Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 3.4.21.118 extracted from

  • Ramachandran, R.; Eissa, A.; Mihara, K.; Oikonomopoulou, K.; Saifeddine, M.; Renaux, B.; Diamandis, E.; Hollenberg, M.D.
    Proteinase-activated receptors (PARs): differential signalling by kallikrein-related peptidases KLK8 and KLK14 (2012), Biol. Chem., 393, 421-427.
    View publication on PubMed
Search for more literature for 3.4.21.118

Inhibitors

Inhibitors Comment Organism Structure
additional information inhibitor screening by molecular modeling and ligand docking study, interactions with the active site, overview Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

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

Synonyms Comment Organism
KLK8
-
 Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
 assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
8
-
 assay at Homo sapiens

General Information

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