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Literature summary for 3.4.21.22 extracted from

  • Sturzebecher, J.; Kopetzki, E.; Bode, W.; Hopfner, K.P.
    Dramatic enhancement of the catalytic activity of coagulation factor IXa by alcohols (1997), FEBS Lett., 412, 295-300.
    View publication on PubMed
Search for more literature for 3.4.21.22

Activating Compound

Activating Compound Comment Organism Structure
1,2-propanediol 25-40% v/v, up to 20fold increase of the activity, methoxycarbonyl-D-Nle-Gly-Arg-p-nitroanilide as substrate, rFIXa Homo sapiens
1,3-Propanediol affect the activity only to a slight extent Homo sapiens
1,3-Propanediol affect the activity only to a slight extent, rFIXa Homo sapiens
1,4-Butanediol affect the activity only to a slight extent, rFIXa Homo sapiens
diethylene glycol increases the activity 2fold Homo sapiens
ethanol 25% v/v, 6fold increase of the activity, methoxycarbonyl-D-Nle-Gly-Arg-p-nitroanilide as substrate, rFIXa, alcohols modify the conformation of FIXa rendering the active-site cleft more easily accessible to tripeptide substrates with a hydrophobic residue in the P3-position Homo sapiens
ethylene glycol 25-40% v/v, up to 20fold increase of the activity, methoxycarbonyl-D-Nle-Gly-Arg-p-nitroanilide as substrate, rFIXa Homo sapiens
glycerol 50% v/v, 6fold increase of the activity, methoxycarbonyl-D-Nle-Gly-Arg-p-nitroanilide as substrate, rFIXa Homo sapiens
i-erythritol 50% v/v, 1.5fold increase of the activity, methoxycarbonyl-D-Nle-Gly-Arg-p-nitroanilide as substrate, rFIXa Homo sapiens
methanol 25% v/v, 4fold increase of the activity, methoxycarbonyl-D-Nle-Gly-Arg-p-nitroanilide as substrate, rFIXa, alcohols modify the conformation of FIXa rendering the active-site cleft more easily accessible to tripeptide substrates with a hydrophobic residue in the P3-position Homo sapiens
tert-butanol up to 10% v/v, increase of the activity, higher concentrations lead to a drastic activity decrease, methoxycarbonyl-D-Nle-Gly-Arg-p-nitroanilide as substrate, rFIXa, alcohols modify the conformation of FIXa rendering the active-site cleft more easily accessible to tripeptide substrates with a hydrophobic residue in the P3-position Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
Polyethylene glycol inhibition with increasing concentration Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
1.43
-
 methylsulfonyl-D-cyclohexylglycyl-Gly-Arg-p-nitroanilide rFIXa, at pH 7.4, in the presence of 33% v/v ethylene glycol Homo sapiens
3.62
-
 methoxycarbonyl-D-Nle-Gly-Arg-p-nitroanilide rFIXa, at pH 7.4, in the presence of 33% v/v ethylene glycol Homo sapiens
5.99
-
 methylsulfonyl-D-hexahydrotyrosyl-Gly-Arg-p-nitroanilide rFIXa, at pH 7.4, in the presence of 33% v/v ethylene glycol Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
factor X + H2O Homo sapiens a chymotrypsin homologue, and one of the gamma-carboxyglutamic acid-containing blood coagulation factors. The proenzyme factor IX is activated by factor XIa ?
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
factor X + H2O a chymotrypsin homologue, and one of the gamma-carboxyglutamic acid-containing blood coagulation factors. The proenzyme factor IX is activated by factor XIa Homo sapiens ?
-
 ?
factor X + H2O
-
 Homo sapiens factor Xa
-
 ?
methoxycarbonyl-D-Nle-Gly-Arg-p-nitroanilide + H2O rFIXa, ethanol, 25% v/v enhances the activity 6fold, methanol 4fold, ethylene glycol, 25-40% v/v enhances the activity up to 20fold, glycerol, 50% v/v enhances the activity 6fold Homo sapiens ?
-
 ?
methylsulfonyl-D-cyclohexylglycyl-Gly-Arg-p-nitroanilide + H2O
-
 Homo sapiens methylsulfonyl-D-cyclohexylglycyl-Gly-Arg + 4-nitroaniline
-
 ?
methylsulfonyl-D-hexahydrotyrosyl-Gly-Arg-p-nitroanilide + H2O
-
 Homo sapiens ?
-
 ?

Synonyms

Synonyms Comment Organism
FIXa recombinant coagulation factor IXa, rFIXa Homo sapiens

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
2.01
-
 methoxycarbonyl-D-Nle-Gly-Arg-p-nitroanilide rFIXa, at pH 7.4, in the presence of 33% v/v ethylene glycol Homo sapiens
5.67
-
 methylsulfonyl-D-cyclohexylglycyl-Gly-Arg-p-nitroanilide rFIXa, at pH 7.4, in the presence of 33% v/v ethylene glycol Homo sapiens
6.11
-
 methylsulfonyl-D-hexahydrotyrosyl-Gly-Arg-p-nitroanilide rFIXa, at pH 7.4, in the presence of 33% v/v ethylene glycol Homo sapiens