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Literature summary for 3.4.21.B12 extracted from

  • Swedberg, J.E.; Ghani, H.A.; Harris, J.M.; de Veer, S.J.; Craik, D.J.
    Potent, selective, and cell-penetrating inhibitors of kallikrein-related peptidase 4 based on the cyclic peptide MCoTI-II (2018), ACS Med. Chem. Lett., 9, 1258-1262 .
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.4.21.B12

Inhibitors

Inhibitors Comment Organism Structure
MCoTI-II a 34-amino acid cyclic peptide found in the seeds of Momordica cochinchinensis. By grafting a preferred KLK4 cleavage sequence into MCoTI-II, a highly potent KLK4 inhibitor is produced that displays 100000fold selectivity over related kallikreins and the ability to penetrate cells. Additionally, by substituting positively charged noncontact residues in this compound, a potent and selective KLK4 inhibitor is produced that does not penetrate cells. The inhibitors are shown to be nontoxic to human cells and stable in human serum. These KLK4 inhibitors provide useful chemical tools to further define the role(s) of both intracellular and extracellular KLK4 in prostate cancer cell lines and disease models Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.065
-
 acetyl-FVQR-4-nitroanilide pH 7.4, temperature not specified in the publication Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens Q9Y5K2
-
-

Purification (Commentary)

Purification (Comment) Organism
-
 Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
HeLa cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
acetyl-FVQR-4-nitroanilide + H2O
-
 Homo sapiens acetyl-FVQR + 4-nitroaniline
-
 ?

Synonyms

Synonyms Comment Organism
kallikrein-related peptidase 4
-
 Homo sapiens
KLK4
-
 Homo sapiens