Literature summary for 3.4.21.6 extracted from

Monnaie, D.; Arosio, D.; Griffon, N.; Rose, T.; Rezaie, A.R.; Di Cera, E.
Identification of a binding site for quaternary amines in factor Xa (2000), Biochemistry, 39, 5349-5354.

Search for more literature for 3.4.21.6

Activating Compound

Activating Compound	Comment	Organism	Structure
K+	slightly activating	Homo sapiens
additional information	not affected by NH4+ and Li+	Homo sapiens
Na+	4fold activation at 150 mM	Homo sapiens

Protein Variants

Protein Variants	Comment	Organism
F174N	site-directed mutagenesis, reduced binding of inhibitor trimethylphenylammonium	Homo sapiens
Y99T	site-directed mutagenesis, 25fold reduced binding of inhibitor trimethylphenylammonium	Homo sapiens

Inhibitors

Inhibitors	Comment	Organism	Structure
4-aminobenzamidine	competitive	Homo sapiens
choline	positively linked to Na+ binding	Homo sapiens
additional information	not affected by NH4+ and Li+	Homo sapiens
trimethylphenylammonium	i.e. TMPA, strong and highly specific inhibition, inhibits substrate hydrolysis competitively, does not inhibit the binding of 4-aminobenzamidine to the S1-pocket, and is positively linked to Na+ binding rsulting in 10fold increase in binding of inhibitor at 0.15 M Na+, interacts with Y99, F174, and W215 via van der Waals interactions, and the charged amine coupling electrostatically with the carboxylates of E97	Homo sapiens

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	-	-	-

Reaction

Reaction	Comment	Organism	Reaction ID
selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin	scutelarin has similar specificity	Homo sapiens	a

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
L-Arg-Gly-Arg-4-nitroanilide + H2O	chromogenic substrate	Homo sapiens	L-Arg-Gly-Arg + 4-nitroaniline	-	?

Synonyms

Synonyms	Comment	Organism
More	the enzyme belongs to the peptidase family S1, i.e. trypsin family	Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C]	Temperature Optimum Maximum [°C]	Comment	Organism
25	-	assay at	Homo sapiens

pH Optimum

pH Optimum Minimum	pH Optimum Maximum	Comment	Organism
8	-	assay at	Homo sapiens

Ki Value [mM]

Ki Value [mM]	Ki Value maximum [mM]	Inhibitor	Comment	Organism	Structure
additional information	-	additional information	inhibition kinetics	Homo sapiens
0.085	-	4-aminobenzamidine	pH 8.0, 25°C, with wild-type enzyme	Homo sapiens
5	-	trimethylphenylammonium	pH 8.0, 25°C, with wild-type enzyme	Homo sapiens
20	-	trimethylphenylammonium	pH 8.0, 25°C, with mutant F174N enzyme	Homo sapiens
107	-	trimethylphenylammonium	pH 8.0, 25°C, with mutant Y99T enzyme	Homo sapiens

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Release 2023.1 (January 2023)