Information on EC 3.4.21.77 - semenogelase

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The expected taxonomic range for this enzyme is: Eutheria

EC NUMBER
COMMENTARY
3.4.21.77
-
RECOMMENDED NAME
GeneOntology No.
semenogelase
-
REACTION
REACTION DIAGRAM
COMMENTARY
ORGANISM
UNIPROT
LITERATURE
Preferential cleavage: -Tyr-/-
show the reaction diagram
enzyme contains a serine residue in the substrate binding pocket; enzyme is a serine protease; enzyme shows chymotrypsin-like activity
-
Preferential cleavage: -Tyr-/-
show the reaction diagram
participation of His41, Asp96 and Ser189 in the active site
-
Preferential cleavage: -Tyr-/-
show the reaction diagram
enzyme shows chymotrypsin-like activity
-
Preferential cleavage: -Tyr-/-
show the reaction diagram
cleaves at the C-terminal side of several amino acids residues, like tyrosine, glutamine, histidine, asparic acid, leucine, serine, and asparagine, not at arginine, lysine, phenylalanine, tryptophan, or methionine residues; enzyme shows a substrate specificty different from trypsin, chymotrypsin, and kallikrein 1 and 2
-
Preferential cleavage: -Tyr-/-
show the reaction diagram
enzyme is a serine protease
-
Preferential cleavage: -Tyr-/-
show the reaction diagram
enzyme is a serine protease; enzyme shows chymotrypsin-like activity
-
Preferential cleavage: -Tyr-/-
show the reaction diagram
-
-
-
-
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
hydrolysis of peptide bond
-
-
-
-
SYNONYMS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
7S nerve growth factor gamma chain
-
antigen (human clone lambdaHPSA-1 prostate-specific protein moiety reduced)
-
-
-
-
antigen PSA (human clone 5P1 protein moiety reduced)
-
-
-
-
antigen PSA (human prostate-specific)
-
-
-
-
gamma-NGF
-
gamma-seminoglycoprotein (human protein moiety reduced)
-
-
-
-
gamma-seminoprotein
-
gamma-seminoprotein
-
gamma-SM
-
-
-
-
glandular kallikrein
-
-
-
-
glandular kallikrein 3
-
hK3/PSA
-
exhibits a chymotrypsin-like specificity preferring large hydrophobic or polar residues at the P1 position
kallikrein 3
-
-
-
-
kallikrein 3
-
-
kallikrein-related peptidase 3
-
-
kallikrein-related peptidase 3
-
-
kallikrein-related peptidase-3
-
KLK3
-
-
P-30 antigen
-
-
-
-
prostate specific antigen
-
prostate specific antigen
-
-
prostate stem cell antigen
-
-
prostate-specific antigen
-
-
prostate-specific antigen kallikrein
-
-
Prostate-specific membrane antigen
-
-
PSA
-
-
-
-
PSA
-
-
PSA-SV5
-
-
PSCA
-
-
PSMA
-
-
S01.162
-
-
-
-
seminal proteinase
-
-
seminin
-
-
-
-
six-transmembrane epithelial antigen of the prostate
-
-
STEAP
-
-
tissue kallikrein
-
CAS REGISTRY NUMBER
COMMENTARY
110157-83-0
-
95829-41-7
-
ORGANISM
COMMENTARY
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
2 isozyme of the zymogen with different pI, several isoforms with different pIs of the mature enzyme
-
-
Manually annotated by BRENDA team
American veterans before diagnosis of prostate cancer
-
-
Manually annotated by BRENDA team
enzyme precursor; gene KLK3 or APS
SwissProt
Manually annotated by BRENDA team
isoform prostate specific antigen
-
-
Manually annotated by BRENDA team
isoform tissue kallikrein 4, hK4
-
-
Manually annotated by BRENDA team
enzyme presursor; gene KLK3 or APS; rhesus macaque
SwissProt
Manually annotated by BRENDA team
gene KLK3 or NGFG; glandular kallikrein K3 precursor
SwissProt
Manually annotated by BRENDA team
gene KLK3; glandular kallikrein 3 fragment
SwissProt
Manually annotated by BRENDA team
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
malfunction
-
diminished PSA during acute myocardial infarction and correlation of variation of PSA with coronary lesions and occurrence of major adverse cardiac events. Formation of irreversible PSA complexes (reflected by increased bound PSA) has significant correlation with high-sensitivity C-reactive protein
malfunction
-
recombinant mutant PSA, that lacks enzymatic activity towards a small chromogenic PSA substrate, also exerts antiangiogenic activity. HUVEC tube formation model shows that inactive PSA isoforms do not have antiangiogenic activity. Inhibition of PSA, either by a monoclonal antibody or small molecule inhibitors abolishes the effect of PSA
physiological function
-
risk of prostate cancer increases as PSA, and/or abnormal digital rectal examination increases, but PSA and digital rectal examination are not 100% sensitive for prostate cancer. 16% of cancers are missed by using age-specific PSA and digital rectal examination alone
physiological function
-
in a large-scale cohort of elderly individuals considered healthy and evaluated for a considerable follow-up, the average annual prostate-specific antigen velocity as well as the average fluctuation from the lowest to the highest PSA value are insignificant
physiological function
-
PSA derived from prostate cancer cells can enhance insulin-like growth factor bioavailability in the bone microenvironment of prostate cancer metastasis, thereby permitting prostate cancer survival and malignant progression in the bone microenvironment. Inactive insulin-like growth factor binding protein 5 complex is changed to biologically active insulin-like growth factor through degradation of insulin-like growth factor binding protein 5 by enzymatically active PSA. PSA induces insulin-like growth factor-mediated type I insulin-like growth factor receptor phosphorylation
physiological function
-
role of PSA as a biomarker for prostate cancer, plays an important role in the pathobiology of prostate cancer. In primary cultures of prostatic epithelial cells, PSA activates specifically the small latent form of TGFbeta2. Active PSA can release cytokines involved in bone turnover such as insulin-like growth factor-1 and TGFbeta2. PSA can alter the bone metastatic phenotype from osteoclastic to osteoblastic through PTHrP degradation. Role for active PSA in preferential adhesion of prostate cancer cells to bone. PSA-expressing SaOS-2 cells markedly upregulate expression of genes associated with osteoblast differentiation including runx-2 and osteocalcin. PSA inhibits angiogenesis both in vitro and in vivo. Purified PSA inhibits human umbilical vein endothelial cell proliferation, migration, and invasion. PSA inhibits endothelial cell response to the angiogenic stimulators fibroblast growth factor 2 and vascular endothelial growth factor
physiological function
-
PSA inhibits fibroblast growth factor mediated angiogenesis in a Matrigel plug assay. It can inactivate PTHrP-stimulated cAMP accumulation in mouse osteoblasts
physiological function
-
after treatment with recombinant semenogelin, spermatozoa can be washed and treated with PSA, partially reversing the inhibition of progressive motility
physiological function
-
both increasing patient age and PSA level are significantly correlated with an increased incidence of both all and significant prostate cancers. PSA level in patients with insignificant prostate cancer is not significantly different from that in patients without cancer
physiological function
-
a faster time to reach a PSA nadir after the initiation of androgen-deprivation therapy is associated with shorter survival duration in men with metastatic hormone-sensitive prostate cancer. Association between time to PSA nadir and survival is limited only to patients who have a PSA nadir more than 0.2 ng/ml
physiological function
-
prostate-specific antigen levels between various diagnoses of cancer and size strata have minimal variation. In patients with prostate volumes greater than 50 cm3, prostate-specific antigen density levels have minimal variation between any histologic diagnosis, benign or malignant. The median prostate-specific antigen density levels in men without cancer in small or intermediate prostates (greater than 30 cm3 and 30-50 cm3, respectively) are similar. The prostate-specific antigen density in patients with cancer (low or high grade) is significantly higher in smaller prostates compared with intermediate-sized prostates
physiological function
-
125I-labeled specific monoclonal antibodies demonstrate strong binding to PSA on the surface of LNCaP cells
physiological function
-
increased PSA serum levels during prolonged cardiopulmonary resuscitation, cardiac surgery, extracorporeal cardiopulmonary bypass, cardiogenic shock due to acute myocardial infarction and acute myocardial infarction
physiological function
-
PSA is secreted as an inactive pro-enzyme containing an N-terminal seven amino acid (Ala-Pro-Leu-Ile-Leu-Ser-Arg) activation peptide, which is removed extracellularly in vivo
physiological function
-
in Japanese men, significant cancer is associated with a larger PSA density, PSA density for transition zone and a smaller free-to-total, when compared with indolent cancer. Significant differences of prostate volume and PSA density between indolent cancer and non-cancer
physiological function
-
total PSA significantly correlates with prostate volume in Chinese men with biopsy-proven benign prostatic hyperplasia, but the correlation between free PSA and prostate volume is much stronger. Age does not significantly correlate with PSA, slight associations between age and both prostate volume and free PSA
physiological function
-
in mice bearing xenograft tumors, 68% of the immunoreactive PSA occurrs in complex. After 18 h most of PSA added to mouse and human serum is also complexed: and when added to mouse serum, over 70% of PSA forms complexes that comprises alpha2-macroglobulin and members of the alpha1-antitrypsin family. The complex formation of PSA produced by xenograft tumor models in mice is similar to that of human prostate tumors with respect to the complexation of PSA. Circulating levels of PSA in mice bearing LNCaP and 22RV1 xenograft tumors correlate with tumor volume: concentration of total and free PSA decreases rapidly as a result of complex formation
physiological function
-
PSA bounces are found predominantly in the low-dose-rate-brachytherapy group (42% vs. 23%/20% after high-dose-rate-brachytherapy/external-beam radiotherapy). More patients reach a PSA lower than 0.5 ng/ml after brachytherapy in comparison to external-beam radiotherapy already after 12 months. The percentage increases in the following years, the majority of patients present with a PSA more than 0.2 ng/ml 36 months after brachytherapy
physiological function
-
active PSA exerts chymotrypsin-like enzymatic activity and efficiently digests semenogelins, which leads to liquefaction of the seminal clot. PSA inhibits angiogenesis both in in vitro and in vivo models. The antiangiogenic activity of PSA is related to its enzymatic activity and may be associated with the slow growth of prostate cancer. Purified PSA reduces the fibroblast growth factor 2-stimulated proliferation of HUVECs, bovine adrenal capillary endothelial cells and human microvascular dermal cells, while B16BL6 and human prostate cancer (PC3) cells are unaffected. Angiogenesis inducing cysteine-rich 61 is dramatically down-regulated by PSA in PC-3M and LNCaP prostate cancer cell lines. Inhibitory effect of enzymatically active PSA in seminal fluid is dose-dependent and significant inhibition is observed at a concentration of 0.0001 mM, which is over 10fold lower that found in the extracellular fluid in the prostate. Subcutaneously injected PSA reduces angiogenesis and xenograft tumor growth in mice and subcutaneously administered PSA reduces the metastatic propensity of intravenously injected melanoma cells
physiological function
-
patient group 1 (PSA levels, 2.5-4.0 ng/mL) and patient group 2 (PSA levels, 4.0-10.0 ng/mL) of Korean men with normal digital rectal examination and transrectal ultrasonography findings have statistically significant differences in age, prostate volume, and PSA density, but not in prostate cancer detection rates, which are 21.8% in the group 1 and 20.2% in the group 2
physiological function
-
PSA regulates galectin-3 in human semen and may regulate galectin-3 function during prostate cancer progression
physiological function
-
the enzyme is responsible for the advancement of prostate tumor progression
physiological function
-
the main biological function of the enzyme is the liquefaction of the clot formed after ejaculation by cleavage of semenogelins I and II in seminal fluid. The enzyme also cleaves several other substrates, which may explain its putative functions in prostate cancer and its antiangiogenic activity. Analysis of the effect of PSA-degraded protein fragments on angiogenesis by the endothelial cell tube formation model, overview
malfunction
-
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
additional information
-
the enzyme is a chymotrypsin-like serine protease
additional information
-
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
SUBSTRATE
PRODUCT                      
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
LITERATURE
(Substrate)
COMMENTARY
(Product)
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
4-morpholinecarbonyl-HSSKLQ-7-amido-4-methylcoumarin + HO
?
