopropylamidino)-2-benzimidazolyl]-2,4-di-phenyl-cyclobutane dihydrochloride
-
-
1-ethyl-3(3-dimethyl-amino-propyl)-carbodiimide*HCl
-
1.0 mM inhibitor, 29% inhibition, 5.0 mM inhibitor, 64% inhibition
2,2'-dithiodipyridine
-
1.0 mM inhibitor, 32% inhibition, 2.5 mM inhibitor, 98% inhibition
2,4,6-trinitrobenzene sufonic acid trihydrate
-
1.0 mM inhibitor, 52% inhibition, 2.5 mM inhibitor, 89% inhibition
2-(3H-imidazol-4-yl)-1H-benzoimidazole-5-carboxamidine hydrochloride
-
; complete inhibition at 0.1 mM
2-(3H-imidazol-4-yl)-1H-benzoimidazole-5-imidazolinylamidine hydrochloride
-
; complete inhibition at 0.1 mM
2-mercaptoethanol
2-[(E)-2-phenylethenyl]-1H-benzimidazole
-
-
3,3'-dithiobis(6-nitrobenzoic acid)
-
13% residual activity at 2.5 mM, beta-mercaptoethanol and dithiothreitlol completely restores enzyme activity
3,4-dichloroisocoumarin
4,4'-dithiodipyridine
-
inactivation of wild-type dipeptidyl peptidase III after incubation at pH 8.0 at 25°C, after 5 min incubation loss of 30% enzyme activity, after 15 min incubation loss of 62% enzyme activity
4-(2-aminoethyl) benzenesulfonyl fluoride
-
0.01 mM, 89% inhibition
4-Chlorobenzoic acid
-
0.5 mM, 42% inhibition
4-nitrophenyl iodoacetate
-
0.5 mM, 57% inhibition
5,5'-dithiobis(2-nitrobenzoate)
6-(4,5-dihydro-1H-imidazol-2-yl)-2-[(E)-2-phenylethenyl]-1H-benzimidazole
-
-
Acetyl-L-Leu-L-arginal
-
-
alpha1 anti-trypsin
-
1.0 mM inhibitor, 61% inhibition
-
amastatin
-
30% inhibition at 0.1 mM
angiotensin II
Angiotensin III
Angiotensins
-
-
-
Aprotinin
-
1.0 mM inhibitor, 59% inhibition, 5.0 mM inhibitor, 99% inhibition
Arg-Arg
Arg-Arg-2-naphthylamide
-
above 0.1 mM
benzamidine HCl
-
1.0 mM inhibitor, 29% inhibition, 5.0 mM inhibitor, 61% inhibition
bestatin
bis-p-nitrophenyl phosphate
-
-
Co2+
-
activation up to 50% at 0.001-0.0001 mM, inbhibitory above 0.002 mM
cysteine
-
-
diisopropylfluorophosphate
dimethyl sulfoxide
-
inhibitory effect with more than 5% (v/v) dimethyl sulfoxide
dithioerythreitol
-
-
dithiothreitol
DTNB
-
1.0 mM inhibitor, 54% inhibition, 2.5 mM inhibitor, 87% inhibition
E-64
-
i.e. L-trans-epoxysuccinyl-leucylamido(4-guanidino)butane, 10% inhibition at 0.1 mM
Egg white trypsin inhibitor
-
1.0 mM inhibitor, 34% inhibition
-
EGTA
-
96% inhibition in the presence of 1 mM EGTA, but 110% activity in the presence of the two inhibitors 1 mM EGTA and 1 mM Zn2+
ethanol
-
the enzyme loses about half of its activity at 5% (v/v) ethanol
glutathione
-
-
Gly-Gly-Phe-Leu
Gly-L-Glu
-
36% inhibition at 1 mM
Gly-L-Phe
-
46% inhibition at 1 mM
Gly-L-Phe-L-Leu
-
non-competitive inhibitor, 82% inhibition at 1 mM
His-Phe-Arg-Trp
iodoacetamide
iodoacetic acid
-
1.0 mM inhibitor, 25% inhibition, 5.0 mM inhibitor, 48% inhibition
IVYPW
-
hemorphin.like peptide, non-competitive, 50% inhibition at 0.00016 mM
K+
-
82.0% residual activity at 0.1 mM
L-Ala-L-Ala-L-Ala
-
4% inhibition at 1 mM
L-Ala-L-Ala-L-Ala-L-Ala
-
58% inhibition at 0.5 mM
L-Arg-L-Phe
-
56% inhibition at 1 mM
L-Arg-L-Phe-L-Ala
-
competitive inhibitor, 99% inhibition at 1 mM
L-Arg-L-Trp
-
