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4-morpholinecarbonyl-HSSKLQ-7-amido-4-methylcoumarin + H2O
?
a fluorogenic enzyme substrate
-
-
?
4-morpholinecarbonyl-HSSKLQ-AMC + H2O
?
-
-
-
-
?
4-morpholinecarbonyl-SKLQ-7-amido-4-methylcoumarin + H2O
?
-
hydrolysis rate is 29.6 pmol/min per 100 pmol of PSA
-
-
?
4-morpholinecarbonyl-SRKSQQY-7-amido-4-methylcoumarin + H2O
?
-
-
-
-
?
Arg-Pro-Tyr 4-nitroanilide + H2O
Arg-Pro-Tyr + 4-nitroaniline
-
-
-
-
?
Bovine serum albumin + H2O
?
-
is more readily hydrolysed than casein
-
-
?
casein + H2O
?
-
proteolytic activity at pH 7.5
-
-
?
EHSSKLQ-7-amido-4-methylcoumarin + H2O
EHSSKLQ + 7-amino-4-methylcoumarin
-
-
-
-
?
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
-
water soluble paclitaxel prodrug that is activated specifically by PSA in prostate tissue and prostate carcinoma
-
-
?
GSAKLQ + H2O
?
-
207.2% relative hydrolysis rate
-
-
?
GSSALQ + H2O
?
-
43.2% relative hydrolysis rate
-
-
?
GSSKLA + H2O
?
-
31.5% relative hydrolysis rate
-
-
?
GSSKLH + H2O
?
-
170.6% relative hydrolysis rate
-
-
?
GSSKLQ + H2O
?
-
100% relative hydrolysis rate
-
-
?
GSSKPQ + H2O
?
-
7.2% relative hydrolysis rate
-
-
?
GSSKYQ + H2O
?
-
256.9% relative hydrolysis rate
-
-
?
GSSSLQ + H2O
?
-
52.6% relative hydrolysis rate
-
-
?
HSSKLQ-7-amido-4-methylcoumarin + H2O
?
-
hydrolysis rate is 62.7 pmol/min per 100 pmol of PSA
-
-
?
HSSKLQ-7-amido-4-methylcoumarin + H2O
HSSKLQ + 7-amino-4-methylcoumarin
-
-
-
-
?
HSSKLQ-7-amido-4-trifluoromethyl-coumarin + H2O
?
-
-
-
-
?
insulin-like growth factor binding protein 5 + H2O
?
-
is degraded by PSA in a dose- and time-dependent manner. Under nonreducing conditions is degraded into two fragments with approximate molecular masses of 20 and 15 kDa. Under reducing conditions, is degraded into 4 distinct fragments with approximate molecular masses of 22 kDa, 21 kDa, 18 kDa and 13 kDa
-
-
?
insulin-like growth factor binding protein-3 + H2O
insulin-like growth factor I + ?
-
i.e. IGF-I
?
insulin-like growth factor binding protein-3 + H2O
insulin-like growth factor-1
-
-
-
-
?
KGISSQY-7-amido-4-methylcoumarin + H2O
KGISSQY + 7-amino-4-methylcoumarin
-
fluorogenic substrate
-
-
?
Laminin + H2O
?
-
-
-
-
?
LSEPAELTDAVK + H2O
PAELTDAVK + LSE
-
-
-
-
?
Lys-Val-Tyr 4-nitroanilide + H2O
Lys-Val-Tyr + 4-nitroaniline
-
-
-
-
?
Mca-QFYSSNK(epsilon-dinitrophenyl) + H2O
?
-
-
-
-
?
MeO-Suc-Arg-Pro-Tyr-4-nitroanilide + H2O
?
a chromogenic substrate
-
-
?
methoxy-succinyl-Arg-Pro-Tyr-4-nitroanilide + H2O
methoxy-succinyl-Arg-Pro-Tyr + 4-nitroaniline
methoxysuccinyl-Arg-Pro-Tyr-p-nitroanilide + H2O
?
-
-
-
?
morpholinocarbonyl-His-Ser-Ser-Lys-Leu-Gln-7-amido-4-(trifluoromethyl)-coumarin + H2O
?
-
-
-
?
morpholinocarbonyl-Lys-Gly-Ile-Ser-Ser-Gln-Tyr-7-amido-4-(trifluoromethyl)-coumarin + H2O
?
-
-
-
-
?
morpholinocarbonyl-Ser-Arg-Lys-Gln-Gln-Tyr-7-amido-4-methylcoumarin + H2O
?
-
-
-
-
?
Mu-SRKSQQY-7-amido-4-methylcoumarin + H2O
Mu-SRKSQQY + 7-amino-4-methylcoumarin
-
-
-
?
N,N-dimethylated casein + H2O
?
-
-
-
-
?
N-alpha-benzoyl-DL-Arg 4-nitroanilide + H2O
N-alpha-benzoyl-DL-Arg + 4-nitroaniline
-
trypsin-like activity
-
-
?
N-succinyl-(Ala)3-p-nitroanilide + H2O
?
-
prostate-specific antigen shows limited activity
-
-
?
N-succinyl-Ala-Ala-Pro-Phe-Ala-p-nitroanilide + H2O
?
-
prostate-specific antigen shows limited activity
-
-
?
N-succinyl-Ala-Ala-Pro-Val-p-nitroanilide + H2O
?
-
prostate-specific antigen shows limited activity
-
-
?
N-succinyl-Gly-Pro-Lys-p-nitroanilide + H2O
?
-
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
-
chymotrypsin-like activity
-
-
?
nidogen-1 + H2O
?
-
-
-
?
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
-
fluorogenic substrate
-
-
?
plasminogen + H2O
angiostatin-like fragments
-
-
-
-
?
plasminogen + H2O
plasmin + ?
-
-
-
?
polypeptide + H2O
peptides
proform of transforming growth factor-beta + H2O
transforming growth factor-beta + ?
-
i.e. IGF-beta
?
semenogelin + H2O
semenogelin fractions
semenogelin + H2O
semenogelin fragments
semenogelin I + H2O
?
from human seminal fluid
-
-
?
semenogelin I + H2O
semenogelin fragments
-
-
-
-
?
semenogelin II + H2O
?
from human seminal fluid
-
-
?
semenogelin II + H2O
semenogelin fragments
-
-
-
-
?
succinyl-AAPF-7-amido-4-methylcoumarin + H2O
succinyl-AAPF + 7-amino-4-methylcoumarin
-
-
-
-
?
succinyl-Ala-Ala-Phe-7-amido-4-methylcoumarin + H2O
succinyl-Ala-Ala-Phe + 7-amino-4-methylcoumarin
-
-
-
-
?
