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Literature summary for 3.4.21.B12 extracted from

  • Ramsay, A.J.; Dong, Y.; Hunt, M.L.; Linn, M.; Samaratunga, H.; Clements, J.A.; Hooper, J.D.
    Kallikrein-related peptidase (KLK) 4 initiates intracellular signalling via protease-activated receptors (PARs). KLK4 and PAR-2 are co-expressed during prostate cancer progression (2008), J. Biol. Chem., 283, 12293-12304.
    View publication on PubMed
Search for more literature for 3.4.21.B12

Activating Compound

Activating Compound Comment Organism Structure
Thermolysin activates recombinant KLK4 Homo sapiens

Application

Application Comment Organism
medicine KLK4 initiates Ca2+ mobilization via PAR-1 and PAR-2 but not via PAR-4. KLK4 has greater efficacy for initiating Ca2+ signalling via PAR-2 than PAR-1. Signals induced by KLK4 via PARs may be important in prostate cancer Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
KLK4-pIB/V5-His construct expressed in Sf9 cells. PC-3 cell stimulated with KLK4 Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.008
-
 (Abz)-SKGR-SLIGK(N-[2,4-dintrophenyl]ethylenediamine)-Asp-OH
-
 Homo sapiens
0.0469
-
 benzyl-FVR-p-nitroanilide thermolysin activated recombinant KLK4 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Purification (Commentary)

Purification (Comment) Organism
on Ni-NTA resin Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
glandular epithelium co-expression of KLK4 and PAR-2 Homo sapiens
-
PC-3 cell KLK4 induces loss of PAR-2 from the cell surface and receptor internalisation Homo sapiens
-
prostate cancer cell line co-expression of agonist and PAR-2 in primary prostate cancer (benign glands of benign prostatic hyperplasia, prostatic intraepithelial neoplasia and cancer) and prostate cancer bone metastasis Homo sapiens
-

Storage Stability

Storage Stability Organism
-80°C, phosphate buffer, pH 7.4 Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
(Abz)-SKGR-SLIGK(N-[2,4-dintrophenyl]ethylenediamine)-Asp-OH fluorescence quenched peptide spanning the PAR-2 activation site, is rapidly cleaved by KLK4 Homo sapiens ?
-
 ?
benzyl-FVR-p-nitroanilide + H2O
-
 Homo sapiens ?
-
 ?
additional information KLK4 initiates phosphorylation of ERK1/2 via PAR-2 Homo sapiens ?
-
 ?

Synonyms

Synonyms Comment Organism
kallikrein-related peptidase
-
 Homo sapiens
KLK4
-
 Homo sapiens

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
1.8
-
 benzyl-FVR-p-nitroanilide thermolysin activated recombinant KLK4 Homo sapiens
7.9
-
 (Abz)-SKGR-SLIGK(N-[2,4-dintrophenyl]ethylenediamine)-Asp-OH
-
 Homo sapiens