BRENDA - Enzyme Database show
show all sequences of 3.4.21.22

Dramatic enhancement of the catalytic activity of coagulation factor IXa by alcohols

Sturzebecher, J.; Kopetzki, E.; Bode, W.; Hopfner, K.P.; FEBS Lett. 412, 295-300 (1997)

Data extracted from this reference:

Activating Compound
Activating Compound
Commentary
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; 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
Commentary
Organism
Structure
Polyethylene glycol
inhibition with increasing concentration
Homo sapiens
KM Value [mM]
KM Value [mM]
KM Value Maximum [mM]
Substrate
Commentary
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
Commentary (Nat. Sub.)
Natural Products
Commentary (Nat. Pro.)
Organism (Nat. Pro.)
Reversibility
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
Primary Accession No. (UniProt)
Commentary
Textmining
Homo sapiens
-
-
-
Substrates and Products (Substrate)
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
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
95341
Homo sapiens
?
-
-
-
-
factor X + H2O
-
95341
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
95341
Homo sapiens
?
-
-
-
?
methylsulfonyl-D-cyclohexylglycyl-Gly-Arg-p-nitroanilide + H2O
-
95341
Homo sapiens
methylsulfonyl-D-cyclohexylglycyl-Gly-Arg + 4-nitroaniline
-
-
-
?
methylsulfonyl-D-hexahydrotyrosyl-Gly-Arg-p-nitroanilide + H2O
-
95341
Homo sapiens
?
-
-
-
?
Turnover Number [1/s]
Turnover Number Minimum [1/s]
Turnover Number Maximum [1/s]
Substrate
Commentary
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
Activating Compound (protein specific)
Activating Compound
Commentary
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; 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 (protein specific)
Inhibitors
Commentary
Organism
Structure
Polyethylene glycol
inhibition with increasing concentration
Homo sapiens
KM Value [mM] (protein specific)
KM Value [mM]
KM Value Maximum [mM]
Substrate
Commentary
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) (protein specific)
Natural Substrates
Organism
Commentary (Nat. Sub.)
Natural Products
Commentary (Nat. Pro.)
Organism (Nat. Pro.)
Reversibility
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
?
-
-
-
Substrates and Products (Substrate) (protein specific)
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
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
95341
Homo sapiens
?
-
-
-
-
factor X + H2O
-
95341
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
95341
Homo sapiens
?
-
-
-
?
methylsulfonyl-D-cyclohexylglycyl-Gly-Arg-p-nitroanilide + H2O
-
95341
Homo sapiens
methylsulfonyl-D-cyclohexylglycyl-Gly-Arg + 4-nitroaniline
-
-
-
?
methylsulfonyl-D-hexahydrotyrosyl-Gly-Arg-p-nitroanilide + H2O
-
95341
Homo sapiens
?
-
-
-
?
Turnover Number [1/s] (protein specific)
Turnover Number Minimum [1/s]
Turnover Number Maximum [1/s]
Substrate
Commentary
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
Other publictions for EC 3.4.21.22
No.
1st author
Pub Med
title
organims
journal
volume
pages
year
Activating Compound
Application
Cloned(Commentary)
Crystallization (Commentary)
Engineering
General Stability
Inhibitors
KM Value [mM]
Localization
Metals/Ions
Molecular Weight [Da]
Natural Substrates/ Products (Substrates)
Organic Solvent Stability
Organism
Oxidation Stability
Posttranslational Modification
Purification (Commentary)
Reaction
Renatured (Commentary)
Source Tissue
Specific Activity [micromol/min/mg]
Storage Stability
Substrates and Products (Substrate)
Subunits
Temperature Optimum [°C]
Temperature Range [°C]
Temperature Stability [°C]
Turnover Number [1/s]
pH Optimum
pH Range
pH Stability
Cofactor
Ki Value [mM]
pI Value
IC50 Value
Activating Compound (protein specific)
Application (protein specific)
Cloned(Commentary) (protein specific)
Cofactor (protein specific)
Crystallization (Commentary) (protein specific)
Engineering (protein specific)
General Stability (protein specific)
IC50 Value (protein specific)
Inhibitors (protein specific)
Ki Value [mM] (protein specific)
KM Value [mM] (protein specific)
Localization (protein specific)
Metals/Ions (protein specific)
Molecular Weight [Da] (protein specific)
Natural Substrates/ Products (Substrates) (protein specific)
Organic Solvent Stability (protein specific)
Oxidation Stability (protein specific)
Posttranslational Modification (protein specific)
Purification (Commentary) (protein specific)
Renatured (Commentary) (protein specific)
Source Tissue (protein specific)
Specific Activity [micromol/min/mg] (protein specific)
Storage Stability (protein specific)
Substrates and Products (Substrate) (protein specific)
Subunits (protein specific)
Temperature Optimum [°C] (protein specific)
Temperature Range [°C] (protein specific)
Temperature Stability [°C] (protein specific)
Turnover Number [1/s] (protein specific)
pH Optimum (protein specific)
pH Range (protein specific)
pH Stability (protein specific)
pI Value (protein specific)
Expression
General Information
General Information (protein specific)
Expression (protein specific)
KCat/KM [mM/s]
KCat/KM [mM/s] (protein specific)
731259
Venkateswarlu
Structural insights into the i ...
