3.4.21.77: semenogelase
This is an abbreviated version!
For detailed information about semenogelase, go to the full flat file.
Word Map on EC 3.4.21.77
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3.4.21.77
-
gleason
-
prostatectomy
-
androgen
-
rectal
-
radiotherapy
-
preoperative
-
hyperplasia
-
transrectal
-
urinary
-
metastases
-
adenocarcinoma
-
lymph
-
node
-
castration-resistant
-
testosterone
-
postoperative
-
ultrasound
-
oncology
-
univariate
-
high-risk
-
urological
-
pelvic
-
beam
-
surveillance
-
progression-free
-
staging
-
high-grade
-
lncap
-
low-risk
-
docetaxel
-
nadir
-
cancer-specific
-
brachytherapy
-
transurethral
-
androgen-independent
-
ultrasound-guided
-
multiparametric
-
neoadjuvant
-
intermediate-risk
-
nomogram
-
suspicious
-
urologist
-
mcrpc
-
antiandrogens
-
ultrasonography
-
lymphadenectomy
-
erectile
-
incontinence
-
actuarial
-
cause-specific
-
analysis
-
medicine
-
diagnostics
-
drug development
- 3.4.21.77
-
gleason
-
prostatectomy
- androgen
- rectal
-
radiotherapy
-
preoperative
- hyperplasia
-
transrectal
- urinary
- metastases
- adenocarcinoma
- lymph
- node
-
castration-resistant
- testosterone
-
postoperative
-
ultrasound
-
oncology
-
univariate
-
high-risk
- urological
-
pelvic
-
beam
-
surveillance
-
progression-free
-
staging
-
high-grade
-
lncap
-
low-risk
- docetaxel
-
nadir
-
cancer-specific
-
brachytherapy
-
transurethral
-
androgen-independent
-
ultrasound-guided
-
multiparametric
-
neoadjuvant
-
intermediate-risk
-
nomogram
-
suspicious
-
urologist
-
mcrpc
-
antiandrogens
-
ultrasonography
-
lymphadenectomy
-
erectile
- incontinence
-
actuarial
-
cause-specific
- analysis
- medicine
- diagnostics
- drug development
Reaction
Preferential cleavage: -Tyr-/- =
Synonyms
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), gama-SM protein, gamma-NGF, gamma-seminoglycoprotein (human protein moiety reduced), gamma-seminoprotein, gamma-SM, GK3, glandular kallikrein, glandular kallikrein 3, hK3/PSA, K3, K4, kallikrein 3, kallikrein-related peptidase 3, kallikrein-related peptidase-3, KLK3, P-30 antigen, prostate specific antigen, prostate stem cell antigen, prostate-specific antigen, prostate-specific antigen kallikrein, Prostate-specific membrane antigen, PSA, PSA-SV5, PSCA, PSMA, S01.162, seminal proteinase, seminin, six-transmembrane epithelial antigen of the prostate, STEAP, tissue kallikrein
ECTree
3.4.21.77 semenogelaseAdvanced search results
results (
results (Inhibitors
Inhibitors on EC 3.4.21.77 - semenogelase
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INHIBITOR 
ORGANISM
UNIPROT
COMMENTARY 
LITERATURE
IMAGE
(1S)-4-bromo-1-[(3aS,4R,6R,7aR)-3a,5,5-trimethylhexahydro-4,6-methano-1,3,2-benzodioxaborol-2-yl]butan-1-amine
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(2R,3R)-benzyl 1-(2-(3-(benzyloxycarbonyl)phenyl)acetyl)-3-(4-hydroxybenzyl)-4-oxoazetidine-2-carboxylate
-
-
(2R,3R)-benzyl 3-benzyl-1-(2-(3-(benzyloxycarbonyl)phenyl)acetyl)-4-oxoazetidine-2-carboxylate
-
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(2S,3S)-benzyl 1-(2-(3-(benzyloxycarbonyl)phenyl)acetyl)-3-(4-hydroxybenzyl)-4-oxoazetidine-2-carboxylate
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(2S,3S)-benzyl 3-benzyl-1-(2-(3-(benzyloxycarbonyl)phenyl)acetyl)-4-oxoazetidine-2-carboxylate
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(3,4-dimethoxyphenyl)(5-(4-fluorobenzylamino)-3-phenyl-1H-1,2,4-triazol-1-yl)methanone
-
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(3aR,4R,6R,7aS)-2-[(1R)-1-amino-2-phenylethyl]-5,5-dimethyltetrahydro-4,6-methano-1,3,2-benzodioxaborol-3a(4H)-ol
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(4-[[([(2S,3S)-3-benzyl-1-[(3-carboxyphenyl)acetyl]-4-oxoazetidin-2-yl]carbonyl)oxy]methyl]phenyl)methanaminium trifluoroacetate
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(5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(3,4-dimethoxyphenyl)methanone
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360 nanomol inhibits by 83%
(5-amino-3-(pyridin-3-yl)-1H-1,2,4-triazol-1-yl)(4-methoxyphenyl)methanone
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360 nanomol inhibits by 56%
(6-[bis[(pyridin-2-yl-kappaN)methyl]amino-kappaN]hexanoyl)(tricarbonyl)rhenium(3+)-Ser-Ser-Gln-Nle-Leu-B(OH)2
-
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2-(2-methyl-3-nitrophenyl)-4H-3,1-benzoxazin-4-one
-
360 nanomol inhibits by 61%
2-mercaptoethanol
incubation with 3 mM for 30 min at 25°C, in 0.1 ml 0.1 M Tris buffer, pH 7.8, causes 84% loss of activity
