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Literature summary for 3.4.21.118 extracted from

  • Eissa, A.; Amodeo, V.; Smith, C.R.; Diamandis, E.P.
    Kallikrein-related peptidase-8 (KLK8) is an active serine protease in human epidermis and sweat and is involved in a skin barrier proteolytic cascade (2011), J. Biol. Chem., 286, 687-706.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.4.21.118

Activating Compound

Activating Compound Comment Organism Structure
kallikrein 5
-
 Homo sapiens
lysyl endopeptidase
-
 Homo sapiens
additional information pro-KLK8 is activated by trypsin-like cleavage at Lys32–Val33 Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Pichia pastoris strain GS115 Homo sapiens

General Stability

General Stability Organism
KLK8 displays 2.5fold higher activity in 100 mM sodium phosphate buffer than in 50 mM Tris-HCl buffer Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
alpha2-antiplasmin
-
 Homo sapiens
Aprotinin
-
 Homo sapiens
chymostatin
-
 Homo sapiens
additional information KLK8 is not inhibited by EDTA and alpha1-antitrypsin; mature KLK8 activity is attenuated by autocleavage after Arg164 Homo sapiens
phenylmethylsulfonyl fluoride
-
 Homo sapiens
Protein C inhibitor
-
 Homo sapiens
Zn2+ 28.6% residual activity at 10 mM Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0238
-
 tert-butyloxycarbonyl-Val-Pro-Arg-7-amido-4-methylcoumarin in 100 mM sodium phosphate, 0.01% (v/v) Tween 20, pH 8.5, at 37°C Homo sapiens
0.1165
-
 tert-butyloxycarbonyl-Leu-Arg-Arg-7-amido-4-methylcoumarin in 100 mM sodium phosphate, 0.01% (v/v) Tween 20, pH 8.5, at 37°C Homo sapiens
0.1407
-
 tert-butyloxycarbonyl-Leu-Lys-Arg-7-amido-4-methylcoumarin in 100 mM sodium phosphate, 0.01% (v/v) Tween 20, pH 8.5, at 37°C Homo sapiens
0.1533
-
 Pro-Phe-Arg-7-amido-4-methylcoumarin in 100 mM sodium phosphate, 0.01% (v/v) Tween 20, pH 8.5, at 37°C Homo sapiens
0.1844
-
 tert-butyloxycarbonyl-Gln-Ala-Arg-7-amido-4-methylcoumarin in 100 mM sodium phosphate, 0.01% (v/v) Tween 20, pH 8.5, at 37°C Homo sapiens
0.2247
-
 tert-butyloxycarbonyl-Gln-Arg-Arg-7-amido-4-methylcoumarin in 100 mM sodium phosphate, 0.01% (v/v) Tween 20, pH 8.5, at 37°C Homo sapiens
0.2983
-
 tert-butyloxycarbonyl-Phe-Ser-Arg-7-amido-4-methylcoumarin in 100 mM sodium phosphate, 0.01% (v/v) Tween 20, pH 8.5, at 37°C Homo sapiens
0.3326
-
 tert-butyloxycarbonyl-Val-Leu-Lys-7-amido-4-methylcoumarin in 100 mM sodium phosphate, 0.01% (v/v) Tween 20, pH 8.5, at 37°C Homo sapiens
0.3699
-
 tert-butyloxycarbonyl-Gln-Gly-Arg-7-amido-4-methylcoumarin in 100 mM sodium phosphate, 0.01% (v/v) Tween 20, pH 8.5, at 37°C Homo sapiens
0.4312
-
 benzyloxycarbonyl-Gly-Gly-Arg-7-amido-4-methylcoumarin in 100 mM sodium phosphate, 0.01% (v/v) Tween 20, pH 8.5, at 37°C Homo sapiens
0.6897
-
 tosyl-Gly-Pro-Arg-7-amido-4-methylcoumarin in 100 mM sodium phosphate, 0.01% (v/v) Tween 20, pH 8.5, at 37°C Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
Ca2+ 150.2% activity at 10 mM Homo sapiens
Mg2+ 142% activity at 10 mM Homo sapiens
additional information KLK8 is not influenced by Na+ and K+ Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
LL-37 antimicrobial peptide + H2O Homo sapiens i.e. LLGDFFRKSKEKIGKEFKRIVQRIKDFLRNLVPRTES ?
-
 ?
pro-kallikrein 1 + H2O Homo sapiens
-
 kallikrein 1
-
 ?
pro-kallikrein 11 + H2O Homo sapiens
-
 kallikrein 11
-
 ?