Homo sapiens
Biochem. Biophys. Res. Commun.
452
408-414
2014
1
-
-
-
-
-
-
-
-
-
-
1
-
1
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
732759
Majumder
Soluble phosphatidylserine bin ...
Homo sapiens
PLoS ONE
9
e100006
2014
2
-
-
-
-
-
-
-
-
-
-
1
-
3
-
-
-
-
-
-
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
731813
Branchini
Replacement of the Y450 (c234) ...
Homo sapiens
FEBS Lett.
587
3249-3253
2013
-
-
-
-
3
-
-
-
-
-
1
1
-
1
-
-
-
-
-
-
-
-
1
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
3
-
-
-
-
-
-
-
1
1
-
-
-
-
-
-
-
-
1
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
732094
Yang
Residues of the 39-loop restri ...
Bos taurus, Mus musculus
J. Biol. Chem.
288
12692-12698
2013
-
-
-
-
-
-
2
-
-
-
-
2
-
4
-
-
-
-
-
2
-
-
4
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
2
-
-
-
-
-
2
-
-
-
-
-
2
-
-
4
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
732114
Bloem
A3 domain region 1803-1818 con ...
Homo sapiens
J. Biol. Chem.
288
26105-26111
2013
1
-
-
-
-
-
-
-
-
-
-
1
-
1
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
732118
Wakabayashi
Replacing the factor VIII C1 d ...
Homo sapiens
J. Biol. Chem.
288
31289-31297
2013
1
-
-
-
-
-
-
-
-
-
-
1
-
1
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
732043
Sullenger
Potent anticoagulant aptamer d ...
Homo sapiens
J. Biol. Chem.
287
12779-12786
2012
2
-
-
-
-
-
1
-
-
-
-
1
-
3
-
-
1
-
-
1
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
2
-
-
-
-
-
-
-
1
-
-
-
-
-
1
-
-
-
1
-
1
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
732075
Geng
A sequential mechanism for exo ...
Homo sapiens
J. Biol. Chem.
287
38200-38209
2012
1
-
-
-
-
-
-
-
-
-
-
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
732403
Neuenschwander
Correlation of factor IXa subs ...
Homo sapiens
J. Thromb. Haemost.
10
382-389
2012
2
-
-
-
-
-
-
-
-
1
-
1
-
1
-
-
-
-
-
-
-
-
6
-
-
-
-
-
-
-
-
-
-
-
-
2
-
-
-
-
-
-
-
-
-
-
-
1
-
1
-
-
-
-
-
-
-
-
6
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
718138
Chang
Sustained release of transgeni ...
Homo sapiens
Mol. Pharm.
8
1767-1774
2011
1
1
1
-
-
-
-
-
-
-
-
-
-
3
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
1
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
718434
Cunha
Accumulation of functional rec ...
Homo sapiens
Transgenic Res.
20
841-855
2011
1
-
1
-
-
-
-
-
-
-
1
2
-
4
-
-
-
-
-
2
-
1
2
1
-
-
-
-
-
-
-
-
-
-
-
1
-
1
-
-
-
-
-
-
-
-
-
-
1
2
-
-
-
-
-
2
-
1
2
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
717103
Hosseini
A study of the expression of f ...
Homo sapiens
Appl. Biochem. Biotechnol.
162
1599-1611
2010
-
-
1
-
-
-
-
-
-
-
1
2
-
3
-
-
-
-
-
2
-
-
2
1
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
1
2
-
-
-
-
-
2
-
-
2
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
717254
Misenheimer
The regulation of factor IXa b ...
