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Literature summary for 3.4.21.109 extracted from

  • Tamberg, T.; Hong, Z.; De Schepper, D.; Skovbjerg, S.; Dupont, D.M.; Vitved, L.; Schar, C.R.; Skjoedt, K.; Vogel, L.K.; Jensen, J.K.
    Blocking the proteolytic activity of zymogen matriptase with antibody-based inhibitors (2019), J. Biol. Chem., 294, 314-326 .
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.4.21.109

Cloned(Commentary)

Cloned (Comment) Organism
expression in Pichia pastoris Homo sapiens

Crystallization (Commentary)

Crystallization (Comment) Organism
mutant N164Q/R614A/S805A, to 2.5 A resolution. The structure of zymogen matriptase reveals a classical chymotrypsin-like zymogen fold Homo sapiens

Protein Variants

Protein Variants Comment Organism
N164Q mutation introduced to avoid N-glycosylation Homo sapiens
N164Q/R614A mutation at activation cleavage site, variant is locked in the zymogen form, about 3% of wild-type activity Homo sapiens
N164Q/R614A/S805A mutation at activatio, plus mutant cleavage site, variant is locked in the zymogen form, plus mutation S805A to prevent unwanted proteolytic degradation during crystallization Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
additional information generation of monoclonal antibodies against mutant N164Q/R614A and use as inhibitors. Two antibodies are competitive inhibitors and able to block the activity of wild-type full-length matriptase in complex biological samples by binding near the active site Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.256
-
 Ile-Pro-Arg-p-nitroanilide mutant N164Q/R614A, 37°C, pH 7.4 Homo sapiens
0.387
-
 Ile-Pro-Arg-p-nitroanilide wild-type, pH 7.4, 37°C Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens Q9Y5Y6
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Ile-Pro-Arg-p-nitroanilide + H2O
-
 Homo sapiens Ile-Pro + Arg-p-nitroanilide
-
 ?

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
7700
-
 Ile-Pro-Arg-p-nitroanilide mutant N164Q/R614A, 37°C, pH 7.4 Homo sapiens
390000
-
 Ile-Pro-Arg-p-nitroanilide wild-type, pH 7.4, 37°C Homo sapiens

kcat/KM [mM/s]

kcat/KM Value [1/mMs-1] kcat/KM Value Maximum [1/mMs-1] Substrate Comment Organism Structure
30078
-
 Ile-Pro-Arg-p-nitroanilide mutant N164Q/R614A, 37°C, pH 7.4 Homo sapiens
1011000
-
 Ile-Pro-Arg-p-nitroanilide wild-type, pH 7.4, 37°C Homo sapiens