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Literature summary for 3.4.21.35 extracted from

  • Pimenta, D.C.; Fogaca, S.E.; Melo, R.L.; Juliano, L.; Juliano, M.A.
    Specificity of S'1 and S'2 subsites of human tissue kallikrein using the reactive-centre loop of kallistatin: the importance of P'1 and P'2 positions in design of inhibitors (2003), Biochem. J., 371, 1021-1025.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.4.21.35

Inhibitors

Inhibitors Comment Organism Structure
acetyl-D-Lys-L-Phe-L-Arg-D-Arg-L-Gln-N-(2,4-dinitrophenyl)ethylene diamine
-
 Homo sapiens
acetyl-D-Lys-L-Phe-L-Arg-D-Arg-L-Gln-NH2
-
 Homo sapiens
acetyl-D-Lys-L-Phe-L-Arg-D-Arg-NH2
-
 Homo sapiens
acetyl-D-Lys-L-Phe-L-Arg-L-Leu-L-Glu-NH2
-
 Homo sapiens
acetyl-Lys-Phe-Phe-Pro-Leu-Glu-NH2 leader compound for design of specific inhibitors of K1; weak inhibition Homo sapiens
o-aminobenzoyl-AIKFFARE-N-(2,4-dinitrophenyl)ethylene diamine compound gets poorly hydrolyzed as substrate and is a competitive inhibitor Homo sapiens
o-aminobenzoyl-AIKFFERE-N-(2,4-dinitrophenyl)ethylene diamine compound gets poorly hydrolyzed as substrate and is a competitive inhibitor Homo sapiens
o-aminobenzoyl-AIKFFKRE-N-(2,4-dinitrophenyl)ethylene diamine compound gets poorly hydrolyzed as substrate and is a competitive inhibitor Homo sapiens
o-aminobenzoyl-AIKFFLRE-N-(2,4-dinitrophenyl)ethylene diamine compound gets poorly hydrolyzed as substrate and is a competitive inhibitor Homo sapiens
o-aminobenzoyl-AIKFFNRE-N-(2,4-dinitrophenyl)ethylene diamine compound gets poorly hydrolyzed as substrate and is a competitive inhibitor Homo sapiens
o-aminobenzoyl-AIKFFPRE-N-(2,4-dinitrophenyl)ethylene diamine
-
 Homo sapiens
o-aminobenzoyl-AIKFFRRE-N-(2,4-dinitrophenyl)ethylene diamine compound gets poorly hydrolyzed as substrate and is a competitive inhibitor Homo sapiens
o-aminobenzoyl-AIKFFSEE-N-(2,4-dinitrophenyl)ethylene diamine compound gets poorly hydrolyzed as substrate and is a competitive inhibitor Homo sapiens
o-aminobenzoyl-AIKFFSIE-N-(2,4-dinitrophenyl)ethylene diamine compound gets poorly hydrolyzed as substrate and is a competitive inhibitor Homo sapiens
o-aminobenzoyl-AIKFFSLE-N-(2,4-dinitrophenyl)ethylene diamine compound gets poorly hydrolyzed as substrate and is a competitive inhibitor Homo sapiens
o-aminobenzoyl-AIKFFSNE-N-(2,4-dinitrophenyl)ethylene diamine compound gets poorly hydrolyzed as substrate and is a competitive inhibitor Homo sapiens