Homo sapiens
Biochemistry
49
9997-10005
2010
-
-
1
-
7
-
2
-
-
-
-
1
-
1
-
-
-
-
-
-
-
-
3
-
-
-
-
-
-
-
-
-
15
-
-
-
-
1
-
-
7
-
-
2
15
-
-
-
-
1
-
-
-
-
-
-
-
-
3
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
717800
Yang
Role of the residues of the 39 ...
Homo sapiens
J. Biol. Chem.
285
28488-28495
2010
1
-
-
-
1
-
1
4
-
-
-
1
-
1
-
-
-
-
-
1
-
-
2
-
-
-
-
4
-
-
-
-
-
-
-
1
-
-
-
-
1
-
-
1
-
4
-
-
-
1
-
-
-
-
-
1
-
-
2
-
-
-
-
4
-
-
-
-
-
-
-
-
4
4
717963
Wang
Studies of benzothiophene temp ...
Homo sapiens
J. Med. Chem.
53
1465-1472
2010
-
-
1
-
-
-
35
-
-
-
-
-
-
1
-
-
1
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
36
-
-
-
-
1
-
-
-
-
-
35
36
-
-
-
-
-
-
-
-
1
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
717964
Wang
Structure based drug design: d ...
Homo sapiens
J. Med. Chem.
53
1473-1482
2010
-
-
-
-
-
-
39
-
-
-
-
-
-
1
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
39
-
-
-
-
-
-
-
-
-
-
39
39
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
718322
Johnson
Molecular basis of factor IXa ...
Homo sapiens
Proc. Natl. Acad. Sci. USA
107
645-650
2010
1
-
1
1
-
-
1
-
-
2
-
1
-
1
-
-
1
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
1
-
1
-
1
-
-
-
1
-
-
-
2
-
1
-
-
-
1
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
2
2
-
-
-
718429
Wu
Mg(II)-induced binding of fact ...
Homo sapiens
Toxicon
55
1358-1364
2010
-
-
-
-
-
-
-
-
-
1
-
1
-
2
-
-
-
-
-
1
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
1
-
-
-
-
-
1
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
691159
Zoegg
Activation mechanisms of coagu ...
Homo sapiens
Biol. Chem.
390
391-400
2009
1
-
-
-
-
-
-
-
-
2
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
693470
Yang
Novel autoantibodies against t ...
Homo sapiens
J. Immunol.
182
1674-1680
2009
-
-
-
-
-
-
-
-
-
-
-
-
-
2
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
707152
Becker
Antidote-controlled antithromb ...
Homo sapiens
Ann. N. Y. Acad. Sci.
1175
61-70
2009
-
1
-
-
-
-
1
-
-
-
-
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
708509
Gettins
Activation of antithrombin as ...
Homo sapiens
FEBS Lett.
583
3397-3400
2009
-
-
-
-
-
-
1
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
709195
Kim
Effect of Ca2+ and Mg2+ concen ...
Homo sapiens
J. Biotechnol.
142
275-278
2009
-
-
1
-
-
-
-
-
-
2
-
-
-
3
-
-
-
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
2
-
-
-
-
-
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
709724
Hartmann
Factor IX mutants with enhance ...
Homo sapiens
J. Thromb. Haemost.
7
1656-1662
2009
1
-
-
-
5
-
-
10
-
-
1
3
-
1
-
-
1
-
-
2
-
-
3
-
-
-
-
12
-
-
-
-
-
-
-
1
-
-
-
-
5
-
-
-
-
10
-
-
1
3
-
-
-
1
-
2
-
-
3
-
-
-
-
12
-
-
-
-
-
-
-
-
16
16
710578
Zögg
Structural basis of the cofact ...
Homo sapiens
Structure
17
1669-1678
2009
-
-
1
1
-
-
-
-
-
-
-
-
-
2
-
-
1
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
683827
Scheiflinger
Enhancement of the enzymatic a ...
Homo sapiens
J. Thromb. Haemost.
6
315-322
2008
3
-
-
-
-
-
-
-
1
2
-
1
-
2
-
-
-
-
-
2
-
-
2
-
1
-
-
-
1
-
-
-
-
-
-
3
-
-
-
-
-
-
-
-
-
-
1
2
-
1
-
-
-
-
-
2
-
-
2
-
1
-
-
-
1
-
-
-
-
-
-
-
-
-
683165
Misenheimer
The heparin-binding exosite is ...