46% inhibition at 1 mM
L-Arg-L-Val
-
49% inhibition at 1 mM
L-Asp-L-Ala
-
25% inhibition at 1 mM
L-His-L-Leu
-
76% inhibition at 1 mM
L-His-L-Lys
-
41% inhibition at 1 mM
L-His-L-Phe
-
46% inhibition at 1 mM
L-His-L-Pro
-
16% inhibition at 1 mM
L-Ile-L-His
-
34% inhibition at 1 mM
L-Leu-L-Arg
-
complete inhibition at 0.5 mM
L-Leu-L-Trp
-
competitive inhibitor, 90% inhibition at 1 mM
L-Leu-L-Trp-L-Met
-
competitive inhibitor, 92% inhibition at 1 mM
L-Leu-L-Trp-L-Met-L-Arg-L-Phe-L-Ala
-
competitive inhibitor, complete inhibition at 1 mM
L-Lys-L-Ala
-
23% inhibition at 1 mM
L-Met-L-Arg
-
99% inhibition at 1 mM
L-Phe-L-Ala
-
41% inhibition at 1 mM
L-Phe-L-Arg
-
75% inhibition at 1 mM
L-Phe-L-Leu
-
58% inhibition at 1 mM
L-Phe-L-Met
-
85% inhibition at 1 mM
L-Pro-L-Arg-OH
-
54% inhibition at 1 mM
L-Pro-L-Glu
-
34% inhibition at 1 mM
L-Pro-L-Phe
-
56% inhibition at 1 mM
L-Ser-L-Met
-
32% inhibition at 1 mM
L-Trp-L-Met
-
competitive inhibitor, 94% inhibition at 1 mM
L-Trp-L-Met-L-Asp-L-Phe
-
82% inhibition at 1 mM
L-tryptophyl-L-methionyl-L-alpha-aspartyl-L-phenylalaninamide
-
competitive inhibition
L-Tyr-Gly
-
31% inhibition at 1 mM
L-Tyr-Gly-Gly-L-Phe
-
53% inhibition at 1 mM
L-Tyr-L-Ile
-
72% inhibition at 1 mM
L-tyrosyl-glycine hydroxamic acid
-
-
L-tyrosyl-L-phenylalanine hydroxamic acid
-
-
L-Val-L-Tyr
-
competitive inhibitor, 84% inhibition at 1 mM
Leu-enkephalin
-
i.e. L-Tyr-Gly-Gly-L-Phe-L-Leu, 92% inhibition at 1 mM, competitive inhibitor
Leu-Trp-Met-Arg-Phe
Leu-Val-Val-Tyr-Pro-Trp-Thr-Gln-Arg
-
Leu-valorphin-Arg
leupeptin
Li+
-
73.0% residual activity at 0.1 mM
Lys-Val-Ile-Leu-Phe
Met-enkephalin
-
i.e. L-Tyr-Gly-Gly-L-Phe-L-Met, 61% inhibition at 0.5 mM, competitive inhibitor
N-ethylmaleimide
N-hydroxy-succinimide
-
1.0 mM inhibitor, 30% inhibition, 5.0 mM inhibitor, 51% inhibition
Nalpha-tosyl-L-Phe-chloromethyl ketone
-
60% inhibition at 0.1 mM
-
o-phenanthroline
p-aminophenyl mercuric acetate
-
1.0 mM inhibitor, 42% inhibition, 2.5 mM inhibitor, 94% inhibition
p-chloromercuribenzoate
p-Chloromercuriphenylsulfonic acid
-
-
p-Chlorophenylsulfonate
-
-
p-hydroxymercuribenzoate
p-hydroxymercuriphenyl-sulfonic acid
-
1.0 mM inhibitor, 22% inhibition, 2.5 mM inhibitor, 96% inhibition
p-nitrocatecholsulfate
-
1.0 mM inhibitor, 37% inhibition, 5.0 mM inhibitor, 58% inhibition
Pb(CH3COO)2
-
1.0 mM inhibitor, 53% inhibition, 2.5 mM inhibitor, 97% inhibition
Pb2+
-
-
Pepstatin
-
1 mM, 43% inhibition
pepstatin A
-
5.0 mM inhibitor, 92% inhibition
Phenylmethanesulfonylfluoride
probestin
-
85% inhibition at 0.1 mM
Proctolin
Propioxanthin A and B
-
-
-
puromycin
Soybean trypsin inhibitor
-
1.0 mM inhibitor, 64% inhibition, 2.5 mM inhibitor, 76% inhibition
-
thioglycolic acid
-
-
TLCK
-
1.0 mM inhibitor, 27% inhibition, 5.0 mM inhibitor, 63% inhibition
TPCK
-
1.0 mM inhibitor, 75% inhibition, 5.0 mM inhibitor, 88% inhibition
tynorphin
Tyr(SO3H)-Gly-Gly-Phe-Leu
-
-
Tyr-Ala-Gly-Phe-Leu
-
Ala2-Leu-enkephalin
Tyr-Arg
Tyr-D-Ala-Gly-Phe-Leu
-
D-Ala2-Leu-enkephalin
Tyr-Gly-Gly-Phe
-
enkephalin fragment
Tyr-Gly-Gly-Phe-Leu