TGFbeta2 + H2O
activated TGFbeta2
-
-
-
-
?
urokinase-type plasminogen activator receptor + H2O
?
-
-
cleavage within D1-D2 linker sequence and in its D3 juxtamembrane domain
-
?
additional information
?
-
Fibronectin + H2O
?
-
-
-
-
?
Fibronectin + H2O
?
-
-
-
?
Fibronectin + H2O
?
-
enzyme participates in sperm liquefaction by cleaving fibronectin and semenogelins, the major components of the seminal vesicle coagulum after ejaculation
-
-
?
Galectin-3 + H2O
?
-
-
-
?
Galectin-3 + H2O
?
-
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
-
?
Galectin-3 + H2O
?
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
-
-
?
Gelatin + H2O
?
-
-
-
?
Gelatin + H2O
?
-
proteolytic activity at pH 7.5
-
-
?
methoxy-succinyl-Arg-Pro-Tyr-4-nitroanilide + H2O
methoxy-succinyl-Arg-Pro-Tyr + 4-nitroaniline
-
chromogenic substrate
-
-
?
methoxy-succinyl-Arg-Pro-Tyr-4-nitroanilide + H2O
methoxy-succinyl-Arg-Pro-Tyr + 4-nitroaniline
-
i.e. S2586
-
-
?
o-aminobenzoyl-ISYQSSSTEEQ ethylene diamine 2,4-dinitrophenyl + 2 H2O
o-aminobenzoyl-ISYQ + SSST + EEQ ethylene diamine 2,4-dinitrophenyl
-
substrate is intramolecularly quenched
-
?
o-aminobenzoyl-ISYQSSSTEEQ ethylene diamine 2,4-dinitrophenyl + 2 H2O
o-aminobenzoyl-ISYQ + SSST + EEQ ethylene diamine 2,4-dinitrophenyl
-
synthetic fluorogenic substrate, that encompasses a sequence containing a major ex vivo cleavage site , the Gln266-Ser267 bond of semenogelin I
-
?
o-aminobenzoyl-ISYQSSSTEEQ ethylene diamine 2,4-dinitrophenyl + H2O
o-aminobenzoyl-ISY + QSSSTEEQ ethylene diamine 2,4-dinitrophenyl
-
substrate is intramolecularly quenched
-
?
o-aminobenzoyl-ISYQSSSTEEQ ethylene diamine 2,4-dinitrophenyl + H2O
o-aminobenzoyl-ISY + QSSSTEEQ ethylene diamine 2,4-dinitrophenyl
-
synthetic fluorogenic substrate
-
?
o-aminobenzoyl-NKISYQSSSQ ethylene diamine 2,4-dinitrophenyl + H2O
o-aminobenzoyl-NKISY + Q + SSSQ ethylene diamine 2,4-dinitrophenyl
-
substrate is intramolecularly quenched
-
?
o-aminobenzoyl-NKISYQSSSQ ethylene diamine 2,4-dinitrophenyl + H2O
o-aminobenzoyl-NKISY + Q + SSSQ ethylene diamine 2,4-dinitrophenyl
-
synthetic fluorogenic substrate
-
?
o-aminobenzoyl-SSIYSNTEEQ ethylene diamine 2,4-dinitrophenyl + H2O
o-aminobenzoyl-SSIY + SNTEEQ ethylene diamine 2,4-dinitrophenyl
-
substrate is intramolecularly quenched
-
?
o-aminobenzoyl-SSIYSNTEEQ ethylene diamine 2,4-dinitrophenyl + H2O
o-aminobenzoyl-SSIY + SNTEEQ ethylene diamine 2,4-dinitrophenyl
-
synthetic fluorogenic substrate
-
?
o-aminobenzoyl-SSIYSNTEEQ ethylene diamine 2,4-dinitrophenyl + H2O
o-aminobenzoyl-SSIY + SNTEEQ ethylene diamine 2,4-dinitrophenyl
-
sequence contains ex vivo cleavage sites of semenogelin I
-
?
o-aminobenzoyl-SSQYSNTEEQ ethylene diamine 2,4-dinitrophenyl + H2O
o-aminobenzoyl-SSQY + SNTEEQ ethylene diamine 2,4-dinitrophenyl
-
substrate is intramolecularly quenched
-
?
o-aminobenzoyl-SSQYSNTEEQ ethylene diamine 2,4-dinitrophenyl + H2O
o-aminobenzoyl-SSQY + SNTEEQ ethylene diamine 2,4-dinitrophenyl
-
synthetic fluorogenic substrate
-
?
o-aminobenzoyl-SSQYSNTEEQ ethylene diamine 2,4-dinitrophenyl + H2O
o-aminobenzoyl-SSQY + SNTEEQ ethylene diamine 2,4-dinitrophenyl
-
sequence contains ex vivo cleavage sites of semenogelin I
-
?
polypeptide + H2O
peptides
-
-
-
?
polypeptide + H2O
peptides
-
-
-
?
polypeptide + H2O
peptides
-
-
-
?
polypeptide + H2O
peptides
-
-
-
?
polypeptide + H2O
peptides
-
-
-
?
polypeptide + H2O
peptides
-
-
-
?
polypeptide + H2O
peptides
-
-
-
?
polypeptide + H2O
peptides
-
-
?
polypeptide + H2O
peptides
-
enzyme possibly is involved in the processing of insulin-like growth factor binding protein 3
-
?
polypeptide + H2O
peptides
enzyme possibly is involved in the processing of insulin-like growth factor binding protein 3
-
?
PTHrP + H2O
?
-
-
-
-
?
semenogelin + H2O
semenogelin fractions
-
-
-
?
semenogelin + H2O
semenogelin fractions
-
-
-
?
semenogelin + H2O
semenogelin fractions
-
-
-
-
?
semenogelin + H2O
semenogelin fractions
-
-
-
?
semenogelin + H2O
semenogelin fractions
-
enzyme participates in sperm liquefaction by cleaving fibronectin and semenogelins, the major components of the seminal vesicle coagulum after ejaculation
-
-
?
semenogelin + H2O
semenogelin fractions
-
semenogelins I and II, cleavage results in liquefaction and release of motil spermatozoa
-
?
semenogelin + H2O
semenogelin fragments
-
-
-
-
?
semenogelin + H2O
semenogelin fragments
-
-
-
?
semenogelin + H2O
semenogelin fragments
-
-
-
?
semenogelin + H2O
semenogelin fragments
-
-
-
-
?
semenogelin + H2O
semenogelin fragments
-
semenogelins I and II
-
?
semenogelin + H2O
semenogelin fragments
semenogelins I and II
-
-
?
semenogelin + H2O
semenogelin fragments
-
semenogelin I contains 18 cleavage sites, semenogelin II contains 16 cleavage sites
-
?
additional information
?