Homo sapiens
Biochemistry
46
7886-7895
2007
3
-
1
-
5
-
1
12
1
2
-
1
-
2
-
1
-
-
-
2
1
-
3
-
1
-
-
11
1
-
-
-
-
-
-
3
-
1
-
-
5
-
-
1
-
12
1
2
-
1
-
-
1
-
-
2
1
-
3
-
1
-
-
11
1
-
-
-
-
-
-
-
-
-
683154
London
PAR-1-stimulated factor IXa bi ...
Homo sapiens
Biochemistry
45
7289-7298
2006
-
-
-
-
-
-
-
-
-
1
-
1
-
1
-
-
-
-
-
1
-
-
1
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
1
-
-
-
-
-
1
-
-
1
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
683625
Neuenschwander
Heparin modulates the 99-loop ...
Homo sapiens
J. Biol. Chem.
281
23066-23074
2006
2
-
1
-
2
-
6
-
1
1
-
1
-
1
-
1
1
-
-
2
-
-
3
-
1
-
-
-
1
-
-
-
1
-
-
2
-
1
-
-
2
-
-
6
1
-
1
1
-
1
-
-
1
1
-
2
-
-
3
-
1
-
-
-
1
-
-
-
-
-
-
-
-
-
683821
Gale
Intrinsic stability and functi ...
Homo sapiens
J. Thromb. Haemost.
4
1315-1322
2006
2
-
-
-
-
-
-
-
1
-
-
1
-
1
-
-
-
-
-
2
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
2
-
-
-
-
-
-
-
-
-
-
1
-
-
1
-
-
-
-
-
2
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
684024
Yang
Expression, purification and c ...
Homo sapiens
Protein Expr. Purif.
50
196-202
2006
1
-
1
-
3
-
1
2
-
2
-
2
-
1
-
1
1
-
-
1
-
-
5
1
1
-
-
2
1
-
-
-
-
-
-
1
-
1
-
-
3
-
-
1
-
2
-
2
-
2
-
-
1
1
-
1
-
-
5
1
1
-
-
2
1
-
-
-
-
-
-
-
-
-
684077
Gopalakrishna
The influence of sodium ion bi ...
Homo sapiens
Thromb. Haemost.
95
936-941
2006
1
-
-
-
-
-
3
4
1
3
-
1
-
1
-
-
-
-
-
2
1
-
2
-
1
-
-
5
1
-
-
-
-
-
-
1
-
-
-
-
-
-
-
3
-
4
1
3
-
1
-
-
-
-
-
2
1
-
2
-
1
-
-
5
1
-
-
-
-
-
-
-
-
-
667506
Yang
An ordered sequential mechanis ...
Homo sapiens
Biochem. J.
390
157-167
2005
1
-
1
-
-
-
-
9
-
-
2
1
-
1
-
-
1
-
-
-
-
-
1
1
-
-
-
4
-
-
-
-
-
-
-
1
-
1
-
-
-
-
-
-
-
9
-
-
2
1
-
-
-
1
-
-
-
-
1
1
-
-
-
4
-
-
-
-
-
-
-
-
-
-
667957
Qiao
5-Amidinobenzo[b]thiophenes as ...
Homo sapiens
Bioorg. Med. Chem. Lett.
15
29-35
2005
-
1
-
-
-
-
33
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
33
-
-
-
1
-
-
-
-
-
-
33
33
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
669860
Schmidt
Na+ site in blood coagulation ...
Homo sapiens
J. Mol. Biol.
350
78-91
2005
4
-
1
-
1
-
2
8
-
1
1
-
-
1
-
-
1
-
-
-
-
-
3
-
-
-
-
8
-
-
-
-
7
-
-
4
-
1
-
-
1
-
-
2
7
8
-
1
1
-
-
-
-
1
-
-
-
-
3
-
-
-
-
8
-
-
-
-
-
-
-
-
-
-
670057
Ndonwi
The first epidermal growth fac ...
Homo sapiens
J. Thromb. Haemost.
3
112-118
2005
1
-
1
-
-
-
-
-
-
-
-
-
-
1
-
-
1
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
1
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
667479
Panteleev
Kinetics of Factor X activatio ...
Homo sapiens
Biochem. J.
381
779-794
2004
1
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
667599
Neuenschwander
Exosite occupation by heparin ...
Homo sapiens
Biochemistry
43
2978-2986
2004
2
-
-
-
-
-
3
-
-
-
-
1
-
2
-
-
-
-
-
-
-
-
3
-
-
-
-
-
-
-
-
-
3
-
-
2
-
-
-
-
-
-
-
3
3
-
-
-
-
1
-
-
-
-
-
-
-
-
3
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
667946
Batt
5-Amidinoindoles as dual inhib ...