o-aminobenzoyl-AIKFFSQE-N-(2,4-dinitrophenyl)ethylene diamine compound gets poorly hydrolyzed as substrate and is a competitive inhibitor Homo sapiens
o-aminobenzoyl-AIKFFSTE-N-(2,4-dinitrophenyl)ethylene diamine compound gets poorly hydrolyzed as substrate and is a competitive inhibitor Homo sapiens
o-aminobenzoyl-AIKFFSVE-N-(2,4-dinitrophenyl)ethylene diamine compound gets poorly hydrolyzed as substrate and is a competitive inhibitor Homo sapiens
o-aminobenzoyl-AIKFFVRE-N-(2,4-dinitrophenyl)ethylene diamine compound gets poorly hydrolyzed as substrate and is a competitive inhibitor Homo sapiens
o-aminobenzoyl-D-Lys-L-Phe-L-Arg-D-Arg-L-Gln-N-(2,4-dinitrophenyl)ethylene diamine
-
 Homo sapiens
o-aminobenzoyl-D-Lys-L-Phe-L-Arg-L-Pro-L-Arg-L-Gln N-(2,4-dinitrophenyl)ethylene diamine
-
 Homo sapiens
o-aminobenzoyl-D-Lys-L-Phe-L-Phe-D-Arg-L-Gln-N-(2,4-dinitrophenyl)ethylene diamine
-
 Homo sapiens
o-aminobenzoyl-D-Lys-L-Phe-L-Phe-L-Pro-L-Arg-L-Gln N-(2,4-dinitrophenyl)ethylene diamine
-
 Homo sapiens
o-aminobenzoyl-D-Lys-L-Phe-L-Phe-L-Pro-L-Leu-L-Glu N-(2,4-dinitrophenyl)ethylene diamine
-
 Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.00013
-
 o-aminobenzoyl-AIKFFQRE-N-(2,4-dinitrophenyl)ethylene diamine pH 9.0, 37°C Homo sapiens
0.00021
-
 o-aminobenzoyl-AIKFFSKE-N-(2,4-dinitrophenyl)ethylene diamine pH 9.0, 37°C Homo sapiens
0.00023
-
 o-aminobenzoyl-AIKFFTRE-N-(2,4-dinitrophenyl)ethylene diamine pH 9.0, 37°C Homo sapiens
0.00027
-
 o-aminobenzoyl-AIKFFIRE-N-(2,4-dinitrophenyl)ethylene diamine pH 9.0, 37°C Homo sapiens
0.00036
-
 o-aminobenzoyl-AIKFFSRE-N-(2,4-dinitrophenyl)ethylene diamine pH 9.0, 37°C Homo sapiens
0.00094
-
 o-aminobenzoyl-AIKFFSSE-N-(2,4-dinitrophenyl)ethylene diamine pH 9.0, 37°C Homo sapiens
0.0013
-
 o-aminobenzoyl-AIKFFSPE-N-(2,4-dinitrophenyl)ethylene diamine pH 9.0, 37°C Homo sapiens
0.0018
-
 o-aminobenzoyl-AIKFFSAE-N-(2,4-dinitrophenyl)ethylene diamine pH 9.0, 37°C Homo sapiens
0.07
-
 Pro-Phe-Arg-4-methylcoumarin 7-amide pH 9.0, 37°C Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
polypeptide + H2O Homo sapiens S1' and S2' subsites of the enzyme play a determinant role in the recognition and hydrolysis of substrates peptides
-
 ?
polypeptide + H2O Homo sapiens serine at position P1' and arginine at position P2' results in high activity peptides
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Reaction