2-[(3S)-3-[[N-(6-aminohexanoyl)-L-phenylalanyl]amino]-4-hydroxy-2-oxobutyl]-N1-[(2S)-1-([(1S)-4-bromo-1-[(3aR,4S,6S,7R,7aS)-5,5,7-trimethylhexahydro-4,6-methano-1,3,2-benzodioxaborol-2-yl]butyl]amino)-1-oxohexan-2-yl]pentanediamide
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3-(2-((2R,3R)-3-benzyl-2-((4-carboxybenzyloxy)carbonyl)-4-oxoazetidin-1-yl)-2-oxoethyl)benzoic acid
-
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3-(2-((2S,3S)-3-benzyl-2-((4-carboxybenzyloxy)carbonyl)-4-oxoazetidin-1-yl)-2-oxoethyl)benzoic acid
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3-(2-(3-benzyl-2-((4-carboxybenzyloxy)carbonyl)-4-oxoazetidin-1-yl)-2-oxoethyl)benzoic acid
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4-(((2R,3R)-1-(2-(3-(benzyloxycarbonyl)phenyl)acetyl)-3-(4-hydroxybenzyl)-4-oxoazetidine-2-carbonyloxy)methyl)benzoic acid
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4-(((2R,3R)-3-benzyl-1-(2-(3-((4-carboxybenzyloxy)carbonyl)phenyl)acetyl)-4-oxoazetidine-2-carbonyloxy)methyl)benzoic acid
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4-(((2R,3R)-3-benzyl-1-(2-(3-(benzyloxycarbonyl)phenyl)acetyl)-4-oxoazetidine-2-carbonyloxy)methyl)benzoic acid
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4-(((2S,3S)-1-(2-(3-(benzyloxycarbonyl)phenyl)acetyl)-3-(4-hydroxybenzyl)-4-oxoazetidine-2-carbonyloxy)methyl)benzoic acid
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4-(((2S,3S)-3-benzyl-1-(2-(3-((4-carboxybenzyloxy)carbonyl)phenyl)acetyl)-4-oxoazetidine-2-carbonyloxy)methyl)benzoic acid
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4-(((2S,3S)-3-benzyl-1-(2-(3-(benzyloxycarbonyl)phenyl)acetyl)-4-oxoazetidine-2-carbonyloxy)methyl)benzoic acid
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4-((1-(2-(3-(benzyloxycarbonyl)phenyl)acetyl)-3-(4-hydroxybenzyl)-4-oxoazetidine-2-carbonyloxy)methyl)benzoic acid
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4-((3-benzyl-1-(2-(3-((4-carboxybenzyloxy)carbonyl)phenyl)acetyl)-4-oxoazetidine-2-carbonyloxy)methyl)benzoic acid
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4-((3-benzyl-1-(2-(3-(benzyloxycarbonyl)phenyl)acetyl)-4-oxoazetidine-2-carbonyloxy)methyl)benzoic acid
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4-[([[(2S,3S)-3-benzyl-1-([3-[(benzyloxy)carbonyl]phenyl]acetyl)-4-oxoazetidin-2-yl]carbonyl]oxy)methyl]benzoic acid
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4-[([[(2S,3S)-3-benzyl-4-oxo-1-(phenylacetyl)azetidin-2-yl]carbonyl]oxy)methyl]benzoic acid
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4-[[(3-[2-[(2S,3S)-3-benzyl-2-[[(4-carboxybenzyl)oxy]carbonyl]-4-oxoazetidin-1-yl]-2-oxoethyl]benzoyl)oxy]methyl]benzoic acid
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benzyl (2S,3S)-1-([3-[(benzyloxy)carbonyl]phenyl]acetyl)-3-(4-hydroxybenzyl)-4-oxoazetidine-2-carboxylate
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benzyl (2S,3S)-3-benzyl-1-([3-[(benzyloxy)carbonyl]phenyl]acetyl)-4-oxoazetidine-2-carboxylate
-
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benzyl 1-(2-(3-(benzyloxycarbonyl)phenyl)acetyl)-3-(4-hydroxybenzyl)-4-oxoazetidine-2-carboxylate
-
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benzyl 1-([3-[(benzyloxy)carbonyl]phenyl]acetyl)-3-(4-hydroxybenzyl)-4-oxoazetidine-2-carboxylate
-
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benzyl 3-benzyl-1-(2-(3-(benzyloxycarbonyl)phenyl)acetyl)-4-oxoazetidine-2-carboxylate
-
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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
dihydrolipoate
incubation with 3 mM for 30 min at 25°C, in 0.1 ml 0.1 M Tris buffer, pH 7.8, causes 65% loss of activity
dithiothreitol
incubation with 3 mM for 30 min at 25°C, in 0.1 ml 0.1 M Tris buffer, pH 7.8, causes a complete loss of activity. Alterates the molecular structure probably associated with an altered loading of the protein with dodecyl sulfate anions. Inactivation of the enzyme appears to follow an all-or-none reaction. Residues Cys22-Cys157 and Cys191-Cys220 are dithiothreitol-sensitive
glutathione
incubation with 3 mM for 30 min at 25°C, in 0.1 ml 0.1 M Tris buffer, pH 7.8, causes 35% loss of activity
insulin-like growth factor binding protein 5
-
PSA induced insulin-like growth factor-mediated type I insulin-like growth factor receptor phosphorylation is inhibited by coincubation with insulin-like growth factor binding protein 5
-
iodoacetate
-
3 mM inhibits at pH 7.5 with casein as a substrate and at pH 3.5 with bovine serum albumin as a substrate
methylmethane thiosulphonate
-
1 mM completely inhibits with bovine serum albumin as a substrate at pH 3.5
