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Literature summary for 3.4.21.68 extracted from

  • Ke, S.H.; Tachias, K.; Lamba, D.; Bode, W.; Madison, E.L.
    Identification of a hydrophobic exosite on tissue type plasminogen activator that modulates specificity for plasminogen (1997), J. Biol. Chem., 272, 1811-1816.
    View publication on PubMed

Activating Compound

Activating Compound Comment Organism Structure
Fibrin activity of wild-type t-PA is stimulated by Homo sapiens

Application

Application Comment Organism
medicine t-PA has been widely and successfully used as a therapeutic fibrinolytic agent to treat acute myocardial infarction and pulmonary embolism Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
hybridoma cell lines expressing Mabs expression of wild-type and mutant enzyme cDNA by transient transfection of COS cells Homo sapiens

Protein Variants

Protein Variants Comment Organism
F423A two chain form, site-directed mutagenesis Homo sapiens
F423A/R275E single-chain form, site-directed mutagenesis Homo sapiens
F423E two chain form, site-directed mutagenesis Homo sapiens
F423E/R275E single-chain form, site-directed mutagenesis Homo sapiens
L420A two chain form, site-directed mutagenesis Homo sapiens
L420A/R275E single-chain form, site-directed mutagenesis Homo sapiens
L420E two chain form, site-directed mutagenesis Homo sapiens
L420E/R275E single-chain form, site-directed mutagenesis Homo sapiens
P422A two chain form, site-directed mutagenesis Homo sapiens
P422A/R275E single-chain form, site-directed mutagenesis Homo sapiens
P422E/R275E single-chain form, site-directed mutagenesis Homo sapiens
P422G/R275E single-chain form, site-directed mutagenesis Homo sapiens
R275E single-chain form, site-directed mutagenesis Homo sapiens
R275E/P422E site-directed mutagenesis Homo sapiens
R275E/P422G site-directed mutagenesis Homo sapiens
S421E two chain form, site-directed mutagenesis Homo sapiens
S421E/R275E single-chain form, site-directed mutagenesis Homo sapiens
S421G two chain form, site-directed mutagenesis Homo sapiens
S421G/R275E single-chain form, site-directed mutagenesis Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.00001
-
Lys-plasminogen pH 7.2, 37°C, mutant R275E and P422A/R275E, single-chain form, presence of soluble fibrin Homo sapiens
0.000011
-
Lys-plasminogen pH 7.2, 37°C, wild-type, two-chain form, presence of soluble fibrin Homo sapiens
0.000013
-
Lys-plasminogen pH 7.2, 37°C, mutant P422A, two-chain form, presence of soluble fibrin Homo sapiens
0.000014
-
Lys-plasminogen pH 7.2, 37°C, two-chain form of mutant F423A, single-chain form of mutant L420A/R275E, presence of soluble fibrin Homo sapiens
0.000015
-
Lys-plasminogen pH 7.2, 37°C, mutant F423E/R275E, single-chain form, presence of soluble fibrin Homo sapiens
0.000016
-
Lys-plasminogen pH 7.2, 37°C, mutant S421G, two-chain form, presence of soluble fibrin Homo sapiens
0.000018
-
Lys-plasminogen pH 7.2, 37°C, two-chain form of mutant S421E, single-chain form of mutant L420E/R275E, presence of soluble fibrin Homo sapiens
0.000019
-
Lys-plasminogen pH 7.2, 37°C, mutant L420A, two-chain form, presence of soluble fibrin Homo sapiens
0.000021
-
Lys-plasminogen pH 7.2, 37°C, mutant L420E, two-chain form, presence of soluble fibrin Homo sapiens
0.000022
-
Lys-plasminogen pH 7.2, 37°C, mutant F423A/R275E, single-chain form, presence of soluble fibrin Homo sapiens
