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Literature summary for 3.4.21.7 extracted from

  • Law, R.H.P.; Wu, G.; Leung, E.W.W.; Hidaka, K.; Quek, A.J.; Caradoc-Davies, T.T.; Jeevarajah, D.; Conroy, P.J.; Kirby, N.M.; Norton, R.S.; Tsuda, Y.; Whisstock, J.C.
    X-ray crystal structure of plasmin with tranexamic acid-derived active site inhibitors (2017), Blood Adv., 1, 766-771 .
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.4.21.7

Activating Compound

Activating Compound Comment Organism Structure
tissue plasminogen activator
-
 Homo sapiens
urokinase plasminogen activator
-
 Homo sapiens

Crystallization (Commentary)

Crystallization (Comment) Organism
in complex with trans-4-aminomethylcyclohexanecarbonyl-L-tyrosine-n-octylamide, using 10% (w/v) polyethylene glycol 6000, 4% (v/v) 2-methyl-2,4-pentanediol, and 0.1 M MES (pH 5.0) at 20°C Homo sapiens

Protein Variants

Protein Variants Comment Organism
F587A binding site mutant Homo sapiens
F587A/K607A binding site mutant Homo sapiens
K607A binding site mutant Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
L-lysine
-
 Homo sapiens
additional information L-methionine and L-alanine show minimal reductions of enzyme activity, even at 125 mM Homo sapiens
PSI-112
-
 Homo sapiens
Tranexamic acid
-
 Homo sapiens
trans-4-aminomethylcyclohexanecarbonyl-L-(O-picolyl)tyrosine-N-octylamide
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Synonyms

Synonyms Comment Organism
Plm
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00017
-
 mutant enzyme K607A, pH and temperature not specified in the publication Homo sapiens trans-4-aminomethylcyclohexanecarbonyl-L-(O-picolyl)tyrosine-N-octylamide
0.00024
-
 wild type enzyme, pH and temperature not specified in the publication Homo sapiens trans-4-aminomethylcyclohexanecarbonyl-L-(O-picolyl)tyrosine-N-octylamide
0.00037
-
 mutant enzyme K607A, pH and temperature not specified in the publication Homo sapiens PSI-112
0.00038
-
 wild type enzyme, pH and temperature not specified in the publication Homo sapiens PSI-112
0.0011
-
 mutant enzyme F587A/K607A, pH and temperature not specified in the publication Homo sapiens trans-4-aminomethylcyclohexanecarbonyl-L-(O-picolyl)tyrosine-N-octylamide
0.00115
-
 mutant enzyme F587A, pH and temperature not specified in the publication Homo sapiens trans-4-aminomethylcyclohexanecarbonyl-L-(O-picolyl)tyrosine-N-octylamide
0.00148
-
 mutant enzyme F587A, pH and temperature not specified in the publication Homo sapiens PSI-112
0.00175
-
 mutant enzyme F587A/K607A, pH and temperature not specified in the publication Homo sapiens PSI-112
0.08679
-
 wild type enzyme, pH and temperature not specified in the publication Homo sapiens Tranexamic acid