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
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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
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N-[(3S)-3-[(6-aminohexanoyl)amino]-4-(naphthalen-2-yl)butanoyl]-L-seryl-L-glutaminyl-N-[(1S)-1-(dihydroxyboranyl)-2-phenylethyl]-L-norleucinamide
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N-[(3S)-3-[(6-aminohexanoyl)amino]-4-(naphthalen-2-yl)butanoyl]-L-seryl-L-glutaminyl-N-[(1S)-4-bromo-1-(dihydroxyboranyl)butyl]-L-norleucinamide
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N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-3-cyclohexyl-L-alanyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-norleucinamide
-
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N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-alanyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-norleucinamide
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N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-alpha-aspartyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-norleucinamide
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N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-alpha-glutamyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-norleucinamide
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N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-asparaginyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-norleucinamide
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N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-glutaminyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-norleucinamide
-
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N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-homoseryl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-norleucinamide
-
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N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-(4S)-4-hydroxy-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-prolinamide
-
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N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-3-(2-naphthyl)-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-alaninamide
-
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N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-3-cyclohexyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-alaninamide
-
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N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-4-bromo-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-phenylalaninamide
-
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N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(1S)-2-oxo-1-phenylethyl]-L-leucinamide
-
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N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-1-(4-hydroxyphenyl)-3-oxopropan-2-yl]-L-leucinamide
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N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-1-(acetylamino)-3-oxopropan-2-yl]-L-leucinamide
-
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N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-1-(benzoylamino)-3-oxopropan-2-yl]-L-leucinamide
-
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N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-1-(formylamino)-3-oxopropan-2-yl]-L-leucinamide
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N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-1-oxo-3-(propanoylamino)propan-2-yl]-L-leucinamide
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N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-1-oxo-3-phenylpropan-2-yl]-L-leucinamide
-
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N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-1-oxohexan-2-yl]-L-leucinamide
-
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N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-1-[(2-methylpropanoyl)amino]-3-oxopropan-2-yl]-L-leucinamide
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N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-3-methyl-1-oxobutan-2-yl]-L-leucinamide
-
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N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-(dimethylamino)-1,4-dioxobutan-2-yl]-L-leucinamide
-
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N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-(methylsulfanyl)-1-oxobutan-2-yl]-L-leucinamide
-
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N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-(methylsulfinyl)-1-oxobutan-2-yl]-L-leucinamide