0.000023
-
Lys-plasminogen pH 7.2, 37°C, two-chain form of mutant F423E, single-chain form of mutant S421E/R275E, presence of soluble fibrin Homo sapiens
0.000026
-
Lys-plasminogen pH 7.2, 37°C, two-chain form of mutant P422G, single-chain form of mutant S421G/R275E, presence of soluble fibrin Homo sapiens
0.000027
-
Lys-plasminogen pH 7.2, 37°C, mutant P422G/R275E, single-chain form, presence of soluble fibrin Homo sapiens
0.000028
-
Lys-plasminogen pH 7.2, 37°C, mutant P422E/R275E, single-chain form, presence of soluble fibrin Homo sapiens
0.000029
-
Lys-plasminogen pH 7.2, 37°C, mutant P422E, two-chain form, presence of soluble fibrin Homo sapiens
0.0006
-
Lys-plasminogen pH 7.2, 37°C, mutant P422G, two-chain form, absence of soluble fibrin Homo sapiens
0.0007
-
Lys-plasminogen pH 7.2, 37°C, mutant L420E and P422E, two-chain form, absence of soluble fibrin Homo sapiens
0.001
-
Lys-plasminogen pH 7.2, 37°C, mutant L420A, two-chain form, absence of soluble fibrin Homo sapiens
0.003
-
Lys-plasminogen pH 7.2, 37°C, mutant S421E, two-chain form, absence of soluble fibrin Homo sapiens
0.004
-
Lys-plasminogen pH 7.2, 37°C, two-chain form of mutant S421G, F423A and P422A, single chain form of mutant S421G/R275E and P422G/R275E, absence of soluble fibrin Homo sapiens
0.005
-
Lys-plasminogen pH 7.2, 37°C, mutant L420E/R275E, single-chain form, absence of soluble fibrin Homo sapiens
0.005
-
Lys-plasminogen pH 7.2, 37°C, two-chain form of wild-type and mutant F423E, single-chain form of mutant P422E/R275E, absence of soluble fibrin Homo sapiens
0.007
-
Lys-plasminogen pH 7.2, 37°C, mutant S421E/R275E, single-chain form, absence of soluble fibrin Homo sapiens
0.008
-
Lys-plasminogen pH 7.2, 37°C, mutant F423E/R275E, single-chain form, absence of soluble fibrin Homo sapiens
0.009
-
Lys-plasminogen pH 7.2, 37°C, mutant L420A/R275E, single-chain form, absence of soluble fibrin Homo sapiens
0.01
-
Lys-plasminogen pH 7.2, 37°C, mutant F423A/R275E, single-chain form, absence of soluble fibrin Homo sapiens
0.013
-
Lys-plasminogen pH 7.2, 37°C, mutant P422A/R275E, single-chain form, absence of soluble fibrin Homo sapiens
0.017
-
Lys-plasminogen pH 7.2, 37°C, mutant R275E, single-chain form, absence of soluble fibrin Homo sapiens
0.4
-
spectrozyme tPA pH 7.2, 37°C, wild-type t-PA, mutant L420A, L420E, S421G, S421E, P422A, P422E, two-chain form Homo sapiens
0.5
-
spectrozyme tPA pH 7.2, 37°C, mutant F423A, F422E, two-chain form Homo sapiens
0.6
-
spectrozyme tPA pH 7.2, 37°C, P422G, two-chain form Homo sapiens
0.9
-
spectrozyme tPA pH 7.2, 37°C, mutant L420E/R275E, F423E/R275E, single chain form Homo sapiens
1
-
spectrozyme tPA pH 7.2, 37°C, mutant R275E, F423A/R275E, single-chain form Homo sapiens
1.1
-
spectrozyme tPA pH 7.2, 37°C, mutant P422E/R275E, single chain form Homo sapiens
1.2
-
spectrozyme tPA pH 7.2, 37°C, mutant P422A/R275E, single chain form Homo sapiens
1.3
-
spectrozyme tPA pH 7.2, 37°C, mutant L420A/R275E, single chain form Homo sapiens
1.7
-
spectrozyme tPA pH 7.2, 37°C, mutant P422G/R275E, single chain form Homo sapiens
2.3
-
spectrozyme tPA pH 7.2, 37°C, mutant S421E/R275E, single chain form Homo sapiens
4.6
-
spectrozyme tPA pH 7.2, 37°C, mutant L420A/R275E, single chain form Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
plasminogen + H2O Homo sapiens
-
plasmin + ?
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
human
-