Organic Solvent Stability

Organic Solvent Comment Organism
Tween-20 KLK8 shows 1.25-fold higher activity when 0.01% Tween-20 is added as a carrier in the reaction mix Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Posttranslational Modification

Posttranslational Modification Comment Organism
glycoprotein KLK8 has one glycosylation site at Asn100 Homo sapiens

Purification (Commentary)

Purification (Comment) Organism
Sepharose column chromatography and Source15S column chromatography and Superdex 200 gel filtration Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
epidermis
-
 Homo sapiens
-
keratinocyte
-
 Homo sapiens
-
additional information KLK8 is not secreted by human melanocytes or dermal fibroblasts Homo sapiens
-
stratum corneum
-
 Homo sapiens
-
sweat
-
 Homo sapiens
-

Storage Stability

Storage Stability Organism
-20°C, 0.01 M acetic acid containing 250 mM NaCl, pH 4.76, 1 month, no loss of activity Homo sapiens
-80°C, 0.01 M acetic acid containing 250 mM NaCl, pH 4.76, 12 months, no loss of activity Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
benzyloxycarbonyl-Gly-Gly-Arg-7-amido-4-methylcoumarin + H2O 1.2% activity compared to tert-butyloxycarbonyl-Val-Pro-Arg-7-amido-4-methylcoumarin Homo sapiens benzyloxycarbonyl-Gly-Gly-Arg + 7-amino-4-methylcoumarin
-
 ?
LL-37 antimicrobial peptide + H2O i.e. LLGDFFRKSKEKIGKEFKRIVQRIKDFLRNLVPRTES Homo sapiens ?
-
 ?
additional information kallikrein 8 shows highest preference for (R/K)(S/T)(A/V) at P1-P1’-P2’ Homo sapiens ?
-
 ?
additional information no activity with Ala-Ala-Pro-Val-7-amido-4-methylcoumarin, Ala-Ala-Pro-Phe-7-amido-4-methylcoumarin, Leu-Leu-Val-Tyr-7-amido-4-methylcoumarin, tosyl-Gly-Pro-Lys-7-amido-4-methylcoumarin, and ter-butyloxycarbonyl-Glu-Lys-Lys-7-amido-4-methylcoumarin Homo sapiens ?
-
 ?
pro-kallikrein 1 + H2O
-
 Homo sapiens kallikrein 1
-
 ?
pro-kallikrein 11 + H2O
-
 Homo sapiens kallikrein 11
-
 ?
Pro-Phe-Arg-7-amido-4-methylcoumarin + H2O 10% activity compared to tert-butyloxycarbonyl-Val-Pro-Arg-7-amido-4-methylcoumarin Homo sapiens Pro-Phe-Arg + 7-amino-4-methylcoumarin
-
 ?
tert-butyloxycarbonyl-Gln-Ala-Arg-7-amido-4-methylcoumarin + H2O 11% activity compared to tert-butyloxycarbonyl-Val-Pro-Arg-7-amido-4-methylcoumarin Homo sapiens tert-butyloxycarbonyl-Gln-Ala-Arg + 7-amino-4-methylcoumarin
-
 ?
tert-butyloxycarbonyl-Gln-Arg-Arg-7-amido-4-methylcoumarin + H2O 5.0% activity compared to tert-butyloxycarbonyl-Val-Pro-Arg-7-amido-4-methylcoumarin Homo sapiens tert-butyloxycarbonyl-Gln-Arg-Arg + 7-amino-4-methylcoumarin
-
 ?
tert-butyloxycarbonyl-Gln-Gly-Arg-7-amido-4-methylcoumarin + H2O 1.4% activity compared to tert-butyloxycarbonyl-Val-Pro-Arg-7-amido-4-methylcoumarin Homo sapiens tert-butyloxycarbonyl-Gln-Gly-Arg + 7-amino-4-methylcoumarin
-
 ?
tert-butyloxycarbonyl-Leu-Arg-Arg-7-amido-4-methylcoumarin + H2O 4.9% activity compared to tert-butyloxycarbonyl-Val-Pro-Arg-7-amido-4-methylcoumarin Homo sapiens tert-butyloxycarbonyl-Leu-Arg-Arg + 7-amino-4-methylcoumarin
-
 ?
tert-butyloxycarbonyl-Leu-Lys-Arg-7-amido-4-methylcoumarin + H2O 3.9% activity compared to tert-butyloxycarbonyl-Val-Pro-Arg-7-amido-4-methylcoumarin Homo sapiens tert-butyloxycarbonyl-Leu-Lys-Arg + 7-amino-4-methylcoumarin
-
 ?
tert-butyloxycarbonyl-Phe-Ser-Arg-7-amido-4-methylcoumarin + H2O 4.2% activity compared to tert-butyloxycarbonyl-Val-Pro-Arg-7-amido-4-methylcoumarin Homo sapiens tert-butyloxycarbonyl-Phe-Ser-Arg + 7-amino-4-methylcoumarin
-
 ?
tert-butyloxycarbonyl-Val-Leu-Lys-7-amido-4-methylcoumarin + H2O 3.8% activity compared to tert-butyloxycarbonyl-Val-Pro-Arg-7-amido-4-methylcoumarin Homo sapiens tert-butyloxycarbonyl-Val-Leu-Lys + 7-amino-4-methylcoumarin
-
 ?
tert-butyloxycarbonyl-Val-Pro-Arg-7-amido-4-methylcoumarin + H2O 100% activity Homo sapiens tert-butyloxycarbonyl-Val-Pro-Arg + 7-amino-4-methylcoumarin
-
 ?
tosyl-Gly-Pro-Arg-7-amido-4-methylcoumarin + H2O 1.0% activity compared to tert-butyloxycarbonyl-Val-Pro-Arg-7-amido-4-methylcoumarin Homo sapiens tosyl-Gly-Pro-Arg + 7-amino-4-methylcoumarin
-
 ?

