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Literature summary for 3.4.21.77 extracted from

  • Kostova, M.B.; Rosen, D.M.; Chen, Y.; Mease, R.C.; Denmeade, S.R.
    Structural optimization, biological evaluation, and application of peptidomimetic prostate specific antigen inhibitors (2013), J. Med. Chem., 56, 4224-4235.
    View publication on PubMedView publication on EuropePMC

Inhibitors

Inhibitors Comment Organism Structure
(1S)-4-bromo-1-[(3aS,4R,6R,7aR)-3a,5,5-trimethylhexahydro-4,6-methano-1,3,2-benzodioxaborol-2-yl]butan-1-amine
-
Homo sapiens
(3aR,4R,6R,7aS)-2-[(1R)-1-amino-2-phenylethyl]-5,5-dimethyltetrahydro-4,6-methano-1,3,2-benzodioxaborol-3a(4H)-ol
-
Homo sapiens
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
-
Homo sapiens
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
-
Homo sapiens
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
-
Homo sapiens
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
-
Homo sapiens
N-[(3S)-3-[(6-aminohexanoyl)amino]-4-(naphthalen-2-yl)butanoyl]-L-seryl-L-glutaminyl-N-[(1S)-1-(dihydroxyboranyl)-2-phenylethyl]-L-norleucinamide
-
Homo sapiens
N-[(3S)-3-[(6-aminohexanoyl)amino]-4-(naphthalen-2-yl)butanoyl]-L-seryl-L-glutaminyl-N-[(1S)-4-bromo-1-(dihydroxyboranyl)butyl]-L-norleucinamide
-
Homo sapiens
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
-
Homo sapiens
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
-
Homo sapiens
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
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P07288
-
-

Source Tissue

Source Tissue Comment Organism Textmining
prostate
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Mu-SRKSQQY-7-amido-4-methylcoumarin + H2O
-
Homo sapiens Mu-SRKSQQY + 7-amino-4-methylcoumarin
-
?

Synonyms

Synonyms Comment Organism
prostate-specific antigen
-
Homo sapiens
PSA
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.8
-
assay at Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000072
-
N2-[(5S)-5-[[N-(6-aminohexanoyl)-L-alanyl]amino]-2-(3-amino-3-oxopropyl)-6-hydroxy-4-oxohexanoyl]-N-[(1S)-1-(dihydroxyboranyl)-2-phenylethyl]-L-norleucinamide pH 7.8, 37°C Homo sapiens