Purification (Commentary)

Purification (Comment) Organism
wild type and recombinant enzyme Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Lys-plasminogen + H2O
-
Homo sapiens plasmin + ?
-
?
plasminogen + H2O
-
Homo sapiens plasmin + ?
-
?
spectrozyme tPA + H2O
-
Homo sapiens ?
-
?

Synonyms

Synonyms Comment Organism
tissue type plasminogen activator
-
Homo sapiens

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.0005
-
Lys-plasminogen pH 7.2, 37°C, mutant P422E/R275E, single-chain form, absence of soluble fibrin Homo sapiens
0.0008
-
Lys-plasminogen pH 7.2, 37°C, mutant P422G/R275E, single-chain form, absence of soluble fibrin Homo sapiens
0.001
-
Lys-plasminogen pH 7.2, 37°C, mutant S421G/R275E, single-chain form, absence of soluble fibrin Homo sapiens
0.0015
-
Lys-plasminogen pH 7.2, 37°C, mutant P422E, two-chain form, absence of soluble fibrin Homo sapiens
0.002
-
Lys-plasminogen pH 7.2, 37°C, mutant L420E/R275E and S421E/R275E, single-chain form, absence of soluble fibrin Homo sapiens
0.0028
-
Lys-plasminogen pH 7.2, 37°C, mutant P422G, two-chain form, absence of soluble fibrin Homo sapiens
0.003
-
Lys-plasminogen pH 7.2, 37°C, mutant F423E/R275E, single-chain form, absence of soluble fibrin Homo sapiens
0.004
-
Lys-plasminogen pH 7.2, 37°C, mutant F423A/R275E, single-chain form, absence of soluble fibrin Homo sapiens
0.005
-
Lys-plasminogen pH 7.2, 37°C, mutant L420E, two-chain form, absence of soluble fibrin Homo sapiens
0.007
-
Lys-plasminogen pH 7.2, 37°C, mutant P422A/R275E, single-chain form, absence of soluble fibrin Homo sapiens
0.008
-
Lys-plasminogen pH 7.2, 37°C, mutant L420A/R275E, single-chain form, absence of soluble fibrin Homo sapiens
0.014
-
Lys-plasminogen pH 7.2, 37°C, mutant L420A, two-chain form, absence of soluble fibrin Homo sapiens
0.016
-
Lys-plasminogen pH 7.2, 37°C, mutant S421E, two-chain form, absence of soluble fibrin Homo sapiens
0.017
-
Lys-plasminogen pH 7.2, 37°C, mutant F423E, two-chain form, absence of soluble fibrin Homo sapiens
0.018
-
Lys-plasminogen pH 7.2, 37°C, mutant S421G, two-chain form, absence of soluble fibrin Homo sapiens
0.02
-
Lys-plasminogen pH 7.2, 37°C, mutant F423A, two-chain form, absence of soluble fibrin Homo sapiens
0.024
-
Lys-plasminogen pH 7.2, 37°C, mutant R275E, single-chain form, absence of soluble fibrin Homo sapiens
0.028
-
Lys-plasminogen pH 7.2, 37°C, mutant P422A, two-chain form, absence of soluble fibrin Homo sapiens
0.068
-
Lys-plasminogen pH 7.2, 37°C, wild-type, two-chain form, absence of soluble fibrin Homo sapiens
0.1
-
Lys-plasminogen pH 7.2, 37°C, wild-type, two-chain form, presence of soluble fibrin Homo sapiens
0.11
-
Lys-plasminogen pH 7.2, 37°C, mutant S421G and P422A, two-chain form, presence of soluble fibrin Homo sapiens
0.12
-
Lys-plasminogen pH 7.2, 37°C, two-chain form of mutant F423A, presence of soluble fibrin Homo sapiens
0.13
-
Lys-plasminogen pH 7.2, 37°C, mutant R275E, single-chain form, presence of soluble fibrin Homo sapiens
0.15
-
Lys-plasminogen pH 7.2, 37°C, two-chain form of mutant S421E, P422E and P422G, single chain form of mutant L420E/R275E, P422A/R275E and F423E/R275E, presence of soluble fibrin Homo sapiens
0.17
-
Lys-plasminogen pH 7.2, 37°C, two-chain form of mutant L420E and L420A, single chain form of mutant P422E/R275E, presence of soluble fibrin Homo sapiens
0.18
-
Lys-plasminogen pH 7.2, 37°C, two-chain form of mutant F423E, single-chain form of mutant L420A/R275E, presence of soluble fibrin Homo sapiens
0.19
-
Lys-plasminogen pH 7.2, 37°C, mutant S421G/R275E, single-chain form, presence of soluble fibrin Homo sapiens
0.2
-
Lys-plasminogen pH 7.2, 37°C, mutant F423A/R275E, single-chain form, presence of soluble fibrin Homo sapiens
0.21
-
Lys-plasminogen pH 7.2, 37°C, mutant P422G/R275E and S421E/R275E, single-chain form, presence of soluble fibrin Homo sapiens
2 8 spectrozyme tPA pH 7.2, 37°C, mutant F423E/R275E, single chain form Homo sapiens
3 6 spectrozyme tPA pH 7.2, 37°C, mutant S421G, two-chain form Homo sapiens
14
-
spectrozyme tPA pH 7.2, 37°C, mutant P422G/R275E, single chain form Homo sapiens
23
-
spectrozyme tPA pH 7.2, 37°C, mutant S421G/R275E, single chain form Homo sapiens
26
-
spectrozyme tPA pH 7.2, 37°C, mutant S421E/R275E, single chain form Homo sapiens
27
-
spectrozyme tPA pH 7.2, 37°C, mutant F423A/R275E, single chain form Homo sapiens
29
-
spectrozyme tPA pH 7.2, 37°C, mutant L420E/R275E, single chain form Homo sapiens
31
-
spectrozyme tPA pH 7.2, 37°C, mutant P422E/R275E, single chain form Homo sapiens
32
-
spectrozyme tPA pH 7.2, 37°C, mutant P422A/R275E, single chain form Homo sapiens
33
-
spectrozyme tPA pH 7.2, 37°C, mutant R275E, single chain form Homo sapiens
42
-
spectrozyme tPA pH 7.2, 37°C, mutant L420A/R275E, single chain form Homo sapiens
45
-
spectrozyme tPA pH 7.2, 37°C, mutant L420A, L420E, two-chain form Homo sapiens
46
-
spectrozyme tPA pH 7.2, 37°C, mutant S421E, two-chain form Homo sapiens
47
-
spectrozyme tPA pH 7.2, 37°C, wild-type t-PA, mutant P422A, two-chain form Homo sapiens
49
-
spectrozyme tPA pH 7.2, 37°C, mutant L420A/R275E, two-chain form Homo sapiens
57
-
spectrozyme tPA pH 7.2, 37°C, mutant F423E, two-chain form Homo sapiens
60
-
spectrozyme tPA pH 7.2, 37°C, mutant P422E, F423A, two-chain form Homo sapiens