show the reaction diagram
-
a fluorogenic enzyme substrate
-
-
?
4-morpholinecarbonyl-HSSKLQ-AMC + H2O
?
show the reaction diagram
-
-
-
-
?
4-morpholinecarbonyl-SKLQ-7-amido-4-methylcoumarin + H2O
?
show the reaction diagram
-
hydrolysis rate is 29.6 pmol/min per 100 pmol of PSA
-
-
?
4-morpholinecarbonyl-SRKSQQY-7-amido-4-methylcoumarin + H2O
?
show the reaction diagram
-
-
-
-
?
Arg-Pro-Tyr 4-nitroanilide + H2O
Arg-Pro-Tyr + 4-nitroaniline
show the reaction diagram
-
-
-
?
Bovine serum albumin + H2O
?
show the reaction diagram
-
is more readily hydrolysed than casein
-
-
?
casein + H2O
?
show the reaction diagram
-
proteolytic activity at pH 7.5
-
-
?
EHSSKLQ-7-amido-4-methylcoumarin + H2O
EHSSKLQ + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
?
epsilon-maleimidocaproyl-Arg-Ser-Ser-Tyr-Tyr-Ser-Leu-p-aminobenzyloxycarbonyl-paclitaxel + H2O
epsilon-maleimidocaproyl-Arg-Ser-Ser-Tyr-Tyr + Ser-Leu-p-aminobenzyloxycarbonyl-paclitaxel
show the reaction diagram
-
water soluble paclitaxel prodrug that is activated specifically by PSA in prostate tissue and prostate carcinoma
-
?
Fibronectin + H2O
?
show the reaction diagram
-
-
-
-
?
Fibronectin + H2O
?
show the reaction diagram
-
-
-
?
Fibronectin + H2O
?
show the reaction diagram
-
-
-
-
?
Fibronectin + H2O
?
show the reaction diagram
-
enzyme participates in sperm liquefaction by cleaving fibronectin and semenogelins, the major components of the seminal vesicle coagulum after ejaculation
-
-
?
Galectin-3 + H2O
?
show the reaction diagram
-
-
-
-
?
Galectin-3 + H2O
?
show the reaction diagram
-
carbohydrate-binding protein involved in cell adhesion, cell cycle control, immunomodulation, and cancer progression, including prostate cancer
PSA cleaves galactin-3 between residues Y107 and G108 to produce an active, monovalent lectin
-
?
Galectin-3 + H2O
?
show the reaction diagram
-
galectin-3 Tyr-107 is phosphorylated by c-Abl. It can be cleaved at this site by the enzyme after Tyr107, resulting in loss of galectin-3 multivalency while preserving its carbohydrate binding activity
-
-
?
Gelatin + H2O
?
show the reaction diagram
-
-
-
-
?
Gelatin + H2O
?
show the reaction diagram
-
proteolytic activity at pH 7.5
-
-
?
GSAKLQ + H2O
?
show the reaction diagram
-
207.2% relative hydrolysis rate
-
-
?
GSSALQ + H2O
?
show the reaction diagram
-
43.2% relative hydrolysis rate
-
-
?
GSSKLA + H2O
?
show the reaction diagram
-
31.5% relative hydrolysis rate
-
-
?
GSSKLH + H2O
?
show the reaction diagram
-
170.6% relative hydrolysis rate
-
-
?
GSSKLQ + H2O
?
show the reaction diagram
-
100% relative hydrolysis rate
-
-
?
GSSKPQ + H2O
?
show the reaction diagram
-
7.2% relative hydrolysis rate
-
-
?
GSSKYQ + H2O
?
show the reaction diagram
-
256.9% relative hydrolysis rate
-
-
?
GSSSLQ + H2O
?
show the reaction diagram
-
52.6% relative hydrolysis rate
-
-
?
HSSKLQ-7-amido-4-methylcoumarin + H2O
?
show the reaction diagram
-
hydrolysis rate is 62.7 pmol/min per 100 pmol of PSA
-
-
?
HSSKLQ-7-amido-4-methylcoumarin + H2O
HSSKLQ + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
?
HSSKLQ-7-amido-4-trifluoromethyl-coumarin + H2O
?
show the reaction diagram
-
-
-
-
?
IGFBP-3 + H2O
?
show the reaction diagram
-
-
-
-
?
insulin-like growth factor binding protein 5 + H2O
?
show the reaction diagram
-
is degraded by PSA in a dose- and time-dependent manner. Under nonreducing conditions is degraded into two fragments with approximate molecular masses of 20 and 15 kDa. Under reducing conditions, is degraded into 4 distinct fragments with approximate molecular masses of 22 kDa, 21 kDa, 18 kDa and 13 kDa
-
-
?
insulin-like growth factor binding protein-3 + H2O
insulin-like growth factor I + ?
show the reaction diagram
-
i.e. IGF-I
?
insulin-like growth factor binding protein-3 + H2O
insulin-like growth factor-1
show the reaction diagram
-
-
-
?
KGISSQY-7-amino-4-methylcoumarin + H2O
KGISSQY + 7-amino-4-methylcoumarin
show the reaction diagram
-
fluorogenic substrate
-
?
Laminin + H2O
?
show the reaction diagram
-
-
-
-
?
LSEPAELTDAVK + H2O
PAELTDAVK + LSE
show the reaction diagram
-
-
-
?
Lys-Val-Tyr 4-nitroanilide + H2O
Lys-Val-Tyr + 4-nitroaniline
show the reaction diagram
-
-
-
?
Mca-QFYSSNK(epsilon-dinitrophenyl) + H2O
?
show the reaction diagram
-
-
-
-
?
MeO-Suc-Arg-Pro-Tyr-4-nitroanilide + H2O
?
show the reaction diagram
-
a chromogenic substrate
-
-
?
methoxy-succinyl-Arg-Pro-Tyr-4-nitroanilide + H2O
methoxy-succinyl-Arg-Pro-Tyr + 4-nitroaniline
show the reaction diagram
-
chromogenic substrate, i.e. S2586
-
?
morpholinocarbonyl-His-Ser-Ser-Lys-Leu-Gln-7-amido-4-(trifluoromethyl)-coumarin + H2O
?
show the reaction diagram
-
-
-
-
?
morpholinocarbonyl-Lys-Gly-Ile-Ser-Ser-Gln-Tyr-7-amido-4-(trifluoromethyl)-coumarin + H2O
?
show the reaction diagram
-
-
-
-
?
morpholinocarbonyl-Ser-Arg-Lys-Gln-Gln-Tyr-7-amido-4-methylcoumarin + H2O
?
show the reaction diagram
-
-
-
-
?
Mu-SRKSQQY-7-amido-4-methylcoumarin + H2O
Mu-SRKSQQY + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
?
N,N-dimethylated casein + H2O
?
show the reaction diagram
-
-
-
-
?
N-alpha-benzoyl-DL-Arg 4-nitroanilide + H2O
N-alpha-benzoyl-DL-Arg + 4-nitroaniline
show the reaction diagram
-
trypsin-like activity
-
-
N-succinyl-(Ala)3-p-nitroanilide + H2O
?
show the reaction diagram
-
prostate-specific antigen shows limited activity
-
-
?
