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Information on EC 3.4.21.77 - semenogelase and Organism(s) Homo sapiens and UniProt Accession P07288

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EC Tree
     3 Hydrolases
         3.4 Acting on peptide bonds (peptidases)
             3.4.21 Serine endopeptidases
                3.4.21.77 semenogelase
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Select one or more organisms in this record: ?
This record set is specific for:
Homo sapiens
UNIPROT: P07288 not found.
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Word Map
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The taxonomic range for the selected organisms is: Homo sapiens
The enzyme appears in selected viruses and cellular organisms
Reaction Schemes
hide
Preferential cleavage: -Tyr-/-
Synonyms
prostate-specific antigen, prostate stem cell antigen, gamma-sm, gamma-seminoprotein, steap, gamma-ngf, six-transmembrane epithelial antigen of the prostate, kallikrein-related peptidase 3, kallikrein 3, seminal proteinase, more
SYNONYM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
gama-SM protein
-
gamma-seminoprotein
-
kallikrein 3
-
kallikrein-related peptidase-3
-
prostate specific antigen
-
antigen (human clone lambdaHPSA-1 prostate-specific protein moiety reduced)
-
-
-
-
antigen PSA (human clone 5P1 protein moiety reduced)
-
-
-
-
antigen PSA (human prostate-specific)
-
-
-
-
gamma-seminoglycoprotein (human protein moiety reduced)
-
-
-
-
gamma-SM
-
-
-
-
glandular kallikrein
-
-
-
-
hK3/PSA
-
exhibits a chymotrypsin-like specificity preferring large hydrophobic or polar residues at the P1 position
kallikrein 3
kallikrein-related peptidase 3
-
-
P-30 antigen
-
-
-
-
prostate specific antigen
-
-
prostate stem cell antigen
-
-
prostate-specific antigen kallikrein
-
-
Prostate-specific membrane antigen
-
-
PSA-SV5
-
-
PSCA
-
-
PSMA
-
-
S01.162
-
-
-
-
seminal proteinase
-
-
seminin
-
-
-
-
six-transmembrane epithelial antigen of the prostate
-
-
STEAP
-
-
REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
Preferential cleavage: -Tyr-/-
show the reaction diagram
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
-
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 + H2O
?
show the reaction diagram
a fluorogenic enzyme substrate
-
-
?
Fibronectin + H2O
?
show the reaction diagram
-
-
-
?
Galectin-3 + H2O
?
show the reaction diagram
Gelatin + H2O
?
show the reaction diagram
-
-
-
?
IGFBP-3 + H2O
?
show the reaction diagram
-
-
-
?
insulin-like growth factor binding protein-3 + H2O
insulin-like growth factor I + ?
show the reaction diagram
-
i.e. IGF-I
?
MeO-Suc-Arg-Pro-Tyr-4-nitroanilide + H2O
?
show the reaction diagram
a chromogenic substrate
-
-
?
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
-
-
-
?
Mu-SRKSQQY-7-amido-4-methylcoumarin + H2O
Mu-SRKSQQY + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
?
nidogen-1 + H2O
?
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
?
semenogelin + H2O
semenogelin fractions
show the reaction diagram
-
-
-
?
semenogelin + H2O
semenogelin fragments
show the reaction diagram
semenogelins I and II
-
-
?
semenogelin I + H2O
?
show the reaction diagram
from human seminal fluid
-
-
?
semenogelin II + H2O
?
show the reaction diagram
from human seminal fluid
-
-
?
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
-
carbohydrate-binding protein involved in cell adhesion, cell cycle control, immunomodulation, and cancer progression, including prostate cancer
PSA cleaves galactin-3 between residues Y107 and G108 to produce an active, monovalent lectin
-
?
Gelatin + H2O
?
show the reaction diagram
-
proteolytic activity at pH 7.5
-
-
?
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
-
-
-
-
?
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-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
-
-
-
-
?
methoxy-succinyl-Arg-Pro-Tyr-4-nitroanilide + H2O
methoxy-succinyl-Arg-Pro-Tyr + 4-nitroaniline
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
-
-
-
-
?
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
-
-
?
o-aminobenzoyl-ISYQSSSTEEQ ethylene diamine 2,4-dinitrophenyl + 2 H2O
o-aminobenzoyl-ISYQ + SSST + EEQ ethylene diamine 2,4-dinitrophenyl
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-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
-
-
-
-
?
polypeptide + H2O
peptides
show the reaction diagram
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
semenogelin fragments
show the reaction diagram
-
-
-
-
?
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 SUBSTRATE
NATURAL PRODUCT
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
galectin-3 Tyr-107 is phosphorylated by c-Abl. It can be cleaved at this site by the enzyme after Tyr107, resulting in loss of galectin-3 multivalency while preserving its carbohydrate binding activity
-
-
?
insulin-like growth factor binding protein-3 + H2O
insulin-like growth factor I + ?
show the reaction diagram
-
i.e. IGF-I
?
plasminogen + H2O
plasmin + ?
show the reaction diagram
-
-
-
?
polypeptide + H2O
peptides
show the reaction diagram
enzyme possibly is involved in the processing of insulin-like growth factor binding protein 3
-
?
proform of transforming growth factor-beta + H2O
transforming growth factor-beta + ?
show the reaction diagram
-
i.e. IGF-beta
?
semenogelin + H2O
semenogelin fractions
show the reaction diagram
-
-
-
?
semenogelin I + H2O
?
show the reaction diagram
from human seminal fluid
-
-
?
Fibronectin + H2O
?
show the reaction diagram
-
enzyme participates in sperm liquefaction by cleaving fibronectin and semenogelins, the major components of the seminal vesicle coagulum after ejaculation
-
-
?
