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Literature summary extracted from

  • Sexton, D.J.; Chen, T.; Martik, D.; Kuzmic, P.; Kuang, G.; Chen, J.; Nixon, A.E.; Zuraw, B.L.; Forteza, R.M.; Abraham, W.M.; Wood, C.R.
    Specific inhibition of tissue kallikrein 1 with a human monoclonal antibody reveals a potential role in airway diseases (2009), Biochem. J., 422, 383-392.
    View publication on PubMed

Activating Compound

EC Number Activating Compound Comment Organism Structure
3.4.21.35 additional information exposure of tracheobronchial epithelial cells to reactive oxygen species results in a significant increase in the amount of active KLK1 Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.21.35 4-(2-aminoethyl)benzenesulfonyl fluoride is an active-site-directed covalent inhibitor Homo sapiens
3.4.21.35 D-Pro-Phe-Arg-chloromethane is an active-site-directed covalent inhibitor Homo sapiens
3.4.21.35 DX-2300 DX-2300 is a fully human antibody that inhibits KLK1 via a competitive inhibition mechanism. Completely inhibits KLK1-like activity in urine and saliva, inhibits KLK1-like activity by 70% in bronchoalveolar lavage fluid. Inability of DX-2300 to bind either KLK1 covalently modified with 4-(2-aminoethyl)benzenesulfonyl fluoride or D-Pro-Phe-Arg-chloromethane, thus DX-2300 binds at or near the active site of the enzyme. DX-2300 blocks oxidative-stress-induced epidermal-growth-factor receptor activation and downstream mucus cell proliferation and hypersecretion, which is mediated by KLK1. DX-2300 is a potent and specific inhibitor of KLK1 that is efficacious in in vitro and in vivo models of airway disease Homo sapiens
3.4.21.35 DX-2300 completely inhibits KLK1-like activity in urine. In an allergic sheep model of asthma, inhalation of either 1 or 5 mg of DX-2300 inhibits high-molecular mass kininogen-induced bronchoconstriction by 49 and 68%, respectively Ovis aries
3.4.21.35 additional information DX-2300 is a fully human antibody, it does not inhibit the KLK1-like activity in mouse urine Mus musculus

Organism

EC Number Organism UniProt Comment Textmining
3.4.21.34 Homo sapiens
-
-
-
3.4.21.35 Homo sapiens
-
-
-
3.4.21.35 Mus musculus
-
-
-
3.4.21.35 Ovis aries
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.4.21.35 blood plasma
-
 Homo sapiens
-
3.4.21.35 bronchoalveolar lavage fluid
-
 Homo sapiens
-
3.4.21.35 saliva
-
 Homo sapiens
-
3.4.21.35 serum
-
 Homo sapiens
-
3.4.21.35 tracheobronchial epithelial cell
-
 Homo sapiens
-
3.4.21.35 urine
-
 Mus musculus
-
3.4.21.35 urine
-
 Homo sapiens
-
3.4.21.35 urine
-
 Ovis aries
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.4.21.35 Pro-Phe-Arg-7-amido-4-methylcoumarin + H2O
-
 Mus musculus Pro-Phe-Arg + 7-amino-4-methylcoumarin
-
 ?
3.4.21.35 Pro-Phe-Arg-7-amido-4-methylcoumarin + H2O
-
 Homo sapiens Pro-Phe-Arg + 7-amino-4-methylcoumarin
-
 ?
3.4.21.35 Pro-Phe-Arg-7-amido-4-methylcoumarin + H2O
-
 Ovis aries Pro-Phe-Arg + 7-amino-4-methylcoumarin
-
 ?
3.4.21.35 Val-Leu-Arg-4-nitroanilide + H2O tracheobronchial epithelial cells grown at the air/liquid interface Homo sapiens Val-Leu-Arg + 4-nitroaniline
-
 ?

Synonyms

EC Number Synonyms Comment Organism
3.4.21.34 KLKb1
-
 Homo sapiens
3.4.21.34 plasma kallikrein
-
 Homo sapiens
3.4.21.35 KLK1
-
 Mus musculus
3.4.21.35 KLK1
-
 Homo sapiens
3.4.21.35 KLK1
-
 Ovis aries
3.4.21.35 tissue kallikrein 1
-
 Mus musculus
3.4.21.35 tissue kallikrein 1
-
 Homo sapiens
3.4.21.35 tissue kallikrein 1
-
 Ovis aries

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.4.21.35 0.00000013
-
 DX-2300 in 20 mM Tris/HCl buffer, pH 7.5, 150 mM NaCl, 1 mM EDTA, 0.1% poly(ethylene glycol)-8000 and 0.1% Triton X-100 Homo sapiens