N-succinyl-Ala-Ala-Pro-Phe-Ala-p-nitroanilide + H2O
?
show the reaction diagram
-
prostate-specific antigen shows limited activity
-
-
?
N-succinyl-Ala-Ala-Pro-Val-p-nitroanilide + H2O
?
show the reaction diagram
-
prostate-specific antigen shows limited activity
-
-
?
N-succinyl-Gly-Pro-Lys-p-nitroanilide + H2O
?
show the reaction diagram
-
prostate-specific antigen activity is 3times higher towards this substrate than towards other synthetic substrates
-
-
?
N-succinyl-L-Ala-L-Ala-L-Pro-L-Phe 4-nitroanilide + H2O
N-succinyl-L-Ala-L-Ala-L-Pro-L-Phe + 4-nitroaniline
show the reaction diagram
-
chymotrypsin-like activity
-
?
nidogen-1 + H2O
?
show the reaction diagram
-
-
-
-
o-aminobenzoyl-ISYQSSSTEEQ ethylene diamine 2,4-dinitrophenyl + H2O
o-aminobenzoyl-ISYQ + SSST + EEQ ethylene diamine 2,4-dinitrophenyl
show the reaction diagram
-
substrate is intramolecularly quenched, 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
show the reaction diagram
-
substrate is intramolecularly quenched, synthetic fluorogenic substrate
-
?
o-aminobenzoyl-NKISYQSSSQ ethylene diamine 2,4-dinitrophenyl + H2O
o-aminobenzoyl-NKISY + Q + SSSQ ethylene diamine 2,4-dinitrophenyl
show the reaction diagram
-
substrate is intramolecularly quenched, synthetic fluorogenic substrate
-
?
o-aminobenzoyl-SSIYSNTEEQ ethylene diamine 2,4-dinitrophenyl + H2O
o-aminobenzoyl-SSIY + SNTEEQ ethylene diamine 2,4-dinitrophenyl
show the reaction diagram
-
substrate is intramolecularly quenched, synthetic fluorogenic substrate, 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
show the reaction diagram
-
substrate is intramolecularly quenched, synthetic fluorogenic substrate, sequence contains ex vivo cleavage sites of semenogelin I
-
?
PFR-7-amido-4-methylcoumarin + H2O
PFR + 7-amino-4-methylcoumarin
show the reaction diagram
-
fluorogenic substrate
-
?
plasminogen + H2O
plasmin + ?
show the reaction diagram
-
-
?
plasminogen + H2O
angiostatin-like fragments
show the reaction diagram
-
-
-
?
polypeptide + H2O
peptides
show the reaction diagram
-
-
-
?
polypeptide + H2O
peptides
show the reaction diagram
-
-
-
?
polypeptide + H2O
peptides
show the reaction diagram
-
-
-
?
polypeptide + H2O
peptides
show the reaction diagram
-
-
-
?
polypeptide + H2O
peptides
show the reaction diagram
-
-
-
?
polypeptide + H2O
peptides
show the reaction diagram
-
-
-
?
polypeptide + H2O
peptides
show the reaction diagram
-
-
-
?
polypeptide + H2O
peptides
show the reaction diagram
-
-
?
polypeptide + H2O
peptides
show the reaction diagram
-
enzyme possibly is involved in the processing of insulin-like growth factor binding protein 3
-
?
polypeptide + H2O
peptides
show the reaction diagram
enzyme possibly is involved in the processing of insulin-like growth factor binding protein 3
-
?
proform of transforming growth factor-beta + H2O
transforming growth factor-beta + ?
show the reaction diagram
-
i.e. IGF-beta
?
PTHrP + H2O
?
show the reaction diagram
-
-
-
-
?
semenogelin + H2O
semenogelin fragments
show the reaction diagram
-
-
-
?
semenogelin + H2O
semenogelin fragments
show the reaction diagram
-
-
-
?
semenogelin + H2O
semenogelin fragments
show the reaction diagram
-
-
-
?
semenogelin + H2O
semenogelin fragments
show the reaction diagram
-
-
-
?
semenogelin + H2O
semenogelin fragments
show the reaction diagram
-
-
-
?
semenogelin + H2O
semenogelin fragments
show the reaction diagram
-
semenogelins I and II
-
?
semenogelin + H2O
semenogelin fragments
show the reaction diagram
semenogelins I and II
-
?
semenogelin + H2O
semenogelin fragments
show the reaction diagram
-
semenogelin I contains 18 cleavage sites, semenogelin II contains 16 cleavage sites
-
?
semenogelin + H2O
semenogelin fractions
show the reaction diagram
-
-
-
?
semenogelin + H2O
semenogelin fractions
show the reaction diagram
-
-
-
?
semenogelin + H2O
semenogelin fractions
show the reaction diagram
-
-
-
?
semenogelin + H2O
semenogelin fractions
show the reaction diagram
-
-
?
semenogelin + H2O
semenogelin fractions
show the reaction diagram
-
enzyme participates in sperm liquefaction by cleaving fibronectin and semenogelins, the major components of the seminal vesicle coagulum after ejaculation
-
?
semenogelin + H2O
semenogelin fractions
show the reaction diagram
-
semenogelins I and II, cleavage results in liquefaction and release of motil spermatozoa
-
?
semenogelin I + H2O
?
show the reaction diagram
-
from human seminal fluid
-
-
?
semenogelin I + H2O
semenogelin fragments
show the reaction diagram
-
-
-
?
semenogelin II + H2O
?
show the reaction diagram
-
from human seminal fluid
-
-
?
semenogelin II + H2O
semenogelin fragments
show the reaction diagram
-
-
-
?
succinyl-AAPF-7-amido-4-methylcoumarin + H2O
succinyl-AAPF + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
?
succinyl-Ala-Ala-Phe-7-amido-4-methylcoumarin + H2O
succinyl-Ala-Ala-Phe + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
?
TGFbeta2 + H2O
activated TGFbeta2
show the reaction diagram
-
-
-
?
urokinase-type plasminogen activator receptor + H2O
?
show the reaction diagram
-
-
cleavage within D1-D2 linker sequence and in its D3 juxtamembrane domain
-
?
methoxysuccinyl-Arg-Pro-Tyr-p-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
additional information
?
-
-
substrate specificity, overview
-
-
-
additional information
?
-
-
enzyme has no kininogenase activity
-
-
-
additional information
?
-
-
no activation of single-chain urokinase, enzyme shows no trypsin-like activity
-
-
-
additional information
?
-
-
enzyme shows no trypsin-like activity, 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, 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
?
-
-
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
-
-
-
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
-
-
-
NATURAL SUBSTRATES
NATURAL PRODUCTS
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
LITERATURE
(Substrate)
COMMENTARY
(Product)
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
Fibronectin + H2O
?
show the reaction diagram
P07288
-
-
-
?
Fibronectin + H2O
?
show the reaction diagram
-
enzyme participates in sperm liquefaction by cleaving fibronectin and semenogelins, the major components of the seminal vesicle coagulum after ejaculation
-
-
?
Galectin-3 + H2O
?
show the reaction diagram
-
carbohydrate-binding protein involved in cell adhesion, cell cycle control, immunomodulation, and cancer progression, including prostate cancer
PSA cleaves galactin-3 between residues Y107 and G108 to produce an active, monovalent lectin
-
?
Galectin-3 + H2O
?
show the reaction diagram
-
galectin-3 Tyr-107 is phosphorylated by c-Abl. It can be cleaved at this site by the enzyme after Tyr107, resulting in loss of galectin-3 multivalency while preserving its carbohydrate binding activity
-
-
?
plasminogen + H2O
plasmin + ?
show the reaction diagram
P07288
-
-
?
polypeptide + H2O
peptides
show the reaction diagram
-
-
-
?
polypeptide + H2O
peptides
show the reaction diagram
-
-
-
?
polypeptide + H2O
peptides
show the reaction diagram
-
-
-
?
polypeptide + H2O
peptides
show the reaction diagram
-
-
-
?
polypeptide + H2O
peptides
show the reaction diagram
-
-
-
?
polypeptide + H2O
peptides
show the reaction diagram
-
-
-
?
polypeptide + H2O
peptides
show the reaction diagram
-
enzyme possibly is involved in the processing of insulin-like growth factor binding protein 3
-
?
polypeptide + H2O
peptides
show the reaction diagram
P07288
enzyme possibly is involved in the processing of insulin-like growth factor binding protein 3
-
?
proform of transforming growth factor-beta + H2O
transforming growth factor-beta + ?
show the reaction diagram
P07288
-
i.e. IGF-beta
?
semenogelin + H2O
semenogelin fractions
show the reaction diagram
-
-
-
?
semenogelin + H2O
semenogelin fractions
show the reaction diagram
-
-
-
?
semenogelin + H2O
semenogelin fractions
show the reaction diagram
P07288
-
-
?
semenogelin + H2O
semenogelin fractions
show the reaction diagram
-
enzyme participates in sperm liquefaction by cleaving fibronectin and semenogelins, the major components of the seminal vesicle coagulum after ejaculation
-
?
semenogelin + H2O
semenogelin fractions
show the reaction diagram
-
semenogelins I and II, cleavage results in liquefaction and release of motil spermatozoa
-
?
semenogelin I + H2O
?
show the reaction diagram
-
from human seminal fluid
-
-
?
insulin-like growth factor binding protein-3 + H2O
insulin-like growth factor I + ?
show the reaction diagram
P07288
-
i.e. IGF-I
?
additional information
?
-
P07288
enzyme is regulated by steroid hormones, it contains 2 androgen-response elements in the proximal PSA promotor, stimulates cell detachment and facilitates tumor spread
-
-
-
additional information
?