Galectin-3 + H2O
?
show the reaction diagram
-
carbohydrate-binding protein involved in cell adhesion, cell cycle control, immunomodulation, and cancer progression, including prostate cancer
PSA cleaves galactin-3 between residues Y107 and G108 to produce an active, monovalent lectin
-
?
polypeptide + H2O
peptides
show the reaction diagram
semenogelin + H2O
semenogelin fractions
show the reaction diagram
additional information
?
-
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(1S)-4-bromo-1-[(3aS,4R,6R,7aR)-3a,5,5-trimethylhexahydro-4,6-methano-1,3,2-benzodioxaborol-2-yl]butan-1-amine
-
(3aR,4R,6R,7aS)-2-[(1R)-1-amino-2-phenylethyl]-5,5-dimethyltetrahydro-4,6-methano-1,3,2-benzodioxaborol-3a(4H)-ol
-
2-mercaptoethanol
incubation with 3 mM for 30 min at 25°C, in 0.1 ml 0.1 M Tris buffer, pH 7.8, causes 84% loss of activity
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-nitrophenyl boronic acid
inhibits PSA
alpha1-Aantichymotrypsin
in circulation, the majority of the enzyme is complexed with protease inhibitors, including alpha1-antichymotrypsin. The proportion of the enzyme-alpha1-antichymotrypsin complex is higher in patients with prostate cancer than in controls without cancer
-
alpha1-Antichymotrypsin
inhibits PSA
-
Boric acid
inhibits PSA
dihydrolipoate
incubation with 3 mM for 30 min at 25°C, in 0.1 ml 0.1 M Tris buffer, pH 7.8, causes 65% loss of activity
dithiothreitol
incubation with 3 mM for 30 min at 25°C, 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
dutasteride
inhibits PSA
finasteride
inhibits PSA
glutathione
incubation with 3 mM for 30 min at 25°C, in 0.1 ml 0.1 M Tris buffer, pH 7.8, causes 35% loss of activity
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
-
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
-
norleucine
inhibits PSA
norvaline
inhibits PSA
R/S-diphenyl[N-benzyloxycarbonylamino(4-carbamoylphenyl)methyl]phosphonate
-
Tris[2-carboxyethyl] phosphine
incubation with 3 mM for 30 min at 25°C, in 0.1 ml 0.1 M Tris buffer, pH 7.8, causes 87% loss of activity
Z-SSKL(boro)L
inhibits PSA
((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
-
-
(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
-
-
(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-phenyl-4H-3,1-benzoxazin-4-one
-
-
2-phenylquinazolin-4(3H)-one
-
-
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-Aantichymotrypsin
-
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
diisopropylfluorophosphate
-
-
EDTA
-
10 mM inhibits at pH 3.5
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-[(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
-
-
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
-
-
-
serum
-
inhibits the mature enzyme
-
Soybean trypsin inhibitor
-
-
-
spermidine
-
-
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
androgens
upregulation
-
CVAYCIEHHCWTC
CVFAHNYDYLVC
progestins
upregulation in breast cancer
17-allylamine-17-demethoxygeldanamycin
-
-
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
-
-
-
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
additional information
-
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
1.58
4-morpholinecarbonyl-HSSKLQ-7-amido-4-methylcoumarin
pH 7.4, 37°C
5.72
MeO-Suc-Arg-Pro-Tyr-4-nitroanilide
pH 7.4, 37°C
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)
-
-
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
pH 7.4, 37°C
0.75
MeO-Suc-Arg-Pro-Tyr-4-nitroanilide
pH 7.4, 37°C
0.028
Arg-Pro-Tyr 4-nitroanilide
-
-
0.022
Lys-Val-Tyr 4-nitroanilide
-
-
0.075
N-succinyl-L-Ala-L-Ala-L-Pro-L-Phe 4-nitroanilide
-
-
kcat/KM VALUE [1/mMs-1]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.122
4-morpholinecarbonyl-HSSKLQ-7-amido-4-methylcoumarin
pH 7.4, 37°C
0.133
MeO-Suc-Arg-Pro-Tyr-4-nitroanilide
pH 7.4, 37°C
23000
HSSKLQ-7-amido-4-methylcoumarin
-
-
3900
Mca-QFYSSNK(epsilon-dinitrophenyl)
-
-
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
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, 37°C
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
-
-
1
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-alpha-glutamyl-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
-
-
1
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-alpha-glutamine
-
-
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
-
-
0.2652
Z-Gln-Leu-B(OH)2
-
-
1
Z-Gln-Nle-H
-
-
1
Z-KL-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
-
-
1
Z-QL-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
-
-
1
Z-Ser-Ser-Lys-Leu-D-Nle-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
-
-
1
Z-SSKLD-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, 37°C, with methoxy-succinyl-Arg-Pro-Tyr-4-nitrophenyl
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.15
dithiothreitol
Homo sapiens
at 25°C, 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
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
Homo sapiens
-
-
0.08
1-benzyl-3-phenyl-1H-pyrazol-5-amine
Homo sapiens
-
-
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
Homo sapiens
-
-
0.08
2-(3-nitrophenyl)-4H-3,1-benzoxazin-4-one
Homo sapiens
-
-
0.08
2-(4-bromophenyl)quinazolin-4(3H)-one
Homo sapiens
-
-
0.08
2-(4-methylphenyl)-4H-3,1-benzoxazin-4-one
Homo sapiens
-
-
0.08
2-phenyl-4H-3,1-benzoxazin-4-one
Homo sapiens
-
-
0.08
2-phenylquinazolin-4(3H)-one
Homo sapiens
-
-
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
-
-
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
7.4
assay at
7.8
assay at
3.5
-
bovine serum albumin is degraded 3-4times faster at pH 3.5 than at pH 7.5
8.3
-
assay at
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
37
-
assay at
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
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
breast carcinoma cell line, enzyme is upregulated by progestins and androgens
Manually annotated by BRENDA team
breast carcinoma cell line, enzyme is upregulated by progestins and androgens
Manually annotated by BRENDA team
-
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
-
surgical specimens from female patients with breast cancer
Manually annotated by BRENDA team
-
minute amounts
Manually annotated by BRENDA team
-
prostate cancer cell, expressing GRP78 on its surface
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
-
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
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
metabolism
the HSP protein family and the gama-SM protein are related in two critical ways: the fact that silencing HSPs may be directly correlated with reduced gama-SM protein expression and their high potential as biomarkers for PCa. A direct proportional relationship between Hsp70 and the gama-SM protein
physiological function
malfunction
physiological function
additional information
UNIPROT
ENTRY NAME
ORGANISM
NO. OF AA
NO. OF TRANSM. HELICES
MOLECULAR WEIGHT[Da]
SOURCE
SEQUENCE
LOCALIZATION PREDICTION?
