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Literature summary for 3.4.21.83 extracted from

  • Swenerton, R.K.; Zhang, S.; Sajid, M.; Medzihradszky, K.F.; Craik, C.S.; Kelly, B.L.; McKerrow, J.H.
    The oligopeptidase B of Leishmania regulates parasite enolase and immune evasion (2011), J. Biol. Chem., 286, 429-440.
    View publication on PubMedView publication on EuropePMC

Inhibitors

Inhibitors Comment Organism Structure
antipain 0.1 mM, no residual activity Leishmania donovani
benzamidine 1 mM, 27% residual activity Leishmania donovani
Ca2+ 0.01 mM, 69% residual activity Leishmania donovani
leupeptin 0.1 mM, no residual activity Leishmania donovani
Mg2+ 0.01 mM, 73% residual activity Leishmania donovani
Mn2+ 0.01 mM, 73% residual activity Leishmania donovani
Pefabloc SC 2 mM, no residual activity Leishmania donovani
Phe-Pro-Arg-chloromethylketone 0.01 mM, no residual activity Leishmania donovani
tosyl-L-Lys-chloromethylketone 0.1 mM, no residual activity Leishmania donovani
Zn2+ 0.01 mM, no residual activity Leishmania donovani

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.00308
-
benzoyl-Gly-Gly-L-Arg-7-amido-4-methylcoumarin pH 8.0, 25°C Leishmania donovani
0.00776
-
benzoyl-Gly-L-Pro-L-Arg-7-amido-4-methylcoumarin pH 8.0, 25°C Leishmania donovani

Organism

Organism UniProt Comment Textmining
Leishmania donovani C9EF60
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
benzoyl-Gly-Gly-L-Arg-7-amido-4-methylcoumarin + H2O
-
Leishmania donovani benzoyl-Gly-Gly-L-Arg + 7-amino-4-methylcoumarin
-
?
benzoyl-Gly-L-Pro-L-Arg-7-amido-4-methylcoumarin + H2O
-
Leishmania donovani benzoyl-Gly-L-Pro-L-Arg + 7-amino-4-methylcoumarin
-
?
additional information OPB has a strong preference for lysine or arginine residues at P1. OPB can accommodate several amino acids in the P2–P4 positions, with a preference for glycine in P2, serine, glycine, alanine, asparagine, proline, and threonine in P3, and proline in P4. Bulky hydrophobic groups, such as tyrosine, phenylalanine, and tryptophan, are least preferred Leishmania donovani ?
-
?

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
4250
-
benzoyl-Gly-L-Pro-L-Arg-7-amido-4-methylcoumarin pH 8.0, 25°C Leishmania donovani
6830
-
benzoyl-Gly-Gly-L-Arg-7-amido-4-methylcoumarin pH 8.0, 25°C Leishmania donovani

General Information

General Information Comment Organism
physiological function knock-out of OPB results in the disappearance of the serine protease activity of Leishmania extracts. OPB null parasites show an elevated content of enolase protein. This enolase is enzymatically inactive and associated with the parasite membrane. OPB deletion results in a striking alteration in macrophage responses to Leishmania. Whereas wild type parasites elicited little, if any, response from infected macrophages, OPB deletion parasites induce a massive up-regulation in gene transcription. These OPB deletion parasites display decreased virulence in the murine footpad indection model Leishmania donovani

kcat/KM [mM/s]

kcat/KM Value [1/mMs-1] kcat/KM Value Maximum [1/mMs-1] Substrate Comment Organism Structure
547700
-
benzoyl-Gly-L-Pro-L-Arg-7-amido-4-methylcoumarin pH 8.0, 25°C Leishmania donovani
2218000
-
benzoyl-Gly-Gly-L-Arg-7-amido-4-methylcoumarin pH 8.0, 25°C Leishmania donovani