-
-
enzyme can be activated by recombinant kallikrein 2
-
-
-
INHIBITORS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
((2R,3R)-3-benzyl-1-(ethylsulfonyl)-4-oxoazetidin-2-yl)methyl benzoate
-
-
((2R,3R)-3-benzyl-4-oxo-1-(phenylsulfonyl)azetidin-2-yl)methyl benzoate
-
-
((2R,3R)-3-benzyl-4-oxo-1-tosylazetidin-2-yl)methyl benzoate
-
-
((2S,3S)-3-benzyl-1-(ethylsulfonyl)-4-oxoazetidin-2-yl)methyl benzoate
-
-
((2S,3S)-3-benzyl-4-oxo-1-(phenylsulfonyl)azetidin-2-yl)methyl benzoate
-
-
((2S,3S)-3-benzyl-4-oxo-1-tosylazetidin-2-yl)methyl benzoate
-
-
(1S)-4-bromo-1-[(3aS,4R,6R,7aR)-3a,5,5-trimethylhexahydro-4,6-methano-1,3,2-benzodioxaborol-2-yl]butan-1-amine
-
-
(2-methoxyphenyl)(3-phenyl-1H-1,2,4-triazol-1-yl)methanone
-
-
(2R,3R)-benzyl 1-(2-(3-(benzyloxycarbonyl)phenyl)acetyl)-3-(4-hydroxybenzyl)-4-oxoazetidine-2-carboxylate
-
-
(2R,3R)-benzyl 1-benzoyl-3-(4-hydroxybenzyl)-4-oxoazetidine-2-carboxylate
-
-
(2R,3R)-benzyl 3-benzyl-1-(2-(3-(benzyloxycarbonyl)phenyl)acetyl)-4-oxoazetidine-2-carboxylate
-
-
(2R,3R)-ethyl 3-benzyl-4-oxo-1-tosylazetidine-2-carboxylate
-
-
(2S,3S)-benzyl 1-(2-(3-(benzyloxycarbonyl)phenyl)acetyl)-3-(4-hydroxybenzyl)-4-oxoazetidine-2-carboxylate
-
-
(2S,3S)-benzyl 1-benzoyl-3-(4-hydroxybenzyl)-4-oxoazetidine-2-carboxylate
-
-
(2S,3S)-benzyl 3-benzyl-1-(2-(3-(benzyloxycarbonyl)phenyl)acetyl)-4-oxoazetidine-2-carboxylate
-
-
(2S,3S)-ethyl 3-benzyl-4-oxo-1-tosylazetidine-2-carboxylate
-
-
(3,4-dimethoxyphenyl)(5-(4-fluorobenzylamino)-3-phenyl-1H-1,2,4-triazol-1-yl)methanone
-
-
(3-benzyl-1-(ethylsulfonyl)-4-oxoazetidin-2-yl)methyl benzoate
-
-
(3-benzyl-4-oxo-1-tosylazetidin-2-yl)methyl benzoate
-
-
(3aR,4R,6R,7aS)-2-[(1R)-1-amino-2-phenylethyl]-5,5-dimethyltetrahydro-4,6-methano-1,3,2-benzodioxaborol-3a(4H)-ol
-
-
(4-[[([(2S,3S)-3-benzyl-1-[(3-carboxyphenyl)acetyl]-4-oxoazetidin-2-yl]carbonyl)oxy]methyl]phenyl)methanaminium trifluoroacetate
-
-
(5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(2-chlorophenyl)methanone
-
-
(5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(2-methoxyphenyl)methanone
-
-
(5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(3,4-dimethoxyphenyl)methanone
-
360 nanomol inhibits by 83%
(5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(4-chlorophenyl)methanone
-
-
(5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(4-fluorophenyl)methanone
-
-
(5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(4-methoxyphenyl)methanone
-
360 nanomol inhibits by 56%
(5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(4-nitrophenyl)methanone
-
-
(5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(p-tolyl)methanone
-
-
(5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(phenyl)methanone
-
-
(5-amino-3-phenyl-1H-1,2,4-triazol-1-yl)(3,4-dimethoxyphenyl)methanone
-
-
(6-[bis[(pyridin-2-yl-kappaN)methyl]amino-kappaN]hexanoyl)(tricarbonyl)rhenium(3+)-Ser-Ser-Gln-Nle-Leu-B(OH)2
-
-
1-(3-chlorobenzyl)-3-phenyl-1H-pyrazol-5-amine
-
-
1-benzyl-3-phenyl-1H-pyrazol-5-amine
-
-
2-(2-methyl-3-nitrophenyl)-4-oxo-4H-3,1-benzoxazin-6-yl acetate
-
-
2-(2-methyl-3-nitrophenyl)-4H-3,1-benzoxazin-4-one
-
360 nanomol inhibits by 61%
2-(2-methylphenyl)-4H-3,1-benzoxazin-4-one
-
-
2-(2-nitrophenyl)-4H-3,1-benzoxazin-4-one
-
-
2-(3-methylphenyl)-4H-3,1-benzoxazin-4-one
-
-
2-(3-nitrophenyl)-4H-3,1-benzoxazin-4-one
-
-
2-(4-bromophenyl)quinazolin-4(3H)-one
-
-
2-(4-methylphenyl)-4H-3,1-benzoxazin-4-one
-
-
2-mercaptoethanol
-
incubation with 3 mM for 30 min at 25C, in 0.1 ml 0.1 M Tris buffer, pH 7.8, causes 84% loss of activity
2-phenyl-4H-3,1-benzoxazin-4-one
-
-
2-phenylquinazolin-4(3H)-one
-
-
2-[(3S)-3-[[N-(6-aminohexanoyl)-L-phenylalanyl]amino]-4-hydroxy-2-oxobutyl]-N1-[(2S)-1-([(1S)-4-bromo-1-[(3aR,4S,6S,7R,7aS)-5,5,7-trimethylhexahydro-4,6-methano-1,3,2-benzodioxaborol-2-yl]butyl]amino)-1-oxohexan-2-yl]pentanediamide
-
-
3-(2-((2R,3R)-3-benzyl-2-((4-carboxybenzyloxy)carbonyl)-4-oxoazetidin-1-yl)-2-oxoethyl)benzoic acid
-
-
3-(2-((2S,3S)-3-benzyl-2-((4-carboxybenzyloxy)carbonyl)-4-oxoazetidin-1-yl)-2-oxoethyl)benzoic acid
-
-
3-(2-(3-benzyl-2-((4-carboxybenzyloxy)carbonyl)-4-oxoazetidin-1-yl)-2-oxoethyl)benzoic acid
-
-
4-(((2R,3R)-1-(2-(3-(benzyloxycarbonyl)phenyl)acetyl)-3-(4-hydroxybenzyl)-4-oxoazetidine-2-carbonyloxy)methyl)benzoic acid
-
-
4-(((2R,3R)-3-benzyl-1-(2-(3-((4-carboxybenzyloxy)carbonyl)phenyl)acetyl)-4-oxoazetidine-2-carbonyloxy)methyl)benzoic acid
-
-
4-(((2R,3R)-3-benzyl-1-(2-(3-(benzyloxycarbonyl)phenyl)acetyl)-4-oxoazetidine-2-carbonyloxy)methyl)benzoic acid
-
-
4-(((2S,3S)-1-(2-(3-(benzyloxycarbonyl)phenyl)acetyl)-3-(4-hydroxybenzyl)-4-oxoazetidine-2-carbonyloxy)methyl)benzoic acid
-
-
4-(((2S,3S)-3-benzyl-1-(2-(3-((4-carboxybenzyloxy)carbonyl)phenyl)acetyl)-4-oxoazetidine-2-carbonyloxy)methyl)benzoic acid
-
-
4-(((2S,3S)-3-benzyl-1-(2-(3-(benzyloxycarbonyl)phenyl)acetyl)-4-oxoazetidine-2-carbonyloxy)methyl)benzoic acid
-
-
4-((1-(2-(3-(benzyloxycarbonyl)phenyl)acetyl)-3-(4-hydroxybenzyl)-4-oxoazetidine-2-carbonyloxy)methyl)benzoic acid
-
-
4-((3-benzyl-1-(2-(3-((4-carboxybenzyloxy)carbonyl)phenyl)acetyl)-4-oxoazetidine-2-carbonyloxy)methyl)benzoic acid
-
-
4-((3-benzyl-1-(2-(3-(benzyloxycarbonyl)phenyl)acetyl)-4-oxoazetidine-2-carbonyloxy)methyl)benzoic acid
-
-
4-(4-oxo-4H-benzo[d][1,3]oxazin-2-yl)phenyl acetate
-
-
4-[([[(2S,3S)-3-benzyl-1-([3-[(benzyloxy)carbonyl]phenyl]acetyl)-4-oxoazetidin-2-yl]carbonyl]oxy)methyl]benzoic acid
-
-
4-[([[(2S,3S)-3-benzyl-4-oxo-1-(phenylacetyl)azetidin-2-yl]carbonyl]oxy)methyl]benzoic acid
-
-
4-[[(3-[2-[(2S,3S)-3-benzyl-2-[[(4-carboxybenzyl)oxy]carbonyl]-4-oxoazetidin-1-yl]-2-oxoethyl]benzoyl)oxy]methyl]benzoic acid
-
-
6-bromo-2-(2-methyl-3-nitrophenyl)-4H-3,1-benzoxazin-4-one
-
-
6-[bis(pyridin-2-ylmethyl)amino]hexanoyl-Ser-Ser-Gln-Nle-Leu-B(OH)2
-
-
alpha1-Antichymotrypsin
-
-
-
alpha1-Antichymotrypsin
-
complex formation
-
alpha1-Antichymotrypsin
-
can block the PSA antiangiogenic effect
-
alpha1-Antichymotrypsin
-
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
-
alpha2-Macroglobulin
-
-
-
Aprotinin
-
-
Aprotinin
-
efficient inhibition
AUY922
-
-
benzyl (2S,3S)-1-([3-[(benzyloxy)carbonyl]phenyl]acetyl)-3-(4-hydroxybenzyl)-4-oxoazetidine-2-carboxylate
-
-
benzyl (2S,3S)-3-benzyl-1-([3-[(benzyloxy)carbonyl]phenyl]acetyl)-4-oxoazetidine-2-carboxylate
-
-
benzyl 1-(2-(3-(benzyloxycarbonyl)phenyl)acetyl)-3-(4-hydroxybenzyl)-4-oxoazetidine-2-carboxylate
-
-
benzyl 1-([3-[(benzyloxy)carbonyl]phenyl]acetyl)-3-(4-hydroxybenzyl)-4-oxoazetidine-2-carboxylate
-
-
benzyl 1-benzoyl-3-(4-hydroxybenzyl)-4-oxoazetidine-2-carboxylate
-
-
benzyl 3-benzyl-1-(2-(3-(benzyloxycarbonyl)phenyl)acetyl)-4-oxoazetidine-2-carboxylate
-
-
benzyl 3-benzyl-4-oxo-1-(phenylsulfonyl)azetidine-2-carboxylate
-
-
Bovine pancreatic trypsin inhibitor
-
efficient inhibition
-
Cbz-Ser-Ser-Gln-Nle-(boro)-Leu
-
attachment of a bulky metal chelating group to the amino terminal of this peptide does not adversely affect PSA inhibition
Cbz-Ser-Ser-Lys-(4-bromo)Phe-Lys-aldehyde
-
-
Cbz-SSKDL-CHO
-
-
Cbz-SSKLL-CHO
-
-
Cbz-SSKPL-CHO
-
-
Cbz-SSKWL-CHO
-
-
Cbz-SSKYL-CHO
-
-
Cd2+
-
competitive to other metal ions
Co2+
-
competitive to other metal ions
Cu2+
-
competitive to other metal ions
dihydrolipoate
-
incubation with 3 mM for 30 min at 25C, in 0.1 ml 0.1 M Tris buffer, pH 7.8, causes 65% loss of activity
diisopropylfluorophosphate
-
-
dithiothreitol
-