KLK3_HUMAN
261
0
28741
Swiss-Prot
Secretory Pathway (Reliability: 1)
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
25000
x * 25000, Western blot analysis and SDS-PAGE. x * 22500-35500, zymographic assay
54000
1 * 55000, SDS-PAGE, proPSA, 1 * 54000, SDS-PAGE, active PSA
55000
1 * 55000, SDS-PAGE, proPSA, 1 * 54000, SDS-PAGE, active PSA
160000
-
Western blotting of PSA-spiked mouse serum
200000
-
Western blotting of PSA-spiked mouse serum
26080
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
33000
34000
36000
-
x * 36000, SDS-PAGE, pro-PSA
65000
-
Western blotting of PSA-spiked mouse serum
85000
-
Western blotting of PSA-spiked mouse serum
87000
-
inactive zymogen peak 1, gel filtration
SUBUNIT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
monomer
1 * 55000, SDS-PAGE, proPSA, 1 * 54000, SDS-PAGE, active PSA
dimer
-
crystallography
additional information
-
active mature enzyme consists of only 1 chain
POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
proteolytic modification
enzyme can be activated by recombinant kallikrein 2
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
-80°C
-
4°C, Tris-HCl buffer
-
PURIFICATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
by gel filtration
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
native active enzyme from seminal plasma by immunoaffinity chromatography and anion-exchange chromatography
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 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
-
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
gene hK3 or KLK3, genetic organization and structure of the kallikrein gene family, clustered on chromosome 19q13.3-q13.4
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)
expressed in Escherichia coli M15(pREP4) cells
-
expressed in HUVEC cells
-
gene structure
-
male C57BL/6 mice injected with recombinant adenoviruses containing rAd/PSMA, rAd/PSCA and rAd/STEAP
-
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
-
RENATURED/Commentary
ORGANISM
UNIPROT
LITERATURE
APPLICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
analysis
mass spectrometry annotation can identify more molecular forms of PSA compared with Western and zymographic analyses. Observation of various isoforms of PSA in patients may contribute to the further identification of disease-relevant heterogeneity of PSA, including transcriptional and post-translational modifications present due to various stages and causes of prostate disease
diagnostics
drug development
the gama-SM protein can be a drug target in prostate cancer therapy
medicine
analysis
diagnostics
-
concentration of enzyme in nonprostatic tissue represents less than 1% of the amount in normal prostate. Thus enzyme released from sources other than the prostate may add to the plasma pool, but it is unlikely that nonprostatic enzyme normally can interfere with the diagnosis of prostate cancer
drug development
medicine
additional information
-
human seminal proteinase and prostate-specific antigen are identical
REF.
AUTHORS
TITLE
JOURNAL
VOL.
PAGES
YEAR
ORGANISM (UNIPROT)
PUBMED ID
SOURCE
Boeckmann, B.; Bairoch, A.; Apweiler, R.; Blatter, M.C.; Estreicher, A.; Gasteiger, E.; Martin M.J.; Michoud, K.; O'Donovan, C.; Phan, I.; Pilbout, S.; Schneider, M.
The SWISS-PROT protein knowledgebase and its supplement TrEMBL
Nucleic Acids Res.
31
365-370
2003
Mus musculus (P00756), Homo sapiens (P07288), Rattus norvegicus (P15950), Macaca mulatta (P33619)
Manually annotated by BRENDA team
Yousef, G.M.; Diamandis, E.P.
The new human tissue kallikrein gene family: structure, function, and association to disease
Endocr. Rev.
22
184-204
2001
Homo sapiens (P07288), Homo sapiens
Manually annotated by BRENDA team
Christensson, A.; Laurell, C.B.; Lilja, H.
Enzymatic activity of prostate-specific antigen and its reactions with extracellular serine proteinase inhibitors
Eur. J. Biochem.
194
755-763
1990
Homo sapiens
Manually annotated by BRENDA team
Digby, M.; Zhang, X.Y.; Richards, R.I.
Human prostate specific antigen (PSA) gene: structure and linkage to the kallikrein-like gene, hGK-1
Nucleic Acids Res.
17
2137
1989
Homo sapiens
Manually annotated by BRENDA team
Schaller, J.; Akiyama, K.; Tsuda, R.; Hara, M.; Marti, T.; Rickli, E.E.
Isolation, characterization and amino-acid sequence of gamma-seminoprotein, a glycoprotein from human seminal plasma
Eur. J. Biochem.
170
111-120
1987
Homo sapiens
Manually annotated by BRENDA team
Watt, K.W.K.; Lee, P.J.; M`Timkulu, T.; Chan, W.P.; Loor, R.