Tyr-Gly-Gly-Phe-Leu-Arg-Arg-Ile
-
dynorphin A 1-8
Tyr-Gly-Gly-Phe-Met
Tyr-Phe-NHOH
-
-
Tyr-Pro-Phe-Phe-NH2
-
endomorphin-2
Tyr-Pro-Phe-Val-Glu-Pro-Ile
-
human beta-casomorphin
Tyr-Pro-Trp-Phe-NH2
-
endomorphin-1
Tyr-Tyr
Urea
-
sensitive to very low concentrations of urea
Val-Val-Tyr-Pro-Trp-Thr-Gln
-
valorphin
WVYPW
-
hemorphin.like peptide, non-competitive, 50% inhibition at 0.00024 mM
additional information
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
aFas
-
anti-fas antibody, aFas treated cells release lysosomal hydrolases into the culture medium
-
dimethyl sulfoxide
-
the activity progressively increases with increase in dimethyl sulfoxide concentration up to 5% (v/v)
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.299 - 0.441
Ala-Ala-2-naphthylamide
0.00621 - 0.3
Arg-Arg-2-naphthylamide
0.022
Arg-Arg-4-methoxy-2-naphthylamide
-
-
0.039
Arg-Arg-4-methoxy-beta-naphthylamide
-
-
0.055
Arg-Arg-4-methylcoumarin 7-amide
-
-
0.004
Arg-Tyr-Leu-Pro-Thr
-
25°C
0.0045
Arg-Tyr-Leu-Pro-Thr, proctolin
-
-
0.0945 - 0.2316
L-Ala-L-Ala 2-naphthylamide
0.0026 - 0.0251
L-Arg-L-Arg 2-naphthylamide
0.07 - 0.2
L-Lys-L-Ala-2-naphthylamide
0.0057 - 0.22
Leu-enkephalin
0.053
Met-enkephalin
-
-
0.0038 - 0.0045
Proctolin
0.0419
Tyr-Gly-Gly-Phe-Met
-
-
0.0081
Tyr-Pro-Trp-Phe-NH2
-
endomorphin-1
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.02 - 0.35
Ala-Ala-2-naphthylamide
0.09 - 31.5
Arg-Arg-2-naphthylamide
0.039
Arg-Arg-4-methoxy-beta-naphthylamide
Capra hircus
-
-
50
Gly-Gly-Phe-Leu
Rattus norvegicus
-
-
0.002 - 7.25
L-Ala-L-Ala 2-naphthylamide
0.003 - 0.953
L-Arg-L-Arg 2-naphthylamide
0.4 - 1.4
L-Lys-L-Ala-2-naphthylamide
167
Trp-Met-Asp-Phe-NH2
Rattus norvegicus
-
-
13.2
Tyr-Gly-Gly-Phe-Leu
Rattus norvegicus
-
-
5
Tyr-Pro-Trp-Phe-NH2
Homo sapiens
-
endomorphin-1
additional information
additional information
Rattus norvegicus
-
-
-
kcat/KM VALUE [1/mMs-1]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.053 - 1.17
Ala-Ala-2-naphthylamide
6480
10.21 - 1879
Arg-Arg-2-naphthylamide
1916
0.012 - 76.7
L-Ala-L-Ala 2-naphthylamide
202280
0.133 - 3202
L-Arg-L-Arg 2-naphthylamide
202279
5.5 - 12
L-Lys-L-Ala-2-naphthylamide
31526
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0002
1,3-di-[5-(2-imidazolinyl)-2-benzimidazolyl]-2,4-di-phenyl-cyclobutane dihydrochloride
-
-
0.00066 - 0.00083
angiotensin II
0.000024 - 0.00009
Angiotensin III
0.0235 - 0.074
Gly-Gly-Phe-Leu
0.015
Gly-L-Phe-L-Leu
-
in 50 mM Tris-HCl, pH 8.5, with 100 mM NaCl and 1 mM beta-mercaptoethanol, at 37°C
0.0065 - 0.01
His-Phe-Arg-Trp
0.0001
IVYPW
-
-
0.004
L-Arg-L-Phe-L-Ala
-
in 50 mM Tris-HCl, pH 8.5, with 100 mM NaCl and 1 mM beta-mercaptoethanol, at 37°C
0.039
L-Leu-L-Trp
-
in 50 mM Tris-HCl, pH 8.5, with 100 mM NaCl and 1 mM beta-mercaptoethanol, at 37°C
0.031
L-Leu-L-Trp-L-Met
-
in 50 mM Tris-HCl, pH 8.5, with 100 mM NaCl and 1 mM beta-mercaptoethanol, at 37°C
0.007
L-Leu-L-Trp-L-Met-L-Arg-L-Phe-L-Ala
-
in 50 mM Tris-HCl, pH 8.5, with 100 mM NaCl and 1 mM beta-mercaptoethanol, at 37°C
0.38
L-Trp-L-Met
-