Reaction Comment Organism Reaction ID
Preferential cleavage of Arg-/- bonds in small molecule substrates. Highly selective action to release kallidin (lysyl-bradykinin) from kininogen involves hydrolysis of Met-/- or Leu-/-. The rat enzyme is unusual in liberating bradykinin directly from autologous kininogens by cleavage at two Arg-/- bonds serine at position P1' and arginine at position P2' result in high activity Homo sapiens
a

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
low-molecular-weight kininogen + H2O
-
 Homo sapiens kallidin + kinin kallidin is Lys-bradykinin ?
o-aminobenzoyl-AIKFFIRE-N-(2,4-dinitrophenyl)ethylene diamine + H2O
-
 Homo sapiens o-aminobenzoyl-AIKFF + IRE-N-(2,4-dinitrophenyl)ethylene diamine
-
 ?
o-aminobenzoyl-AIKFFQRE-N-(2,4-dinitrophenyl)ethylene diamine + H2O
-
 Homo sapiens o-aminobenzoyl-AIKFF + QRE-N-(2,4-dinitrophenyl)ethylene diamine
-
 ?
o-aminobenzoyl-AIKFFSAE-N-(2,4-dinitrophenyl)ethylene diamine + H2O
-
 Homo sapiens o-aminobenzoyl-AIKFF + SAE-N-(2,4-dinitrophenyl)ethylene diamine
-
 ?
o-aminobenzoyl-AIKFFSKE-N-(2,4-dinitrophenyl)ethylene diamine + H2O
-
 Homo sapiens o-aminobenzoyl-AIKFF + SKE-N-(2,4-dinitrophenyl)ethylene diamine
-
 ?
o-aminobenzoyl-AIKFFSPE-N-(2,4-dinitrophenyl)ethylene diamine + H2O
-
 Homo sapiens o-aminobenzoyl-AIKFF + SPE-N-(2,4-dinitrophenyl)ethylene diamine
-
 ?
o-aminobenzoyl-AIKFFSRE-N-(2,4-dinitrophenyl)ethylene diamine + H2O
-
 Homo sapiens o-aminobenzoyl-AIKFF + SRE-N-(2,4-dinitrophenyl)ethylene diamine
-
 ?
o-aminobenzoyl-AIKFFSRQ-N-(2,4-dinitrophenyl)ethylene diamine + H2O substrate sequence is derived from the kallistatin reactive centre loop sequence Homo sapiens o-aminobenzoyl-AIKFF + SRQ-N-(2,4-dinitrophenyl)ethylene diamine
-
 ?
o-aminobenzoyl-AIKFFSSE-N-(2,4-dinitrophenyl)ethylene diamine + H2O
-
 Homo sapiens o-aminobenzoyl-AIKFF + SSE-N-(2,4-dinitrophenyl)ethylene diamine
-
 ?
o-aminobenzoyl-AIKFFTRE-N-(2,4-dinitrophenyl)ethylene diamine + H2O
-
 Homo sapiens o-aminobenzoyl-AIKFF + TRE-N-(2,4-dinitrophenyl)ethylene diamine
-
 ?
polypeptide + H2O S1' and S2' subsites of the enzyme play a determinant role in the recognition and hydrolysis of substrates Homo sapiens peptides
-
 ?
polypeptide + H2O serine at position P1' and arginine at position P2' result in high activity Homo sapiens peptides
-
 ?
polypeptide + H2O serine at position P1' and arginine at position P2' results in high activity Homo sapiens peptides
-
 ?
Pro-Phe-Arg-4-methylcoumarin 7-amide + H2O
-
 Homo sapiens ?
-
 ?
Pro-Phe-Arg-7-amido-4-methylcoumarin + H2O
-
 Homo sapiens Pro-Phe-Arg + 7-amino-4-methylcoumarin
-
 ?