Human prostate-specific antigen: structural and functional similarity with serine proteases
Proc. Natl. Acad. Sci. USA
83
3166-3170
1986
Homo sapiens
Manually annotated by BRENDA team
Riegman, P.H.J.; Vlietstra, R.J.; van der Korput, J.A.G.M.; Romijn, J.C.; Trapman, J.
Characterization of the prostate-specific antigen gene: a novel human kallikrein-like gene
Biochem. Biophys. Res. Commun.
159
95-102
1989
Homo sapiens
Manually annotated by BRENDA team
Lundwall, A.; Lilja, H.
Molecular cloning of human prostate specific antigen cDNA
FEBS Lett.
214
317-322
1987
Homo sapiens
Manually annotated by BRENDA team
Lundwall, A.
Characterization of the gene for prostate-specific antigen, a human glandular kallikrein
Biochem. Biophys. Res. Commun.
161
1151-1159
1989
Homo sapiens
Manually annotated by BRENDA team
Frenette, G.; Tremblay, R.R.; Lazure, C.; Dube, J.Y.
Prostatic kallikrein hK2, but not prostate-specific antigen (hK3), activates single-chain urokinase-type plasminogen activator
Int. J. Cancer
71
897-899
1997
Homo sapiens
Manually annotated by BRENDA team
Deperthes, D.; Marceau, F.; Frenette, G.; Lazure, C.; Tremblay, R.R.; Dube, J.Y.
Human kallikrein hK2 has low kininogenase activity while prostate-specific antigen (hK3) has none
Biochim. Biophys. Acta
1343
102-106
1997
Homo sapiens
Manually annotated by BRENDA team
Bourgeois, L.; Brillard-Bourdet, M.; Deperthes, D.; Juliano, M.A.; Juliano, L.; Tremblay, R.R.; Dube, J.Y.; Gauthier, F.
Serpin-derived peptide substrates for investigating the substrate specificity of human tissue kallikreins hK1 and hK2
J. Biol. Chem.
272
29590-29595
1997
Homo sapiens
Manually annotated by BRENDA team
Visanen, V.; Lovgren, J.; Hellman, J.; Piironen, T.; Lilja, H.; Pettersson, K.
Characterization and processing of prostate specific antigen (hK3) and human glandular kallikrein (hK2) secreted by LNCaP cells
Prostate Cancer Prostatic. Dis.
2
91-97
1999
Homo sapiens
Manually annotated by BRENDA team
Malm, J.; Hellman, J.; Hogg, P.; Lilja, H.
Enzymatic action of prostate-specific antigen (PSA or hK3): substrate specificity and regulation by Zn(2+), a tight-binding inhibitor
Prostate
45
132-139
2000
Homo sapiens
Manually annotated by BRENDA team
Brillard-Bourdet, M.; Rehault, S.; Juliano, L.; Ferrer, M.; Moreau, T.; Gauthier, F.
Amidolytic activity of prostatic acid phosphatase on human semenogelins and semenogelin-derived synthetic substrates
Eur. J. Biochem.
269
390-395
2002
Homo sapiens
Manually annotated by BRENDA team
Rehault, S.; Brillard-Bourdet, M.; Bourgois, L.; Frenette, G.; Juliano, L.; Gauthier, F.; Moreau, T.
Design of new and sensitive fluorogenic substrates for human kallikrein hK3 (prostate-specific antigen) derived from semenogelin sequences
Biochim. Biophys. Acta
1596
55-62
2002
Homo sapiens
Manually annotated by BRENDA team
Beaufort, N.; Debela, M.; Creutzburg, S.; Kellermann, J.; Bode, W.; Schmitt, M.; Pidard, D.; Magdolen, V.
Interplay of human tissue kallikrein 4 (hK4) with the plasminogen activation system: hK4 regulates the structure and functions of the urokinase-type plasminogen activator receptor (uPAR)
Biol. Chem.
387
217-222
2006
Homo sapiens
Manually annotated by BRENDA team
Olsson, A.Y.; Bjartell, A.; Lilja, H.; Lundwall, A.
Expression of prostate-specific antigen (PSA) and human glandular kallikrein 2 (hK2) in ileum and other extraprostatic tissues
Int. J. Cancer
113
290-297
2005
Homo sapiens
Manually annotated by BRENDA team
Acevedo, B.; Perera, Y.; Torres, E.; Penton, D.; Ayala, M.; Gavilondo, J.
Fast and novel purification method to obtain the prostate specific antigen (PSA) from human seminal plasma
Prostate
66
1029-1036
2006
Homo sapiens
Manually annotated by BRENDA team
Pampalakis, G.; Scorilas, A.; Sotiropoulou, G.
Novel splice variants of prostate-specific antigen and applications in diagnosis of prostate cancer
Clin. Biochem.
41
591-597
2008
Homo sapiens
Manually annotated by BRENDA team
Debela, M.; Magdolen, V.; Schechter, N.; Valachova, M.; Lottspeich, F.; Craik, C.S.; Choe, Y.; Bode, W.; Goettig, P.
Specificity profiling of seven human tissue kallikreins reveals individual subsite preferences
J. Biol. Chem.
281
25678-25688
2006
Homo sapiens
Manually annotated by BRENDA team
Jeong, S.; Lee, S.W.
Expression and purification of recombinant active prostate-specific antigen from Escherichia coli
J. Microbiol. Biotechnol.
17
840-846
2007
Homo sapiens (P07288), Homo sapiens
Manually annotated by BRENDA team
Menez, R.; Michel, S.; Muller, B.H.; Bossus, M.; Ducancel, F.; Jolivet-Reynaud, C.; Stura, E.A.
Crystal structure of a ternary complex between human prostate-specific antigen, its substrate acyl intermediate and an activating antibody
J. Mol. Biol.
376
1021-1033
2008
Homo sapiens
Manually annotated by BRENDA team
Sengupta, S.; Amling, C.; DAmico, A.V.; Blute, M.L.
