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4-morpholinecarbonyl-HSSKLQ-7-amido-4-methylcoumarin + H2O
?
a fluorogenic enzyme substrate
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?
4-morpholinecarbonyl-HSSKLQ-AMC + H2O
?
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?
4-morpholinecarbonyl-SKLQ-7-amido-4-methylcoumarin + H2O
?
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hydrolysis rate is 29.6 pmol/min per 100 pmol of PSA
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?
4-morpholinecarbonyl-SRKSQQY-7-amido-4-methylcoumarin + H2O
?
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?
Arg-Pro-Tyr 4-nitroanilide + H2O
Arg-Pro-Tyr + 4-nitroaniline
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?
Bovine serum albumin + H2O
?
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is more readily hydrolysed than casein
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?
casein + H2O
?
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proteolytic activity at pH 7.5
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?
EHSSKLQ-7-amido-4-methylcoumarin + H2O
EHSSKLQ + 7-amino-4-methylcoumarin
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?
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
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water soluble paclitaxel prodrug that is activated specifically by PSA in prostate tissue and prostate carcinoma
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?
GSAKLQ + H2O
?
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207.2% relative hydrolysis rate
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?
GSSALQ + H2O
?
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43.2% relative hydrolysis rate
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?
GSSKLA + H2O
?
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31.5% relative hydrolysis rate
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?
GSSKLH + H2O
?
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170.6% relative hydrolysis rate
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?
GSSKLQ + H2O
?
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100% relative hydrolysis rate
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?
GSSKPQ + H2O
?
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7.2% relative hydrolysis rate
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?
GSSKYQ + H2O
?
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256.9% relative hydrolysis rate
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?
GSSSLQ + H2O
?
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52.6% relative hydrolysis rate
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?
HSSKLQ-7-amido-4-methylcoumarin + H2O
?
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hydrolysis rate is 62.7 pmol/min per 100 pmol of PSA
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?
HSSKLQ-7-amido-4-methylcoumarin + H2O
HSSKLQ + 7-amino-4-methylcoumarin
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?
HSSKLQ-7-amido-4-trifluoromethyl-coumarin + H2O
?
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?
insulin-like growth factor binding protein 5 + H2O
?
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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
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?
insulin-like growth factor binding protein-3 + H2O
insulin-like growth factor I + ?
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i.e. IGF-I
?
insulin-like growth factor binding protein-3 + H2O
insulin-like growth factor-1
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?
KGISSQY-7-amido-4-methylcoumarin + H2O
KGISSQY + 7-amino-4-methylcoumarin
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fluorogenic substrate
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?
Laminin + H2O
?
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?
LSEPAELTDAVK + H2O
PAELTDAVK + LSE
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?
Lys-Val-Tyr 4-nitroanilide + H2O
Lys-Val-Tyr + 4-nitroaniline
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?
Mca-QFYSSNK(epsilon-dinitrophenyl) + H2O
?
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?
MeO-Suc-Arg-Pro-Tyr-4-nitroanilide + H2O
?
a chromogenic substrate
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?
methoxy-succinyl-Arg-Pro-Tyr-4-nitroanilide + H2O
methoxy-succinyl-Arg-Pro-Tyr + 4-nitroaniline
methoxysuccinyl-Arg-Pro-Tyr-p-nitroanilide + H2O
?
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?
morpholinocarbonyl-His-Ser-Ser-Lys-Leu-Gln-7-amido-4-(trifluoromethyl)-coumarin + H2O
?
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?
morpholinocarbonyl-Lys-Gly-Ile-Ser-Ser-Gln-Tyr-7-amido-4-(trifluoromethyl)-coumarin + H2O
?
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?
morpholinocarbonyl-Ser-Arg-Lys-Gln-Gln-Tyr-7-amido-4-methylcoumarin + H2O
?
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?
Mu-SRKSQQY-7-amido-4-methylcoumarin + H2O
Mu-SRKSQQY + 7-amino-4-methylcoumarin
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?
N,N-dimethylated casein + H2O
?
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?