Homo sapiens
Bioorg. Med. Chem. Lett.
14
5269-5273
2004
-
1
-
-
-
-
25
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
25
-
-
-
1
-
-
-
-
-
-
25
25
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
669217
Lu
Formation of factors IXa and X ...
Homo sapiens
J. Biol. Chem.
279
17241-17249
2004
1
-
-
-
-
-
-
1
-
-
-
-
-
1
-
-
-
-
-
1
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
1
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
669228
Butenas
The significance of circulatin ...
Homo sapiens
J. Biol. Chem.
279
22875-22882
2004
-
-
-
-
-
-
1
1
-
-
-
-
-
2
-
-
-
-
-
1
-
-
1
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
1
-
-
-
-
-
-
-
-
-
1
-
-
1
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
669281
Yang
Identification of residues Asn ...
Homo sapiens
J. Biol. Chem.
279
46400-46405
2004
-
-
1
-
7
-
-
15
-
-
-
1
-
1
-
-
1
-
-
-
-
-
3
-
-
-
-
7
-
-
-
-
-
-
-
-
-
1
-
-
7
-
-
-
-
15
-
-
-
1
-
-
-
1
-
-
-
-
3
-
-
-
-
7
-
-
-
-
-
-
-
-
-
-
650224
Bedsted
Heparin and calcium ions drama ...
Homo sapiens
Biochemistry
42
8143-8152
2003
1
-
-
-
-
-
1
-
-
1
-
1
-
1
-
-
-
-
-
-
-
-
3
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
1
-
-
-
1
-
1
-
-
-
-
-
-
-
-
3
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
652413
Yang
Contribution of basic residues ...
Homo sapiens
J. Biol. Chem.
278
25032-25038
2003
2
-
1
-
4
-
-
1
-
1
-
1
-
1
-
-
1
-
-
-
-
-
2
-
-
-
-
2
-
-
-
-
-
-
-
2
-
1
-
-
4
-
-
-
-
1
-
1
-
1
-
-
-
1
-
-
-
-
2
-
-
-
-
2
-
-
-
-
-
-
-
-
-
-
652433
Blostein
The Gla domain of factor IXa b ...
Homo sapiens
J. Biol. Chem.
278
31297-31302
2003
1
-
-
-
-
-
1
-
-
-
-
1
-
1
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
1
-
-
-
1
-
-
1
-
-
-
-
1
-
-
-
-
-
1
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
652454
Wiebe
Mechanism of catalysis of inhi ...
Homo sapiens
J. Biol. Chem.
278
35767-35774
2003
-
-
-
-
-
-
1
-
-
-
-
1
-
1
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
1
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
652507
Rohlena
Residues Phe342-Asn346 of acti ...
Homo sapiens
J. Biol. Chem.
278
9394-9401
2003
2
-
1
-
2
-
1
-
-
1
-
1
-
1
-
-
1
-
-
1
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
2
-
1
-
-
2
-
-
1
-
-
-
1
-
1
-
-
-
1
-
1
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
650104
Ahmad
Coordinate binding studies of ...
Homo sapiens
Biochemistry
41
11269-11276
2002
2
-
-
-
-
-
-
-
-
1
-
1
-
1
-
1
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
2
-
-
-
-
-
-
-
-
-
-
-
1
-
1
-
-
1
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
652345
Wilkinson
Residues 88-109 of factor IXa ...
Homo sapiens
J. Biol. Chem.
277
5725-5733
2002
1
-
1
-
2
-
-
3
-
-
-
1
-
1
-
-
1
-
-
-
-
-
1
-
-
-
-
-
-
-
-
1
-
-
-
1
-
1
1
-
2
-
-
-
-
3
-
-
-
1
-
-
-
1
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
653340
Rusconi
RNA aptamers as reversible ant ...
Homo sapiens
Nature
419
90-94
2002
-
-
-
-
-
-
1
-
-
-
-
1
-
2
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
1
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
652114
Bajaj
Factor IXa:factor VIIIa intera ...
Homo sapiens
J. Biol. Chem.
276
16302-16309
2001
2
-
-
-
1
-
-
1
-
1
-
1
-
1
-
-
-
-
-
1
-
-
1
-
-
-
-
1
-
-
-
-
-
-
-
2
-
-
-
-
1
-
-
-
-
1
-
1
-
1
-
-
-
-
-
1
-
-
1
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
95343
London
Zymogen factor IX potentiates ...
