Information on EC 3.4.21.77 - semenogelase

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The expected taxonomic range for this enzyme is: Eutheria

EC NUMBER
COMMENTARY hide
3.4.21.77
-
RECOMMENDED NAME
GeneOntology No.
semenogelase
-
REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
Preferential cleavage: -Tyr-/-
show the reaction diagram
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
hydrolysis of peptide bond
-
-
-
-
CAS REGISTRY NUMBER
COMMENTARY hide
110157-83-0
-
95829-41-7
-
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
enzyme presursor; gene KLK3 or APS; rhesus macaque
SwissProt
Manually annotated by BRENDA team
gene KLK3; glandular kallikrein 3 fragment
SwissProt
Manually annotated by BRENDA team
-
-
-
Manually annotated by BRENDA team
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
malfunction
physiological function
additional information
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
4-morpholinecarbonyl-HSSKLQ-7-amido-4-methylcoumarin + HO
?
show the reaction diagram
-
a fluorogenic enzyme substrate
-
-
?
4-morpholinecarbonyl-HSSKLQ-AMC + H2O
?
show the reaction diagram
-
-
-
-
?
4-morpholinecarbonyl-SKLQ-7-amido-4-methylcoumarin + H2O
?
show the reaction diagram
-
hydrolysis rate is 29.6 pmol/min per 100 pmol of PSA
-
-
?
4-morpholinecarbonyl-SRKSQQY-7-amido-4-methylcoumarin + H2O
?
show the reaction diagram
-
-
-
-
?
Arg-Pro-Tyr 4-nitroanilide + H2O
Arg-Pro-Tyr + 4-nitroaniline
show the reaction diagram
-
-
-
-
?
Bovine serum albumin + H2O
?
show the reaction diagram
-
is more readily hydrolysed than casein
-
-
?
casein + H2O
?
show the reaction diagram
-
proteolytic activity at pH 7.5
-
-
?
EHSSKLQ-7-amido-4-methylcoumarin + H2O
EHSSKLQ + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
epsilon-maleimidocaproyl-Arg-Ser-Ser-Tyr-Tyr-Ser-Leu-p-aminobenzyloxycarbonyl-paclitaxel + H2O
epsilon-maleimidocaproyl-Arg-Ser-Ser-Tyr-Tyr + Ser-Leu-p-aminobenzyloxycarbonyl-paclitaxel
show the reaction diagram
-
water soluble paclitaxel prodrug that is activated specifically by PSA in prostate tissue and prostate carcinoma
-
-
?
Fibronectin + H2O
?
show the reaction diagram
Galectin-3 + H2O
?
show the reaction diagram
Gelatin + H2O
?
show the reaction diagram
GSAKLQ + H2O
?
show the reaction diagram
-
207.2% relative hydrolysis rate
-
-
?
GSSALQ + H2O
?
show the reaction diagram
-
43.2% relative hydrolysis rate
-
-
?
GSSKLA + H2O
?
show the reaction diagram
-
31.5% relative hydrolysis rate
-
-
?
GSSKLH + H2O
?
show the reaction diagram
-
170.6% relative hydrolysis rate
-
-
?
GSSKLQ + H2O
?
show the reaction diagram
-
100% relative hydrolysis rate
-
-
?
GSSKPQ + H2O
?
show the reaction diagram
-
7.2% relative hydrolysis rate
-
-
?
GSSKYQ + H2O
?
show the reaction diagram
-
256.9% relative hydrolysis rate
-
-
?
GSSSLQ + H2O
?
show the reaction diagram
-
52.6% relative hydrolysis rate
-
-
?
HSSKLQ-7-amido-4-methylcoumarin + H2O
?
show the reaction diagram
-
hydrolysis rate is 62.7 pmol/min per 100 pmol of PSA
-
-
?
HSSKLQ-7-amido-4-methylcoumarin + H2O
HSSKLQ + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
HSSKLQ-7-amido-4-trifluoromethyl-coumarin + H2O
?
show the reaction diagram
-
-
-
-
?
IGFBP-3 + H2O
?
show the reaction diagram
-
-
-
-
?
insulin-like growth factor binding protein 5 + H2O
?
show the reaction diagram
-
is degraded by PSA in a dose- and time-dependent manner. Under nonreducing conditions is degraded into two fragments with approximate molecular masses of 20 and 15 kDa. Under reducing conditions, is degraded into 4 distinct fragments with approximate molecular masses of 22 kDa, 21 kDa, 18 kDa and 13 kDa
-
-
?
insulin-like growth factor binding protein-3 + H2O
insulin-like growth factor I + ?
show the reaction diagram
-
i.e. IGF-I
?
insulin-like growth factor binding protein-3 + H2O
insulin-like growth factor-1
show the reaction diagram
-
-
-
-
?
KGISSQY-7-amido-4-methylcoumarin + H2O
KGISSQY + 7-amino-4-methylcoumarin
show the reaction diagram
-
fluorogenic substrate
-
-
?
Laminin + H2O
?
show the reaction diagram
-
-
-
-
?
LSEPAELTDAVK + H2O
PAELTDAVK + LSE
show the reaction diagram
-
-
-
-
?
Lys-Val-Tyr 4-nitroanilide + H2O
Lys-Val-Tyr + 4-nitroaniline
show the reaction diagram
-
-
-
-
?
Mca-QFYSSNK(epsilon-dinitrophenyl) + H2O
?
show the reaction diagram
-
-
-
-
?
MeO-Suc-Arg-Pro-Tyr-4-nitroanilide + H2O
?
show the reaction diagram
-
a chromogenic substrate
-
-
?
methoxy-succinyl-Arg-Pro-Tyr-4-nitroanilide + H2O
methoxy-succinyl-Arg-Pro-Tyr + 4-nitroaniline
show the reaction diagram
methoxysuccinyl-Arg-Pro-Tyr-p-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
morpholinocarbonyl-His-Ser-Ser-Lys-Leu-Gln-7-amido-4-(trifluoromethyl)-coumarin + H2O
?
show the reaction diagram
-
-
-
-
?
morpholinocarbonyl-Lys-Gly-Ile-Ser-Ser-Gln-Tyr-7-amido-4-(trifluoromethyl)-coumarin + H2O
?
show the reaction diagram
-
-
-
-
?
morpholinocarbonyl-Ser-Arg-Lys-Gln-Gln-Tyr-7-amido-4-methylcoumarin + H2O
?
show the reaction diagram
-
-
-
-
?
Mu-SRKSQQY-7-amido-4-methylcoumarin + H2O
Mu-SRKSQQY + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
N,N-dimethylated casein + H2O
?
show the reaction diagram
-
-
-
-
?
N-alpha-benzoyl-DL-Arg 4-nitroanilide + H2O
N-alpha-benzoyl-DL-Arg + 4-nitroaniline
show the reaction diagram
-
trypsin-like activity
-
-
-
N-succinyl-(Ala)3-p-nitroanilide + H2O
?
show the reaction diagram
-
prostate-specific antigen shows limited activity
-
-
?
N-succinyl-Ala-Ala-Pro-Phe-Ala-p-nitroanilide + H2O
?
show the reaction diagram
-
prostate-specific antigen shows limited activity
-
-
?
N-succinyl-Ala-Ala-Pro-Val-p-nitroanilide + H2O
?
show the reaction diagram
-
prostate-specific antigen shows limited activity
-
-
?