N-alpha-benzoyl-DL-Arg 4-nitroanilide + H2O
N-alpha-benzoyl-DL-Arg + 4-nitroaniline
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trypsin-like activity
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?
N-succinyl-(Ala)3-p-nitroanilide + H2O
?
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prostate-specific antigen shows limited activity
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?
N-succinyl-Ala-Ala-Pro-Phe-Ala-p-nitroanilide + H2O
?
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prostate-specific antigen shows limited activity
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?
N-succinyl-Ala-Ala-Pro-Val-p-nitroanilide + H2O
?
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prostate-specific antigen shows limited activity
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?
N-succinyl-Gly-Pro-Lys-p-nitroanilide + H2O
?
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prostate-specific antigen activity is 3times higher towards this substrate than towards other synthetic substrates
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?
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
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chymotrypsin-like activity
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?
nidogen-1 + H2O
?
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?
o-aminobenzoyl-ISYQSSSTEEQ ethylene diamine 2,4-dinitrophenyl + 2 H2O
o-aminobenzoyl-ISYQ + SSST + EEQ ethylene diamine 2,4-dinitrophenyl
o-aminobenzoyl-ISYQSSSTEEQ ethylene diamine 2,4-dinitrophenyl + H2O
o-aminobenzoyl-ISY + QSSSTEEQ ethylene diamine 2,4-dinitrophenyl
o-aminobenzoyl-NKISYQSSSQ ethylene diamine 2,4-dinitrophenyl + H2O
o-aminobenzoyl-NKISY + Q + SSSQ ethylene diamine 2,4-dinitrophenyl
o-aminobenzoyl-SSIYSNTEEQ ethylene diamine 2,4-dinitrophenyl + H2O
o-aminobenzoyl-SSIY + SNTEEQ ethylene diamine 2,4-dinitrophenyl
o-aminobenzoyl-SSQYSNTEEQ ethylene diamine 2,4-dinitrophenyl + H2O
o-aminobenzoyl-SSQY + SNTEEQ ethylene diamine 2,4-dinitrophenyl
PFR-7-amido-4-methylcoumarin + H2O
PFR + 7-amino-4-methylcoumarin
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fluorogenic substrate
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?
plasminogen + H2O
angiostatin-like fragments
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?
plasminogen + H2O
plasmin + ?
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polypeptide + H2O
peptides
proform of transforming growth factor-beta + H2O
transforming growth factor-beta + ?
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i.e. IGF-beta
?
semenogelin + H2O
semenogelin fractions
semenogelin + H2O
semenogelin fragments
semenogelin I + H2O
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from human seminal fluid
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?
semenogelin I + H2O
semenogelin fragments
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?
semenogelin II + H2O
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from human seminal fluid
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semenogelin II + H2O
semenogelin fragments
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?
succinyl-AAPF-7-amido-4-methylcoumarin + H2O
succinyl-AAPF + 7-amino-4-methylcoumarin
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?
succinyl-Ala-Ala-Phe-7-amido-4-methylcoumarin + H2O
succinyl-Ala-Ala-Phe + 7-amino-4-methylcoumarin
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?
TGFbeta2 + H2O
activated TGFbeta2
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?
urokinase-type plasminogen activator receptor + H2O
?
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cleavage within D1-D2 linker sequence and in its D3 juxtamembrane domain
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additional information
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Fibronectin + H2O
?
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Fibronectin + H2O
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Fibronectin + H2O
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enzyme participates in sperm liquefaction by cleaving fibronectin and semenogelins, the major components of the seminal vesicle coagulum after ejaculation
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?
Galectin-3 + H2O
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Galectin-3 + H2O
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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
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?
Galectin-3 + H2O
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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
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?