Homo sapiens
Biochemistry
39
9850-9858
2000
1
-
-
-
-
-
-
-
-
-
-
1
-
1
-
-
-
-
-
-
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
649923
Blostein
Amphipathic helices support fu ...
Homo sapiens
Biochemistry
39
12000-12006
2000
4
-
-
-
-
-
-
3
-
1
-
1
-
1
-
-
-
-
-
-
-
-
1
-
-
-
-
3
-
-
-
-
-
-
-
4
-
-
-
-
-
-
-
-
-
3
-
1
-
1
-
-
-
-
-
-
-
-
1
-
-
-
-
3
-
-
-
-
-
-
-
-
-
-
649933
Falls
Role of phosphatidylethanolami ...
Homo sapiens
Biochemistry
39
13216-13222
2000
2
-
-
-
-
-
-
2
-
1
-
1
-
1
-
-
-
-
-
-
-
-
1
-
-
-
-
3
-
-
-
-
-
-
-
2
-
-
-
-
-
-
-
-
-
2
-
1
-
1
-
-
-
-
-
-
-
-
1
-
-
-
-
3
-
-
-
-
-
-
-
-
-
-
95344
Hopfner
Coagulation factor IXa: the re ...
Homo sapiens
Structure Fold. Des.
7
989-996
1999
-
-
-
1
-
-
-
-
-
-
-
1
-
3
-
-
-
-
-
-
-
-
3
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
3
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
95345
Fay
The A1 and the A2 subunits of ...
Homo sapiens
J. Biol. Chem.
274
15401-15406
1999
1
-
-
-
-
-
-
-
-
-
-
1
-
1
-
-
-
-
-
-
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
95341
Sturzebecher
Dramatic enhancement of the ca ...
Homo sapiens
FEBS Lett.
412
295-300
1997
10
-
-
-
-
-
1
3
-
-
-
1
-
2
-
-
-
-
-
-
-
-
5
-
-
-
-
3
-
-
-
-
-
-
-
10
-
-
-
-
-
-
-
1
-
3
-
-
-
1
-
-
-
-
-
-
-
-
5
-
-
-
-
3
-
-
-
-
-
-
-
-
-
-
95342
Morita
gamma-Carboxylglutamic acid (G ...
Bos taurus
J. Biochem.
110
990-996
1991
-
-
-
-
-
-
-
6
-
-
2
2
-
2
-
-
1
-
-
-
-
-
3
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
6
-
-
2
2
-
-
-
1
-
-
-
-
3
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
95346
Ahmed
Comparative platelet binding a ...
Homo sapiens
J. Biol. Chem.
265
20907-20911
1990
1
-
-
-
2
-
-
3
-
-
-
1
-
2
-
-
-
-
-
-
-
-
2
-
-
-
-
6
-
-
-
-
-
-
-
1
-
-
-
-
2
-
-
-
-
3
-
-
-
1
-
-
-
-
-
-
-
-
2
-
-
-
-
6
-
-
-
-
-
-
-
-
-
-
95337
Thompson
Structure, function and molecu ...
Homo sapiens
Blood
67
565-572
1986
3
-
-
-
-
-
1
-
-
1
-
1
-
1
-
-
-
-
-
2
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
3
-
-
-
-
-
-
-
1
-
-
-
1
-
1
-
-
-
-
-
2
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
95338
Van Dieijen
-
Purification of coagulation fa ...
Bos taurus
Methods Enzym. Anal. , 3rd Ed. (Bergmeyer, H. U. , ed. )
5
390-394
1986
-
-
-
-
-
-
-
-
-
-
1
1
-
1
-
-
1
-
-
1
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
1
-
-
-
1
-
1
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
95339
Osterud
Human blood coagulation factor ...
Homo sapiens
J. Biol. Chem.
253
5946-5951
1978
-
-
-
-
-
-
-
-
-
1
3
1
-
2
-
-
1
-
-
1
-
-
2
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
3
1
-
-
-
1
-
1
-
-
2
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
36535
Fujikawa
The mechanism of activation of ...
Bos taurus
Biochemistry
13
4508-4516
1974
-
-
-
-
-
-
-
-
-
-
3
1
-
2
-
-
1
1
-
1
-
1
2
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
3
1
-
-
-
1
-
1
-
1
2
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-