in 50 mM Tris-HCl, pH 8.5, with 100 mM NaCl and 1 mM beta-mercaptoethanol, at 37°C
0.055
L-tryptophyl-L-methionyl-L-alpha-aspartyl-L-phenylalaninamide
-
in 50 mM Tris-HCl, pH 8.5, with 100 mM NaCl and 1 mM beta-mercaptoethanol, at 37°C
0.0105 - 0.351
L-tyrosyl-glycine hydroxamic acid
0.00015 - 0.00427
L-tyrosyl-L-phenylalanine hydroxamic acid
0.25
L-Val-L-Tyr
-
in 50 mM Tris-HCl, pH 8.5, with 100 mM NaCl and 1 mM beta-mercaptoethanol, at 37°C
0.09
Leu-enkephalin
-
in 50 mM Tris-HCl, pH 8.5, with 100 mM NaCl and 1 mM beta-mercaptoethanol, at 37°C
0.00009 - 0.00013
Leu-Trp-Met-Arg-Phe
0.00341
Leu-Val-Val-Tyr-Pro-Trp-Thr-Gln-Arg
-
-
0.00021 - 0.0004
Lys-Val-Ile-Leu-Phe
0.13
Met-enkephalin
-
in 50 mM Tris-HCl, pH 8.5, with 100 mM NaCl and 1 mM beta-mercaptoethanol, at 37°C
0.00015 - 0.00043
Proctolin
0.000075
tynorphin
-
37°C, pH 7.4
0.0434
Tyr(SO3H)-Gly-Gly-Phe-Leu
-
-
0.000375
Tyr-Ala-Gly-Phe-Leu
-
-
0.027
Tyr-D-Ala-Gly-Phe-Leu
-
-
0.004
Tyr-Gly-Gly-Phe
-
-
0.00365 - 0.0337
Tyr-Gly-Gly-Phe-Leu
0.0699
Tyr-Gly-Gly-Phe-Leu-Arg-Arg-Ile
-
-
0.027 - 0.0343
Tyr-Gly-Gly-Phe-Met
0.000146 - 0.000234
Tyr-Phe-NHOH
0.00249
Tyr-Pro-Phe-Phe-NH2
-
-
0.00056
Tyr-Pro-Phe-Val-Glu-Pro-Ile
-
-
0.005
Tyr-Pro-Trp-Phe-NH2
-
-
0.000049
Val-Val-Tyr-Pro-Trp-Thr-Gln
-
-
0.00013
WVYPW
-
-
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0017
1,3-di-[5-(2-imidazolinyl)-2-benzimidazolyl]-2,4-di-o-chlorophenyl-cyclobutane dihydrochloride
Homo sapiens
-
; at pH 7.4 for 10 min at 25°C
0.0028
1,3-di-[5-(2-imidazolinyl)-2-benzimidazolyl]-2,4-di-phenyl-cyclobutane dihydrochloride
Homo sapiens
-
; at pH 7.4 for 10 min at 25°C
0.008
1,3-di-[5-(2-imidazolinyl)-2-benzoimidazolyl]-2,4-di-(2-furyl)-cyclobutane dihydrochloride
Homo sapiens
-
; at pH 7.4 for 10 min at 25°C
0.001
1,3-di-[5-(2-imidazolinyl)-2-benzoimidazolyl]-2,4-di-(2-thienyl)-cyclobutane dihydrochloride
Homo sapiens
-
-
0.01
1,3-di-[5-(2-imidazolinyl)-2-benzoimidazolyl]-2,4-di-(2-thienyl)-cyclobutanedihydrochloride
Homo sapiens
-
at pH 7.4 for 10 min at 25°C
0.007
1,3-di-[5-(N-amidino)-2-benzimidazolyl]-2,4-di-o-chlorophenyl-cyclobutane dihydrochloride
Homo sapiens
-
; at pH 7.4 for 10 min at 25°C
0.0056
1,3-di-[5-(N-amidino)-2-benzimidazolyl]-2,4-di-phenyl-cyclobutane dihydrochloride
Homo sapiens
-
; at pH 7.4 for 10 min at 25°C
0.006
1,3-di-[5-(N-isopropylamidino)-2-benzimidazolyl]-2,4-di-o-chlorophenyl-cyclobutane dihydrochloride
Homo sapiens
-
-
0.006
1,3-di-[5-(N-isopropylamidino)-2-benzimidazolyl]-2,4-di-o-chlorophenylcyclobutane dihydrochloride
Homo sapiens
-
at pH 7.4 for 10 min at 25°C
0.01
1,3-di-[5-(N-isopropylamidino)-2-benzimidazolyl]-2,4-di-phenyl-cyclobutane dihydrochloride
Homo sapiens
-
; at pH 7.4 for 10 min at 25°C, IC50 above 0.01 mM
0.053
2-(3H-imidazol-4-yl)-1H-benzoimidazole-5-carboxamidine hydrochloride
Homo sapiens
-
; at pH 7.4 for 10 min at 25°C
0.018
2-(3H-imidazol-4-yl)-1H-benzoimidazole-5-imidazolinylamidine hydrochloride
Homo sapiens
-
; at pH 7.4 for 10 min at 25°C
0.1
2-[(E)-2-phenylethenyl]-1H-benzimidazole
Homo sapiens
-
-
0.01
6-(4,5-dihydro-1H-imidazol-2-yl)-2-[(E)-2-phenylethenyl]-1H-benzimidazole