-
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N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-cyano-1-oxobutan-2-yl]-L-leucinamide
-
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N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-alaninamide
-
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N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-alpha-asparagine
-
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N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-alpha-glutamine
-
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N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-histidinamide
-
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N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-homoserinamide
-
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N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-isoleucinamide
-
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N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-leucinamide
-
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N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-lysinamide
-
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N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-4-methyl-1-oxopentan-2-yl]-L-methioninamide
-
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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
-
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N-[(benzyloxy)carbonyl]-L-seryl-L-seryl-L-lysyl-N-[(2S)-5-amino-1,5-dioxopentan-2-yl]-L-leucinamide
-
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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
-
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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
-
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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
R/S-diphenyl[N-benzyloxycarbonylamino(4-carbamoylphenyl)methyl]phosphonate
-
Tris[2-carboxyethyl] phosphine
incubation with 3 mM for 30 min at 25°C, in 0.1 ml 0.1 M Tris buffer, pH 7.8, causes 87% loss of activity
alpha1-Aantichymotrypsin
in circulation, the majority of the enzyme is complexed with protease inhibitors, including alpha1-antichymotrypsin. The proportion of the enzyme-alpha1-antichymotrypsin complex is higher in patients with prostate cancer than in controls without cancer
-
leupeptin
-
1 mM completely inhibits with bovine serum albumin as a substrate at pH 3.5
PMSF
-
suppresses the insulin-like growth factor binding protein 5 degradation associated with PSA treatment
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+
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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+
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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
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3 mM ascorbate for 30 min at 25°C, in 0.1 ml 0.1 M Tris buffer, pH 7.8, is devoid of inactivating potential. Loss of activity by reduction can be readily reversed by re-oxidation. Inactivation is associated with the reduction of two out of five conserved disulfides. Accessabilty of the Cys191-Cys220 disulfide near the catalytic serine 195 decides on the ability of reductants to inactivate the proteolytic activity of PSA
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50 mM EDTA does not inhibit insulin-like growth factor binding protein 5 degradation
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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
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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
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preference for hydrophobic residues in the P2 position and amino acids with the potential to hydrogen bond in the P3 position
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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
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after antibacterial therapy for 2 weeks, the PSA decreases from 14.0 ng/ml to 10.4 ng/ml
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structure-based drug design of diphenyl alpha-aminoalkylphosphonates as prostate-specific antigen antagonists, overview. Molecular docking and modeling of covalent and noncovalent binding of this class of inhibitors, interactions between the lead compound and residues Thr190, Ser217, and Ser227 in the P1 pocket
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