Inhibitors | Comment | Organism | Structure |
---|---|---|---|
additional information | inhibitor screening by molecular modeling and ligand docking study, interactions with the active site, overview | Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
GDDSTPSILPAPRGYPGQV + H2O | the tethered ligand is GYPGQV | Homo sapiens | GDDSTPSILPAPR + GYPGQV | - |
? | |
GPNSKGRSLIGRLDTPYGGC + H2O | the tethered ligand is SLIGRL | Homo sapiens | GPNSKGR + SLIGRLDTPYGC | - |
? | |
GTNRSSKGRSLIGKVDGTSHVTGKGVT + H2O | the tethered ligand is SLIGKV | Homo sapiens | GTNRSSKGR + SLIGKVDGTSHVTGKGVT | - |
? | |
additional information | substrate specificity, overview. No activity with NATLDPRSFLLRNPNDKYE. Analysis of processing of synthetic human and rat proteinase-activated receptor 2, PAR2, derived sequences, representing the cleavage activation domain of PAR2, by kallikrein 8 versus kallikrein 14. KLKs 8 and 14 can both cleave the synthetic PAR2 tethered ligand-containing synthetic peptides to unmask a potential receptor-activating sequence, but each KLK exhibits distinct signalling properties via PARs 1 and 2 | Homo sapiens | ? | - |
? | |
proteinase-activated receptor 2 peptide precursor + H2O | the enzyme can unmask a PAR2 receptor-activating sequence from a peptide precursor | Homo sapiens | ? | - |
? | |
Rattus norvegicus proteinase-activated receptor 2 + H2O | no activity witht the human proteinase-activated receptor 2 | Homo sapiens | ? | - |
? |
Synonyms | Comment | Organism |
---|---|---|
KLK8 | - |
Homo sapiens |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
37 | - |
assay at | Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
8 | - |
assay at | Homo sapiens |
General Information | Comment | Organism |
---|---|---|
physiological function | human enzyme can activate rat but not human proteinase-activated receptor 2, PAR2, calcium signalling, and the enzyme is not able to stimulate human PAR2 clustering and internalization. In human kidney-derived HEK cells, the enzyme is not able to signal via either PAR1 or PAR2. Also KLK8 is not able to activate MAP kinase and does not trigger interactions between human PAR2 and beta-arrestins | Homo sapiens |