Gelatin + H2O
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Gelatin + H2O
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proteolytic activity at pH 7.5
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?
methoxy-succinyl-Arg-Pro-Tyr-4-nitroanilide + H2O
methoxy-succinyl-Arg-Pro-Tyr + 4-nitroaniline
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chromogenic substrate
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?
methoxy-succinyl-Arg-Pro-Tyr-4-nitroanilide + H2O
methoxy-succinyl-Arg-Pro-Tyr + 4-nitroaniline
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i.e. S2586
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?
o-aminobenzoyl-ISYQSSSTEEQ ethylene diamine 2,4-dinitrophenyl + 2 H2O
o-aminobenzoyl-ISYQ + SSST + EEQ ethylene diamine 2,4-dinitrophenyl
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substrate is intramolecularly quenched
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?
o-aminobenzoyl-ISYQSSSTEEQ ethylene diamine 2,4-dinitrophenyl + 2 H2O
o-aminobenzoyl-ISYQ + SSST + EEQ ethylene diamine 2,4-dinitrophenyl
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synthetic fluorogenic substrate, that encompasses a sequence containing a major ex vivo cleavage site , the Gln266-Ser267 bond of semenogelin I
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?
o-aminobenzoyl-ISYQSSSTEEQ ethylene diamine 2,4-dinitrophenyl + H2O
o-aminobenzoyl-ISY + QSSSTEEQ ethylene diamine 2,4-dinitrophenyl
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substrate is intramolecularly quenched
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?
o-aminobenzoyl-ISYQSSSTEEQ ethylene diamine 2,4-dinitrophenyl + H2O
o-aminobenzoyl-ISY + QSSSTEEQ ethylene diamine 2,4-dinitrophenyl
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synthetic fluorogenic substrate
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?
o-aminobenzoyl-NKISYQSSSQ ethylene diamine 2,4-dinitrophenyl + H2O
o-aminobenzoyl-NKISY + Q + SSSQ ethylene diamine 2,4-dinitrophenyl
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substrate is intramolecularly quenched
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?
o-aminobenzoyl-NKISYQSSSQ ethylene diamine 2,4-dinitrophenyl + H2O
o-aminobenzoyl-NKISY + Q + SSSQ ethylene diamine 2,4-dinitrophenyl
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synthetic fluorogenic substrate
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?
o-aminobenzoyl-SSIYSNTEEQ ethylene diamine 2,4-dinitrophenyl + H2O
o-aminobenzoyl-SSIY + SNTEEQ ethylene diamine 2,4-dinitrophenyl
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substrate is intramolecularly quenched
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?
o-aminobenzoyl-SSIYSNTEEQ ethylene diamine 2,4-dinitrophenyl + H2O
o-aminobenzoyl-SSIY + SNTEEQ ethylene diamine 2,4-dinitrophenyl
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synthetic fluorogenic substrate
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?
o-aminobenzoyl-SSIYSNTEEQ ethylene diamine 2,4-dinitrophenyl + H2O
o-aminobenzoyl-SSIY + SNTEEQ ethylene diamine 2,4-dinitrophenyl
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sequence contains ex vivo cleavage sites of semenogelin I
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?
o-aminobenzoyl-SSQYSNTEEQ ethylene diamine 2,4-dinitrophenyl + H2O
o-aminobenzoyl-SSQY + SNTEEQ ethylene diamine 2,4-dinitrophenyl
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substrate is intramolecularly quenched
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?
o-aminobenzoyl-SSQYSNTEEQ ethylene diamine 2,4-dinitrophenyl + H2O
o-aminobenzoyl-SSQY + SNTEEQ ethylene diamine 2,4-dinitrophenyl
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synthetic fluorogenic substrate
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?
o-aminobenzoyl-SSQYSNTEEQ ethylene diamine 2,4-dinitrophenyl + H2O
o-aminobenzoyl-SSQY + SNTEEQ ethylene diamine 2,4-dinitrophenyl
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sequence contains ex vivo cleavage sites of semenogelin I
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?
polypeptide + H2O
peptides
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polypeptide + H2O
peptides
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polypeptide + H2O
peptides
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?
polypeptide + H2O
peptides
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?
polypeptide + H2O
peptides
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polypeptide + H2O
peptides
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polypeptide + H2O
peptides
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?
polypeptide + H2O
peptides
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?
polypeptide + H2O
peptides
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enzyme possibly is involved in the processing of insulin-like growth factor binding protein 3
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?
polypeptide + H2O
peptides
enzyme possibly is involved in the processing of insulin-like growth factor binding protein 3
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?
