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Literature summary for 3.4.21.117 extracted from

  • de Veer, S.J.; Furio, L.; Swedberg, J.E.; Munro, C.A.; Brattsand, M.; Clements, J.A.; Hovnanian, A.; Harris, J.M.
    Selective substrates and inhibitors for kallikrein-related peptidase 7 (KLK7) shed light on KLK proteolytic activity in the stratum corneum (2017), J. Invest. Dermatol., 137, 430-439 .
    View publication on PubMed
Search for more literature for 3.4.21.117

Cloned(Commentary)

Cloned (Comment) Organism
expression in Pichia pastoris Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
GKCLFSEPPICFPN peptide inhibitor based on sunflower trypsin inhibitor-1 Homo sapiens
GKCLFSNPPICFPN peptide inhibitor based on sunflower trypsin inhibitor-1, displays at least 1000fold selectivity over several proteases that are related by function (KLK5 and KLK14) or specificity (chymotrypsin) Homo sapiens
GKCLFSSPPICFPN peptide inhibitor based on sunflower trypsin inhibitor-1 Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.044
-
 KHLY-4-nitroanilide pH 8.0, 23°C Homo sapiens
0.048
-
 KHLF-4-nitroanilide pH 8.0, 23°C Homo sapiens
0.049
-
 QHLY-4-nitroanilide pH 8.0, 23°C Homo sapiens
0.65
-
 methoxy-succinyl-Arg-Pro-Tyr-4-nitroanilide pH 8.0, 23°C Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P49862
-
-

Source Tissue

Source Tissue Comment Organism Textmining
stratum corneum
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
KHLF-4-nitroanilide + H2O
-
 Homo sapiens KLHLF + 4-nitroaniline
-
 ?
KHLY-4-nitroanilide + H2O
-
 Homo sapiens KLHLY + 4-nitroaniline
-
 ?
methoxy-succinyl-Arg-Pro-Tyr-4-nitroanilide + H2O
-
 Homo sapiens methoxy-succinyl-Arg-Pro-Tyr + 4-nitroaniline
-
 ?
QHLY-4-nitroanilide + H2O
-
 Homo sapiens QLHLY + 4-nitroaniline
-
 ?

Synonyms

Synonyms Comment Organism
KLK7
-
 Homo sapiens

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
1.2
-
 methoxy-succinyl-Arg-Pro-Tyr-4-nitroanilide pH 8.0, 23°C Homo sapiens
7.4
-
 KHLF-4-nitroanilide pH 8.0, 23°C Homo sapiens
7.7
-
 QHLY-4-nitroanilide pH 8.0, 23°C Homo sapiens
12
-
 KHLY-4-nitroanilide pH 8.0, 23°C Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00000014
-
 GKCLFSNPPICFPN pH 8.0, 23°C Homo sapiens
0.0000014
-
 GKCLFSSPPICFPN pH 8.0, 23°C Homo sapiens
0.0000031
-
 GKCLFSEPPICFPN pH 8.0, 23°C Homo sapiens

General Information

General Information Comment Organism
physiological function inhibition of KLK7 alone is sufficient to block shedding, whereas KLK5 is also a major contributor Homo sapiens

kcat/KM [mM/s]

kcat/KM Value [1/mMs-1] kcat/KM Value Maximum [1/mMs-1] Substrate Comment Organism Structure
1.8
-
 methoxy-succinyl-Arg-Pro-Tyr-4-nitroanilide pH 8.0, 23°C Homo sapiens
150
-
 KHLF-4-nitroanilide pH 8.0, 23°C Homo sapiens
160
-
 QHLY-4-nitroanilide pH 8.0, 23°C Homo sapiens
270
-
 KHLY-4-nitroanilide pH 8.0, 23°C Homo sapiens