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Literature summary for 3.4.21.5 extracted from

  • Pineda, A.O.; Chen, Z.W.; Bah, A.; Garvey, L.C.; Mathews, F.S.; Di Cera, E.
    Crystal structure of thrombin in a self-inhibited conformation (2006), J. Biol. Chem., 281, 32922-32928.
    View publication on PubMed
Search for more literature for 3.4.21.5

Crystallization (Commentary)

Crystallization (Comment) Organism
D120N mutant thrombin slow enzyme form in a self-inhibited conformation, X-ray diffraction structure determination and analysis at 1.87 A resolution Homo sapiens

Protein Variants

Protein Variants Comment Organism
D120N site-directed mutagenesis, the mutant shows conformational changes compared to the wild-type enzyme Homo sapiens
R77aA site-directed mutagenesis, inactive mutant Homo sapiens
W215A site-directed mutagenesis, the mutation significantly compromises cleavage of the anticoagulant protein C but has no effect on the hydrolysis of fibrinogen and PAR1 Homo sapiens
W215P site-directed mutagenesis, the mutation significantly compromises cleavage of the anticoagulant protein C but has no effect on the hydrolysis of fibrinogen and PAR1 Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
Na+ the activating effect of Na+ on thrombin is allosteric and depends on the conformational transition from a low activity Na+-free, slow form to a high activity Na+-bound, fast form, overview, the Na+-free enzyme is in inactive conformation, Trp215, Arg187, and Arg221are involved, Na+ binding kinetics of wild-type and mutant enzymes, overview Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
fibrinogen + H2O Homo sapiens
-
 fibrin + ?
-
 ?
protease-activated receptor 1 + H2O Homo sapiens activation activated protease-activated receptor 1 + ?
-
 ?
protein C zymogen + H2O Homo sapiens activation activated protein C + propeptide
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
fibrinogen + H2O
-
 Homo sapiens fibrin + ?
-
 ?
protease-activated receptor 1 + H2O activation Homo sapiens activated protease-activated receptor 1 + ?
-
 ?
protein C zymogen + H2O activation Homo sapiens activated protein C + propeptide
-
 ?

Subunits

Subunits Comment Organism
More conformational transition from a low activity Na+-free, slow enzyme form to a high activity Na+-bound, fast enzyme form, overview, the Na+-free enzyme is in inactive conformation, Trp215. Arg187, and Arg221 are involved 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