-
substrate specificity, overview
-
-
?
additional information
?
-
-
enzyme has no kininogenase activity
-
-
?
additional information
?
-
-
no activation of single-chain urokinase
-
-
?
additional information
?
-
-
enzyme shows no trypsin-like activity
-
-
?
additional information
?
-
-
enzyme shows no trypsin-like activity
-
-
?
additional information
?
-
-
no activity with carbobenzoxylysine thiobenzyl ester
-
-
?
additional information
?
-
enzyme is regulated by steroid hormones, it contains 2 androgen-response elements in the proximal PSA promotor
-
-
?
additional information
?
-
-
enzyme is regulated by steroid hormones, it contains 2 androgen-response elements in the proximal PSA promotor
-
-
?
additional information
?
-
stimulates cell detachment and facilitates tumor spread
-
-
?
additional information
?
-
-
stimulates cell detachment and facilitates tumor spread
-
-
?
additional information
?
-
-
enzyme can be activated by recombinant kallikrein 2
-
-
?
additional information
?
-
-
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
-
-
?
additional information
?
-
-
proteolytic activity of prostate-specific antigen is essential for inhibition of angiogenesis
-
-
?
additional information
?
-
-
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
-
-
?
additional information
?
-
-
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
-
-
?
additional information
?
-
-
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
-
-
?
additional information
?
-
-
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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((2R,3R)-3-benzyl-1-(ethylsulfonyl)-4-oxoazetidin-2-yl)methyl benzoate
-
-
((2R,3R)-3-benzyl-4-oxo-1-(phenylsulfonyl)azetidin-2-yl)methyl benzoate
-
-
((2R,3R)-3-benzyl-4-oxo-1-tosylazetidin-2-yl)methyl benzoate
-
-
((2S,3S)-3-benzyl-1-(ethylsulfonyl)-4-oxoazetidin-2-yl)methyl benzoate
-
-
((2S,3S)-3-benzyl-4-oxo-1-(phenylsulfonyl)azetidin-2-yl)methyl benzoate
-
-
((2S,3S)-3-benzyl-4-oxo-1-tosylazetidin-2-yl)methyl benzoate
-
-
(1S)-4-bromo-1-[(3aS,4R,6R,7aR)-3a,5,5-trimethylhexahydro-4,6-methano-1,3,2-benzodioxaborol-2-yl]butan-1-amine
-
(2-methoxyphenyl)(3-phenyl-1H-1,2,4-triazol-1-yl)methanone
-
-
(2R,3R)-benzyl 1-(2-(3-(benzyloxycarbonyl)phenyl)acetyl)-3-(4-hydroxybenzyl)-4-oxoazetidine-2-carboxylate
-
-
(2R,3R)-benzyl 1-benzoyl-3-(4-hydroxybenzyl)-4-oxoazetidine-2-carboxylate
-
-
(2R,3R)-benzyl 3-benzyl-1-(2-(3-(benzyloxycarbonyl)phenyl)acetyl)-4-oxoazetidine-2-carboxylate
-
-
(2R,3R)-ethyl 3-benzyl-4-oxo-1-tosylazetidine-2-carboxylate
-
-
(2S,3S)-benzyl 1-(2-(3-(benzyloxycarbonyl)phenyl)acetyl)-3-(4-hydroxybenzyl)-4-oxoazetidine-2-carboxylate
-
-
(2S,3S)-benzyl 1-benzoyl-3-(4-hydroxybenzyl)-4-oxoazetidine-2-carboxylate
-
-
(2S,3S)-benzyl 3-benzyl-1-(2-(3-(benzyloxycarbonyl)phenyl)acetyl)-4-oxoazetidine-2-carboxylate
-
-
(2S,3S)-ethyl 3-benzyl-4-oxo-1-tosylazetidine-2-carboxylate
-
-
(3,4-dimethoxyphenyl)(5-(4-fluorobenzylamino)-3-phenyl-1H-1,2,4-triazol-1-yl)methanone
-
-
(3-benzyl-1-(ethylsulfonyl)-4-oxoazetidin-2-yl)methyl benzoate
-
-
(3-benzyl-4-oxo-1-tosylazetidin-2-yl)methyl benzoate
-
-
(3aR,4R,6R,7aS)-2-[(1R)-1-amino-2-phenylethyl]-5,5-dimethyltetrahydro-4,6-methano-1,3,2-benzodioxaborol-3a(4H)-ol
-
(4-[[([(2S,3S)-3-benzyl-1-[(3-carboxyphenyl)acetyl]-4-oxoazetidin-2-yl]carbonyl)oxy]methyl]phenyl)methanaminium trifluoroacetate
-
-
(5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(2-chlorophenyl)methanone
-
-
(5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(2-methoxyphenyl)methanone
-
-
(5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(3,4-dimethoxyphenyl)methanone
-
360 nanomol inhibits by 83%
(5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(4-chlorophenyl)methanone
-
-
(5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(4-fluorophenyl)methanone
-
-
(5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(4-methoxyphenyl)methanone
-
360 nanomol inhibits by 56%
(5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(4-nitrophenyl)methanone
-
-
(5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(p-tolyl)methanone
-
-
(5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(phenyl)methanone
-
-
(5-amino-3-phenyl-1H-1,2,4-triazol-1-yl)(3,4-dimethoxyphenyl)methanone
-
-
(6-[bis[(pyridin-2-yl-kappaN)methyl]amino-kappaN]hexanoyl)(tricarbonyl)rhenium(3+)-Ser-Ser-Gln-Nle-Leu-B(OH)2
-
-
1-(3-chlorobenzyl)-3-phenyl-1H-pyrazol-5-amine
-
-
1-benzyl-3-phenyl-1H-pyrazol-5-amine
-
-
2-(2-methyl-3-nitrophenyl)-4-oxo-4H-3,1-benzoxazin-6-yl acetate
-
-
2-(2-methyl-3-nitrophenyl)-4H-3,1-benzoxazin-4-one
-
360 nanomol inhibits by 61%
2-(2-methylphenyl)-4H-3,1-benzoxazin-4-one
-
-
2-(2-nitrophenyl)-4H-3,1-benzoxazin-4-one
-
-
2-(3-methylphenyl)-4H-3,1-benzoxazin-4-one
-
-
2-(3-nitrophenyl)-4H-3,1-benzoxazin-4-one
-
-
2-(4-bromophenyl)quinazolin-4(3H)-one
-
-
2-(4-methylphenyl)-4H-3,1-benzoxazin-4-one
-
-
2-mercaptoethanol
incubation with 3 mM for 30 min at 25°C, in 0.1 ml 0.1 M Tris buffer, pH 7.8, causes 84% loss of activity
2-phenyl-4H-3,1-benzoxazin-4-one
-
-
2-phenylquinazolin-4(3H)-one
-
-
2-[(3S)-3-[[N-(6-aminohexanoyl)-L-phenylalanyl]amino]-4-hydroxy-2-oxobutyl]-N1-[(2S)-1-([(1S)-4-bromo-1-[(3aR,4S,6S,7R,7aS)-5,5,7-trimethylhexahydro-4,6-methano-1,3,2-benzodioxaborol-2-yl]butyl]amino)-1-oxohexan-2-yl]pentanediamide
-
3-(2-((2R,3R)-3-benzyl-2-((4-carboxybenzyloxy)carbonyl)-4-oxoazetidin-1-yl)-2-oxoethyl)benzoic acid
-
-
3-(2-((2S,3S)-3-benzyl-2-((4-carboxybenzyloxy)carbonyl)-4-oxoazetidin-1-yl)-2-oxoethyl)benzoic acid
-
-
3-(2-(3-benzyl-2-((4-carboxybenzyloxy)carbonyl)-4-oxoazetidin-1-yl)-2-oxoethyl)benzoic acid
-
-
3-nitrophenyl boronic acid
inhibits PSA
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
-
alpha1-Antichymotrypsin
inhibits PSA
-
alpha2-Macroglobulin
-
-
-
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
-
-
Cd2+
-
competitive to other metal ions
Co2+
-
competitive to other metal ions
Cu2+
-
competitive to other metal ions
dihydrolipoate
incubation with 3 mM for 30 min at 25°C, in 0.1 ml 0.1 M Tris buffer, pH 7.8, causes 65% loss of activity
diisopropylfluorophosphate
-
-
dithiothreitol
incubation with 3 mM for 30 min at 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
EDTA
-
10 mM inhibits at pH 3.5
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
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
-
-
methylmethane thiosulphonate
-
1 mM completely inhibits with bovine serum albumin as a substrate at pH 3.5
morpholinocarbonyl-Ser-Ser-Gln-Nle-Leu-B(OH)2
-
-
N-p-tosyl-Lys chloromethyl ketone
-
3 mM inhibits at pH 3.5 with bovine serum albumin as a substrate but does not inhibit enzyme activity at pH 7.5 with casein as a substrate
N-tosyl-Phe chloromethyl ketone
-
3 mM inhibits at pH 3.5 with bovine serum albumin as a substrate but does not inhibit enzyme activity at pH 7.5 with casein as a substrate
N-[(2S)-8-amino-5-[[(2S)-1-[[(1S)-1-(dihydroxyboranyl)-2-phenylethyl]amino]-1-oxohexan-2-yl]carbamoyl]-1-hydroxy-3,8-dioxooctan-2-yl]-Na-(6-aminohexanoyl)-L-phenylalaninamide
-
N-[(2S)-8-amino-5-[[(2S)-1-[[(1S)-4-bromo-1-(dihydroxyboranyl)butyl]amino]-1-oxohexan-2-yl]carbamoyl]-1-hydroxy-3,8-dioxooctan-2-yl]-Na-(6-aminohexanoyl)-L-phenylalaninamide
-
N-[(2S)-8-amino-5-[[(2S)-1-[[(1S)-4-bromo-1-(dihydroxyboranyl)butyl]amino]-1-oxohexan-2-yl]carbamoyl]-1-hydroxy-3,8-dioxooctan-2-yl]-Na-[6-[(4-iodobenzoyl)amino]hexanoyl]-L-phenylalaninamide