Subunits

Subunits Comment Organism
? x * about 28000, calculated from amino acid sequence Homo sapiens
? x * about 31000, SDS-PAGE Homo sapiens

Synonyms

Synonyms Comment Organism
kallikrein-related peptidase-8
-
 Homo sapiens
KLK8
-
 Homo sapiens

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
1.43
-
 tert-butyloxycarbonyl-Gln-Gly-Arg-7-amido-4-methylcoumarin in 100 mM sodium phosphate, 0.01% (v/v) Tween 20, pH 8.5, at 37°C Homo sapiens
1.49
-
 benzyloxycarbonyl-Gly-Gly-Arg-7-amido-4-methylcoumarin in 100 mM sodium phosphate, 0.01% (v/v) Tween 20, pH 8.5, at 37°C Homo sapiens
1.56
-
 tert-butyloxycarbonyl-Leu-Lys-Arg-7-amido-4-methylcoumarin in 100 mM sodium phosphate, 0.01% (v/v) Tween 20, pH 8.5, at 37°C Homo sapiens
1.62
-
 tert-butyloxycarbonyl-Leu-Arg-Arg-7-amido-4-methylcoumarin in 100 mM sodium phosphate, 0.01% (v/v) Tween 20, pH 8.5, at 37°C Homo sapiens
2.11
-
 tosyl-Gly-Pro-Arg-7-amido-4-methylcoumarin in 100 mM sodium phosphate, 0.01% (v/v) Tween 20, pH 8.5, at 37°C Homo sapiens
3.39
-
 tert-butyloxycarbonyl-Gln-Arg-Arg-7-amido-4-methylcoumarin in 100 mM sodium phosphate, 0.01% (v/v) Tween 20, pH 8.5, at 37°C Homo sapiens
3.57
-
 tert-butyloxycarbonyl-Phe-Ser-Arg-7-amido-4-methylcoumarin in 100 mM sodium phosphate, 0.01% (v/v) Tween 20, pH 8.5, at 37°C Homo sapiens
4.45
-
 Pro-Phe-Arg-7-amido-4-methylcoumarin in 100 mM sodium phosphate, 0.01% (v/v) Tween 20, pH 8.5, at 37°C Homo sapiens
5.75
-
 tert-butyloxycarbonyl-Gln-Ala-Arg-7-amido-4-methylcoumarin in 100 mM sodium phosphate, 0.01% (v/v) Tween 20, pH 8.5, at 37°C Homo sapiens
6.76
-
 tert-butyloxycarbonyl-Val-Pro-Arg-7-amido-4-methylcoumarin in 100 mM sodium phosphate, 0.01% (v/v) Tween 20, pH 8.5, at 37°C Homo sapiens
9.64
-
 tert-butyloxycarbonyl-Val-Leu-Lys-7-amido-4-methylcoumarin in 100 mM sodium phosphate, 0.01% (v/v) Tween 20, pH 8.5, at 37°C Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
8.5
-
-
 Homo sapiens