incubation with 3 mM for 30 min at 25C, in 0.1 ml 0.1 M Tris buffer, pH 7.8, causes a complete loss of activity. Alterates the molecular structure probably associated with an altered loading of the protein with dodecyl sulfate anions. Inactivation of the enzyme appears to follow an all-or-none reaction. Residues Cys22-Cys157 and Cys191-Cys220 are dithiothreitol-sensitive
EDTA
-
10 mM inhibits at pH 3.5
glutathione
-
incubation with 3 mM for 30 min at 25C, in 0.1 ml 0.1 M Tris buffer, pH 7.8, causes 35% loss of activity
Hg2+
-
-
Hg2+
-
competitive to other metal ions
insulin-like growth factor binding protein 5
-
PSA induced insulin-like growth factor-mediated type I insulin-like growth factor receptor phosphorylation is inhibited by coincubation with insulin-like growth factor binding protein 5
-
iodoacetate
-
3 mM inhibits at pH 7.5 with casein as a substrate and at pH 3.5 with bovine serum albumin as a substrate
L-1-tosylamido-2-phenylethyl chloromethyl ketone
-
-
Leupeptin
-
-
Leupeptin
-
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
PMSF
-
suppresses the insulin-like growth factor binding protein 5 degradation associated with PSA treatment
Pregnancy-zone protein
-
-
-
R/S-diphenyl[N-benzyloxycarbonylamino(4-carbamoylphenyl)methyl]phosphonate
-
-
-
Serum
-
inhibits the mature enzyme
-
Soybean trypsin inhibitor
-
-
-
spermidine
-
-
Tris[2-carboxyethyl] phosphine
-
incubation with 3 mM for 30 min at 25C, in 0.1 ml 0.1 M Tris buffer, pH 7.8, causes 87% loss of activity
Z-Gln-Leu-B(OH)2
-
-
Z-Gln-Nle-H
-
-
Z-KL-H
-
-
Z-KLL-H
-
-
Z-Lys-Leu-B(OH)2
-
-
Z-Lys-Leu-Leu-B(OH)2
-
-
Z-Lys-Leu-Nle-B(OH)2
-
-
Z-Lys-Leu-Nle-H
-
-
Z-Lys-Nle-H
-
-
Z-QL-H
-
-
Z-Ser-(N-Me)Ser-(N2-Me)Lys-(N-Me)Leu-Leu-B(OH)2
-
-
Z-Ser-(N-Me)Ser-Lys-(N-Me)Leu-Leu-B(OH)2
-
-
Z-Ser-(N-Me)Ser-Lys-Leu-Leu-B(OH)2
-
-
Z-Ser-Ser-(N2-Me)Lys-Leu-Leu-B(OH)2
-
-
Z-Ser-Ser-Gln-Nle-Leu-B(OH)2
-
-
Z-Ser-Ser-Lys-(N-Me)Leu-Leu-B(OH)2
-
-
Z-Ser-Ser-Lys-Leu-B(OH)2
-
-
Z-Ser-Ser-Lys-Leu-D-Leu-H
-
-
Z-Ser-Ser-Lys-Leu-D-Nle-H
-
-
Z-Ser-Ser-Lys-Leu-Leu-B(OH)2
-
-
Z-Ser-Ser-Lys-Leu-Nle-B(OH)2
-
-
Z-Ser-Ser-Lys-Leu-Nle-H
-
-
Z-Ser-Ser-Lys-Nle-B(OH)2
-
-
Z-Ser-Ser-Lys-Nle-H
-
-
Z-Ser-Ser-Lys-Nle-Leu-B(OH)2
-
-
Z-SKLL-H
-
-
Z-SSKAL-H
-
-
Z-SSKF(4-Br)L-H
-
-
Z-SSKFL-H
-
-
Z-SSKIL-H
-
-
Z-SSKKL-H
-
-
Z-SSKL-H
-
-
Z-SSKLD-H
-
-
Z-SSKLL-H
-
-
Z-SSKML-H
-
-
Z-SSKQL-H
-
-
Z-SSKTL-H
-
-
Z-SSKVL-H
-
-
Z-SSKYL-H
-
-
Z-YL-H
-
-
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+
methylmethane thiosulphonate
-
1 mM completely inhibits with bovine serum albumin as a substrate at pH 3.5
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 25C, 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
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
17-allylamine-17-demethoxygeldanamycin
-
-
androgens
-
upregulation
-
AUY922
-
reduces PSA concentration in a dose-dependent manner (2fold more than insulin-like growth factor-binding protein 2) and is accompanied by androgen receptor decrease
B2-peptide
-
-
-
CVAYCIEHHCWTC
-
-
CVAYCIEHHCWTC
-
with disulfide bridges between cysteines 1-13 and 5-10, stimulates the activity of the enzyme towards small peptide substrates, and also enhances the proteolytic activity towards protein substrates
CVFAHNYDYLVC
-
-
-
CVFAHNYDYLVC
-
stimulates the activity of the enzyme towards small peptide substrates, and also enhances the proteolytic activity towards protein substrates. No activation of the enzyme by the inactive derivative of peptide B2-NH2, CVFAHNADALVC, with a disulfide bridge between cysteines 1-12
-
dihydrotestosterone
-
hormonal treatment of BT-474 cells with dihydrotestosterone (an androgen) for 48 h triggers an increase of prostate-specific antigen concentration in the supernatant of these cells
norgestrel
-
hormonal treatment of BT-474 cells with norgestrel (an androgenic progestin) for 48 h triggers an increase of prostate-specific antigen concentration in the supernatant of these cells
progestins
-
upregulation in breast cancer
insulin-like growth factor-binding protein 2
-
-
-
additional information
-
inactive proPSA enzyme can be activated by recombinant kallikrein 2 to the mature form
-
additional information
-
monoclonal antibody 8G8F5 enhances enzymatic activity. It recognizes an epitope composed of five discontinuous segments including residues from the kallikrein loop and stabilizes PSA in an open and active conformation that accelerates catalysis
-
additional information
-
rate of PSA increase is related to the aggressiveness of the prostate cancer and associated with clinical stage, biopsy grade and initial PSA
-
additional information
-
serum PSA also increases with benign prostatic hypertrophy, prostatitis, prostate trauma and drugs
-
additional information
-
PSA is produced at high levels by both androgen-dependent and -independent prostate cancers
-
additional information
-
PSA-alpha1-antichymotrypsin complex is cleared from the blood, but as its concentration increases its clearance mechanism becomes saturated and only then do the PSA-alpha1-antichymotrypsin complexes accumulate in the blood
-
additional information
-
the prostate that produce several proteases can activate proPSA. A peptide that stimulates the activity of PSA enhaces the antiangiogenic effect
-
additional information
-
nidogen-1, galectin-3 or their fragments produced by the enzyme do not have any effect on endothelial cell tube formation
-
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
1.58
4-morpholinecarbonyl-HSSKLQ-7-amido-4-methylcoumarin
-
pH 7.4, 37C
-
1.4
4-morpholinecarbonyl-HSSKLQ-AMC
-
prostate-specific antigen without inhibitor
1.5
4-morpholinecarbonyl-HSSKLQ-AMC
-
prostate-specific antigen and inhibitor 2-(2-methyl-3-nitrophenyl)-4H-3,1-benzoxazin-4-one (25 micromol)
1.6
4-morpholinecarbonyl-HSSKLQ-AMC
-
prostate-specific antigen and inhibitor 2-(2-methyl-3-nitrophenyl)-4H-3,1-benzoxazin-4-one (5 micromol)
2.6
4-morpholinecarbonyl-HSSKLQ-AMC
-
prostate-specific antigen and inhibitor (5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(4-methoxyphenyl)methanone (5 micromol)
4.2
4-morpholinecarbonyl-HSSKLQ-AMC
-
prostate-specific antigen and inhibitor (5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(3,4-dimethoxyphenyl)methanone (5 micromol)
0.14
4-morpholinecarbonyl-SRKSQQY-7-amido-4-methylcoumarin
-
in 50 mM Tris buffer, 0.1 M NaCl, pH 7.8
1.7
Arg-Pro-Tyr 4-nitroanilide
-
-
0.47
HSSKLQ-7-amido-4-methylcoumarin
-
-
1.3
Lys-Val-Tyr 4-nitroanilide
-
-
0.077
Mca-QFYSSNK(epsilon-dinitrophenyl)
-
-
5.72
MeO-Suc-Arg-Pro-Tyr-4-nitroanilide
-
pH 7.4, 37C
-
15.3
N-succinyl-L-Ala-L-Ala-L-Pro-L-Phe 4-nitroanilide
-
-
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.19
4-morpholinecarbonyl-HSSKLQ-7-amido-4-methylcoumarin
Homo sapiens
-
pH 7.4, 37C
-
0.028
Arg-Pro-Tyr 4-nitroanilide
Homo sapiens
-
-
0.022
Lys-Val-Tyr 4-nitroanilide
Homo sapiens
-
-
0.75
MeO-Suc-Arg-Pro-Tyr-4-nitroanilide
Homo sapiens
-
pH 7.4, 37C
-
0.075
N-succinyl-L-Ala-L-Ala-L-Pro-L-Phe 4-nitroanilide
Homo sapiens
-
-
kcat/KM VALUE [1/mMs-1]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.122
4-morpholinecarbonyl-HSSKLQ-7-amido-4-methylcoumarin
Homo sapiens
-
pH 7.4, 37C
202426
23000
HSSKLQ-7-amido-4-methylcoumarin
Homo sapiens
-
-
40604
3900
Mca-QFYSSNK(epsilon-dinitrophenyl)
Homo sapiens
-
-
81549
0.133
MeO-Suc-Arg-Pro-Tyr-4-nitroanilide
Homo sapiens
-
pH 7.4, 37C
173724
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.00134
(4-[[([(2S,3S)-3-benzyl-1-[(3-carboxyphenyl)acetyl]-4-oxoazetidin-2-yl]carbonyl)oxy]methyl]phenyl)methanaminium trifluoroacetate
-
-
0.0284
(6-[bis[(pyridin-2-yl-kappaN)methyl]amino-kappaN]hexanoyl)(tricarbonyl)rhenium(3+)-Ser-Ser-Gln-Nle-Leu-B(OH)2
-
-
0.00898