Homo sapiens
-
-
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
0.0001
-
purification step, homogenate
0.0004
-
purification step, acid precipitation
0.0012
-
purification step, ammonium sulfate fractionation, 35-65% pellet
0.0092
-
purification step, gel filtration chromatography on a Sephadex G-100 column
0.0126
-
purification step, cation exchange chromatography on a CM Sephadex A-50 column
0.0652
-
purification step, anion exchange chromatography on a DEAE Sephadex A-50 column
0.107
-
purification step, adsorption chromatography on a hydroxyapatite column
0.65
-
at the end of ripening stage, postsalting, thawed ham
0.78
-
at the end of ripening stage, salting, thawed ham
0.83
-
at the end of ripening stage, postsalting, fresh ham
1.21
-
at the end of ripening stage, salting, fresh ham
1.43
-
mutant W300L, pH 8.0, 37°C
1.6
-
-
3.6
-
-
14.2
-
-
24.9
-
mutant W300F, pH 8.0, 37°C
45.6
-
wild-type, pH 8.0, 37°C
84.9
-
-
87.5
-
in the presence of 10 microM CoCl2
additional information
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
6 - 6.5
-
substrate Met-enkephalin
7.3 - 8
-
substrate angiotensin II
7.5
-
substrate Leu-enkephalin
8.5 - 9
-
-
8.7 - 8.8
-
-
pH RANGE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
5 - 9
-
depending on substrate
6 - 11
-
the enzyme has 50% activity at pH 6 in the lower range and at pH 11 in the higher range
6.5 - 10.5
-
more than 15% of maximal activity
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
25
-
activity assay
TEMPERATURE RANGE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
40
-
the enzyme shows a considerable heat stability up to 40°C, 30% activity is lost at 45°C
pI VALUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
-
normal, benign and malignant
Manually annotated by BRENDA team
-
-
Manually annotated by BRENDA team
-
highest activity in seeds germinated for 48 h
Manually annotated by BRENDA team
-
superficial laminae of the spinal cord dorsal horn
Manually annotated by BRENDA team
-
-
Manually annotated by BRENDA team
additional information
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
27000
-
1 * 32800, 1 * 27000, SDS-PAGE
32800
-
1 * 32800, 1 * 27000, SDS-PAGE
44000
-
2 * 44000, SDS-PAGE
60000
-
gel filtration
66000
-
gel filtration
69000
-
determined by SDS-PAGE, gel filtration and MALDI-TOF analysis
76000
-
SDS-PAGE, assumed, one isoform
80000 - 86000
80000
-
SDS-PAGE, assumed, one isoform
82500
-
x * 82500, mass spectrometry
93000
-
gel filtration
158000
-
gel filtration
SUBUNITS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
heterodimer
-
1 * 32800, 1 * 27000, SDS-PAGE
monomer
POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
no glycoprotein
-
six potential glycosylation sites, but no glycosylation detectable
Crystallization/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