pH Range

pH Minimum pH Maximum Comment Organism
7 9
-
 Homo sapiens

Expression

Organism Comment Expression
Homo sapiens KLK8 protein expression increases during terminal keratinocyte differentiation up

kcat/KM [mM/s]

kcat/KM Value [1/mMs-1] kcat/KM Value Maximum [1/mMs-1] Substrate Comment Organism Structure
3.05
-
 tosyl-Gly-Pro-Arg-7-amido-4-methylcoumarin in 100 mM sodium phosphate, 0.01% (v/v) Tween 20, pH 8.5, at 37°C Homo sapiens
3.45
-
 benzyloxycarbonyl-Gly-Gly-Arg-7-amido-4-methylcoumarin in 100 mM sodium phosphate, 0.01% (v/v) Tween 20, pH 8.5, at 37°C Homo sapiens
3.85
-
 tert-butyloxycarbonyl-Gln-Gly-Arg-7-amido-4-methylcoumarin in 100 mM sodium phosphate, 0.01% (v/v) Tween 20, pH 8.5, at 37°C Homo sapiens
10.93
-
 tert-butyloxycarbonyl-Val-Leu-Lys-7-amido-4-methylcoumarin in 100 mM sodium phosphate, 0.01% (v/v) Tween 20, pH 8.5, at 37°C Homo sapiens
11.12
-
 tert-butyloxycarbonyl-Leu-Lys-Arg-7-amido-4-methylcoumarin in 100 mM sodium phosphate, 0.01% (v/v) Tween 20, pH 8.5, at 37°C Homo sapiens
11.96
-
 tert-butyloxycarbonyl-Phe-Ser-Arg-7-amido-4-methylcoumarin in 100 mM sodium phosphate, 0.01% (v/v) Tween 20, pH 8.5, at 37°C Homo sapiens
13.91
-
 tert-butyloxycarbonyl-Leu-Arg-Arg-7-amido-4-methylcoumarin in 100 mM sodium phosphate, 0.01% (v/v) Tween 20, pH 8.5, at 37°C Homo sapiens
15.1
-
 tert-butyloxycarbonyl-Gln-Arg-Arg-7-amido-4-methylcoumarin in 100 mM sodium phosphate, 0.01% (v/v) Tween 20, pH 8.5, at 37°C Homo sapiens
29.02
-
 Pro-Phe-Arg-7-amido-4-methylcoumarin in 100 mM sodium phosphate, 0.01% (v/v) Tween 20, pH 8.5, at 37°C Homo sapiens
31.2
-
 tert-butyloxycarbonyl-Gln-Ala-Arg-7-amido-4-methylcoumarin in 100 mM sodium phosphate, 0.01% (v/v) Tween 20, pH 8.5, at 37°C Homo sapiens
283.4
-
 tert-butyloxycarbonyl-Val-Pro-Arg-7-amido-4-methylcoumarin in 100 mM sodium phosphate, 0.01% (v/v) Tween 20, pH 8.5, at 37°C Homo sapiens