-
N-[(3S)-3-[(6-aminohexanoyl)amino]-4-(naphthalen-2-yl)butanoyl]-L-seryl-L-glutaminyl-N-[(1S)-1-(dihydroxyboranyl)-2-phenylethyl]-L-norleucinamide
-
N-[(3S)-3-[(6-aminohexanoyl)amino]-4-(naphthalen-2-yl)butanoyl]-L-seryl-L-glutaminyl-N-[(1S)-4-bromo-1-(dihydroxyboranyl)butyl]-L-norleucinamide
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-3-cyclohexyl-L-alanyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-norleucinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-alanyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-norleucinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-alpha-aspartyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-norleucinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-alpha-glutamyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-norleucinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-asparaginyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-norleucinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-glutaminyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-norleucinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-homoseryl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-norleucinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-(4S)-4-hydroxy-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-prolinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-3-(2-naphthyl)-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-alaninamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-3-cyclohexyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-alaninamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-4-bromo-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-phenylalaninamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(1S)-2-oxo-1-phenylethyl]-L-leucinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-1-(4-hydroxyphenyl)-3-oxopropan-2-yl]-L-leucinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-1-(acetylamino)-3-oxopropan-2-yl]-L-leucinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-1-(benzoylamino)-3-oxopropan-2-yl]-L-leucinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-1-(formylamino)-3-oxopropan-2-yl]-L-leucinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-1-oxo-3-(propanoylamino)propan-2-yl]-L-leucinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-1-oxo-3-phenylpropan-2-yl]-L-leucinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-1-oxohexan-2-yl]-L-leucinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-1-[(2-methylpropanoyl)amino]-3-oxopropan-2-yl]-L-leucinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-3-methyl-1-oxobutan-2-yl]-L-leucinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-(dimethylamino)-1,4-dioxobutan-2-yl]-L-leucinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-(methylsulfanyl)-1-oxobutan-2-yl]-L-leucinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-(methylsulfinyl)-1-oxobutan-2-yl]-L-leucinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-cyano-1-oxobutan-2-yl]-L-leucinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-alaninamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-alpha-asparagine
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-alpha-glutamine
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-histidinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-homoserinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-isoleucinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-leucinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-lysinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-methioninamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-norleucinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-norvalinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-phenylalaninamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-prolinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-serinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-threoninamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-tyrosinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-valinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]glycinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-5-(dimethylamino)-1,5-dioxopentan-2-yl]-L-leucinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-5-amino-1,5-dioxopentan-2-yl]-L-leucinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N1-[(2S)-4-methyl-1-oxopentan-2-yl]-L-aspartamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N1-[(2S)-4-methyl-1-oxopentan-2-yl]-L-glutamamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-S-tert-butyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-cysteinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-methionyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-norleucinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-prolyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-norleucinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-seryl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-norleucinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-threonyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-norleucinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-N-[(1S)-2-[[(2S)-4-methyl-1-oxopentan-2-yl]amino]-2-oxo-1-phenylethyl]-L-lysinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-N-[(2S)-1-[[(2S)-4-methyl-1-oxopentan-2-yl]amino]-4-(methylsulfinyl)-1-oxobutan-2-yl]-L-lysinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-L-serylglycyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-norleucinamide
-
-
N-[(benzyloxy)carbonyl]-L-seryl-N-[(2S)-1-[[(2S)-1-[[(2S)-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-(methylsulfinyl)-1-oxobutan-2-yl]-L-serinamide
-
-
N1-[(2S)-1-([(1S)-4-bromo-1-[(3aR,4S,6S,7R,7aS)-5,5,7-trimethylhexahydro-4,6-methano-1,3,2-benzodioxaborol-2-yl]butyl]amino)-1-oxohexan-2-yl]-2-[(3S)-4-hydroxy-3-[(N-[6-[(4-iodobenzoyl)amino]hexanoyl]-L-phenylalanyl)amino]-2-oxobutyl]pentanediamide
-
N2-[(5S)-5-[[N-(6-aminohexanoyl)-L-alanyl]amino]-2-(3-amino-3-oxopropyl)-6-hydroxy-4-oxohexanoyl]-N-[(1S)-1-(dihydroxyboranyl)-2-phenylethyl]-L-norleucinamide
-
N2-[(5S)-5-[[N-(6-aminohexanoyl)-L-alanyl]amino]-2-(3-amino-3-oxopropyl)-6-hydroxy-4-oxohexanoyl]-N-[(1S)-4-bromo-1-(dihydroxyboranyl)butyl]-L-norleucinamide
-
p-hydroxyphenylmercurisulfonate
-
1 mM completely inhibits with bovine serum albumin as a substrate at pH 3.5
Phenylmethylsulphonyl fluoride
-
3 mM inhibits at pH 7.5 with casein as a substrate and at pH 3.5 with bovine serum albumin as a substrate
Pregnancy-zone protein
-
-
-
R/S-diphenyl[N-benzyloxycarbonylamino(4-carbamoylphenyl)methyl]phosphonate
-
serum
-
inhibits the mature enzyme
-
Soybean trypsin inhibitor
-
-
-
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-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-Leu-B(OH)2
-
-
Z-SSKL(boro)L
inhibits PSA
alpha1-Aantichymotrypsin
-
-
-
alpha1-Aantichymotrypsin
-
complex formation
-
alpha1-Aantichymotrypsin
-
can block the PSA antiangiogenic effect
-
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
-
Aprotinin
-
-
Aprotinin
-
efficient inhibition
Hg2+
-
-
Hg2+
-
competitive to other metal ions
leupeptin
-
-
leupeptin
