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Literature summary extracted from

  • Bania, J.; Kubiak, A.; Wojtachnio, K.; Polanowski, A.
    Pancreatic secretory trypsin inhibitor acts as an effective inhibitor of cysteine proteinases gingipains from Porphyromonas gingivalis (2008), J. Periodont. Res., 43, 232-236.
    View publication on PubMed

Activating Compound

EC Number Activating Compound Comment Organism Structure
3.4.22.37 additional information activation of gingipain R by incubation for 10 min in 200 mM Tris-HCl buffer, pH 7.6, containing 50 mM Gly-Gly, 10 mM CaCl2 and 10 mM Cys-HCl Porphyromonas gingivalis
3.4.22.47 additional information activation of gingipain R by incubation for 10 min in 200 mM Tris-HCl buffer, pH 7.6, containing 50 mM Gly-Gly, 10 mM CaCl2 and 10 mM Cys-HCl Porphyromonas gingivalis

Application

EC Number Application Comment Organism
3.4.22.37 medicine development of potent, gingipain-specific inhibitors might be a helpful tool in a therapeutic strategy to prevent or treat periodontal disease Porphyromonas gingivalis
3.4.22.47 medicine development of potent, gingipain-specific inhibitors might be a helpful tool in a therapeutic strategy to prevent or treat periodontal disease Porphyromonas gingivalis

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.21.4 pancreatic secretory trypsin inhibitor a Kazal-type specific trypsin inhibitor with narrow specificity for the inhibition of trypsin, with very little or no inhibitory capacity against other serine proteinases, even those exhibiting trypsin-like specificity Bos taurus
3.4.22.37 bovine pancreatic secretory trypsin inhibitor i.e. PSTI bovine, about 33% inhibition at 0.0005 mM, 66% at 0.001 mM, and 87% at 0.0025 mM, a Kazal-type serine proteinase inhibitor purified from pancreas, bovine pancreatic secretory trypsin inhibitor having an essential Arg residue at the P1 position of the reactive site, and containing Tyr and Asn residues the P2' and P3' sites, specifically inhibits the activity of the Arg-specific gingipain R, whereas porcine inhibitor, possessing a Lys residue at the P1 position, exhibits activity only against the Lys-specific cysteine proteinase gingipain K, EC 3.4.22.47. The inhibitory effect is eliminated by Arg residue modification in 0.2 M borate buffer, pH 9.0, and 50 mM excess of cyclohexanedione in a 1 : 30 molar ratio at 37°C. The association equilibrium constant is 0.0016 mM Porphyromonas gingivalis
3.4.22.37 carbobenzoxy-Glu(NHN(CH3)Ph)-Lys-CO-NHCH2Ph
-
 Porphyromonas gingivalis
3.4.22.37 carbobenzoxy-Lys-Arg-CO-Lys-N-(CH3)2
-
 Porphyromonas gingivalis
3.4.22.37 chicken ovoinhibitor III and IV domains having Leu and Ser or Leu and Leu, respectively, at the P2' and P3' sites Porphyromonas gingivalis
3.4.22.37 Chloromethylketones
-
 Porphyromonas gingivalis
3.4.22.37 EDTA
-
 Porphyromonas gingivalis
3.4.22.37 iodoacetamide
-
 Porphyromonas gingivalis
3.4.22.37 leupeptin
-
 Porphyromonas gingivalis
3.4.22.37 tetracycline
-
 Porphyromonas gingivalis
3.4.22.47 benzamidine derivatives
-
 Porphyromonas gingivalis
3.4.22.47 carbobenzoxy-Glu(NHN(CH3)Ph)-Lys-CO-NHCH2Ph
-
 Porphyromonas gingivalis
3.4.22.47 carbobenzoxy-Lys-Arg-CO-Lys-N-(CH3)2
-
 Porphyromonas gingivalis
3.4.22.47 Chloromethylketones
-
 Porphyromonas gingivalis
3.4.22.47 EDTA
-
 Porphyromonas gingivalis
3.4.22.47 iodoacetamide
-
 Porphyromonas gingivalis
3.4.22.47 leupeptin
-
 Porphyromonas gingivalis
3.4.22.47 additional information no inhibition by chicken ovoinhibitor III and IV domains Porphyromonas gingivalis
3.4.22.47 porcine pancreatic secretory trypsin inhibitor i.e. PSTI porcine, a Kazal-type serine proteinase inhibitor purified from pancreas, porcine pancreatic secretory trypsin inhibitor having an essential Lys residue at the P1 position of the reactive site, and containing Tyr and Asn residues the P2' and P3' sites, specifically inhibits the activity of the Lys-specific gingipain K, whereas bovine inhibitor, possessing a Arg residue at the P1 position, exhibits activity only against the Arg-specific cysteine proteinase gingipain K, EC 3.4.22.37. The association equilibrium constant is 0.51 mM Porphyromonas gingivalis
3.4.22.47 tetracycline
-
 Porphyromonas gingivalis

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
3.4.22.37 additional information Porphyromonas gingivalis gingipains are key virulence determinants of Porphyromonas gingivalis and play a crucial role in pathogenicity ?
-
 ?
3.4.22.47 additional information Porphyromonas gingivalis gingipains are key virulence determinants of Porphyromonas gingivalis and play a crucial role in pathogenicity ?
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
3.4.21.4 Bos taurus
-
-
-
3.4.22.37 Porphyromonas gingivalis
-
-
-
3.4.22.47 Porphyromonas gingivalis
-
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
3.4.21.4 acetone precipitation and anhydrotrypsin-Sepharose column chromatography Bos taurus

Source Tissue

EC Number Source Tissue Comment Organism Textmining

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.4.21.4 N-alpha-benzoyl-L-Arg-4-nitroanilide + H2O
-
 Bos taurus N-alpha-benzoyl-L-Arg + 4-nitroaniline
-
 ?
3.4.22.37 additional information gingipains are key virulence determinants of Porphyromonas gingivalis and play a crucial role in pathogenicity Porphyromonas gingivalis ?
-
 ?
3.4.22.37 N-alpha-benzoyl-DL-arginine 4-nitroanilide + H2O
-
 Porphyromonas gingivalis N-alpha-benzoyl-DL-arginine + 4-nitroaniline
-
 ?
3.4.22.47 additional information gingipains are key virulence determinants of Porphyromonas gingivalis and play a crucial role in pathogenicity Porphyromonas gingivalis ?
-
 ?
3.4.22.47 N-alpha-benzoyl-DL-lysine 4-nitroanilide + H2O
-
 Porphyromonas gingivalis N-alpha-benzoyl-DL-lysine + 4-nitroaniline
-
 ?

Synonyms

EC Number Synonyms Comment Organism
3.4.21.4 beta-trypsin
-
 Bos taurus
3.4.22.37 Arg-specific cysteine proteinase gingipain
-
 Porphyromonas gingivalis
3.4.22.37 gingipain R
-
 Porphyromonas gingivalis
3.4.22.37 RGP
-
 Porphyromonas gingivalis
3.4.22.47 gingipain K
-
 Porphyromonas gingivalis
3.4.22.47 KGP
-
 Porphyromonas gingivalis
3.4.22.47 Lys-specific cysteine proteinase gingipain
-
 Porphyromonas gingivalis

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
3.4.22.37 22
-
 assay at Porphyromonas gingivalis
3.4.22.47 22
-
 assay at Porphyromonas gingivalis

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
3.4.22.37 7.6 8.3 assay at Porphyromonas gingivalis
3.4.22.47 7.6 8.3 assay at Porphyromonas gingivalis