N-succinyl-Gly-Pro-Lys-p-nitroanilide + H2O
?
show the reaction diagram
-
prostate-specific antigen activity is 3times higher towards this substrate than towards other synthetic substrates
-
-
?
N-succinyl-L-Ala-L-Ala-L-Pro-L-Phe 4-nitroanilide + H2O
N-succinyl-L-Ala-L-Ala-L-Pro-L-Phe + 4-nitroaniline
show the reaction diagram
-
chymotrypsin-like activity
-
-
?
nidogen-1 + H2O
?
show the reaction diagram
-
-
-
-
o-aminobenzoyl-ISYQSSSTEEQ ethylene diamine 2,4-dinitrophenyl + H2O
o-aminobenzoyl-ISY + QSSSTEEQ ethylene diamine 2,4-dinitrophenyl
show the reaction diagram
o-aminobenzoyl-ISYQSSSTEEQ ethylene diamine 2,4-dinitrophenyl + H2O
o-aminobenzoyl-ISYQ + SSST + EEQ ethylene diamine 2,4-dinitrophenyl
show the reaction diagram
o-aminobenzoyl-NKISYQSSSQ ethylene diamine 2,4-dinitrophenyl + H2O
o-aminobenzoyl-NKISY + Q + SSSQ ethylene diamine 2,4-dinitrophenyl
show the reaction diagram
o-aminobenzoyl-SSIYSNTEEQ ethylene diamine 2,4-dinitrophenyl + H2O
o-aminobenzoyl-SSIY + SNTEEQ ethylene diamine 2,4-dinitrophenyl
show the reaction diagram
o-aminobenzoyl-SSQYSNTEEQ ethylene diamine 2,4-dinitrophenyl + H2O
o-aminobenzoyl-SSQY + SNTEEQ ethylene diamine 2,4-dinitrophenyl
show the reaction diagram
PFR-7-amido-4-methylcoumarin + H2O
PFR + 7-amino-4-methylcoumarin
show the reaction diagram
-
fluorogenic substrate
-
-
?
plasminogen + H2O
angiostatin-like fragments
show the reaction diagram
-
-
-
-
?
plasminogen + H2O
plasmin + ?
show the reaction diagram
-
-
-
?
polypeptide + H2O
peptides
show the reaction diagram
proform of transforming growth factor-beta + H2O
transforming growth factor-beta + ?
show the reaction diagram
-
i.e. IGF-beta
?
PTHrP + H2O
?
show the reaction diagram
semenogelin + H2O
semenogelin fractions
show the reaction diagram
semenogelin + H2O
semenogelin fragments
show the reaction diagram
semenogelin I + H2O
?
show the reaction diagram
-
from human seminal fluid
-
-
?
semenogelin I + H2O
semenogelin fragments
show the reaction diagram
-
-
-
-
?
semenogelin II + H2O
?
show the reaction diagram
-
from human seminal fluid
-
-
?
semenogelin II + H2O
semenogelin fragments
show the reaction diagram
-
-
-
-
?
succinyl-AAPF-7-amido-4-methylcoumarin + H2O
succinyl-AAPF + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
succinyl-Ala-Ala-Phe-7-amido-4-methylcoumarin + H2O
succinyl-Ala-Ala-Phe + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
TGFbeta2 + H2O
activated TGFbeta2
show the reaction diagram
-
-
-
-
?
urokinase-type plasminogen activator receptor + H2O
?
show the reaction diagram
-
-
cleavage within D1-D2 linker sequence and in its D3 juxtamembrane domain
-
?
additional information
?
-
NATURAL SUBSTRATES
NATURAL PRODUCTS
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
Fibronectin + H2O
?
show the reaction diagram
Galectin-3 + H2O
?
show the reaction diagram
insulin-like growth factor binding protein-3 + H2O
insulin-like growth factor I + ?
show the reaction diagram
P07288
-
i.e. IGF-I
?
plasminogen + H2O
plasmin + ?
show the reaction diagram
P07288
-
-
-
?
polypeptide + H2O
peptides
show the reaction diagram
proform of transforming growth factor-beta + H2O
transforming growth factor-beta + ?
show the reaction diagram
P07288
-
i.e. IGF-beta
?
semenogelin + H2O
semenogelin fractions
show the reaction diagram
semenogelin I + H2O
?
show the reaction diagram
-
from human seminal fluid
-
-
?
additional information
?
-
INHIBITORS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
((2R,3R)-3-benzyl-1-(ethylsulfonyl)-4-oxoazetidin-2-yl)methyl benzoate
-
-
((2R,3R)-3-benzyl-4-oxo-1-(phenylsulfonyl)azetidin-2-yl)methyl benzoate
-
-
((2R,3R)-3-benzyl-4-oxo-1-tosylazetidin-2-yl)methyl benzoate
-
-
((2S,3S)-3-benzyl-1-(ethylsulfonyl)-4-oxoazetidin-2-yl)methyl benzoate
-
-
((2S,3S)-3-benzyl-4-oxo-1-(phenylsulfonyl)azetidin-2-yl)methyl benzoate
-
-
((2S,3S)-3-benzyl-4-oxo-1-tosylazetidin-2-yl)methyl benzoate
-
-
(1S)-4-bromo-1-[(3aS,4R,6R,7aR)-3a,5,5-trimethylhexahydro-4,6-methano-1,3,2-benzodioxaborol-2-yl]butan-1-amine
-
-
(2-methoxyphenyl)(3-phenyl-1H-1,2,4-triazol-1-yl)methanone
-
-
(2R,3R)-benzyl 1-(2-(3-(benzyloxycarbonyl)phenyl)acetyl)-3-(4-hydroxybenzyl)-4-oxoazetidine-2-carboxylate
-
-
(2R,3R)-benzyl 1-benzoyl-3-(4-hydroxybenzyl)-4-oxoazetidine-2-carboxylate
-
-
(2R,3R)-benzyl 3-benzyl-1-(2-(3-(benzyloxycarbonyl)phenyl)acetyl)-4-oxoazetidine-2-carboxylate
-
-
(2R,3R)-ethyl 3-benzyl-4-oxo-1-tosylazetidine-2-carboxylate
-
-
(2S,3S)-benzyl 1-(2-(3-(benzyloxycarbonyl)phenyl)acetyl)-3-(4-hydroxybenzyl)-4-oxoazetidine-2-carboxylate
-
-
(2S,3S)-benzyl 1-benzoyl-3-(4-hydroxybenzyl)-4-oxoazetidine-2-carboxylate
-
-
(2S,3S)-benzyl 3-benzyl-1-(2-(3-(benzyloxycarbonyl)phenyl)acetyl)-4-oxoazetidine-2-carboxylate
-
-
(2S,3S)-ethyl 3-benzyl-4-oxo-1-tosylazetidine-2-carboxylate
-
-
(3,4-dimethoxyphenyl)(5-(4-fluorobenzylamino)-3-phenyl-1H-1,2,4-triazol-1-yl)methanone
-
-
(3-benzyl-1-(ethylsulfonyl)-4-oxoazetidin-2-yl)methyl benzoate
-
-
(3-benzyl-4-oxo-1-tosylazetidin-2-yl)methyl benzoate
-
-
(3aR,4R,6R,7aS)-2-[(1R)-1-amino-2-phenylethyl]-5,5-dimethyltetrahydro-4,6-methano-1,3,2-benzodioxaborol-3a(4H)-ol
-
-
(4-[[([(2S,3S)-3-benzyl-1-[(3-carboxyphenyl)acetyl]-4-oxoazetidin-2-yl]carbonyl)oxy]methyl]phenyl)methanaminium trifluoroacetate
-
-
(5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(2-chlorophenyl)methanone
-
-
(5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(2-methoxyphenyl)methanone
-
-
(5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(3,4-dimethoxyphenyl)methanone
-
360 nanomol inhibits by 83%
(5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(4-chlorophenyl)methanone
-
-
(5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(4-fluorophenyl)methanone
-
-
(5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(4-methoxyphenyl)methanone
-
360 nanomol inhibits by 56%
(5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(4-nitrophenyl)methanone
-
-
(5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(p-tolyl)methanone
-
-
(5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(phenyl)methanone
-
-