-
1 mM completely inhibits with bovine serum albumin as a substrate at pH 3.5
PMSF
-
-
PMSF
-
suppresses the insulin-like growth factor binding protein 5 degradation associated with PSA treatment
Zn2+
-
-
Zn2+
-
50% inhibition at 0.02 mM, 25fold molar excess of Zn2+ to enzyme; competitive to substrate and other metal ions, modeling; strong, tight-binding inhibitor
Zn2+
-
at pH 7.5, 50% of the PSA enzymatic activity is inhibited by 0.024 mM, 10 mM are needed at pH 5.5 for inhibition. Inhibition is not relieved by monoclonal antibody binding of 8G8F5
Zn2+
-
3 mM inhibits at pH 7.5 with casein as a substrate. When bovine serum albumin is used as a substrate at pH 3.5, prostate-specific antigen or proteinase is not inhibited by 5 mM Zn2+
additional information
-
beta-lactams inhibit PSA in a time-dependent fashion, beta-lactams bind covalently with PSA. Specificity of a lactam inhibitor toward PSA can be strengthened by optimizing its C-3 side chain to maximize the hydrophobic and the polar interactions in the S-1 pocket
-
additional information
3 mM ascorbate for 30 min at 25°C, in 0.1 ml 0.1 M Tris buffer, pH 7.8, is devoid of inactivating potential. Loss of activity by reduction can be readily reversed by re-oxidation. Inactivation is associated with the reduction of two out of five conserved disulfides. Accessabilty of the Cys191-Cys220 disulfide near the catalytic serine 195 decides on the ability of reductants to inactivate the proteolytic activity of PSA
-
additional information
-
5 mM Ca2+ or p-mercaptoethanol do not inhibit
-
additional information
-
50 mM EDTA does not inhibit insulin-like growth factor binding protein 5 degradation
-
additional information
-
structural motifs of the PSA S1 pocket have a distinct architecture and specificity when compared to the S1 pocket of chymotrypsin: glutamine derivative aldehydes are highly specific for PSA while inhibitors with hydrophobic P1 aldehydes are potent inhibitors of both PSA and chymotrypsin
-
additional information
-
beta-lactams inhibit PSA in a time-dependent manner with a 1:1 stoichiometry, competing with substrate, until a majority of PSA is converted into an irreversible inactive state. A stable covalent complex is formed between the beta-lactam and the active site serine residue in PSA. Azapeptides can inhibit PSA effectively. Benzoxazinone compounds are non-competitive inhibitors and triazoles are competitive inhibitors of PSA
-
additional information
-
preference for hydrophobic residues in the P2 position and amino acids with the potential to hydrogen bond in the P3 position
-
additional information
-
proteolytic activity of PSA is inhibited by the formation of irreversible complexes with serum protease inhibitors and other acute-phase proteins, such as alpha1-antichymotrypsin, alpha2-macroglobulin, inter-alpha1-trypsin inhibitor and alpha1-proteinase inhibitor
-
additional information
-
after antibacterial therapy for 2 weeks, the PSA decreases from 14.0 ng/ml to 10.4 ng/ml
-
additional information
structure-based drug design of diphenyl alpha-aminoalkylphosphonates as prostate-specific antigen antagonists, overview. Molecular docking and modeling of covalent and noncovalent binding of this class of inhibitors, interactions between the lead compound and residues Thr190, Ser217, and Ser227 in the P1 pocket
-
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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
-
-
0.000072
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
0.2652
Z-Gln-Leu-B(OH)2
-
-
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
-
-
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
-
-
0.0056
Zn2+
-
pH 8.0, 37°C, with methoxy-succinyl-Arg-Pro-Tyr-4-nitrophenyl
0.00091
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-1-(formylamino)-3-oxopropan-2-yl]-L-leucinamide
-
-
0.000918
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-1-(formylamino)-3-oxopropan-2-yl]-L-leucinamide
-
-
0.0065
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-leucinamide
-
-
0.00651
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-leucinamide
-
-
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additional information
-
human seminal proteinase and prostate-specific antigen are identical
analysis
-
development and employment of counter-SELEX (systematic evolution of ligands by exponential enrichment) procedures to identify specific RNA aptamers against the purified active PSA, wich is not only a specific marker but also a target molecule for diagnosis and therapy of prostate cancer. The aptamers have a specific binding activity against the active PSA, but not for GST or proPSA
analysis
-
development of a simultaneous electrochemical biosensor, using the goldmodified screen-printed carbon dual sensor, for free and total PSA for monitoring PSA production from three different cultures of human androgen-sensitive prostate tumor cells
analysis
-
development of an electrical immunosensor for the detection of PSA using a microgapped electrode array based on enzymatic silver deposition. This electrical immunosensor exhibits a linear response with PSA concentrations over a 6-decade range from 1.0 pg/l to 1.0 microg/l, with detection limit of 0.9 pg/l. PSA concentrations using this immunosensor agree within 10% of those obtained using a commercial chemiluminescent immunoassay
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
analysis
-
development of PSA and Fab anti-PSA biosensor arrays using UV light-assisted molecular immobilization LAMI, aiming at the detection and quantification of PSA, as a cancer marker. The technology involves formation of free, reactive thiol groups upon UV excitation of protein aromatic residues located in spatial proximity of disulfide bridges, conserved in both PSA and Fab molecules. The thiol groups bind onto thiol reactive surfaces leading to oriented covalent protein immobilization. LAMI technology is successful in immobilizing biomedically relevant molecules while preserving their activity
analysis
-
real-time detection of prostate-specific antigen PSA in diluted human serum without labeling by use of an amplitude-sensitive paired surface plasma wave biosensor PSPWB. The detection limit of PSPWB is 8.4 × 10-9 refractive index units, and the PSPWB can measure PSA in a phosphate buffered saline solution from 10 fg/ml to 100 pg/ml, i.e. about 3 pM, successfully, with a linear relationship between PSA concentrations and surface plasmon resonance signals. The PSPWB successfully detects PSA in diluted human serum as well
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
diagnostics
the enzyme is the most useful prostate cancer marker
diagnostics
the ratio of phosphorylated/dephosphorylated galectin-3 might be used as a complementary value to that of prostate specific antigene for prognosis of prostate cancer and another therapeutic target for the treatment of prostate cancer
diagnostics
the gama-SM/PSA, a protein member of the kallikrein family, is the most prominent biomarker for prostate cancer, PCa. Hsp70 can also be used as a co-biomarker for PCa with gama-SM
drug development
-
compounds inhibiting the activity of prostate-specific antigen, prevent the anti-angiogenic effect of prostate-specific antigen in an angiogenesis model
drug development
-