4-[([[(2S,3S)-3-benzyl-1-([3-[(benzyloxy)carbonyl]phenyl]acetyl)-4-oxoazetidin-2-yl]carbonyl]oxy)methyl]benzoic acid
-
-
0.0243
4-[([[(2S,3S)-3-benzyl-4-oxo-1-(phenylacetyl)azetidin-2-yl]carbonyl]oxy)methyl]benzoic acid
-
-
0.00584
4-[[(3-[2-[(2S,3S)-3-benzyl-2-[[(4-carboxybenzyl)oxy]carbonyl]-4-oxoazetidin-1-yl]-2-oxoethyl]benzoyl)oxy]methyl]benzoic acid
-
-
0.0156
6-[bis(pyridin-2-ylmethyl)amino]hexanoyl-Ser-Ser-Gln-Nle-Leu-B(OH)2
-
-
0.000226
benzyl (2S,3S)-1-([3-[(benzyloxy)carbonyl]phenyl]acetyl)-3-(4-hydroxybenzyl)-4-oxoazetidine-2-carboxylate
-
-
0.00143
benzyl (2S,3S)-3-benzyl-1-([3-[(benzyloxy)carbonyl]phenyl]acetyl)-4-oxoazetidine-2-carboxylate
-
-
0.000348
benzyl 1-([3-[(benzyloxy)carbonyl]phenyl]acetyl)-3-(4-hydroxybenzyl)-4-oxoazetidine-2-carboxylate
-
-
0.000025
Cbz-Ser-Ser-Gln-Nle-(boro)-Leu
-
-
0.5
Cbz-Ser-Ser-Lys-(4-bromo)Phe-Lys-aldehyde
-
in 50 mM Tris buffer, 100 mM NaCl, pH 7.8, 10% DMSO
1
Cbz-SSKDL-CHO
-
in 50 mM Tris buffer, 100 mM NaCl, pH 7.8, 10% DMSO
0.00651
Cbz-SSKLL-CHO
-
in 50 mM Tris buffer, 100 mM NaCl, pH 7.8, 10% DMSO
0.5
Cbz-SSKPL-CHO
-
in 50 mM Tris buffer, 100 mM NaCl, pH 7.8, 10% DMSO
0.1553
Cbz-SSKWL-CHO
-
in 50 mM Tris buffer, 100 mM NaCl, pH 7.8, 10% DMSO
0.01309
Cbz-SSKYL-CHO
-
in 50 mM Tris buffer, 100 mM NaCl, pH 7.8, 10% DMSO
0.0253
morpholinocarbonyl-Ser-Ser-Gln-Nle-Leu-B(OH)2
-
-
0.0131
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-3-cyclohexyl-L-alanyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-norleucinamide
-
-
0.5
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-alanyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-norleucinamide
-
-
1
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-alpha-aspartyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-norleucinamide
-
-
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
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
-
-
0.00984
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
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
-
-
0.05
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-lysinamide
-
-
0.0137
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-methioninamide
-
-
0.0036
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-norleucinamide
-
-
0.0044
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-norvalinamide
-
-
0.0119
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-phenylalaninamide
-
-
0.5
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-prolinamide
-
-
0.05
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-serinamide
-
-
0.1
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-threoninamide
-
-
0.0131
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-tyrosinamide
-
-
0.05
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-valinamide
-
-
1
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]glycinamide
-
-
0.00253
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-5-(dimethylamino)-1,5-dioxopentan-2-yl]-L-leucinamide
-
-
0.04521
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-5-amino-1,5-dioxopentan-2-yl]-L-leucinamide
-
-
0.0419
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N1-[(2S)-4-methyl-1-oxopentan-2-yl]-L-aspartamide
-
-
0.0218
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N1-[(2S)-4-methyl-1-oxopentan-2-yl]-L-glutamamide
-
-
0.05
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-S-tert-butyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-cysteinamide
-
-
0.0075
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-methionyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-norleucinamide
-
-
1
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-prolyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-norleucinamide
-
-
0.0199
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-seryl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-norleucinamide
-
-
0.0438
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-threonyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-norleucinamide
-
-
0.05
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-N-[(1S)-2-[[(2S)-4-methyl-1-oxopentan-2-yl]amino]-2-oxo-1-phenylethyl]-L-lysinamide
-
-
0.0128
N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-N-[(2S)-1-[[(2S)-4-methyl-1-oxopentan-2-yl]amino]-4-(methylsulfinyl)-1-oxobutan-2-yl]-L-lysinamide
-
-
1
N-[(benzyloxy)carbonyl]-L-seryl-L-serylglycyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-norleucinamide
-
-
0.0259
N-[(benzyloxy)carbonyl]-L-seryl-N-[(2S)-1-[[(2S)-1-[[(2S)-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-(methylsulfinyl)-1-oxobutan-2-yl]-L-serinamide
-
-
0.000072
N2-[(5S)-5-[[N-(6-aminohexanoyl)-L-alanyl]amino]-2-(3-amino-3-oxopropyl)-6-hydroxy-4-oxohexanoyl]-N-[(1S)-1-(dihydroxyboranyl)-2-phenylethyl]-L-norleucinamide
-
pH 7.8, 37C
0.2652
Z-Gln-Leu-B(OH)2
-
-
1
Z-Gln-Nle-H
-
-
1
Z-KL-H
-
-
0.1
Z-KLL-H
-
-
0.3535
Z-Lys-Leu-B(OH)2
-
-
0.00598
Z-Lys-Leu-Leu-B(OH)2
-
-
0.02357
Z-Lys-Leu-Nle-B(OH)2
-
-
0.4141
Z-Lys-Leu-Nle-H
-
-
1
Z-Lys-Nle-H
-
-
1
Z-QL-H
-
-
0.05
Z-Ser-(N-Me)Ser-(N2-Me)Lys-(N-Me)Leu-Leu-B(OH)2
-
-
0.0056
Z-Ser-(N-Me)Ser-Lys-(N-Me)Leu-Leu-B(OH)2
-
-
0.0002
Z-Ser-(N-Me)Ser-Lys-Leu-Leu-B(OH)2
-
-
0.0199
Z-Ser-Ser-(N2-Me)Lys-Leu-Leu-B(OH)2
-
-
0.0275
Z-Ser-Ser-Gln-Nle-Leu-B(OH)2
-
-
0.0025
Z-Ser-Ser-Lys-(N-Me)Leu-Leu-B(OH)2
-
-
0.01849
Z-Ser-Ser-Lys-Leu-B(OH)2
-
-
1
Z-Ser-Ser-Lys-Leu-D-Leu-H
-
-
1
Z-Ser-Ser-Lys-Leu-D-Nle-H
-
-
0.000065
Z-Ser-Ser-Lys-Leu-Leu-B(OH)2
-
-
0.000398
Z-Ser-Ser-Lys-Leu-Nle-B(OH)2
-
-
0.01124
Z-Ser-Ser-Lys-Leu-Nle-H
-
-
0.03421
Z-Ser-Ser-Lys-Nle-B(OH)2
-
-
1
Z-Ser-Ser-Lys-Nle-H
-
-
0.0484
Z-Ser-Ser-Lys-Nle-Leu-B(OH)2
-
-
0.04243
Z-SKLL-H
-
-
0.1
Z-SSKAL-H
-
-
0.5
Z-SSKF(4-Br)L-H
-
-
0.0119
Z-SSKFL-H
-
-
0.03743
Z-SSKIL-H
-
-
0.05785
Z-SSKKL-H
-
-
1
Z-SSKL-H
-
-
1
Z-SSKLD-H
-
-
0.0065
Z-SSKLL-H
-
-
0.0137
Z-SSKML-H
-
-
0.02179
Z-SSKQL-H
-
-
0.1
Z-SSKTL-H
-
-
0.07071
Z-SSKVL-H
-
-
0.0139
Z-SSKYL-H
-
-
0.5
Z-YL-H
-
-
0.0056
Zn2+
-
pH 8.0, 37C, with methoxy-succinyl-Arg-Pro-Tyr-4-nitrophenyl
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.08
(2-methoxyphenyl)(3-phenyl-1H-1,2,4-triazol-1-yl)methanone
Homo sapiens
-
-
0.1
(2R,3R)-ethyl 3-benzyl-4-oxo-1-tosylazetidine-2-carboxylate
Homo sapiens
-
-
0.0011
(2S,3S)-ethyl 3-benzyl-4-oxo-1-tosylazetidine-2-carboxylate
Homo sapiens
-
-
0.08
(3,4-dimethoxyphenyl)(5-(4-fluorobenzylamino)-3-phenyl-1H-1,2,4-triazol-1-yl)methanone
Homo sapiens
-
-
0.0022
(3-benzyl-1-(ethylsulfonyl)-4-oxoazetidin-2-yl)methyl benzoate
Homo sapiens
-
-
0.0163
(5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(2-chlorophenyl)methanone
Homo sapiens
-
-
0.0298
(5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(2-methoxyphenyl)methanone
Homo sapiens
-
-
0.0005
(5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(3,4-dimethoxyphenyl)methanone
Homo sapiens
-
-
0.0022
(5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(4-chlorophenyl)methanone
Homo sapiens
-
-
0.0041
(5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(4-fluorophenyl)methanone
Homo sapiens
-
-
0.0009
(5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(4-methoxyphenyl)methanone
Homo sapiens
-
-
0.08
(5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(4-nitrophenyl)methanone
Homo sapiens
-
-
0.0038
(5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(p-tolyl)methanone
Homo sapiens
-
-
0.0096
(5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(phenyl)methanone
Homo sapiens
-
-
0.0169
(5-amino-3-phenyl-1H-1,2,4-triazol-1-yl)(3,4-dimethoxyphenyl)methanone
Homo sapiens
-
-
0.08
