EC Number   |
Inhibitors |
Structure |
|---|
   3.4.21.B12 | alpha2-antiplasmin |
- |
 |
| 3.4.21.B12 | Aprotinin |
complex formation with the self-activated recombinant, chimeric enzyme |
  |
| 3.4.21.B12 | Aprotinin |
markedly decreases migratory potential of K4 clones |
|
| 3.4.21.B12 | benzamidine |
93% inhibition at 10 mM |
|
| 3.4.21.B12 | Co2+ |
- |
|
| 3.4.21.B12 | 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 |
|
| 3.4.21.B12 | more |
inhibition of KLK4 expression results in diminished invasive potential in OSCC cell lines |
|
| 3.4.21.B12 | Nalpha-p-tosyl-L-lysine chloromethyl ketone |
85% inhibition at 1 mM; i.e. TLCK |
|
| 3.4.21.B12 | Ni2+ |
- |
|
| 3.4.21.B12 | siRNA |
mediates knockdown of endogenous KLK4 in LNCaP prostate cancer cells whereby inhibiting their proliferation |
|