structures of human DPP III and its complex with the opioid peptide tynorphin, to 1.8 A and 2.4 and.0 A resolution, respectively. Structures rationalize the enzyme’s substrate specificity and reveal an exceptionally large domain motion upon ligand binding. Microcalorimetric analyses point at an entropy-dominated process, with the release of water molecules from the binding cleft as the major thermodynamic driving force
-
the C130S mutant is crystallized by sitting drop vapour diffusion method, in 20% (w/v) polyethylene glycol 3350 and 900 mM MgCl2 in 100 mM Tris-HCl (pH 7.0)
-
pH STABILITY
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
6.5 - 8
-
-
36179
6.7 - 9
-
-
36178
7.5 - 9.5
-
-
732846
TEMPERATURE STABILITY
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
37 - 40
-
up to
40
-
inactivation above
45
-
4 min, 81% activity
75
-
5 min, 10% activity
additional information
-
sensitive to freezing
GENERAL STABILITY
ORGANISM
UNIPROT
LITERATURE
4,4'-dithiodipyridine, inactivation of wild-type dipeptidyl peptidase III after incubation at pH 8.0 at 25°C, after 5 min incubation loss of 30% enzyme activity, after 15 min incubation loss of 62% enzyme activity
-
purified enzyme unstable
-
STORAGE STABILITY
ORGANISM
UNIPROT
LITERATURE
-10°C, 50 mM sodium phosphate buffer, pH 6.8, 1 mM mercaptoethanol, 0.5 M NaCl, 40% glycerol, 1 year
-
-20°C, 50% glycerol, 1 year
-
-20°C, in 50 mM Tris-HCl, pH 7.5, 1 and 6 months, 38.15% and 99.75% loss of activity
-
-20°C, in 50 mM Tris-HCl, pH 7.5, in the presence of 10% (v/v) glycerol, 1 and 6 months, 26.5% and 92% loss of activity
-
-80°C
-
Purification/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
about 28% yield after gel filtration and FPLC for wild-type enzyme
-
by gel filtration on a Sephacryl S-200 column, followed by FPLC on a Mono Q column, recombinant and human erythtocyte DPP III is purified
-
DPP from goat brain is purified by several steps, including acid precipitation, ammonium sulfate fractionation, chromatography on a Sephadex G-100 column, cation, anion and adsorption chromatography
-
expressed in Escherichia coli
-
from seed
-
gel filtration and FPLC on Mono Q column
-
Hi-Trap Q Sepharose chromatography
-
human DPP III is purified from healthy blood donor erythrocytes
-
Ni-NTA resin column chromatography
-
partial
recombinant enzyme
-
the protein is purified from human erythrocytes
-
Cloned/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
expressed in Escherichia coli strain BL21-CodonPlus(DE3)-RIL
-
expression in Escherichia coli
-
expression in Escherichia coli BL21
expression in human glioblastoma, ovarian carcinoma, pancreatic carcinoma and mouse fibroblast cells
-
expression in S2 cells
-
expression in Schneider S2 cells
-
into the pET21b vector for expression in Escherichia coli BL21DE3RIL+ cells
-
EXPRESSION
ORGANISM
UNIPROT
LITERATURE
increased enzyme expression with recombinant constructs with Ets-1/Elk-1 proteins bind to binding motifs
-
ENGINEERING
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
D372A
-
residue Asp372 plays a crucial role in the large scale interdomain closure. During the MD simulation time, the variant remains more open than the wild type protein. Apparently, Ala is not as efficient as Asp in establishing the interdomain interactions