(5-amino-3-phenyl-1H-1,2,4-triazol-1-yl)(3,4-dimethoxyphenyl)methanone
-
-
(6-[bis[(pyridin-2-yl-kappaN)methyl]amino-kappaN]hexanoyl)(tricarbonyl)rhenium(3+)-Ser-Ser-Gln-Nle-Leu-B(OH)2
-
-
1-(3-chlorobenzyl)-3-phenyl-1H-pyrazol-5-amine
-
-
1-benzyl-3-phenyl-1H-pyrazol-5-amine
-
-
2-(2-methyl-3-nitrophenyl)-4-oxo-4H-3,1-benzoxazin-6-yl acetate
-
-
2-(2-methyl-3-nitrophenyl)-4H-3,1-benzoxazin-4-one
-
360 nanomol inhibits by 61%
2-(2-methylphenyl)-4H-3,1-benzoxazin-4-one
-
-
2-(2-nitrophenyl)-4H-3,1-benzoxazin-4-one
-
-
2-(3-methylphenyl)-4H-3,1-benzoxazin-4-one
-
-
2-(3-nitrophenyl)-4H-3,1-benzoxazin-4-one
-
-
2-(4-bromophenyl)quinazolin-4(3H)-one
-
-
2-(4-methylphenyl)-4H-3,1-benzoxazin-4-one
-
-
2-mercaptoethanol
-
incubation with 3 mM for 30 min at 25C, in 0.1 ml 0.1 M Tris buffer, pH 7.8, causes 84% loss of activity
2-phenyl-4H-3,1-benzoxazin-4-one
-
-
2-phenylquinazolin-4(3H)-one
-
-
2-[(3S)-3-[[N-(6-aminohexanoyl)-L-phenylalanyl]amino]-4-hydroxy-2-oxobutyl]-N1-[(2S)-1-([(1S)-4-bromo-1-[(3aR,4S,6S,7R,7aS)-5,5,7-trimethylhexahydro-4,6-methano-1,3,2-benzodioxaborol-2-yl]butyl]amino)-1-oxohexan-2-yl]pentanediamide
-
-
3-(2-((2R,3R)-3-benzyl-2-((4-carboxybenzyloxy)carbonyl)-4-oxoazetidin-1-yl)-2-oxoethyl)benzoic acid
-
-
3-(2-((2S,3S)-3-benzyl-2-((4-carboxybenzyloxy)carbonyl)-4-oxoazetidin-1-yl)-2-oxoethyl)benzoic acid
-
-
3-(2-(3-benzyl-2-((4-carboxybenzyloxy)carbonyl)-4-oxoazetidin-1-yl)-2-oxoethyl)benzoic acid
-
-
4-(((2R,3R)-1-(2-(3-(benzyloxycarbonyl)phenyl)acetyl)-3-(4-hydroxybenzyl)-4-oxoazetidine-2-carbonyloxy)methyl)benzoic acid
-
-
4-(((2R,3R)-3-benzyl-1-(2-(3-((4-carboxybenzyloxy)carbonyl)phenyl)acetyl)-4-oxoazetidine-2-carbonyloxy)methyl)benzoic acid
-
-
4-(((2R,3R)-3-benzyl-1-(2-(3-(benzyloxycarbonyl)phenyl)acetyl)-4-oxoazetidine-2-carbonyloxy)methyl)benzoic acid
-
-
4-(((2S,3S)-1-(2-(3-(benzyloxycarbonyl)phenyl)acetyl)-3-(4-hydroxybenzyl)-4-oxoazetidine-2-carbonyloxy)methyl)benzoic acid
-
-
4-(((2S,3S)-3-benzyl-1-(2-(3-((4-carboxybenzyloxy)carbonyl)phenyl)acetyl)-4-oxoazetidine-2-carbonyloxy)methyl)benzoic acid
-
-
4-(((2S,3S)-3-benzyl-1-(2-(3-(benzyloxycarbonyl)phenyl)acetyl)-4-oxoazetidine-2-carbonyloxy)methyl)benzoic acid
-
-
4-((1-(2-(3-(benzyloxycarbonyl)phenyl)acetyl)-3-(4-hydroxybenzyl)-4-oxoazetidine-2-carbonyloxy)methyl)benzoic acid
-
-
4-((3-benzyl-1-(2-(3-((4-carboxybenzyloxy)carbonyl)phenyl)acetyl)-4-oxoazetidine-2-carbonyloxy)methyl)benzoic acid
-
-
4-((3-benzyl-1-(2-(3-(benzyloxycarbonyl)phenyl)acetyl)-4-oxoazetidine-2-carbonyloxy)methyl)benzoic acid
-
-
4-(4-oxo-4H-benzo[d][1,3]oxazin-2-yl)phenyl acetate
-
-
4-[([[(2S,3S)-3-benzyl-1-([3-[(benzyloxy)carbonyl]phenyl]acetyl)-4-oxoazetidin-2-yl]carbonyl]oxy)methyl]benzoic acid
-
-
4-[([[(2S,3S)-3-benzyl-4-oxo-1-(phenylacetyl)azetidin-2-yl]carbonyl]oxy)methyl]benzoic acid
-
-
4-[[(3-[2-[(2S,3S)-3-benzyl-2-[[(4-carboxybenzyl)oxy]carbonyl]-4-oxoazetidin-1-yl]-2-oxoethyl]benzoyl)oxy]methyl]benzoic acid
-
-
6-bromo-2-(2-methyl-3-nitrophenyl)-4H-3,1-benzoxazin-4-one
-
-
6-[bis(pyridin-2-ylmethyl)amino]hexanoyl-Ser-Ser-Gln-Nle-Leu-B(OH)2
-
-
alpha1-Antichymotrypsin
alpha2-Macroglobulin
-
-
-
Aprotinin
AUY922
-
-
benzyl (2S,3S)-1-([3-[(benzyloxy)carbonyl]phenyl]acetyl)-3-(4-hydroxybenzyl)-4-oxoazetidine-2-carboxylate
-
-
benzyl (2S,3S)-3-benzyl-1-([3-[(benzyloxy)carbonyl]phenyl]acetyl)-4-oxoazetidine-2-carboxylate
-
-
benzyl 1-(2-(3-(benzyloxycarbonyl)phenyl)acetyl)-3-(4-hydroxybenzyl)-4-oxoazetidine-2-carboxylate
-
-
benzyl 1-([3-[(benzyloxy)carbonyl]phenyl]acetyl)-3-(4-hydroxybenzyl)-4-oxoazetidine-2-carboxylate
-
-
benzyl 1-benzoyl-3-(4-hydroxybenzyl)-4-oxoazetidine-2-carboxylate
-
-
benzyl 3-benzyl-1-(2-(3-(benzyloxycarbonyl)phenyl)acetyl)-4-oxoazetidine-2-carboxylate
-
-
benzyl 3-benzyl-4-oxo-1-(phenylsulfonyl)azetidine-2-carboxylate
-
-
Bovine pancreatic trypsin inhibitor
-
efficient inhibition
-
Cbz-Ser-Ser-Gln-Nle-(boro)-Leu
-
attachment of a bulky metal chelating group to the amino terminal of this peptide does not adversely affect PSA inhibition
Cbz-Ser-Ser-Lys-(4-bromo)Phe-Lys-aldehyde
-
-
Cbz-SSKDL-CHO
-
-
Cbz-SSKLL-CHO
-
-
Cbz-SSKPL-CHO
-
-
Cbz-SSKWL-CHO
-
-
Cbz-SSKYL-CHO
-
-
Cd2+
-
competitive to other metal ions
Co2+
-
competitive to other metal ions
Cu2+
-
competitive to other metal ions
dihydrolipoate
-
incubation with 3 mM for 30 min at 25C, in 0.1 ml 0.1 M Tris buffer, pH 7.8, causes 65% loss of activity
diisopropylfluorophosphate
-
-
dithiothreitol
-
incubation with 3 mM for 30 min at 25C, in 0.1 ml 0.1 M Tris buffer, pH 7.8, causes a complete loss of activity. Alterates the molecular structure probably associated with an altered loading of the protein with dodecyl sulfate anions. Inactivation of the enzyme appears to follow an all-or-none reaction. Residues Cys22-Cys157 and Cys191-Cys220 are dithiothreitol-sensitive
EDTA
-
10 mM inhibits at pH 3.5
glutathione
-
incubation with 3 mM for 30 min at 25C, in 0.1 ml 0.1 M Tris buffer, pH 7.8, causes 35% loss of activity
insulin-like growth factor binding protein 5
-
PSA induced insulin-like growth factor-mediated type I insulin-like growth factor receptor phosphorylation is inhibited by coincubation with insulin-like growth factor binding protein 5
-
iodoacetate
-
3 mM inhibits at pH 7.5 with casein as a substrate and at pH 3.5 with bovine serum albumin as a substrate
L-1-tosylamido-2-phenylethyl chloromethyl ketone
-
-
Leupeptin
methylmethane thiosulphonate
-
1 mM completely inhibits with bovine serum albumin as a substrate at pH 3.5
morpholinocarbonyl-Ser-Ser-Gln-Nle-Leu-B(OH)2
-
-
N-p-tosyl-Lys chloromethyl ketone
-
3 mM inhibits at pH 3.5 with bovine serum albumin as a substrate but does not inhibit enzyme activity at pH 7.5 with casein as a substrate
N-tosyl-Phe chloromethyl ketone
-
3 mM inhibits at pH 3.5 with bovine serum albumin as a substrate but does not inhibit enzyme activity at pH 7.5 with casein as a substrate
N-[(2S)-8-amino-5-[[(2S)-1-[[(1S)-1-(dihydroxyboranyl)-2-phenylethyl]amino]-1-oxohexan-2-yl]carbamoyl]-1-hydroxy-3,8-dioxooctan-2-yl]-Na-(6-aminohexanoyl)-L-phenylalaninamide
-
-
