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Literature summary for 3.4.22.37 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
Search for more literature for 3.4.22.37

Activating Compound

Activating Compound Comment Organism Structure
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

Application Comment Organism
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

Inhibitors Comment Organism Structure
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
carbobenzoxy-Glu(NHN(CH3)Ph)-Lys-CO-NHCH2Ph
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 Porphyromonas gingivalis
carbobenzoxy-Lys-Arg-CO-Lys-N-(CH3)2
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 Porphyromonas gingivalis
chicken ovoinhibitor III and IV domains having Leu and Ser or Leu and Leu, respectively, at the P2' and P3' sites Porphyromonas gingivalis
Chloromethylketones
-
 Porphyromonas gingivalis
EDTA
-
 Porphyromonas gingivalis
iodoacetamide
-
 Porphyromonas gingivalis
leupeptin
-
 Porphyromonas gingivalis
tetracycline
-
 Porphyromonas gingivalis

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Porphyromonas gingivalis
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
additional information gingipains are key virulence determinants of Porphyromonas gingivalis and play a crucial role in pathogenicity Porphyromonas gingivalis ?
-
 ?
N-alpha-benzoyl-DL-arginine 4-nitroanilide + H2O
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 Porphyromonas gingivalis N-alpha-benzoyl-DL-arginine + 4-nitroaniline
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 ?

Synonyms

Synonyms Comment Organism
Arg-specific cysteine proteinase gingipain
-
 Porphyromonas gingivalis
gingipain R
-
 Porphyromonas gingivalis
RGP
-
 Porphyromonas gingivalis

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
22
-
 assay at Porphyromonas gingivalis

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.6 8.3 assay at Porphyromonas gingivalis