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Literature summary for 3.4.21.B39 extracted from

  • Teixeira, T.S.; Freitas, R.F.; Abrahao, O.; Devienne, K.F.; de Souza, L.R.; Blaber, S.I.; Blaber, M.; Kondo, M.Y.; Juliano, M.A.; Juliano, L.; Puzer, L.
    Biological evaluation and docking studies of natural isocoumarins as inhibitors for human kallikrein 5 and 7 (2011), Bioorg. Med. Chem. Lett., 21, 6112-6115.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
expressed in insect cell/baculovirus expression system Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
8,8'-paepalantine dimer potent competitive inhibitor Homo sapiens
paepalantine
-
Homo sapiens
vioxanthin potent competitive inhibitor Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.004
-
Abz-KLRSSKQ-EDDnp pH and temperature not specified in the publication Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Abz-KLRSSKQ-EDDnp + H2O
-
Homo sapiens ?
-
?
additional information no activity with Abz-KLYSSKQ-EDDnp Homo sapiens ?
-
?

Synonyms

Synonyms Comment Organism
kallikrein 5
-
Homo sapiens
KLK5
-
Homo sapiens

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
8.5
-
Abz-KLRSSKQ-EDDnp pH and temperature not specified in the publication Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0229
-
vioxanthin pH and temperature not specified in the publication Homo sapiens
0.0244
-
8,8'-paepalantine dimer pH and temperature not specified in the publication Homo sapiens
0.0475
-
paepalantine pH and temperature not specified in the publication Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0537
-
pH and temperature not specified in the publication Homo sapiens vioxanthin
0.0729
-
pH and temperature not specified in the publication Homo sapiens 8,8'-paepalantine dimer
0.3674
-
pH and temperature not specified in the publication Homo sapiens paepalantine

kcat/KM [mM/s]

kcat/KM Value [1/mMs-1] kcat/KM Value Maximum [1/mMs-1] Substrate Comment Organism Structure
2125
-
Abz-KLRSSKQ-EDDnp pH and temperature not specified in the publication Homo sapiens