N-[(2S)-8-amino-5-[[(2S)-1-[[(1S)-4-bromo-1-(dihydroxyboranyl)butyl]amino]-1-oxohexan-2-yl]carbamoyl]-1-hydroxy-3,8-dioxooctan-2-yl]-Na-(6-aminohexanoyl)-L-phenylalaninamide
-
-
N-[(2S)-8-amino-5-[[(2S)-1-[[(1S)-4-bromo-1-(dihydroxyboranyl)butyl]amino]-1-oxohexan-2-yl]carbamoyl]-1-hydroxy-3,8-dioxooctan-2-yl]-Na-[6-[(4-iodobenzoyl)amino]hexanoyl]-L-phenylalaninamide
-
-
N-[(3S)-3-[(6-aminohexanoyl)amino]-4-(naphthalen-2-yl)butanoyl]-L-seryl-L-glutaminyl-N-[(1S)-1-(dihydroxyboranyl)-2-phenylethyl]-L-norleucinamide
-
-
N-[(3S)-3-[(6-aminohexanoyl)amino]-4-(naphthalen-2-yl)butanoyl]-L-seryl-L-glutaminyl-N-[(1S)-4-bromo-1-(dihydroxyboranyl)butyl]-L-norleucinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-3-cyclohexyl-L-alanyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-norleucinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-alanyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-norleucinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-alpha-aspartyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-norleucinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-alpha-glutamyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-norleucinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-asparaginyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-norleucinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-glutaminyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-norleucinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-homoseryl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-norleucinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-(4S)-4-hydroxy-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-prolinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-3-(2-naphthyl)-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-alaninamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-3-cyclohexyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-alaninamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-4-bromo-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-phenylalaninamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(1S)-2-oxo-1-phenylethyl]-L-leucinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-1-(4-hydroxyphenyl)-3-oxopropan-2-yl]-L-leucinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-1-(acetylamino)-3-oxopropan-2-yl]-L-leucinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-1-(benzoylamino)-3-oxopropan-2-yl]-L-leucinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-1-(formylamino)-3-oxopropan-2-yl]-L-leucinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-1-oxo-3-(propanoylamino)propan-2-yl]-L-leucinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-1-oxo-3-phenylpropan-2-yl]-L-leucinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-1-oxohexan-2-yl]-L-leucinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-1-[(2-methylpropanoyl)amino]-3-oxopropan-2-yl]-L-leucinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-3-methyl-1-oxobutan-2-yl]-L-leucinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-(dimethylamino)-1,4-dioxobutan-2-yl]-L-leucinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-(methylsulfanyl)-1-oxobutan-2-yl]-L-leucinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-(methylsulfinyl)-1-oxobutan-2-yl]-L-leucinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-cyano-1-oxobutan-2-yl]-L-leucinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-alaninamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-alpha-asparagine
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-alpha-glutamine
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-histidinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-homoserinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-isoleucinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-leucinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-lysinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-methioninamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-norleucinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-norvalinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-phenylalaninamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-prolinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-serinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-threoninamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-tyrosinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-valinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]glycinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-5-(dimethylamino)-1,5-dioxopentan-2-yl]-L-leucinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-5-amino-1,5-dioxopentan-2-yl]-L-leucinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N1-[(2S)-4-methyl-1-oxopentan-2-yl]-L-aspartamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N1-[(2S)-4-methyl-1-oxopentan-2-yl]-L-glutamamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-S-tert-butyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-cysteinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-methionyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-norleucinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-prolyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-norleucinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-seryl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-norleucinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-threonyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-norleucinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-N-[(1S)-2-[[(2S)-4-methyl-1-oxopentan-2-yl]amino]-2-oxo-1-phenylethyl]-L-lysinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-N-[(2S)-1-[[(2S)-4-methyl-1-oxopentan-2-yl]amino]-4-(methylsulfinyl)-1-oxobutan-2-yl]-L-lysinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-serylglycyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-norleucinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-N-[(2S)-1-[[(2S)-1-[[(2S)-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-(methylsulfinyl)-1-oxobutan-2-yl]-L-serinamide