STEAP is a good immunologic target antigen against prostate cancer and vaccination regimen successfully elicits anti-tumor CTL responses and suppresses tumor growth
drug development
-
development of PSA selective inhibitors as useful tools for the targeted treatment and imaging of prostate cancer
drug development
the gama-SM protein can be a drug target in prostate cancer therapy
medicine
-
enzyme is a marker for prostatic disease
medicine
-
the size of the fraction of free enzyme in serum is a marker to distinguish benign hyperplasia from malignant carcinoma
medicine
enzyme is a marker for cancer
medicine
-
used in the diagnosis of prostate cancer
medicine
used in the diagnosis of prostate cancer
medicine
-
enzyme may modulate the tumor-associated urokinase-type plasminogen activator/urokinase-type plasminogen activator receptor-system activity by either activating the pro-enzyme form of plasminogen activator or cleaving the cell surface-associated receptor
medicine
-
before treatment, prostate specific antigen kinetics may provide valuable prognostic information regarding the risk of treatment failure and subsequent death from cancer. Prostate specific antigen velocity is easier to calculate but prostate specific antigen doubling time may have greater biological justification. Precise cutoff levels require further investigation
medicine
-
biomarker used in the diagnosis of prostate cancer and to monitor therapeutic response. Design and development of potent and specific inhibitors of PSA
medicine
-
important marker for the diagnosis and management of prostate cancer
medicine
purified active PSA has a potential use in prostate cancer diagnostics and/or therapeutics
medicine
-
splice variant PSA-SV5 may have applications as a biomarker in clinical diagnosis of prostate cancer based on its expression in a much higher percentage of prostate cancers compared to benign prostate hyperplasia
medicine
-
kinetics of prostate-specific antigen are indicative of tumour progression and are therefore used in clinical decision-making in men on active surveillance for early prostate cancer. A high prostate-specific antigen velocity or short prostate-specific antigen doubling time are related with an unfavourable outcome and should lead to performing an additional prostate biopsy or to deferred radical treatment during follow-up of active surveillance. A low prostate-specific antigen velocity or a long prostate-specific antigen doubling time is associated with a nonaggressive course of the disease and may justify a more conservative attitude. A prostate-specific antigen doubling time more than 10 years, a static course of the prostate-specific antigen values, or a negative prostate-specific antigen doubling time are generally associated with a good prognosis. A prostate-specific antigen doubling time of less than 3-4 years should lead to the advice to switch to radical treatment
medicine
-
low frequency of positive results in patients with prostatic cancer and a high frequency of positive results in those with benign prostatic hyperplasia seems to discourage the use of prostate-specific antigen-positive circulating cells in the search for a clinical diagnosis of prostate cancer
medicine
-
prostate-specific antigen is identified as a useful serum marker for assessing patients with prostate cancer during their follow-up. It is approved as a tool for detecting the disease in men aged over 50 years. There are limitations of a single prostate-specific antigen measurement, i.e. its low sensitivity and specificity in detecting prostate cancer, which may lead to the over-detection of cancers that pose little threat to health and/or life. Prostate-specific antigen kinetics (prostate-specific antigen velocity, doubling-time, half-time and progression) may be used to predict the outcome in both localized and advanced prostate cancer. Limitations of all prostate-specific antigen kinetics is the choice of many methods for calculation that can result in considerable variation in prediction and even in errors in patient management
medicine
-
prostate-specific antigen kinetics provide unique prognostic information to patients with prostate cancer. Pretreatment prostate-specific antigen velocity plays an important role in risk assessment of men treated by radical prostatectomy and external beam radiation therapy. Prostate-specific antigen doubling time at relapse predicts time to metastasis
medicine
-
prostate-specific antigen velocity is more accurate than prostate-specific antigen doubling time for predicting adverse histology on repeat biopsies, suggesting that prostate-specific antigen velocity shall be used in preference to PSA doubling time to describe prostate-specific antigen kinetics in untreated, localized prostate cancer
medicine
-
the predictive performance for prostate cancer using genetic variants and family history is similar to that of prostate-specific antigen. Such genetic markers may be used to supplement prostate-specific antigen to improve its predictive value
medicine
-
a novel method using molecular, polymerase chain reaction-based detection of cancer cell clusters, which is applied for predicting prostate cancer and to assess the effect of radical prostatectomy on reducing cancer cell clusters and for prognostication of relapse-free survival, as serum total prostate-specific antigen has limited specificity at 4-10 ng/ml
medicine
-
according to partial AUC-ROC (full-range area under the curve of receiver operating characteristics) analyses, pro/free PSA and pro/free/total ratio may be excellent predictive markers for prostate cancer, allowing unnecessary biopsy to be avoided while maintaining high sensitivity at 90% or 95%, in the PSA range 4-20 ng/mL. Not only pro/free PSA, but also age, findings on digital rectal examination and PSA density are independent parameters for predicting biopsy outcomes
medicine
-
although benign prostatic hyperplasia-associated as single marker or ratio to total PSA does not improve the diagnostic performance of percent free PSA or total PSA, the incorporation of benign prostatic hyperplasia-associated/total PSA into an artificial neural network model increases the specificity compared with percent free PSA by 13% and 17% at 90% and 95% sensitivity, respectively. Thus, automated benign prostatic hyperplasia-associated research assay may improve prostate cancer detection when incorporating this new marker into an artificial neural network
medicine
-
decreases in prostate volume over time and the resultant change in prostate-specific antigen performance characteristics may have contributed a bias toward the detection of high-grade disease in the finasteride arm of the Prostate Cancer Prevention Trial. Performance of prostate specific antigen for the detection of any cancer and high-grade cancer is affected by prostate size: prostate-specific antigen performance is significantly better in men with smaller prostates for both the detection of low-grade and high-grade disease
medicine
-
detection rates of nonpalpable prostate cancer in Korean men do not differ significantly in two groups of patients with a lower and a higher PSA range, thus a lower PSA level (2.5 ng/mL may be a more appropriate cutoff point than 4.0 ng/mL) may be considered as an indication for prostate biopsy