PTHrP + H2O
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semenogelin + H2O
semenogelin fractions
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semenogelin + H2O
semenogelin fractions
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semenogelin + H2O
semenogelin fractions
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semenogelin + H2O
semenogelin fractions
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?
semenogelin + H2O
semenogelin fractions
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enzyme participates in sperm liquefaction by cleaving fibronectin and semenogelins, the major components of the seminal vesicle coagulum after ejaculation
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?
semenogelin + H2O
semenogelin fractions
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semenogelins I and II, cleavage results in liquefaction and release of motil spermatozoa
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?
semenogelin + H2O
semenogelin fragments
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semenogelin + H2O
semenogelin fragments
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semenogelin + H2O
semenogelin fragments
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?
semenogelin + H2O
semenogelin fragments
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?
semenogelin + H2O
semenogelin fragments
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semenogelins I and II
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?
semenogelin + H2O
semenogelin fragments
semenogelins I and II
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?
semenogelin + H2O
semenogelin fragments
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semenogelin I contains 18 cleavage sites, semenogelin II contains 16 cleavage sites
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?
additional information
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substrate specificity, overview
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?
additional information
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enzyme has no kininogenase activity
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?
additional information
?
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no activation of single-chain urokinase
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?
additional information
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enzyme shows no trypsin-like activity
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?
additional information
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enzyme shows no trypsin-like activity
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?
additional information
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no activity with carbobenzoxylysine thiobenzyl ester
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?
additional information
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enzyme is regulated by steroid hormones, it contains 2 androgen-response elements in the proximal PSA promotor
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?
additional information
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enzyme is regulated by steroid hormones, it contains 2 androgen-response elements in the proximal PSA promotor
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?
additional information
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stimulates cell detachment and facilitates tumor spread
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?
additional information
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stimulates cell detachment and facilitates tumor spread
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?
additional information
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enzyme can be activated by recombinant kallikrein 2
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?
additional information
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slightly prefers Met over Nle and Ala at the P1 position of the fluorogenic substrates but also tolerates Leu, Tyr, Phe, and the basic residues Arg and Lys, whereas Asp and Thr are not accepted at all, In the S2 subsite Leu is slightly preferred over Ala, Gln, Met, and Tyr
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?
additional information
?
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proteolytic activity of prostate-specific antigen is essential for inhibition of angiogenesis
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?
additional information
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PSMA, PSCA and STEAP are specifically upregulated in the transgenic murine prostate cancer. Significant numbers of STEAP-specific CD8 T cells in the peripheral blood and the spleen of immune mice using MHC I tetramers
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?
additional information
?
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no hydrolysis with NH2-Q-amido-4-methyl coumarin, 4-morpholinecarbonyl-LQ-7-amido-4-methylcoumarin and 4-morpholinecarbonyl-KLQ-7-amido-4-methylcoumarin as substrates
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?
additional information
?
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substrates containing tyrosine in the P1 position are hydrolyzed efficiently by PSA. Substrates with glutamine in the P1 position are less efficiently hydrolyzed, but demonstrate better specificity for PSA. The region spanning the S1 pocket contains several highly conserved residues that are critical for the structural integrity of the pocket and indirectly responsible for the maintenance of enzymatic activity. Residues such as Cys191, Cys220, Pro225, and Ser214 form crucial elements of the architecture surrounding the S1 pocket
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?
additional information
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only P1-4 residues are major determinants of binding affinity and substrate specificity for PSA. The P1 residue binds at the specificity pocket lined by polar residues with the partial hydrophobic side-chains such as Ser217, Thr184, and Tyr219. The P2 residue side-chain is docked against the face of the imidazole ring of the catalytic His41 residue. The P3 residue acts as a lid to the specificity pocket and docks at a location just above the P1 binding site in the specificity pocket. Important role for Glu208 interactions in determining PSA specificity at the P3 residue. The P4 pocket is located in the lower groove area, and mainly formed by His164, Pro165, Gln166, and Trp205 residues
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?