Synonyms

Synonyms Comment Organism
K1
-
 Homo sapiens

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.02
-
 o-aminobenzoyl-AIKFFQRE-N-(2,4-dinitrophenyl)ethylene diamine pH 9.0, 37°C Homo sapiens
0.04
-
 o-aminobenzoyl-AIKFFTRE-N-(2,4-dinitrophenyl)ethylene diamine pH 9.0, 37°C Homo sapiens
0.05
-
 o-aminobenzoyl-AIKFFIRE-N-(2,4-dinitrophenyl)ethylene diamine pH 9.0, 37°C Homo sapiens
0.05
-
 o-aminobenzoyl-AIKFFSPE-N-(2,4-dinitrophenyl)ethylene diamine pH 9.0, 37°C Homo sapiens
0.21
-
 o-aminobenzoyl-AIKFFSKE-N-(2,4-dinitrophenyl)ethylene diamine pH 9.0, 37°C Homo sapiens
0.3
-
 o-aminobenzoyl-AIKFFSSE-N-(2,4-dinitrophenyl)ethylene diamine pH 9.0, 37°C Homo sapiens
0.54
-
 o-aminobenzoyl-AIKFFSAE-N-(2,4-dinitrophenyl)ethylene diamine pH 9.0, 37°C Homo sapiens
3.33
-
 o-aminobenzoyl-AIKFFSRE-N-(2,4-dinitrophenyl)ethylene diamine pH 9.0, 37°C Homo sapiens
12.5
-
 Pro-Phe-Arg-4-methylcoumarin 7-amide pH 9.0, 37°C Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000022
-
 o-aminobenzoyl-D-Lys-L-Phe-L-Arg-D-Arg-L-Gln-N-(2,4-dinitrophenyl)ethylene diamine pH 9.0, 37°C Homo sapiens
0.000029
-
 acetyl-D-Lys-L-Phe-L-Arg-L-Leu-L-Glu-NH2 pH 9.0, 37°C Homo sapiens
0.000029
-
 o-aminobenzoyl-D-Lys-L-Phe-L-Phe-D-Arg-L-Gln-N-(2,4-dinitrophenyl)ethylene diamine pH 9.0, 37°C Homo sapiens
0.00009
-
 o-aminobenzoyl-AIKFFPRE-N-(2,4-dinitrophenyl)ethylene diamine pH 9.0, 37°C Homo sapiens
0.00015
-
 o-aminobenzoyl-AIKFFKRE-N-(2,4-dinitrophenyl)ethylene diamine pH 9.0, 37°C Homo sapiens
0.00019
-
 o-aminobenzoyl-AIKFFSLE-N-(2,4-dinitrophenyl)ethylene diamine pH 9.0, 37°C Homo sapiens
0.00021
-
 o-aminobenzoyl-AIKFFRRE-N-(2,4-dinitrophenyl)ethylene diamine pH 9.0, 37°C Homo sapiens
0.00022
-
 o-aminobenzoyl-AIKFFVRE-N-(2,4-dinitrophenyl)ethylene diamine pH 9.0, 37°C Homo sapiens
0.00032
-
 o-aminobenzoyl-AIKFFLRE-N-(2,4-dinitrophenyl)ethylene diamine pH 9.0, 37°C Homo sapiens
0.00032
-
 o-aminobenzoyl-AIKFFSTE-N-(2,4-dinitrophenyl)ethylene diamine pH 9.0, 37°C Homo sapiens
0.00033
-
 o-aminobenzoyl-AIKFFARE-N-(2,4-dinitrophenyl)ethylene diamine pH 9.0, 37°C Homo sapiens
0.00035
-
 o-aminobenzoyl-AIKFFNRE-N-(2,4-dinitrophenyl)ethylene diamine pH 9.0, 37°C Homo sapiens
0.0004
-
 o-aminobenzoyl-AIKFFERE-N-(2,4-dinitrophenyl)ethylene diamine pH 9.0, 37°C Homo sapiens
0.000424
-
 acetyl-D-Lys-L-Phe-L-Arg-D-Arg-L-Gln-N-(2,4-dinitrophenyl)ethylene diamine pH 9.0, 37°C Homo sapiens
0.000494
-
 acetyl-D-Lys-L-Phe-L-Arg-D-Arg-L-Gln-NH2 pH 9.0, 37°C Homo sapiens
0.00051
-
 o-aminobenzoyl-AIKFFSEE-N-(2,4-dinitrophenyl)ethylene diamine pH 9.0, 37°C Homo sapiens
0.0006
-
 o-aminobenzoyl-AIKFFSQE-N-(2,4-dinitrophenyl)ethylene diamine pH 9.0, 37°C Homo sapiens
0.00073
-
 o-aminobenzoyl-AIKFFSNE-N-(2,4-dinitrophenyl)ethylene diamine pH 9.0, 37°C Homo sapiens
0.001
-
 o-aminobenzoyl-AIKFFSIE-N-(2,4-dinitrophenyl)ethylene diamine pH 9.0, 37°C Homo sapiens
0.0017
-
 o-aminobenzoyl-AIKFFSVE-N-(2,4-dinitrophenyl)ethylene diamine pH 9.0, 37°C Homo sapiens
0.0044
-
 acetyl-D-Lys-L-Phe-L-Arg-D-Arg-NH2 pH 9.0, 37°C Homo sapiens