Prostate specific antigen kinetics in the management of prostate cancer
J. Urol.
179
821-826
2008
Homo sapiens
Manually annotated by BRENDA team
Singh, P.; Williams, S.A.; Shah, M.H.; Lectka, T.; Pritchard, G.J.; Isaacs, J.T.; Denmeade, S.R.
Mechanistic insights into the inhibition of prostate specific antigen by beta-lactam class compounds
Proteins
70
1416-1428
2008
Homo sapiens
Manually annotated by BRENDA team
Weber, W.; Buck, F.; Meyer, A.; Hilz, H.
Prostate specific antigen: one out of five disulfide bridges determines inactivation by reduction
Biochem. Biophys. Res. Commun.
379
1101-1106
2009
Homo sapiens (P07288)
Manually annotated by BRENDA team
Barbero, G.; Destefanis, P.; Procida, S.; Mandili, G.; Ulliers, D.; Ceruti, C.; Fiori, C.; Maule, M.M.; Fontana, D.; Giribaldi, G.; Turrini, F.
Highly specific detection of prostate-specific antigen-positive cells in the blood of patients with prostate cancer or benign prostatic hyperplasia, using a real-time reverse-transcription-polymerase chain reaction method with improved sensitivity
BJU Int.
102
1566-1572
2008
Homo sapiens
Manually annotated by BRENDA team
Fitzpatrick, J.M.; Banu, E.; Oudard, S.
Prostate-specific antigen kinetics in localized and advanced prostate cancer
BJU Int.
103
578-587
2009
Homo sapiens
Manually annotated by BRENDA team
Ng, M.K.; Van As, N.; Thomas, K.; Woode-Amissah, R.; Horwich, A.; Huddart, R.; Khoo, V.; Thompson, A.; Dearnaley, D.; Parker, C.
Prostate-specific antigen (PSA) kinetics in untreated, localized prostate cancer: PSA velocity vs PSA doubling time
BJU Int.
103
872-876
2009
Homo sapiens
Manually annotated by BRENDA team
Zheng, S.L.; Sun, J.; Wiklund, F.; Gao, Z.; Stattin, P.; Purcell, L.D.; Adami, H.O.; Hsu, F.C.; Zhu, Y.; Adolfsson, J.; Johansson, J.E.; Turner, A.R.; Adams, T.S.; Liu, W.; Duggan, D.; Carpten, J.D.; Chang, B.L.; Isaacs, W.B.; Xu, J.; Groenberg, H.
Genetic variants and family history predict prostate cancer similar to prostate-specific antigen
Clin. Cancer Res.
15
1105-1111
2009
Homo sapiens
Manually annotated by BRENDA team
Presti, J.
The use of prostate-specific antigen kinetics to stratify risk in prostate cancer
Curr. Urol. Rep.
9
226-230
2008
Homo sapiens
Manually annotated by BRENDA team
van den Bergh, R.C.; Roemeling, S.; Roobol, M.J.; Wolters, T.; Schroeder, F.H.; Bangma, C.H.
Prostate-specific antigen kinetics in clinical decision-making during active surveillance for early prostate cancer--a review
Eur. Urol.
54
505-516
2008
Homo sapiens
Manually annotated by BRENDA team
Stone, J.G.; Rolston, R.K.; Ueda, M.; Lee, H.G.; Richardson, S.L.; Castellani, R.J.; Perry, G.; Smith, M.A.
Evidence for the Novel Expression of Human Kallikrein-related Peptidase 3, Prostate-Specific Antigen, in the Brain
Int. J. Clin. Exp. Pathol.
2
267-274
2009
Homo sapiens
Manually annotated by BRENDA team
Waheed, A.; Hassan, M.I.; Etten, R.L.; Ahmad, F.
Human seminal proteinase and prostate-specific antigen are the same protein
J. Biosci.
33
195-207
2008
Homo sapiens
Manually annotated by BRENDA team
Kulasingam, V.; Smith, C.R.; Batruch, I.; Buckler, A.; Jeffery, D.A.; Diamandis, E.P.
"Product ion monitoring" assay for prostate-specific antigen in serum using a linear ion-trap
J. Proteome Res.
7
640-647
2008
Homo sapiens
Manually annotated by BRENDA team
White, K.Y.; Rodemich, L.; Nyalwidhe, J.O.; Comunale, M.A.; Clements, M.A.; Lance, R.S.; Schellhammer, P.F.; Mehta, A.S.; Semmes, O.J.; Drake, R.R.
Glycomic characterization of prostate-specific antigen and prostatic acid phosphatase in prostate cancer and benign disease seminal plasma fluids
J. Proteome Res.
8
620-630
2009
Homo sapiens
Manually annotated by BRENDA team
Koistinen, H.; Wohlfahrt, G.; Mattsson, J.M.; Wu, P.; Lahdenperae, J.; Stenman, U.H.
Novel small molecule inhibitors for prostate-specific antigen
Prostate
68
1143-1151
2008
Homo sapiens
Manually annotated by BRENDA team
Kim, S.; Lee, J.B.; Lee, G.K.; Chang, J.
Vaccination with recombinant adenoviruses and dendritic cells expressing prostate-specific antigens is effective in eliciting CTL and suppresses tumor growth in the experimental prostate cancer
Prostate
69
938-948
2009
Homo sapiens
Manually annotated by BRENDA team
Thanigasalam, R.; Mancuso, P.; Tsao, K.; Rashid, P.
Prostate-specific antigen velocity (PSAV): a practical role for PSA?
ANZ. J. Surg.
79
703-706
2009
Homo sapiens
Manually annotated by BRENDA team
Sighinolfi, M.C.; Micali, S.; De Stefani, S.; Cicero, A.; Cianci, F.; Giacometti, M.; Bianchi, G.
