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Literature summary extracted from

  • Krauser, A.; Potempa, J.; Travis, J.; Powers, J.C.
    Inhibition f arginie gingipains (RgpB and HRgpA) with benzamidine inhibitors: zinc increases inhibitory potency (2002), Biol. Chem., 383, 1193-1198.
    View publication on PubMed

Activating Compound

EC Number Activating Compound Comment Organism Structure
3.4.22.37 glycyl-glycine increases the substrate hydrolysis, increases Km and kcat value Porphyromonas gingivalis

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.22.37 benzamidine
-
Porphyromonas gingivalis
3.4.22.37 benzamidine derivatives overview, derivatives with an urea moiety linking the 2 aromatic rings, and derivatives with a less polar ether linker, the latter being less efficient inhibitors Porphyromonas gingivalis
3.4.22.37 bis-benzamidine with urea linker best inhibitor Porphyromonas gingivalis
3.4.22.37 Zn2+ complete inhibition of both enzyme forms at 6.7 mM, increases inhibitory effect of benzamidine derivatives 2-3fold, lowers Ki-values, binding mechanism 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 protein + H2O Porphyromonas gingivalis
-
peptides
-
?

Organism

EC Number Organism UniProt Comment Textmining
3.4.22.37 Porphyromonas gingivalis
-
purified enzyme forms HRgpA and RgpB
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.4.22.37 protein + H2O
-
Porphyromonas gingivalis peptides
-
?

Synonyms

EC Number Synonyms Comment Organism
3.4.22.37 arginine gingipain
-
Porphyromonas gingivalis
3.4.22.37 HRgpA
-
Porphyromonas gingivalis
3.4.22.37 RgpB
-
Porphyromonas gingivalis

pH Optimum

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

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.4.22.37 additional information
-
additional information Ki-values for benzamidine derivatives in presence or absence of Zn2+ Porphyromonas gingivalis
3.4.22.37 0.013
-
bis-benzamidine with urea linker pH 7.6, RgpB, in presence of Zn2+ Porphyromonas gingivalis
3.4.22.37 0.015
-
bis-benzamidine with urea linker pH 7.6, HRgpA, in presence of Zn2+ Porphyromonas gingivalis
3.4.22.37 0.03
-
bis-benzamidine with urea linker pH 7.6, HRgpA and RgpB, in absence of Zn2+ Porphyromonas gingivalis