D496G
-
mutation in S2 subsite, mutant has lost selectivity due to the increase of the Km value. Mutant shows significantly decreased binding of peptides with N-terminal arginine, and of tynorphin
H450Y
-
no activity
H455Y
-
no activity
Q451A
-
no activity
Q451D
-
no activity
Q508A
-
no activity
S504G
-
mutation in S2 subsite, mutant does not show decreased binding of peptides with N-terminal arginine
W300F
-
mutant with slight increase in activity compared to wild-type enzyme
W300L
-
mutant with higher activity compared to wild-type enzyme
Y318F
-
the potential functional role of the well-conserved tyrosine 318 residue in the active center of human DPP III is investigated
Y395F
-
the potential functional role of the well-conserved tyrosine 395 residue in the active center of human DPP III is investigated
Y644F
-
the potential functional role of the well-conserved tyrosine 644 residue in the active center of human DPP III is investigated
C147A
-
activity similar to wild type
C176A
-
25-35% of wild type activity, resistant against p-chloro-mercuri-benzoate and N-ethylmaleimide
C176E
-
no enzymic activity
C176G
-
no enzymic activity
C19A
-
activity similar to wild type
C509A
-
activity similar to wild type
C519A
-
activity similar to wild type
C654A
-
activity similar to wild type
C701A
-
activity similar to wild type
Leu453del
-
activity of mutant Cu(II)-del-DPP III, in which Leu453 is deleted from the metal-binding motif, is only 1-2% of the enzyme activity of del-DPP. The EPR spectra of Cu(II) del-DPP III do not change in the presence of excess Lys-Ala-beta-naphthylamide. The deletion of Leu453 from the HELLGH motif of rat DPP III leads to a complete loss of flexibility in the ligand geometry around the cupric ions
C113S
-
mutation of the cysteine residue
C518S
-
mutation of the cysteine residue
C626S
-
mutation of the cysteine residue
C639S
-
mutant, resistance against p-hydroxy-mercuribenzoate
H578D
-
mutation 122fold lowers the catalytic efficiency for Arg-Arg 2-naphthylamide hydrolysis, and 14fold decreases affinity for hydroxamate inhibitor Tyr-Phe-NHOH
K638L
-
mutation slightly increases the specificity constant for Arg-Arg 2-naphthylamide hydrolysis. The affinity for Tyr-Phe-NHOH, and activity for the substrates with uncharged P2 side chains such as Ala-Ala-, Ala-Arg- and Phe-Arg 2-naphthylamide are dramatically reduced
R582Q
-
mutant exhibits an order of magnitude higher activity with all four dipeptide derivatives examined, compared to the wild type, due to a change in the H-bond networking in the R582Q variant active-site region
C130S
-
the mutant exhibits comparable enzymatic activity to the wild type protein
-
additional information
Renatured/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
incubation of apo-enzyme with Zn2+, Co2+, Ni2+ or Cu2+ completely recovers enzymic activity
-
APPLICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
medicine
Show AA Sequence (110 entries)
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