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Literature summary for 3.4.21.35 extracted from

  • Melo, R.L.; Barbosa Pozzo, R.C.; Pimenta, D.C.; Perissutti, E.; Caliendo, G.; Santagada, V.; Juliano, L.; Juliano, M.A.
    Human tissue kallikrein S1 subsite recognition of non-natural basic amino acids (2001), Biochemistry, 40, 5226-5232.
    View publication on PubMed
Search for more literature for 3.4.21.35

Inhibitors

Inhibitors Comment Organism Structure
o-aminobenzoyl-F-4-(aminomethyl)cyclohexylalanine-SRQ-N-(2,4-dinitrophenyl)ethylene diamine K1, highly specific Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0003
-
 o-aminobenzoyl-GFSPF-4-(aminomethyl)phenylalanine-SSRPQ-N-(2,4-dinitrophenyl)ethylene diamine pH 9.0, 37°C Homo sapiens
0.00064
-
 o-aminobenzoyl-GFSPF-4-piperidinylalanine-SSRPQ-N-(2,4-dinitrophenyl)ethylene diamine pH 9.0, 37°C Homo sapiens
0.0007
-
 o-aminobenzoyl-GFSPF-4-(aminocyclohexyl)alanine-SSRPQ-N-(2,4-dinitrophenyl)ethylene diamine pH 9.0, 37°C Homo sapiens
0.0007
-
 o-aminobenzoyl-Phe-Nim-(dimethyl)histidine-Ser-Arg-Gln-N-(2,4-dinitrophenyl)ethylene diamine pH 9.0, 37°C Homo sapiens
0.001
-
 o-aminobenzoyl-GFSPF-Nim-(dimethyl)histidine-SSRPQ-N-(2,4-dinitrophenyl)ethylene diamine pH 9.0, 37°C Homo sapiens
0.0036
-
 o-aminobenzoyl-Phe-4-(aminomethyl)phenylalanine-Ser-Arg-Gln-N-(2,4-dinitrophenyl)ethylene diamine pH 9.0, 37°C Homo sapiens
0.0038
-
 o-aminobenzoyl-GFSPF-4-(aminomethyl)-N-isopropylphenylalanine-SSRPQ-N-(2,4-dinitrophenyl)ethylene diamine pH 9.0, 37°C Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
extracellular secretion Homo sapiens
-
-

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
polypeptide + H2O Homo sapiens
-
 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 S1 subsite accepts both Arg and Phe and has a preference for basic residues Homo sapiens
a