1-(3-chlorobenzyl)-3-phenyl-1H-pyrazol-5-amine
Homo sapiens
-
-
0.08
1-benzyl-3-phenyl-1H-pyrazol-5-amine
Homo sapiens
-
-
0.0054
2-(2-methyl-3-nitrophenyl)-4-oxo-4H-3,1-benzoxazin-6-yl acetate
Homo sapiens
-
-
0.0003
2-(2-methyl-3-nitrophenyl)-4H-3,1-benzoxazin-4-one
Homo sapiens
-
-
0.0291
2-(2-methylphenyl)-4H-3,1-benzoxazin-4-one
Homo sapiens
-
-
0.0142
2-(2-nitrophenyl)-4H-3,1-benzoxazin-4-one
Homo sapiens
-
-
0.08
2-(3-methylphenyl)-4H-3,1-benzoxazin-4-one
Homo sapiens
-
-
0.08
2-(3-nitrophenyl)-4H-3,1-benzoxazin-4-one
Homo sapiens
-
-
0.08
2-(4-bromophenyl)quinazolin-4(3H)-one
Homo sapiens
-
-
0.08
2-(4-methylphenyl)-4H-3,1-benzoxazin-4-one
Homo sapiens
-
-
0.08
2-phenyl-4H-3,1-benzoxazin-4-one
Homo sapiens
-
-
0.08
2-phenylquinazolin-4(3H)-one
Homo sapiens
-
-
0.0035
4-((1-(2-(3-(benzyloxycarbonyl)phenyl)acetyl)-3-(4-hydroxybenzyl)-4-oxoazetidine-2-carbonyloxy)methyl)benzoic acid
Homo sapiens
-
-
0.0058
4-((3-benzyl-1-(2-(3-((4-carboxybenzyloxy)carbonyl)phenyl)acetyl)-4-oxoazetidine-2-carbonyloxy)methyl)benzoic acid
Homo sapiens
-
-
0.009
4-((3-benzyl-1-(2-(3-(benzyloxycarbonyl)phenyl)acetyl)-4-oxoazetidine-2-carbonyloxy)methyl)benzoic acid
Homo sapiens
-
-
0.08
4-(4-oxo-4H-benzo[d][1,3]oxazin-2-yl)phenyl acetate
Homo sapiens
-
-
0.049
6-bromo-2-(2-methyl-3-nitrophenyl)-4H-3,1-benzoxazin-4-one
Homo sapiens
-
-
0.000001
AUY922
Homo sapiens
-
-
0.00034
benzyl 1-(2-(3-(benzyloxycarbonyl)phenyl)acetyl)-3-(4-hydroxybenzyl)-4-oxoazetidine-2-carboxylate
Homo sapiens
-
-
0.01
benzyl 1-benzoyl-3-(4-hydroxybenzyl)-4-oxoazetidine-2-carboxylate
Homo sapiens
-
-
0.00143
benzyl 3-benzyl-1-(2-(3-(benzyloxycarbonyl)phenyl)acetyl)-4-oxoazetidine-2-carboxylate
Homo sapiens
-
-
0.00308
benzyl 3-benzyl-4-oxo-1-(phenylsulfonyl)azetidine-2-carboxylate
Homo sapiens
-
-
0.15
dithiothreitol
Homo sapiens
-
at 25C, in 0.1 ml 0.1 M Tris buffer, pH 7.8
0.00025
R/S-diphenyl[N-benzyloxycarbonylamino(4-carbamoylphenyl)methyl]phosphonate
Homo sapiens
-
pH and temperature not specified in the publication
-
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
0.004
-
purified recombinant active PSA
additional information
-
-
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
3.5
-
bovine serum albumin is degraded 3-4times faster at pH 3.5 than at pH 7.5
7.4
-
assay at
7.8
-
assay at
8
-
substrate N,N-dimethylated casein
8
-
assay at
8.3
-
assay at
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
pI VALUE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
6.4
-
several isozymes of active mature enzyme
8.2
-
2 enzyme proforms with different pI: pH 8.2 and pH 8.4
8.4
-
2 enzyme proforms with different pI: pH 8.2 and pH 8.4
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
SOURCE
-
prostate cancer cell, expressing GRP78 on its surface
Manually annotated by BRENDA team
-
prostate-specific antigen is absent in the blood of healthy subjects. Low frequency of positive results in patients with prostate cancer and high frequency of positive results in patients with benign prostatic hyperplasia
Manually annotated by BRENDA team
-
from patients with prostate diseases
Manually annotated by BRENDA team
-
kallikrein-related peptidase 3 is present in hippocampal pyramidal neurons
Manually annotated by BRENDA team
-
surgical specimens from female patients with breast cancer
Manually annotated by BRENDA team
-
breast carcinoma cell line, enzyme is upregulated by progestins and androgens
Manually annotated by BRENDA team
-
minute amounts
Manually annotated by BRENDA team
-
prostate cancer cell, expressing GRP78 on its surface
Manually annotated by BRENDA team
-
secretory epithelial cells, concentration of enzyme in nonprostatic tissue represents less than 1% of the amount in normal prostate
Manually annotated by BRENDA team
-
Paneth cells, pronounced expression of enzyme
Manually annotated by BRENDA team
-
prostate cancer cell, no expression of GRP78 on the surface
Manually annotated by BRENDA team
-
highest expression level
Manually annotated by BRENDA team
-
and prostate cancer tissue
Manually annotated by BRENDA team
-
the enzyme forms complexes with alpha1-antichymotrypsin in prostate
Manually annotated by BRENDA team
-
metastatic prostate adenocarcinoma cell line LNCaP; upregulation of gene expression by androgens
Manually annotated by BRENDA team
-
metastatic prostate adenocarcinoma cell line LNCaP; produces equal amounts of zymogen proPSA and one-chain mature enzyme form, no intermediate forms; very low content of free enzyme
Manually annotated by BRENDA team
-
like normal prostate secretory-luminal epithelial cells, produces very high levels of PSA. High levels of active PSA in the milieu surrounding osseous and soft tissue metastases
Manually annotated by BRENDA team
-
PC3 cell, elevated levels of PSA
Manually annotated by BRENDA team
-
the enzyme forms complexes with alpha1-antichymotrypsin in prostate
Manually annotated by BRENDA team
-
concentration of enzyme in nonprostatic tissue represents less than 1% of the amount in normal prostate
Manually annotated by BRENDA team
-
predominantly exists in free form in seminal plasma
Manually annotated by BRENDA team
-
enzyme is mainly complexed to alpha1-antichymotrypsin, i.e. ACT, a small part of free enzyme
Manually annotated by BRENDA team
-
in the serum of patients with prostate cancer
Manually annotated by BRENDA team
-
prostate cancer patients, serum prostate-specific antigen values range from 0.1 to 700 ng/ml. Prostate-specific antigen absent from female serum
Manually annotated by BRENDA team
-
N-linked glycans from prostate-specific antigen isolated from normal control, benign prostatic disease and prostate cancer. For prostate-specific antigen, 40 putative glycoforms
Manually annotated by BRENDA team
-
white men with a total PSA concentration of 0-10 ng/mL, having prostate cancer or no evidence of malignancy, but in great part with benign prostatic hyperplasia
Manually annotated by BRENDA team
-
breast carcinoma cell line, enzyme is upregulated by progestins and androgens
Manually annotated by BRENDA team
-
activation peptide of PSA is filtered from the bloodstream by the kidney, and is detectable in the urine of patients with prostate cancer, but not controls. Serum PSA concentration is dependent on how much PSA gains access to the bloodstream and how efficiently it is removed
Manually annotated by BRENDA team
additional information
-
splice variant PSA-SV5 is absent in normal breast cells and in breast and ovarian cancer cell lines
Manually annotated by BRENDA team
additional information
-
prostate-specific antigen shows low specificity, besides increased levels in prostate cancer, prostate-specific antigen levels are also increased in benign prostatic hyperplasia, and in general inflammatory responses. Shows low sensitivity, prostate-specific antigen levels are highly variable over time, prostate-specific antigen poorly distinguishes indolent from aggressive cancers
Manually annotated by BRENDA team
additional information
-
seminal fluid
Manually annotated by BRENDA team
additional information
-
patients aged more than 75 years and with PSA value lower than 2.0 ng/ml
Manually annotated by BRENDA team
additional information
-
malignant and normal prostate cells
Manually annotated by BRENDA team
additional information
-
different PSA isoforms in seminal fluid, which differ with respect to glycosylation and/or internal cleavages, and enzymatic activity
Manually annotated by BRENDA team
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY
GeneOntology No.