-
-
N1-[(2S)-1-([(1S)-4-bromo-1-[(3aR,4S,6S,7R,7aS)-5,5,7-trimethylhexahydro-4,6-methano-1,3,2-benzodioxaborol-2-yl]butyl]amino)-1-oxohexan-2-yl]-2-[(3S)-4-hydroxy-3-[(N-[6-[(4-iodobenzoyl)amino]hexanoyl]-L-phenylalanyl)amino]-2-oxobutyl]pentanediamide
-
-
N2-[(5S)-5-[[N-(6-aminohexanoyl)-L-alanyl]amino]-2-(3-amino-3-oxopropyl)-6-hydroxy-4-oxohexanoyl]-N-[(1S)-1-(dihydroxyboranyl)-2-phenylethyl]-L-norleucinamide
-
-
N2-[(5S)-5-[[N-(6-aminohexanoyl)-L-alanyl]amino]-2-(3-amino-3-oxopropyl)-6-hydroxy-4-oxohexanoyl]-N-[(1S)-4-bromo-1-(dihydroxyboranyl)butyl]-L-norleucinamide
-
-
p-hydroxyphenylmercurisulfonate
-
1 mM completely inhibits with bovine serum albumin as a substrate at pH 3.5
Phenylmethylsulphonyl fluoride
-
3 mM inhibits at pH 7.5 with casein as a substrate and at pH 3.5 with bovine serum albumin as a substrate
Pregnancy-zone protein
-
-
-
R/S-diphenyl[N-benzyloxycarbonylamino(4-carbamoylphenyl)methyl]phosphonate
-
-
-
Serum
-
inhibits the mature enzyme
-
Soybean trypsin inhibitor
-
-
-
spermidine
-
-
Tris[2-carboxyethyl] phosphine
-
incubation with 3 mM for 30 min at 25C, in 0.1 ml 0.1 M Tris buffer, pH 7.8, causes 87% loss of activity
Z-Gln-Leu-B(OH)2
-
-
Z-Gln-Nle-H
-
-
Z-KL-H
-
-
Z-KLL-H
-
-
Z-Lys-Leu-B(OH)2
-
-
Z-Lys-Leu-Leu-B(OH)2
-
-
Z-Lys-Leu-Nle-B(OH)2
-
-
Z-Lys-Leu-Nle-H
-
-
Z-Lys-Nle-H
-
-
Z-QL-H
-
-
Z-Ser-(N-Me)Ser-(N2-Me)Lys-(N-Me)Leu-Leu-B(OH)2
-
-
Z-Ser-(N-Me)Ser-Lys-(N-Me)Leu-Leu-B(OH)2
-
-
Z-Ser-(N-Me)Ser-Lys-Leu-Leu-B(OH)2
-
-
Z-Ser-Ser-(N2-Me)Lys-Leu-Leu-B(OH)2
-
-
Z-Ser-Ser-Gln-Nle-Leu-B(OH)2
-
-
Z-Ser-Ser-Lys-(N-Me)Leu-Leu-B(OH)2
-
-
Z-Ser-Ser-Lys-Leu-B(OH)2
-
-
Z-Ser-Ser-Lys-Leu-D-Leu-H
-
-
Z-Ser-Ser-Lys-Leu-D-Nle-H
-
-
Z-Ser-Ser-Lys-Leu-Leu-B(OH)2
-
-
Z-Ser-Ser-Lys-Leu-Nle-B(OH)2
-
-
Z-Ser-Ser-Lys-Leu-Nle-H
-
-
Z-Ser-Ser-Lys-Nle-B(OH)2
-
-
Z-Ser-Ser-Lys-Nle-H
-
-
Z-Ser-Ser-Lys-Nle-Leu-B(OH)2
-
-
Z-SKLL-H
-
-
Z-SSKAL-H
-
-
Z-SSKF(4-Br)L-H
-
-
Z-SSKFL-H
-
-
Z-SSKIL-H
-
-
Z-SSKKL-H
-
-
Z-SSKL-H
-
-
Z-SSKLD-H
-
-
Z-SSKLL-H
-
-
Z-SSKML-H
-
-
Z-SSKQL-H
-
-
Z-SSKTL-H
-
-
Z-SSKVL-H
-
-
Z-SSKYL-H
-
-
Z-YL-H
-
-
additional information
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
17-allylamine-17-demethoxygeldanamycin
-
-
androgens
-
upregulation
-
AUY922
-
reduces PSA concentration in a dose-dependent manner (2fold more than insulin-like growth factor-binding protein 2) and is accompanied by androgen receptor decrease
B2-peptide
-
-
-
CVAYCIEHHCWTC
CVFAHNYDYLVC
dihydrotestosterone
-
hormonal treatment of BT-474 cells with dihydrotestosterone (an androgen) for 48 h triggers an increase of prostate-specific antigen concentration in the supernatant of these cells
insulin-like growth factor-binding protein 2
-
-
-
norgestrel
-
hormonal treatment of BT-474 cells with norgestrel (an androgenic progestin) for 48 h triggers an increase of prostate-specific antigen concentration in the supernatant of these cells
progestins
-
upregulation in breast cancer
additional information
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
1.58
4-morpholinecarbonyl-HSSKLQ-7-amido-4-methylcoumarin
-
pH 7.4, 37C
-
1.4 - 4.2
4-morpholinecarbonyl-HSSKLQ-AMC
0.14
4-morpholinecarbonyl-SRKSQQY-7-amido-4-methylcoumarin
-
in 50 mM Tris buffer, 0.1 M NaCl, pH 7.8
1.7
Arg-Pro-Tyr 4-nitroanilide
-
-
0.47
HSSKLQ-7-amido-4-methylcoumarin
-
-
1.3
Lys-Val-Tyr 4-nitroanilide
-
-
0.077
Mca-QFYSSNK(epsilon-dinitrophenyl)
-
-
5.72
MeO-Suc-Arg-Pro-Tyr-4-nitroanilide
-
pH 7.4, 37C
15.3
N-succinyl-L-Ala-L-Ala-L-Pro-L-Phe 4-nitroanilide
-
-
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.19
4-morpholinecarbonyl-HSSKLQ-7-amido-4-methylcoumarin
Homo sapiens
-
pH 7.4, 37C
-
0.028
Arg-Pro-Tyr 4-nitroanilide
Homo sapiens
-
-
0.022
Lys-Val-Tyr 4-nitroanilide
Homo sapiens
-
-
0.75
MeO-Suc-Arg-Pro-Tyr-4-nitroanilide
Homo sapiens
-
pH 7.4, 37C
0.075
N-succinyl-L-Ala-L-Ala-L-Pro-L-Phe 4-nitroanilide
Homo sapiens
-
-
kcat/KM VALUE [1/mMs-1]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.122
4-morpholinecarbonyl-HSSKLQ-7-amido-4-methylcoumarin
Homo sapiens
-
pH 7.4, 37C
202426
23000
HSSKLQ-7-amido-4-methylcoumarin
Homo sapiens
-
-
40604
3900
Mca-QFYSSNK(epsilon-dinitrophenyl)
Homo sapiens
-
-
81549
0.133
MeO-Suc-Arg-Pro-Tyr-4-nitroanilide
Homo sapiens
-
pH 7.4, 37C
173724
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.00134
(4-[[([(2S,3S)-3-benzyl-1-[(3-carboxyphenyl)acetyl]-4-oxoazetidin-2-yl]carbonyl)oxy]methyl]phenyl)methanaminium trifluoroacetate
-
-
0.0284
(6-[bis[(pyridin-2-yl-kappaN)methyl]amino-kappaN]hexanoyl)(tricarbonyl)rhenium(3+)-Ser-Ser-Gln-Nle-Leu-B(OH)2
-
-
0.00898
4-[([[(2S,3S)-3-benzyl-1-([3-[(benzyloxy)carbonyl]phenyl]acetyl)-4-oxoazetidin-2-yl]carbonyl]oxy)methyl]benzoic acid
-
-
0.0243
4-[([[(2S,3S)-3-benzyl-4-oxo-1-(phenylacetyl)azetidin-2-yl]carbonyl]oxy)methyl]benzoic acid
-
-
0.00584
4-[[(3-[2-[(2S,3S)-3-benzyl-2-[[(4-carboxybenzyl)oxy]carbonyl]-4-oxoazetidin-1-yl]-2-oxoethyl]benzoyl)oxy]methyl]benzoic acid
-
-
0.0156
6-[bis(pyridin-2-ylmethyl)amino]hexanoyl-Ser-Ser-Gln-Nle-Leu-B(OH)2
-
-
0.000226
benzyl (2S,3S)-1-([3-[(benzyloxy)carbonyl]phenyl]acetyl)-3-(4-hydroxybenzyl)-4-oxoazetidine-2-carboxylate
-
-
0.00143
benzyl (2S,3S)-3-benzyl-1-([3-[(benzyloxy)carbonyl]phenyl]acetyl)-4-oxoazetidine-2-carboxylate
-
-
0.000348
benzyl 1-([3-[(benzyloxy)carbonyl]phenyl]acetyl)-3-(4-hydroxybenzyl)-4-oxoazetidine-2-carboxylate
-
-
0.000025
Cbz-Ser-Ser-Gln-Nle-(boro)-Leu
-
-
0.5
Cbz-Ser-Ser-Lys-(4-bromo)Phe-Lys-aldehyde
-
in 50 mM Tris buffer, 100 mM NaCl, pH 7.8, 10% DMSO
1
Cbz-SSKDL-CHO
-
in 50 mM Tris buffer, 100 mM NaCl, pH 7.8, 10% DMSO
0.00651
Cbz-SSKLL-CHO
-
in 50 mM Tris buffer, 100 mM NaCl, pH 7.8, 10% DMSO
0.5
Cbz-SSKPL-CHO
-
in 50 mM Tris buffer, 100 mM NaCl, pH 7.8, 10% DMSO
0.1553
Cbz-SSKWL-CHO
-
in 50 mM Tris buffer, 100 mM NaCl, pH 7.8, 10% DMSO
0.01309
Cbz-SSKYL-CHO
-
in 50 mM Tris buffer, 100 mM NaCl, pH 7.8, 10% DMSO
0.0253
morpholinocarbonyl-Ser-Ser-Gln-Nle-Leu-B(OH)2
-
-
0.0131