Retrospective descriptive analysis of the physiological kinetics of prostate-specific antigen in men older than 75 years
Asian J. Androl.
11
493-497
2009
Homo sapiens
Manually annotated by BRENDA team
Maeda, H.; Yonou, H.; Yano, K.; Ishii, G.; Saito, S.; Ochiai, A.
Prostate-specific antigen enhances bioavailability of insulin-like growth factor by degrading insulin-like growth factor binding protein 5
Biochem. Biophys. Res. Commun.
381
311-316
2009
Homo sapiens
Manually annotated by BRENDA team
LeBeau, A.M.; Singh, P.; Isaacs, J.T.; Denmeade, S.R.
Prostate-specific antigen is a "chymotrypsin-like" serine protease with unique P1 substrate specificity
Biochemistry
48
3490-3496
2009
Homo sapiens
Manually annotated by BRENDA team
LeBeau, A.M.; Kostova, M.; Craik, C.S.; Denmeade, S.R.
Prostate-specific antigen: an overlooked candidate for the targeted treatment and selective imaging of prostate cancer
Biol. Chem.
391
333-343
2010
Homo sapiens, Mus musculus
Manually annotated by BRENDA team
Mitra, A.; Richardson, R.T.; ORand, M.G.
Analysis of recombinant human semenogelin as an inhibitor of human sperm motility
Biol. Reprod.
82
489-496
2010
Homo sapiens
Manually annotated by BRENDA team
LeBeau, A.M.; Banerjee, S.R.; Pomper, M.G.; Mease, R.C.; Denmeade, S.R.
Optimization of peptide-based inhibitors of prostate-specific antigen (PSA) as targeted imaging agents for prostate cancer
Bioorg. Med. Chem.
17
4888-4893
2009
Homo sapiens
Manually annotated by BRENDA team
Escamilla-Gomez, V.; Hernandez-Santos, D.; Gonzalez-Garcia, M.B.; Pingarron-Carrazon, J.M.; Costa-Garcia, A.
Simultaneous detection of free and total prostate specific antigen on a screen-printed electrochemical dual sensor
Biosens. Bioelectron.
24
2678-2683
2009
Homo sapiens
Manually annotated by BRENDA team
Jeong, S.; Han, S.R.; Lee, Y.J.; Lee, S.W.
Selection of RNA aptamers specific to active prostate-specific antigen
Biotechnol. Lett.
32
379-385
2010
Homo sapiens
Manually annotated by BRENDA team
Giesing, M.; Suchy, B.; Driesel, G.; Molitor, D.
Clinical utility of antioxidant gene expression levels in circulating cancer cell clusters for the detection of prostate cancer in patients with prostate-specific antigen levels of 4-10 ng/mL and disease prognostication after radical prostatectomy
BJU Int.
105
1000-1010
2010
Homo sapiens
Manually annotated by BRENDA team
Nakagawa, T.; Kanai, Y.; Komiyama, M.; Fujimoto, H.; Kakizoe, T.
Characteristics of prostate cancers found in specimens removed by radical cystoprostatectomy for bladder cancer and their relationship with serum prostate-specific antigen level
Cancer Sci.
100
1880-1884
2009
Homo sapiens
Manually annotated by BRENDA team
Choueiri, T.K.; Xie, W.; DAmico, A.V.; Ross, R.W.; Hu, J.C.; Pomerantz, M.; Regan, M.M.; Taplin, M.E.; Kantoff, P.W.; Sartor, O.; Oh, W.K.
Time to prostate-specific antigen nadir independently predicts overall survival in patients who have metastatic hormone-sensitive prostate cancer treated with androgen-deprivation therapy
Cancer
115
981-987
2009
Homo sapiens
Manually annotated by BRENDA team
Oikonomopoulou, K.; Soosaipillai, A.; Diamandis, E.P.
Evaluation of prostate-specific antigen as a novel biomarker of Hsp90 inhibition
Clin. Biochem.
42
1705-1712
2009
Homo sapiens
Manually annotated by BRENDA team
Elliott, C.S.; Shinghal, R.; Presti, J.C.
The influence of prostate volume on prostate-specific antigen performance: implications for the prostate cancer prevention trial outcomes
Clin. Cancer Res.
15
4694-4699
2009
Homo sapiens
Manually annotated by BRENDA team
Huang, Y.; Wang, T.H.; Jiang, J.H.; Shen, G.L.; Yu, R.Q.
Prostate specific antigen detection using microgapped electrode array immunosensor with enzymatic silver deposition
Clin. Chem.
55
964-971
2009
Homo sapiens
Manually annotated by BRENDA team
Karuppaiya, A.; Cheah, S.H.; Mohd, S.; Kamal, W.H.; Zulkifli, M.H.
Generation and characterization of monoclonal antibodies against prostate-specific antigen
Hybridoma
28
133-137
2009
Homo sapiens
Manually annotated by BRENDA team
Patane, S.; Marte, F.; Sturiale, M.
Prostate-specific antigen kallikrein complexes and acute myocardial infarction
Int. J. Cardiol.
145
227-228
2010
Homo sapiens
Manually annotated by BRENDA team
Voeghtly, L.M.; Thogersen, I.B.; Valnickova, Z.; Sanggaard, K.W.; Chu, C.T.; Oury, T.D.; Enghild, J.J.
Potential clinical importance of the activation peptide of prostate-specific antigen
Int. J. Clin. Exp. Pathol.
2
588-598
2009
Homo sapiens
Manually annotated by BRENDA team
Miyakubo, M.; Ito, K.; Yamamoto, T.; Takechi, H.; Ohi, M.; Suzuki, K.
Proprostate-specific antigen: its usefulness in the era of multiple-core prostate biopsy
Int. J. Urol.