medicine
-
development of a nomogram to predict the probability of clinically significant cancers before biopsy, which is most likely to be useful in the management of patients with moderate to elevated PSA
medicine
-
development of an electrochemical immunosensor for PSA with a self-assembled 4-(2-(4-(acetylthio)phenyl)ethynyl)benzoic acid as a bioreceptor. To enhance the electrochemical activity of PSA detection, poly(amidoamine) dendrimer is linked on the 4-(2-(4-(acetylthio)phenyl)ethynyl)benzoic acid self-assembled monolayer
medicine
-
early detection and treatment of prostate cancer is critical to prognosis, with an initial PSA reading being important to the patients management plan. There is limited evidence that the additional use of prostate-specific antigen velocity compared with a single PSA measurement increases sensitivity and specificity of cancer detection. But PSAV remains a useful practical tool in the management of men with prostate cancer: PSA kinetics are also useful in monitoring men on active surveillance in assessing the status of their disease and the presence of cancer progression
medicine
-
effects of isoflavones and curcumin on PSA production in prostate cells, particularly in combination, may have therapeutic advantages in patients with high PSA level who has negative prostate biopsies. Isoflavones and curcumin may improve the asymptomatic inflammation in prostates with high serum PSA levels
medicine
-
free PSA performs significantly better than total PSA at predicting thresholds of prostate volume: free PSA may be used to estimate prostate volume and can be a useful tool in making therapeutic decisions in Chinese men with benign prostatic hyperplasia
medicine
-
generation of stable hybridomas producing specific monoclonal antibodies of the IgG class against PSA from fusions of splenocytes from immunized mice with myeloma cells, which can be used to develop radioimmunodiagnostic, radioimaging, and immunohistochemistry techniques for the early detection and treatment of prostate cancer
medicine
-
PSA appears to be a useful screening tool for detecting prostate cancers with significant volume
medicine
-
PSA kinetics at the initiation of androgen-deprivation therapy can predict overall survival in patients with metastatic hormone-sensitive prostate cancer
medicine
-
PSA kinetics differ significantly following different radiotherapy methods. A higher radiobiological efficiency of brachytherapy in comparison to external-beam radiotherapy (with a total dose of 70.2 Gy) in respect of normal prostate tissue (lower PSA nadir for patients without biochemical failure) and malignant prostate cells (lower PSA failure rate). PSA bounces occur predominantly in the first three years after treatment, particularly after low-dose-rate-brachytherapy
medicine
-
PSA may serve as a sensitive biomarker of Hsp90 inhibition and may aid in selecting new chemotherapeutics
medicine
-
serum PSA is a very useful biomarker for prostate cancer. PSA at the same time stimulates tumor cell invasion and inhibits the formation of metastatic tumors by inhibiting angiogenesis. High PSA expression in the prostate is associated with low microvessel density, whereas low PSA expression is associated with poor prognosis. PSA is a potential target for prostate cancer treatment and imaging, it may be possible to control tumor angiogenesis and, thus, prostate cancer growth by modulating the proteolytic activity of PSA
medicine
-
urine detection of the PSA activation peptide may represent a clinically sensitive measure of PSA production/secretion and may prove to be a viable alternative/addition to current PSA assays
medicine
-
using changes in PSA-related parameters after antibacterial therapy DELTAPSA, DELTAPSA density, and DELTA free/total PSA improve the prostate cancer detection rate and decrease unnecessary prostate biopsies in patients with asymptomatic prostatitis
medicine
-
analysis of values of serum prostate-specific antigen PSA in American Veterans during the time before their diagnosis of prostate cancer. The values appear to follow an exponential model with respect to time. The model comprises a sum of two exponential functions, one for an early, slowly rising component of PSA and a second for a later, faster rising component. The relative velocity of the slow component is significantly associated with the volume of benign tissue, both the amplitude and relative velocity of the fast component are significantly associated with the volume of tumor. At the time of diagnosis of prostate cancer the level and velocity of PSA reflect the combination of slow and fast components. The model provides insight into how benign and malignant tissues in the prostate determine the dynamics of PSA
medicine
-
development of a water-soluble paclitaxel prodrug that is activated specifically by PSA. epsilon-Maleimidocaproyl-Arg-Ser-Ser-Tyr-Tyr-Ser-Leu-p-aminobenzyloxycarbonyl-paclitaxel is water-soluble and is bound to endogenous and exogenous albumin. The albumin-bound form of the prodrug is cleaved rapidly at the P1-P1' scissile bond releasing the paclitaxel-dipeptide Ser-Leu-p-aminobenzyloxycarbonyl-paclitaxel. Due to the incorporation of a p-aminobenzyloxycarbonyl self-eliminating linker, this dipeptide is rapidly degraded to liberate paclitaxel as a final cleavage product within a few hours in prostate tumour tissue homogenates
medicine
-
evaluation of the use of proPSA, free PSA, and PSA to enhance specificity for detecting overall and high-grade prostate cancer. Study on men in a prospective multi-institutional trial with no history of prostate cancer shows that prostate health index Phi may be useful in prostate cancer screening to reduce unnecessary biopsies in men age over 50 years with PSA values of 2-10 ng/ml and negative digital rectal examination findings, with minimal loss in sensitivity
medicine
-
evaluation of the use of PSA isoforms p2PSA and benign prostatic hyperplasia-associated PSA, BPHA, in prostate cancer predictive value. The p2PSA and Beckman Coulter Prostate Health Index levels differ significantly between men with and without prostate cancer. No difference in BPHA levels is observed. there are significant increases in prostate cancer predictive value and specificity of Beckman Coulter Prostate Health Index and percent free prostate-specific antigen compared to total prostate-specific antigen tPSA and percent free prostate-specific antigen. p2PSA has limited additional value in identifying aggressive prostate cancer
medicine
-
in breast cancer tissue, about 40% of samples express PSA. The immunoexpression of PSA is significantly correlated only with the length of CA polymorphic tandem repeats in the 3'-untranslated region of estrogen receptor beta, genotypes with longer CA repeats being associated with PSA negativity. CAG and TA repeats are not associated with PSA expression
medicine
-
mass spectrometry-based analytical method to measure different glycosylated forms of glycoproteins from complex biological samples by coupling glycopeptide extraction strategy for specific glycosylation with selected reaction monitoring SRM. Using this method, glycosylated and sialylated prostate-specific antigen PSA in prostate cancer and noncancer tissues can be monitored. The relative abundance of glycosylated PSA isoforms is not correlated with total PSA protein levels measured in the same prostate cancer tissue samples by clinical immunoassay. The sialylated PSA is differentially distributed in cancer and noncancer tissues, and elevated in cancer tissues compared to noncancerous tissues