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-3-cyclohexyl-L-alanyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-norleucinamide
-
-
0.5
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-alanyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-norleucinamide
-
-
1
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-alpha-aspartyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-norleucinamide
0.0182
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-asparaginyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-norleucinamide
-
-
0.0039
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-glutaminyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-norleucinamide
-
-
0.0088
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-homoseryl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-norleucinamide
-
-
0.5
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-(4S)-4-hydroxy-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-prolinamide
-
-
0.1
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-3-(2-naphthyl)-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-alaninamide
-
-
0.05
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-3-cyclohexyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-alaninamide
-
-
0.5
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-4-bromo-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-phenylalaninamide
-
-
0.1
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(1S)-2-oxo-1-phenylethyl]-L-leucinamide
-
-
0.00037
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-1-(4-hydroxyphenyl)-3-oxopropan-2-yl]-L-leucinamide
-
-
0.00391
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-1-(acetylamino)-3-oxopropan-2-yl]-L-leucinamide
-
-
0.025
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-1-(benzoylamino)-3-oxopropan-2-yl]-L-leucinamide
-
-
0.00091 - 0.000918
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-1-(formylamino)-3-oxopropan-2-yl]-L-leucinamide
0.00984
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-1-oxo-3-(propanoylamino)propan-2-yl]-L-leucinamide
-
-
0.00057
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-1-oxo-3-phenylpropan-2-yl]-L-leucinamide
-
-
0.01124
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-1-oxohexan-2-yl]-L-leucinamide
-
-
0.01328
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-1-[(2-methylpropanoyl)amino]-3-oxopropan-2-yl]-L-leucinamide
-
-
0.1
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-3-methyl-1-oxobutan-2-yl]-L-leucinamide
-
-
0.01309
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-(dimethylamino)-1,4-dioxobutan-2-yl]-L-leucinamide
-
-
0.00384
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-(methylsulfanyl)-1-oxobutan-2-yl]-L-leucinamide
-
-
0.00725
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-(methylsulfinyl)-1-oxobutan-2-yl]-L-leucinamide
-
-
0.00814
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-cyano-1-oxobutan-2-yl]-L-leucinamide
-
-
0.1
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-alaninamide
-
-
1
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-alpha-asparagine
0.0186
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-histidinamide
-
-
0.0294
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-homoserinamide
-
-
0.0374
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-isoleucinamide
-
-
0.0065 - 0.00651
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-leucinamide
0.05
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-lysinamide
-
-
0.0137
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-methioninamide
-
-
0.0036
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-norleucinamide
-
-
0.0044
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-norvalinamide
-
-
0.0119
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-phenylalaninamide
-
-
0.5
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-prolinamide
-
-
0.05
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-serinamide
-
-
0.1
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-threoninamide
-
-
0.0131
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-tyrosinamide
-
-
0.05
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-valinamide
-
-
1
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]glycinamide
-
-
0.00253
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-5-(dimethylamino)-1,5-dioxopentan-2-yl]-L-leucinamide
-
-
0.04521
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-5-amino-1,5-dioxopentan-2-yl]-L-leucinamide
-
-
0.0419
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N1-[(2S)-4-methyl-1-oxopentan-2-yl]-L-aspartamide
-
-
0.0218
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N1-[(2S)-4-methyl-1-oxopentan-2-yl]-L-glutamamide
-
-
0.05
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-S-tert-butyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-cysteinamide
-
-
0.0075
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-methionyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-norleucinamide
-
-
1
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-prolyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-norleucinamide
-
-
0.0199
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-seryl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-norleucinamide
-
-
0.0438
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-threonyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-norleucinamide
-
-
0.05
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-N-[(1S)-2-[[(2S)-4-methyl-1-oxopentan-2-yl]amino]-2-oxo-1-phenylethyl]-L-lysinamide
-
-
0.0128
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-N-[(2S)-1-[[(2S)-4-methyl-1-oxopentan-2-yl]amino]-4-(methylsulfinyl)-1-oxobutan-2-yl]-L-lysinamide
-
-
1
N-[(benzyloxy)carbonyl]-L-seryl-L-serylglycyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-norleucinamide
-
-
0.0259
N-[(benzyloxy)carbonyl]-L-seryl-N-[(2S)-1-[[(2S)-1-[[(2S)-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-(methylsulfinyl)-1-oxobutan-2-yl]-L-serinamide
-
-
0.000072