16
561-565
2009
Homo sapiens
Manually annotated by BRENDA team
Ohigashi, T.; Kanao, K.; Mizuno, R.; Kikuchi, E.; Nakashima, J.; Oya, M.
Predicting the probability of significant prostate cancer in Japanese men with serum prostate-specific antigen less than 10 ng/mL: development of a novel pre-biopsy nomogram
Int. J. Urol.
17
274-280
2010
Homo sapiens
Manually annotated by BRENDA team
Mao, Q.; Zheng, X.; Jia, X.; Wang, Y.; Qin, J.; Yang, K.; Bai, Y.; Xie, L.
Relationships between total/free prostate-specific antigen and prostate volume in Chinese men with biopsy-proven benign prostatic hyperplasia
Int. Urol. Nephrol.
41
761-766
2009
Homo sapiens
Manually annotated by BRENDA team
Tang, P.; Xie, K.J.; Wang, B.; Deng, X.R.; Ou, R.B.
Antibacterial therapy improves the effectiveness of prostate cancer detection using prostate-specific antigen in patients with asymptomatic prostatitis
Int. Urol. Nephrol.
42
13-18
2010
Homo sapiens
Manually annotated by BRENDA team
Slupianek, A.; Yerrum, S.; Safadi, F.F.; Monroy, M.A.
The chromatin remodeling factor SRCAP modulates expression of prostate specific antigen and cellular proliferation in prostate cancer cells
J. Cell. Physiol.
224
369-375
2010
Homo sapiens
Manually annotated by BRENDA team
Vegvari, A.; Rezeli, M.; Welinder, C.; Malm, J.; Lilja, H.; Marko-Varga, G.; Laurell, T.
Identification of prostate-specific antigen (PSA) isoforms in complex biological samples utilizing complementary platforms
J. proteomics
73
1137-1147
2010
Homo sapiens (P07288)
Manually annotated by BRENDA team
Ide, H.; Tokiwa, S.; Sakamaki, K.; Nishio, K.; Isotani, S.; Muto, S.; Hama, T.; Masuda, H.; Horie, S.
Combined inhibitory effects of soy isoflavones and curcumin on the production of prostate-specific antigen
Prostate
70
1127-1133
2010
Homo sapiens
Manually annotated by BRENDA team
Hekim, C.; Riipi, T.; Zhu, L.; Laakkonen, P.; Stenman, U.H.; Koistinen, H.
Complex formation between human prostate-specific antigen and protease inhibitors in mouse plasma
Prostate
70
482-490
2010
Homo sapiens
Manually annotated by BRENDA team
Singh, P.; LeBeau, A.M.; Lilja, H.; Denmeade, S.R.; Isaacs, J.T.
Molecular insights into substrate specificity of prostate specific antigen through structural modeling
Proteins
77
984-993
2009
Homo sapiens, Sus scrofa
Manually annotated by BRENDA team
Pinkawa, M.; Piroth, M.D.; Holy, R.; Fischedick, K.; Schaar, S.; Borchers, H.; Heidenreich, A.; Eble, M.J.
Prostate-specific antigen kinetics following external-beam radiotherapy and temporary (Ir-192) or permanent (I-125) brachytherapy for prostate cancer
Radiother. Oncol.
96
25-29
2010
Homo sapiens
Manually annotated by BRENDA team
Mattsson, J.M.; Laakkonen, P.; Stenman, U.H.; Koistinen, H.
Antiangiogenic properties of prostate-specific antigen (PSA)
Scand. J. Clin. Lab. Invest.
69
447-451
2009
Homo sapiens
Manually annotated by BRENDA team
Namgung, M.O.; Jung, S.K.; Chung, C.M.; Oh, S.Y.
Electrochemical immunosensor for prostate-specific antigen using self-assembled oligophenylethynylenethiol monolayer containing dendrimer
Ultramicroscopy
109
907-910
2009
Homo sapiens
Manually annotated by BRENDA team
Stephan, C.; Cammann, H.; Deger, S.; Schrader, M.; Meyer, H.A.; Miller, K.; Lein, M.; Jung, K.
Benign prostatic hyperplasia-associated free prostate-specific antigen improves detection of prostate cancer in an artificial neural network
Urology
74
873-877
2009
Homo sapiens
Manually annotated by BRENDA team
Kim, H.S.; Jeon, S.S.; Choi, J.D.; Kim, W.; Han, D.H.; Jeong, B.C.; Seo, S.I.; Lee, K.S.; Lee, S.W.; Lee, H.M.; Choi, H.Y.
Detection rates of nonpalpable prostate cancer in Korean men with prostate-specific antigen levels between 2.5 and 4.0 ng/mL
Urology
76
919-922
2010
Homo sapiens
Manually annotated by BRENDA team
Vollmer, R.T.
Dissecting the dynamics of serum prostate-specific antigen
Am. J. Clin. Pathol.
133
187-193
2010
Homo sapiens
Manually annotated by BRENDA team
Su, L.C.; Chen, R.C.; Li, Y.C.; Chang, Y.F.; Lee, Y.J.; Lee, C.C.; Chou, C.
Detection of prostate-specific antigen with a paired surface plasma wave biosensor
Anal. Chem.
82
3714-3718
2010
Homo sapiens
Manually annotated by BRENDA team
Li, Y.; Tian, Y.; Rezai, T.; Prakash, A.; Lopez, M.F.; Chan, D.W.; Zhang, H.
Simultaneous analysis of glycosylated and sialylated prostate-specific antigen revealing differential distribution of glycosylated prostate-specific antigen isoforms in prostate cancer tissues
Anal. Chem.
