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Literature summary for 3.4.22.37 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

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

Inhibitors

Inhibitors Comment Organism Structure
benzamidine
-
Porphyromonas gingivalis
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
bis-benzamidine with urea linker best inhibitor Porphyromonas gingivalis
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)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
protein + H2O Porphyromonas gingivalis
-
peptides
-
?

Organism

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

Substrates and Products (Substrate)

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

Synonyms

Synonyms Comment Organism
arginine gingipain
-
Porphyromonas gingivalis
HRgpA
-
Porphyromonas gingivalis
RgpB
-
Porphyromonas gingivalis

pH Optimum

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

Ki Value [mM]

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