N2-[(5S)-5-[[N-(6-aminohexanoyl)-L-alanyl]amino]-2-(3-amino-3-oxopropyl)-6-hydroxy-4-oxohexanoyl]-N-[(1S)-1-(dihydroxyboranyl)-2-phenylethyl]-L-norleucinamide
-
pH 7.8, 37C
0.2652
Z-Gln-Leu-B(OH)2
-
-
1
Z-Gln-Nle-H
0.1
Z-KLL-H
-
-
0.3535
Z-Lys-Leu-B(OH)2
-
-
0.00598
Z-Lys-Leu-Leu-B(OH)2
-
-
0.02357
Z-Lys-Leu-Nle-B(OH)2
-
-
0.4141
Z-Lys-Leu-Nle-H
-
-
1
Z-Lys-Nle-H
0.05
Z-Ser-(N-Me)Ser-(N2-Me)Lys-(N-Me)Leu-Leu-B(OH)2
-
-
0.0056
Z-Ser-(N-Me)Ser-Lys-(N-Me)Leu-Leu-B(OH)2
-
-
0.0002
Z-Ser-(N-Me)Ser-Lys-Leu-Leu-B(OH)2
-
-
0.0199
Z-Ser-Ser-(N2-Me)Lys-Leu-Leu-B(OH)2
-
-
0.0275
Z-Ser-Ser-Gln-Nle-Leu-B(OH)2
-
-
0.0025
Z-Ser-Ser-Lys-(N-Me)Leu-Leu-B(OH)2
-
-
0.01849
Z-Ser-Ser-Lys-Leu-B(OH)2
-
-
1
Z-Ser-Ser-Lys-Leu-D-Leu-H
0.000065
Z-Ser-Ser-Lys-Leu-Leu-B(OH)2
-
-
0.000398
Z-Ser-Ser-Lys-Leu-Nle-B(OH)2
-
-
0.01124
Z-Ser-Ser-Lys-Leu-Nle-H
-
-
0.03421
Z-Ser-Ser-Lys-Nle-B(OH)2
-
-
1
Z-Ser-Ser-Lys-Nle-H
-
-
0.0484
Z-Ser-Ser-Lys-Nle-Leu-B(OH)2
-
-
0.04243
Z-SKLL-H
-
-
0.1
Z-SSKAL-H
-
-
0.5
Z-SSKF(4-Br)L-H
-
-
0.0119
Z-SSKFL-H
-
-
0.03743
Z-SSKIL-H
-
-
0.05785
Z-SSKKL-H
-
-
1
Z-SSKL-H
0.0065
Z-SSKLL-H
-
-
0.0137
Z-SSKML-H
-
-
0.02179
Z-SSKQL-H
-
-
0.1
Z-SSKTL-H
-
-
0.07071
Z-SSKVL-H
-
-
0.0139
Z-SSKYL-H
-
-
0.5
Z-YL-H
-
-
0.0056
Zn2+
-
pH 8.0, 37C, with methoxy-succinyl-Arg-Pro-Tyr-4-nitrophenyl
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.08
(2-methoxyphenyl)(3-phenyl-1H-1,2,4-triazol-1-yl)methanone
Homo sapiens
-
-
0.1
(2R,3R)-ethyl 3-benzyl-4-oxo-1-tosylazetidine-2-carboxylate
Homo sapiens
-
-
0.0011
(2S,3S)-ethyl 3-benzyl-4-oxo-1-tosylazetidine-2-carboxylate
Homo sapiens
-
-
0.08
(3,4-dimethoxyphenyl)(5-(4-fluorobenzylamino)-3-phenyl-1H-1,2,4-triazol-1-yl)methanone
Homo sapiens
-
-
0.0022
(3-benzyl-1-(ethylsulfonyl)-4-oxoazetidin-2-yl)methyl benzoate
Homo sapiens
-
-
0.0163
(5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(2-chlorophenyl)methanone
Homo sapiens
-
-
0.0298
(5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(2-methoxyphenyl)methanone
Homo sapiens
-
-
0.0005
(5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(3,4-dimethoxyphenyl)methanone
Homo sapiens
-
-
0.0022
(5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(4-chlorophenyl)methanone
Homo sapiens
-
-
0.0041
(5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(4-fluorophenyl)methanone
Homo sapiens
-
-
0.0009
(5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(4-methoxyphenyl)methanone
Homo sapiens
-
-
0.08
(5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(4-nitrophenyl)methanone
Homo sapiens
-
-
0.0038
(5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(p-tolyl)methanone
Homo sapiens
-
-
0.0096
(5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(phenyl)methanone
Homo sapiens
-
-
0.0169
(5-amino-3-phenyl-1H-1,2,4-triazol-1-yl)(3,4-dimethoxyphenyl)methanone
Homo sapiens
-
-
0.08
1-(3-chlorobenzyl)-3-phenyl-1H-pyrazol-5-amine
0.0054
2-(2-methyl-3-nitrophenyl)-4-oxo-4H-3,1-benzoxazin-6-yl acetate
Homo sapiens
-
-
0.0003
2-(2-methyl-3-nitrophenyl)-4H-3,1-benzoxazin-4-one
Homo sapiens
-
-
0.0291
2-(2-methylphenyl)-4H-3,1-benzoxazin-4-one
Homo sapiens
-
-
0.0142
2-(2-nitrophenyl)-4H-3,1-benzoxazin-4-one
Homo sapiens
-
-
0.08
2-(3-methylphenyl)-4H-3,1-benzoxazin-4-one
0.0035
4-((1-(2-(3-(benzyloxycarbonyl)phenyl)acetyl)-3-(4-hydroxybenzyl)-4-oxoazetidine-2-carbonyloxy)methyl)benzoic acid
Homo sapiens
-
-
0.0058
4-((3-benzyl-1-(2-(3-((4-carboxybenzyloxy)carbonyl)phenyl)acetyl)-4-oxoazetidine-2-carbonyloxy)methyl)benzoic acid
Homo sapiens
-
-
0.009
4-((3-benzyl-1-(2-(3-(benzyloxycarbonyl)phenyl)acetyl)-4-oxoazetidine-2-carbonyloxy)methyl)benzoic acid
Homo sapiens
-
-
0.08
4-(4-oxo-4H-benzo[d][1,3]oxazin-2-yl)phenyl acetate
Homo sapiens
-
-
0.049
6-bromo-2-(2-methyl-3-nitrophenyl)-4H-3,1-benzoxazin-4-one
Homo sapiens
-
-
0.000001
AUY922
Homo sapiens
-
-
0.00034
benzyl 1-(2-(3-(benzyloxycarbonyl)phenyl)acetyl)-3-(4-hydroxybenzyl)-4-oxoazetidine-2-carboxylate
Homo sapiens
-
-
0.01
benzyl 1-benzoyl-3-(4-hydroxybenzyl)-4-oxoazetidine-2-carboxylate
Homo sapiens
-
-
0.00143
benzyl 3-benzyl-1-(2-(3-(benzyloxycarbonyl)phenyl)acetyl)-4-oxoazetidine-2-carboxylate
Homo sapiens
-
-
0.00308
benzyl 3-benzyl-4-oxo-1-(phenylsulfonyl)azetidine-2-carboxylate
Homo sapiens
-
-
0.15
dithiothreitol
Homo sapiens
-
at 25C, in 0.1 ml 0.1 M Tris buffer, pH 7.8
0.00025
R/S-diphenyl[N-benzyloxycarbonylamino(4-carbamoylphenyl)methyl]phosphonate
Homo sapiens
-
pH and temperature not specified in the publication
-
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
0.004
-
purified recombinant active PSA
additional information
-
-
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
3.5
-
bovine serum albumin is degraded 3-4times faster at pH 3.5 than at pH 7.5
7.4
-
assay at
7.8
-
assay at
8.3
-
assay at
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
pI VALUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
6.4
-
several isozymes of active mature enzyme
8.2
-
2 enzyme proforms with different pI: pH 8.2 and pH 8.4
8.4
-
2 enzyme proforms with different pI: pH 8.2 and pH 8.4
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
-
prostate cancer cell, expressing GRP78 on its surface
Manually annotated by BRENDA team
-
kallikrein-related peptidase 3 is present in hippocampal pyramidal neurons
Manually annotated by BRENDA team
-
secretory epithelial cells, concentration of enzyme in nonprostatic tissue represents less than 1% of the amount in normal prostate
Manually annotated by BRENDA team
-
Paneth cells, pronounced expression of enzyme
Manually annotated by BRENDA team
-
-
Manually annotated by BRENDA team
-
breast carcinoma cell line, enzyme is upregulated by progestins and androgens
Manually annotated by BRENDA team
-
activation peptide of PSA is filtered from the bloodstream by the kidney, and is detectable in the urine of patients with prostate cancer, but not controls. Serum PSA concentration is dependent on how much PSA gains access to the bloodstream and how efficiently it is removed
Manually annotated by BRENDA team
additional information
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY hide
GeneOntology No.