Source Tissue

Source Tissue Comment Organism Textmining
urine
-
 Homo sapiens
-

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 ?
additional information no activity with substrate o-aminobenzoyl-FXSRQ-N-(2,4-dinitrophenyl)ethylene diamine harboring at position X a non-natural amino acid like 4-guanidine phenylalanine, 3-pyridylalanine, 4-(aminomethyl)cyclohexylalanine, 4-(aminomethyl)-N-isopropylphenylalanine, 4-piperidinylalanine, and 4-(aminocyclohexyl)alanine Homo sapiens ?
-
 ?
additional information K1, sustrate specificty of S1 subsite, accepts both Arg and Phe Homo sapiens ?
-
 ?
additional information no activity with substrate o-aminobenzoyl-GFSPFXSSRPQ-N-(2,4-dinitrophenyl)ethylene diamine harboring at position X a non-natural amino acid like 4-guanidine phenylalanine, 3-pyridylalanine, and 4-(aminomethyl)cyclohexylalanine Homo sapiens ?
-
 ?
o-aminobenzoyl-GFSPF-4-(aminocyclohexyl)alanine-SSRPQ-N-(2,4-dinitrophenyl)ethylene diamine + H2O synthetic internally quenched fluorescent peptides with substitution for a non-natural amino acid, sequence is based on the human kininogen sequence at the C-terminal region of bradykinin Homo sapiens ?
-
 ?
o-aminobenzoyl-GFSPF-4-(aminomethyl)-N-isopropylphenylalanine-SSRPQ-N-(2,4-dinitrophenyl)ethylene diamine + H2O synthetic internally quenched fluorescent peptides with substitution for a non-natural amino acid, sequence is based on the human kininogen sequence at the C-terminal region of bradykinin Homo sapiens ?
-
 ?
o-aminobenzoyl-GFSPF-4-(aminomethyl)phenylalanine-SSRPQ-N-(2,4-dinitrophenyl)ethylene diamine + H2O synthetic internally quenched fluorescent peptides with substitution for a non-natural amino acid, sequence is based on the human kininogen sequence at the C-terminal region of bradykinin Homo sapiens ?
-
 ?
o-aminobenzoyl-GFSPF-4-piperidinylalanine-SSRPQ-N-(2,4-dinitrophenyl)ethylene diamine + H2O synthetic internally quenched fluorescent peptides with substitution for a non-natural amino acid, sequence is based on the human kininogen sequence at the C-terminal region of bradykinin Homo sapiens ?
-
 ?
o-aminobenzoyl-GFSPF-Nim-(dimethyl)histidine-SSRPQ-N-(2,4-dinitrophenyl)ethylene diamine + H2O synthetic internally quenched fluorescent peptides with substitution for a non-natural amino acid, sequence is based on the human kininogen sequence at the C-terminal region of bradykinin Homo sapiens ?
-
 ?
o-aminobenzoyl-Phe-4-(aminomethyl)phenylalanine-Ser-Arg-Gln-N-(2,4-dinitrophenyl)ethylene diamine + H2O synthetic internally quenched fluorescent peptides with substitution for a non-natural amino acid, sequence is based on the human kininogen sequence at the C-terminal region of bradykinin Homo sapiens o-aminobenzoyl-Phe-4-(aminomethyl)phenylalanine-Ser-Arg + Gln-N-(2,4-dinitrophenyl)ethylene diamine
-
 ?
o-aminobenzoyl-Phe-Nim-(dimethyl)histidine-Ser-Arg-Gln-N-(2,4-dinitrophenyl)ethylene diamine + H2O synthetic internally quenched fluorescent peptides with substitution for a non-natural amino acid, sequence is based on the human kininogen sequence at the C-terminal region of bradykinin Homo sapiens o-aminobenzoyl-Phe-Nim-(dimethyl)histidine-Ser-Arg + Gln-N-(2,4-dinitrophenyl)ethylene diamine
-
 ?
polypeptide + H2O
-
 Homo sapiens peptides
-
 ?

Temperature Optimum [°C]

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

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.51
-
 o-aminobenzoyl-GFSPF-4-(aminocyclohexyl)alanine-SSRPQ-N-(2,4-dinitrophenyl)ethylene diamine pH 9.0, 37°C Homo sapiens
0.61
-
 o-aminobenzoyl-GFSPF-4-piperidinylalanine-SSRPQ-N-(2,4-dinitrophenyl)ethylene diamine pH 9.0, 37°C Homo sapiens
0.81
-
 o-aminobenzoyl-GFSPF-4-(aminomethyl)-N-isopropylphenylalanine-SSRPQ-N-(2,4-dinitrophenyl)ethylene diamine pH 9.0, 37°C Homo sapiens
1
-
 o-aminobenzoyl-Phe-4-(aminomethyl)phenylalanine-Ser-Arg-Gln-N-(2,4-dinitrophenyl)ethylene diamine pH 9.0, 37°C Homo sapiens
1.2
-
 o-aminobenzoyl-Phe-Nim-(dimethyl)histidine-Ser-Arg-Gln-N-(2,4-dinitrophenyl)ethylene diamine pH 9.0, 37°C Homo sapiens
1.8
-
 o-aminobenzoyl-GFSPF-4-(aminomethyl)phenylalanine-SSRPQ-N-(2,4-dinitrophenyl)ethylene diamine pH 9.0, 37°C Homo sapiens
2.1
-
 o-aminobenzoyl-GFSPF-Nim-(dimethyl)histidine-SSRPQ-N-(2,4-dinitrophenyl)ethylene diamine pH 9.0, 37°C Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
9
-
 assay at Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
additional information
-
 additional information
-
 Homo sapiens
0.00005
-
 o-aminobenzoyl-F-4-(aminomethyl)cyclohexylalanine-SRQ-N-(2,4-dinitrophenyl)ethylene diamine pH 9.0, 37°C Homo sapiens