83
240-245
2011
Homo sapiens
Manually annotated by BRENDA team
Elsadek, B.; Graeser, R.; Esser, N.; Schaefer-Obodozie, C.; Ajaj, K.A.; Unger, C.; Warnecke, A.; Saleem, T.; El-Melegy, N.; Madkor, H.; Kratz, F.
Development of a novel prodrug of paclitaxel that is cleaved by prostate-specific antigen: an in vitro and in vivo evaluation study
Eur. J. Cancer
46
3434-3444
2010
Homo sapiens
Manually annotated by BRENDA team
Jansen, F.H.; van Schaik, R.H.; Kurstjens, J.; Horninger, W.; Klocker, H.; Bektic, J.; Wildhagen, M.F.; Roobol, M.J.; Bangma, C.H.; Bartsch, G.
Prostate-specific antigen (PSA) isoform p2PSA in combination with total PSA and free PSA improves diagnostic accuracy in prostate cancer detection
Eur. Urol.
57
921-927
2010
Homo sapiens
Manually annotated by BRENDA team
Misra, U.K.; Payne, S.; Pizzo, S.V.
Ligation of prostate cancer cell surface GRP78 activates a proproliferative and antiapoptotic feedback loop: a role for secreted prostate-specific antigen
J. Biol. Chem.
286
1248-1259
2011
Homo sapiens
Manually annotated by BRENDA team
Catalona, W.J.; Partin, A.W.; Sanda, M.G.; Wei, J.T.; Klee, G.G.; Bangma, C.H.; Slawin, K.M.; Marks, L.S.; Loeb, S.; Broyles, D.L.; Shin, S.S.; Cruz, A.B.; Chan, D.W.; Sokoll, L.J.; Roberts, W.L.; van Schaik, R.H.; Mizrahi, I.A.
A multicenter study of [-2]pro-prostate specific antigen combined with prostate specific antigen and free prostate specific antigen for prostate cancer detection in the 2.0 to 10.0 ng/ml prostate specific antigen range
J. Urol.
185
1650-1655
2011
Homo sapiens
Manually annotated by BRENDA team
Adamy, A.; Yee, D.S.; Matsushita, K.; Maschino, A.; Cronin, A.; Vickers, A.; Guillonneau, B.; Scardino, P.T.; Eastham, J.A.
Role of prostate specific antigen and immediate confirmatory biopsy in predicting progression during active surveillance for low risk prostate cancer
J. Urol.
185
477-482
2011
Homo sapiens
Manually annotated by BRENDA team
Narita, D.; Anghel, A.; Cimpean, A.M.; Izvernariu, D.; Cireap, N.; Ilina, R.; Ursoniu, S.
Interaction between estrogens and androgen receptor genes microsatellites, prostate-specific antigen and androgen receptor expressions in breast cancer
Neoplasma
57
198-206
2010
Homo sapiens
Manually annotated by BRENDA team
Saraswati, S.; Block, A.S.; Davidson, M.K.; Rank, R.G.; Mahadevan, M.; Diekman, A.B.
Galectin-3 is a substrate for prostate specific antigen (PSA) in human seminal plasma
Prostate
71
197-208
2011
Homo sapiens
Manually annotated by BRENDA team
Parracino, A.; Neves-Petersen, M.T.; di Gennaro, A.K.; Pettersson, K.; Loevgren, T.; Petersen, S.B.
Arraying prostate specific antigen PSA and Fab anti-PSA using light-assisted molecular immobilization technology
Protein Sci.
19
1751-1759
2010
Homo sapiens
Manually annotated by BRENDA team
Conway, R.E.; Joiner, K.; Patterson, A.; Bourgeois, D.; Rampp, R.; Hannah, B.C.; McReynolds, S.; Elder, J.M.; Gilfilen, H.; Shapiro, L.H.
Prostate specific membrane antigen produces pro-angiogenic laminin peptides downstream of matrix metalloprotease-2
Angiogenesis
16
847-860
2013
Homo sapiens (P07288)
Manually annotated by BRENDA team
Kojtari, A.; Shah, V.; Babinec, J.S.; Yang, C.; Ji, H.F.
Structure-based drug design of diphenyl alpha-aminoalkylphosphonates as prostate-specific antigen antagonists
J. Chem. Inf. Model.
54
2967-2979
2014
Homo sapiens (P07288)
Manually annotated by BRENDA team
Kostova, M.B.; Rosen, D.M.; Chen, Y.; Mease, R.C.; Denmeade, S.R.
Structural optimization, biological evaluation, and application of peptidomimetic prostate specific antigen inhibitors
J. Med. Chem.
56
4224-4235
2013
Homo sapiens (P07288)
Manually annotated by BRENDA team
Mattsson, J.M.; Ravela, S.; Hekim, C.; Jonsson, M.; Malm, J.; Naervaenen, A.; Stenman, U.H.; Koistinen, H.
Proteolytic activity of prostate-specific antigen (PSA) towards protein substrates and effect of peptides stimulating PSA activity
PLoS ONE
9
e107819
2014
Homo sapiens (P07288)
Manually annotated by BRENDA team
Zhu, L.; Jaeaemaa, S.; Af Haellstroem, T.M.; Laiho, M.; Sankila, A.; Nordling, S.; Stenman, U.H.; Koistinen, H.
PSA forms complexes with alpha1-antichymotrypsin in prostate
Prostate
73
219-226
2013
Homo sapiens (P07288)
Manually annotated by BRENDA team
Kumar, S.; Gurshaney, S.; Adagunodo, Y.; Gage, E.; Qadri, S.; Sharma, M.; Malik, S.; Manne, U.; Singh, U.P.; Singh, R.; Mishra, M.K.
Hsp70 and gama-Semino protein as possible prognostic marker of prostate cancer
Front. Biosci.
23
1987-2000
2018
Homo sapiens (P07288), Homo sapiens
Manually annotated by BRENDA team