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Literature summary for 3.4.21.22 extracted from

  • Misenheimer, T.M.; Sheehan, J.P.
    The regulation of factor IXa by supersulfated low molecular weight heparin (2010), Biochemistry, 49, 9997-10005.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

Cloned (Comment) Organism
expressed in HEK-293 cells Homo sapiens

Protein Variants

Protein Variants Comment Organism
K126A the mutation dramatically (11fold) reduces supersulfated low molecular weight heparin affinity Homo sapiens
K132A the mutation dramatically (20fold) reduces supersulfated low molecular weight heparin affinity Homo sapiens
N129A the mutation moderately (5fold) reduces supersulfated low molecular weight heparin affinity Homo sapiens
N178A the mutant shows wild type affinity towards supersulfated low molecular weight heparin Homo sapiens
R165A the mutation moderately (5fold) reduces supersulfated low molecular weight heparin affinity Homo sapiens
R170A the mutation slightly (0.5fold) reduces supersulfated low molecular weight heparin affinity Homo sapiens
R233A the mutation dramatically (14fold) reduces supersulfated low molecular weight heparin affinity Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
supersulfated low molecular weight heparin inhibits the intrinsic tenase (factor IXa-factor VIIIa) complex in an antithrombin-independent manner by 90% when using factor X as substrate. Supersulfated low molecular weight heparin is 32fold more potent than unmodified low molecular weight heparin in the inhibition of factor X activation by the intrinsic tenase complex Homo sapiens
unmodified low molecular weight heparin
-
Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
Factor X + H2O Homo sapiens
-
Factor Xa + ?
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Factor X + H2O
-
Homo sapiens Factor Xa + ?
-
?
Nalpha-benzyloxycarbonyl-D-Arg-Gly-Arg-4-nitroanilide + H2O S-2765 Homo sapiens Nalpha-benzyloxycarbonyl-D-Arg-Gly-Arg + 4-nitroaniline
-
?
Pefachrome IXa + H2O i.e. CH3O2-D-CHG-Gly-Arg-4-nitroanilide Homo sapiens ?
-
?

Synonyms

Synonyms Comment Organism
factor IXa
-
Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0000025
-
supersulfated low molecular weight heparin mutant enzyme R170A, using factor X as substrate, at pH 7.4, 22┬░C Homo sapiens
0.000003
-
supersulfated low molecular weight heparin wild type enzyme, using factor X as substrate, at pH 7.4, 22┬░C Homo sapiens
0.0000039
-
supersulfated low molecular weight heparin mutant enzyme N178A, using factor X as substrate, at pH 7.4, 22┬░C Homo sapiens
0.0000042
-
supersulfated low molecular weight heparin mutant enzyme N129A, using factor X as substrate, at pH 7.4, 22┬░C Homo sapiens
0.00001
-
supersulfated low molecular weight heparin mutant enzyme K132A, using factor X as substrate, at pH 7.4, 22┬░C Homo sapiens
0.00001
-
unmodified low molecular weight heparin mutant enzyme N129A, using factor X as substrate, at pH 7.4, 22┬░C Homo sapiens
0.000012
-
unmodified low molecular weight heparin mutant enzyme R170A, using factor X as substrate, at pH 7.4, 22┬░C Homo sapiens
0.000012
-
unmodified low molecular weight heparin wild type enzyme, using factor X as substrate, at pH 7.4, 22┬░C Homo sapiens
0.0000141
-
unmodified low molecular weight heparin mutant enzyme N178A, using factor X as substrate, at pH 7.4, 22┬░C Homo sapiens
0.000017
-
supersulfated low molecular weight heparin mutant enzyme R165A, using factor X as substrate, at pH 7.4, 22┬░C Homo sapiens
0.000049
-
unmodified low molecular weight heparin mutant enzyme K132A, using factor X as substrate, at pH 7.4, 22┬░C Homo sapiens
0.000072
-
supersulfated low molecular weight heparin mutant enzyme K126A, using factor X as substrate, at pH 7.4, 22┬░C Homo sapiens
0.00016
-
unmodified low molecular weight heparin mutant enzyme R165A, using factor X as substrate, at pH 7.4, 22┬░C Homo sapiens
0.00017
-
supersulfated low molecular weight heparin mutant enzyme R233A, using factor X as substrate, at pH 7.4, 22┬░C Homo sapiens
0.00032
-
unmodified low molecular weight heparin mutant enzyme K126A, using factor X as substrate, at pH 7.4, 22┬░C Homo sapiens
0.00147
-
unmodified low molecular weight heparin mutant enzyme R233A, using factor X as substrate, at pH 7.4, 22┬░C Homo sapiens