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Literature summary for 3.4.21.117 extracted from

  • Debela, M.; Hess, P.; Magdolen, V.; Schechter, N.M.; Steiner, T.; Huber, R.; Bode, W.; Goettig, P.
    Chymotryptic specificity determinants in the 1.0 A structure of the zinc-inhibited human tissue kallikrein 7 (2007), Proc. Natl. Acad. Sci. USA, 104, 16086-16091.
    View publication on PubMedView publication on EuropePMC

Application

Application Comment Organism
diagnostics the enzyme is a potential biomarker of ovarian cancer Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Escherichia coli and in a baculovirus-insect cell system Homo sapiens

Crystallization (Commentary)

Crystallization (Comment) Organism
kallikrein 7 bound to inhibitors succinyl-Ala-Ala-Pro-Phe-chloromethyl ketone and Ala-Ala-Phe-chloromethyl ketone, sitting-drop vapor diffusion method at 18°C, 0.001 ml protein solution, containing 7 mg/ml enzyme-inhibitor complex, is mixed with 0.001 ml reservoir solution containing 100 mM [bis(2-hydroxyethyl)amino]tris(hydroxymethyl)-methane-HCl, pH 6.0, 25% PEG 3350, and 2.5 M Li2SO4, equilibration against reservoir solution, X-ray diffraction structure determination and analysis at 1.0-2.5 A resolution Homo sapiens
sitting drop vapour diffusion method, with 100 mM [bis(2-hydroxyethyl)amino]tris(hydroxymethyl)-methane-HCl, pH 6.0, 25% PEG 3350, and 2.5 M Li2SO4 or with 100 mM sodium cacodylate, pH 6.5, 200 mM magnesium acetate, and 30% (v/v) 2-methyl-2,4-pentanediol Homo sapiens

Protein Variants

Protein Variants Comment Organism
H41F mutant is inhibited by Zn2+ as the wild type enzyme Homo sapiens
H41F site-directed mutagenesis, the mutant is inhibited by Zn2+ like the wild-type enzyme Homo sapiens
H99A mutant exhibits virtually no Zn2+ inhibition Homo sapiens
H99A site-directed mutagenesis, the mutant shows resistance against inhibition by Zn2+ in contrast to the wild-type enzyme Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
Ala-Ala-Phe-chloromethyl ketone
-
Homo sapiens
Ala-Ala-Phe-chloromethylketone
-
Homo sapiens
Cu2+ inhibition at low micromolar concentrations, structural basis for inhibition, overview; strong inhibitory effect Homo sapiens
succinyl-Ala-Ala-Pro-Phe-chloromethyl ketone
-
Homo sapiens
Zn2+ inhibition at low micromolar concentrations, noncompetitive inhibition type, structural basis for inhibition involving His99, overview; strong inhibitory effect Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0402
-
Phe-7-amido-4-methylcoumarin pH 7.5, 25°C Homo sapiens
0.0402
-
L-Tyr-7-amido-4-methylcoumarin in 50 mM HEPES, pH 7.5, 150 mM NaCl, 0.005% Tween 20, at 25°C Homo sapiens
0.0443
-
Phe-7-amido-4-methylcoumarin pH 7.5, 25°C Homo sapiens
0.0443
-
L-Phe-7-amido-4-methylcoumarin in 50 mM HEPES, pH 7.5, 150 mM NaCl, 0.005% Tween 20, at 25°C Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
Ca2+ slight activation Homo sapiens
Ca2+ slight enhancement of activity Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
additional information Homo sapiens the enzyme participates in skin desquamation but is also implicated in diverse skin diseases and is a potential biomarker of ovarian cancer ?
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens P49862
-
-

Posttranslational Modification

Posttranslational Modification Comment Organism
proteolytic modification pro-kallikrein is activated by proteolytic clavage of the Xaa15-Ile16 bond Homo sapiens

Purification (Commentary)

Purification (Comment) Organism
-
Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
epidermis stronlgy expressed in the upper layers of the epidermis Homo sapiens
-
epidermis the enzyme is strongly expressed in the upper layers of the epidermis Homo sapiens
-
ovary cancer cell
-
Homo sapiens
-
stratum corneum
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
L-Phe-7-amido-4-methylcoumarin + H2O
-
Homo sapiens L-Phe + 7-amino-4-methylcoumarin
-
?
L-Tyr-7-amido-4-methylcoumarin + H2O
-
Homo sapiens L-Tyr + 7-amino-4-methylcoumarin
-
?
additional information the enzyme participates in skin desquamation but is also implicated in diverse skin diseases and is a potential biomarker of ovarian cancer Homo sapiens ?
-
?
additional information active site structure and substrate specificity, overview, kallikrein 7 exhibits large positively charged surface patches, representing putative exosites for prime side substrate recognition, overview Homo sapiens ?
-
?
Phe-7-amido-4-methylcoumarin + H2O
-
Homo sapiens Phe + 7-amino-4-methylcoumarin
-
?
succinyl-Ala-Ala-Pro-Phe-7-amido-4-methylcoumarin + H2O
-
Homo sapiens succinyl-Ala-Ala-Pro-Phe + 7-amino-4-methylcoumarin
-
?
succinyl-Ala-Val-Pro-Phe 4-nitroanilide + H2O
-
Homo sapiens succinyl-Ala-Val-Pro-Phe + 4-nitroaniline
-
?
succinyl-Leu-Leu-Tyr-7-amido-4-methylcoumarin + H2O
-
Homo sapiens succinyl-Leu-Leu-Tyr + 7-amino-4-methylcoumarin
-
?
Tyr-7-amido-4-methylcoumarin + H2O
-
Homo sapiens Tyr + 7-amino-4-methylcoumarin
-
?

Subunits

Subunits Comment Organism
More tertiary and primary structure of kallikrein 7, overview Homo sapiens

Synonyms

Synonyms Comment Organism
hK7
-
Homo sapiens
human stratum corneum chymotryptic enzyme
-
Homo sapiens
KLK7
-
Homo sapiens
More the enzyme belongs to the human tissue kallikrein serine proteinase family Homo sapiens
tissue kallikrein 7
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
25
-
assay at Homo sapiens

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.000016
-
Phe-7-amido-4-methylcoumarin pH 7.5, 25°C Homo sapiens
0.000016
-
L-Phe-7-amido-4-methylcoumarin in 50 mM HEPES, pH 7.5, 150 mM NaCl, 0.005% Tween 20, at 25°C Homo sapiens
0.000033
-
Phe-7-amido-4-methylcoumarin pH 7.5, 25°C Homo sapiens
0.000033
-
L-Tyr-7-amido-4-methylcoumarin in 50 mM HEPES, pH 7.5, 150 mM NaCl, 0.005% Tween 20, at 25°C Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.5
-
assay at Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0006
-
Cu2+ apparent value Homo sapiens
0.0006
-
Cu2+ 25°C Homo sapiens
0.01
-
Zn2+ apparent value Homo sapiens
0.01
-
Zn2+ 25°C Homo sapiens