LITERATURE
SOURCE
-
the enzyme is secreted by human prostate tissues
-
Manually annotated by BRENDA team
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
26080
-
calculation from amino acid sequence
647582
26080
-
calculation from nucleotide sequence, unglycosylated protein
647585
26500
-
calculation from amino acid sequence
647583
28000
-
-
710554
28110 - 30000
-
inactive zymogen peak 2, gel filtration, SDS-PAGE and mass spectrometry
647590
28880 - 30000
-
active mature enzyme, gel filtration and mass spectrometry
647590
30000
-
calculated from the amino acid composition of isolated prostate-specific antigen and proteinase
699063
33000
-
Western blot analysis
698334
33000
-
Western blotting of PSA-spiked mouse serum
710463
34000
-
calculated from the elution profile
699063
65000
-
Western blotting of PSA-spiked mouse serum
710463
85000
-
Western blotting of PSA-spiked mouse serum
710463
87000
-
inactive zymogen peak 1, gel filtration
647590
160000
-
Western blotting of PSA-spiked mouse serum
710463
200000
-
Western blotting of PSA-spiked mouse serum
710463
SUBUNITS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
?
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x * 34000, SDS-PAGE
?
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x * 36000, SDS-PAGE, pro-PSA
?
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x * 25000, Western blot analysis and SDS-PAGE. x * 22500-35500, zymographic assay
?
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x * 22000-30000, active enzyme, SDS-PAGE
dimer
-
crystallography
monomer
-
1 * 55000, SDS-PAGE, proPSA, 1 * 54000, SDS-PAGE, active PSA
additional information
-
active mature enzyme consists of only 1 chain
POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
glycoprotein
-
a single N-linked carbohydrate side chain is attached to Asn45; complex structure of the oligosaccharide
glycoprotein
-
an N-linked carbohydrate side chain is predicted at Asp45, and O-linked carbohydrate side chains are possibly attached to Ser69, Thr70 and Ser71
glycoprotein
-
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
proteolytic modification
-
enzyme can be activated by recombinant kallikrein 2
Crystallization/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
PSA in complex with monoclonal antibody 8G8F5 or PSA in complex with both 8G8F5 and the fluorogenic substrate morpholinocarbonyl-Lys-Gly-Ile-Ser-Ser-Gln-Tyr-7-amido-4-(trifluoromethyl)-coumarin, by sitting-drop vapor diffusion, between 2.83-3.33 A resolution. Belongs to space group P41212
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GENERAL STABILITY
ORGANISM
UNIPROT
LITERATURE
stable at 0.5 M urea in the activity assay, which is needed to prevent coagualtion of th semenogelins
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STORAGE STABILITY
ORGANISM
UNIPROT
LITERATURE
4C, Tris-HCl buffer
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Purification/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
by centrifugation and gel filtration
-
by centrifugation, fractional precipitation by ammonium sulphate, ion-exchange chromatography and gel filtration, purified to homogeneity
-
by gel filtration
-
by HPLC
-
by lysozyme, sonication, and centrifugation, His-tagged PSA solublized from inclusion bodies by urea and purified on nickel-chelate resin. GST-fused PSA solublized from inclusion bodies by sarcosyl and purified on glutathione agarose beads
-
by thiophilic absorption chromatography
-
fast purification method with 90% of purity and 50% of recovery
-
free and complexed PSA, by gel filtration and immunoadsorption
-
from LNCaP cell culture medium
-
from seminal plasma
-
native active enzyme from seminal plasma by immunoaffinity chromatography and anion-exchange chromatography
-
nickel-nitrilotriacetic acid-Sepharose column chromatography and benzamidine-Sepharose column chromatography
-
one third of the purified protein is enzymatically inactive, due to carboxy-terminal cleavage of Lys145
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Cloned/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
expressed in Escherichia coli M15(pREP4) cells
-
expressed in HUVEC cells
-
gene hK3 or KLK3, genetic organization and structure of the kallikrein gene family, clustered on chromosome 19q13.3-q13.4
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gene structure
-
male C57BL/6 mice injected with recombinant adenoviruses containing rAd/PSMA, rAd/PSCA and rAd/STEAP
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proPSA and active PSA cDNA cleaved with EcoRI and HindIII and cloned into vector pET28(a)+, expressed in Escherichia coli strain BL21(DE3). Recombinant vector cleaved with EcoRI and XhoI, inserted into vector pGEX4T-1 and expressed in Escherichia coli strain BL21(DE3)
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recombinant proteins of proPSA and active PSA cloned into pGEX4T-1 expression vector that produces recombinant proteins with N-terminal GST tags. The proteins expressed in Escherichia coli BL21(DE3)
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structure of the gene and linkage to the kallikrein-like gene hGK-1
-
EXPRESSION
ORGANISM
UNIPROT
LITERATURE
PSA-specific monoclonal antibodies block proteolysis of extracellular matrix components and decrease invasion of PSA-producing LNCaP cells in Matrigel invasion assays
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at a dose of 0.00001 mM 17-allylamine-17-demethoxygeldanamycin, PSA expression is reduced by 40%. 17-allylamine-17-demethoxygeldanamycin-treated LNCaP cells reveal about 25% inhibition of PSA secretion. Potency of AUY922 to reduce PSA expression at inhibitor concentrations lower than 0.000005 mM (non-toxic at these levels) is greater (8fold) than the potency of 17-allylamine-17-demethoxygeldanamycin. Hsp90 inhibitors target PSA secretion via the androgen receptor pathway
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shRNA mediated knockdown of SNF2-related CBP activator protein results in decreased H2A.Z binding at the enhancer region of the PSA promoter and decreased expression of PSA in prostate cancer cells
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treatment of LNCaP cells with 10 microg/ml soy isoflavones alone causes 40% inhibition of PSA secretion to the supernatant compared to control, whereas treatment of the cells with 20 micromol curcumin causes 20% inhibition. Combined treatment of curcumin and soy isoflavones enhances inhibition of PSA production and expression of androgen receptor in LNCaP cells: treatment with 10 microg/ml isoflavones combined with 20 micromol curcumin causes almost complete inhibition of PSA production. In a randomized, placebo-controlled clinical trial, a combined treatment of soy isoflavones and curcumin decreases serum PSA in those subjects whose baseline PSA is more than 10 ng/ml
-
PSA expression is lower in malignant than in normal prostatic epithelium and it is further reduced in poorly differentiated tumors
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SNF2-related CBP activator protein is a physiologically relevant mediator of PSA expression: it enhances the transcriptional activity of PSA and this activation is further enhanced in the presence of dihydrotestosterone. SNF2-related CBP activator protein activates hormone-dependent transcription of the androgen responsive, PSA-Luciferase reporter gene in prostate cells
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LNCaP and 22RV1 xenograft tumors express PSA
-
inactive proenzyme is produced at high concentrations by epithelial cells of the prostate
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Renatured/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
APPLICATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
analysis
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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
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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
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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
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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
analysis
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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
diagnostics
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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 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 enzyme is the most useful prostate cancer marker
drug development
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compounds inhibiting the activity of prostate-specific antigen, prevent the anti-angiogenic effect of prostate-specific antigen in an angiogenesis model
drug development
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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
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development of PSA selective inhibitors as useful tools for the targeted treatment and imaging of prostate cancer
medicine
-
enzyme is a marker for cancer; used in the diagnosis of prostate cancer
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
-
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
-
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
-
purified active PSA has a potential use in prostate cancer diagnostics and/or therapeutics
medicine
-
important marker for the diagnosis and management of prostate cancer
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
-
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
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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 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
-
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
-
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
-
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
-
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
-
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 may serve as a sensitive biomarker of Hsp90 inhibition and may aid in selecting new chemotherapeutics
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
-
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
-
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
-
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
-
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
-
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
-
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
-
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
-
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
-
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
-
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
-
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
-
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
-
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
-
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
-
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 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
-
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
-
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
-
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
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
additional information
-
human seminal proteinase and prostate-specific antigen are identical