LITERATURE
SOURCE
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
26500
-
calculation from amino acid sequence
28000
-
-
28110 - 30000
-
inactive zymogen peak 2, gel filtration, SDS-PAGE and mass spectrometry
28880 - 30000
-
active mature enzyme, gel filtration and mass spectrometry
30000
-
calculated from the amino acid composition of isolated prostate-specific antigen and proteinase
34000
-
calculated from the elution profile
65000
-
Western blotting of PSA-spiked mouse serum
85000
-
Western blotting of PSA-spiked mouse serum
87000
-
inactive zymogen peak 1, gel filtration
160000
-
Western blotting of PSA-spiked mouse serum
200000
-
Western blotting of PSA-spiked mouse serum
SUBUNITS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
dimer
-
crystallography
monomer
-
1 * 55000, SDS-PAGE, proPSA, 1 * 54000, SDS-PAGE, active PSA
additional information
-
active mature enzyme consists of only 1 chain
POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
glycoprotein
proteolytic modification
-
enzyme can be activated by recombinant kallikrein 2
Crystallization/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
PSA in complex with monoclonal antibody 8G8F5 or PSA in complex with both 8G8F5 and the fluorogenic substrate morpholinocarbonyl-Lys-Gly-Ile-Ser-Ser-Gln-Tyr-7-amido-4-(trifluoromethyl)-coumarin, by sitting-drop vapor diffusion, between 2.83-3.33 A resolution. Belongs to space group P41212
-
GENERAL STABILITY
ORGANISM
UNIPROT
LITERATURE
stable at 0.5 M urea in the activity assay, which is needed to prevent coagualtion of th semenogelins
-
STORAGE STABILITY
ORGANISM
UNIPROT
LITERATURE
4C, Tris-HCl buffer
-
Purification/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
by centrifugation and gel filtration
-
by centrifugation, fractional precipitation by ammonium sulphate, ion-exchange chromatography and gel filtration, purified to homogeneity
-
by gel filtration
-
by HPLC
-
by lysozyme, sonication, and centrifugation, His-tagged PSA solublized from inclusion bodies by urea and purified on nickel-chelate resin. GST-fused PSA solublized from inclusion bodies by sarcosyl and purified on glutathione agarose beads
-
by thiophilic absorption chromatography
-
fast purification method with 90% of purity and 50% of recovery
-
free and complexed PSA, by gel filtration and immunoadsorption
-
from LNCaP cell culture medium
-
from seminal plasma
-
native active enzyme from seminal plasma by immunoaffinity chromatography and anion-exchange chromatography
-
nickel-nitrilotriacetic acid-Sepharose column chromatography and benzamidine-Sepharose column chromatography
-
one third of the purified protein is enzymatically inactive, due to carboxy-terminal cleavage of Lys145
-
Cloned/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
expressed in Escherichia coli M15(pREP4) cells
-
expressed in HUVEC cells
-
gene hK3 or KLK3, genetic organization and structure of the kallikrein gene family, clustered on chromosome 19q13.3-q13.4
-
gene structure
-
male C57BL/6 mice injected with recombinant adenoviruses containing rAd/PSMA, rAd/PSCA and rAd/STEAP
-
proPSA and active PSA cDNA cleaved with EcoRI and HindIII and cloned into vector pET28(a)+, expressed in Escherichia coli strain BL21(DE3). Recombinant vector cleaved with EcoRI and XhoI, inserted into vector pGEX4T-1 and expressed in Escherichia coli strain BL21(DE3)
-
recombinant proteins of proPSA and active PSA cloned into pGEX4T-1 expression vector that produces recombinant proteins with N-terminal GST tags. The proteins expressed in Escherichia coli BL21(DE3)
-
structure of the gene and linkage to the kallikrein-like gene hGK-1
-
EXPRESSION
ORGANISM
UNIPROT
LITERATURE
at a dose of 0.00001 mM 17-allylamine-17-demethoxygeldanamycin, PSA expression is reduced by 40%. 17-allylamine-17-demethoxygeldanamycin-treated LNCaP cells reveal about 25% inhibition of PSA secretion. Potency of AUY922 to reduce PSA expression at inhibitor concentrations lower than 0.000005 mM (non-toxic at these levels) is greater (8fold) than the potency of 17-allylamine-17-demethoxygeldanamycin. Hsp90 inhibitors target PSA secretion via the androgen receptor pathway
-
inactive proenzyme is produced at high concentrations by epithelial cells of the prostate
-
LNCaP and 22RV1 xenograft tumors express PSA
-
PSA expression is lower in malignant than in normal prostatic epithelium and it is further reduced in poorly differentiated tumors
-
PSA-specific monoclonal antibodies block proteolysis of extracellular matrix components and decrease invasion of PSA-producing LNCaP cells in Matrigel invasion assays
-
shRNA mediated knockdown of SNF2-related CBP activator protein results in decreased H2A.Z binding at the enhancer region of the PSA promoter and decreased expression of PSA in prostate cancer cells
-
SNF2-related CBP activator protein is a physiologically relevant mediator of PSA expression: it enhances the transcriptional activity of PSA and this activation is further enhanced in the presence of dihydrotestosterone. SNF2-related CBP activator protein activates hormone-dependent transcription of the androgen responsive, PSA-Luciferase reporter gene in prostate cells
-
treatment of LNCaP cells with 10 microg/ml soy isoflavones alone causes 40% inhibition of PSA secretion to the supernatant compared to control, whereas treatment of the cells with 20 micromol curcumin causes 20% inhibition. Combined treatment of curcumin and soy isoflavones enhances inhibition of PSA production and expression of androgen receptor in LNCaP cells: treatment with 10 microg/ml isoflavones combined with 20 micromol curcumin causes almost complete inhibition of PSA production. In a randomized, placebo-controlled clinical trial, a combined treatment of soy isoflavones and curcumin decreases serum PSA in those subjects whose baseline PSA is more than 10 ng/ml
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Renatured/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
APPLICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
analysis
diagnostics
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medicine
additional information
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human seminal proteinase and prostate-specific antigen are identical
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