medicine
-
PSA may be involved in a signal transduction-dependent feedback loop, whereby it promotes a more aggressive behavior by human prostate cancer cells. Ligation of prostate cancer cell surface protein GRP78 by its natural ligand, activated alpha2-macroglobulin, results in a 2-3-fold upregulation in the synthesis of PSA. The PSA is secreted into the medium as an active proteinase, where it binds to native alpha2-macroglobulin. The resultant alpha2-macroglobulin-PSA complexes bind to GRP78, causing a 1.5-2fold increase in the activation of MEK1/2, ERK1/2, S6K, and Akt, which is coupled with a 2-3-fold increase in DNA and protein synthesis
medicine
-
with prostate specific antigen included in progression criteria, prostate specific antigen at confirmatory biopsy and positive confirmatory biopsy are independent predictors of progression. When prostate specific antigen is excluded from progression criteria, 2- and 5-year progression-free probability is 91% and 76%, respectively. Prostate specific antigen greater than 10 ng/ml was excluded as a criterion
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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.
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Homo sapiens
brenda
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Human kallikrein hK2 has low kininogenase activity while prostate-specific antigen (hK3) has none
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Homo sapiens
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Homo sapiens
brenda
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Homo sapiens
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Design of new and sensitive fluorogenic substrates for human kallikrein hK3 (prostate-specific antigen) derived from semenogelin sequences
Biochim. Biophys. Acta
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Homo sapiens
brenda
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brenda
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2005
Homo sapiens
brenda
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Fast and novel purification method to obtain the prostate specific antigen (PSA) from human seminal plasma
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Homo sapiens
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Novel splice variants of prostate-specific antigen and applications in diagnosis of prostate cancer
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Homo sapiens
brenda
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Homo sapiens
brenda
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Expression and purification of recombinant active prostate-specific antigen from Escherichia coli
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Homo sapiens (P07288), Homo sapiens
brenda
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Crystal structure of a ternary complex between human prostate-specific antigen, its substrate acyl intermediate and an activating antibody
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Homo sapiens
brenda
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Homo sapiens
brenda
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Mechanistic insights into the inhibition of prostate specific antigen by beta-lactam class compounds
Proteins
70
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2008
Homo sapiens
brenda
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Prostate specific antigen: one out of five disulfide bridges determines inactivation by reduction
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Homo sapiens (P07288)
brenda
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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
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Homo sapiens
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Homo sapiens
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Homo sapiens
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Novel small molecule inhibitors for prostate-specific antigen
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Homo sapiens
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Homo sapiens
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Homo sapiens
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Homo sapiens
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Time to prostate-specific antigen nadir independently predicts overall survival in patients who have metastatic hormone-sensitive prostate cancer treated with androgen-deprivation therapy
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Homo sapiens
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Homo sapiens
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Homo sapiens
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Homo sapiens
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Homo sapiens
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Homo sapiens
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Homo sapiens (P07288)
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Homo sapiens
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Homo sapiens
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Molecular insights into substrate specificity of prostate specific antigen through structural modeling
Proteins
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Homo sapiens, Sus scrofa
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Pinkawa, M.; Piroth, M.D.; Holy, R.; Fischedick, K.; Schaar, S.; Borchers, H.; Heidenreich, A.; Eble, M.J.
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Homo sapiens
brenda
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
brenda
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
brenda
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
brenda
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
brenda
Vollmer, R.T.
Dissecting the dynamics of serum prostate-specific antigen
Am. J. Clin. Pathol.
133
187-193
2010
Homo sapiens
brenda
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
brenda
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
brenda
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
brenda
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
brenda
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
brenda
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
brenda
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
brenda
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
brenda
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
brenda
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
brenda
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)
brenda
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)
brenda
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)
brenda
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)
brenda
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)
brenda
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
brenda