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Literature summary for 3.4.21.35 extracted from
- Tissue kallikrein in cardiovascular, cerebrovascular and renal diseases and skin wound healing (2010), Biol. Chem., 391, 345-355.
Activating Compound
| Activating Compound | Comment | Organism | Structure |
|---|---|---|---|
| additional information | release of tissue kallikrein into the distal tubules of kidney can be stimulated by low sodium levels, high potassium levels and antidiuretic hormone | Homo sapiens |
Application
| Application | Comment | Organism |
|---|---|---|
| medicine | tissue kallikrein therapy is a promising regimen in the treatment of acute ischemic stroke in humans | Homo sapiens |
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| overexpressed in transgenic mice or rats | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| alpha1-antitrypsin | slowly binds to tissue kallikrein and suppresses its activity | Homo sapiens | |
| epidermal growth factor receptor inhibitor | - |
Rattus norvegicus | |
| icatibant | blocks decrease of isoproterenol-induced cardiac hypertrophy and fibrosis by overexpressed tissue kallikrein in transgenic rats | Homo sapiens |  |
| icatibant | - |
Rattus norvegicus | |
| tissue kallikrein-binding protein | rapidly forms a covalent complex with tissue kallikrein | Homo sapiens |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
| Mus musculus | - |
- |
- |
| Rattus norvegicus | - |
- |
- |
| Sus scrofa | - |
- |
- |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| kidney | in the collecting segment of the distal tubule | Homo sapiens | - |
| pancreas | - |
Sus scrofa | - |
| urine | - |
Homo sapiens | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| kininogen + H2O | - |
Mus musculus | kinin + ? | - |
? | |
| kininogen + H2O | - |
Homo sapiens | kinin + ? | - |
? | |
| kininogen + H2O | - |
Rattus norvegicus | kinin + ? | - |
? | |
| kininogen + H2O | - |
Sus scrofa | kinin + ? | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| KLK1 | - |
Mus musculus |
| KLK1 | - |
Homo sapiens |
| KLK1 | - |
Rattus norvegicus |
| KLK1 | - |
Sus scrofa |
| tissue kallikrein | - |
Mus musculus |
| tissue kallikrein | - |
Homo sapiens |
| tissue kallikrein | - |
Rattus norvegicus |
| tissue kallikrein | - |
Sus scrofa |
| urinary kallikrein | - |
Homo sapiens |
Expression
| Organism | Comment | Expression |
|---|---|---|
| Homo sapiens | urinary kallikrein excretion is significantly reduced in patients with mild renal disease, and to a further extent in patients with severe renal failure | down |
General Information
| General Information | Comment | Organism |
|---|---|---|
| malfunction | genetically ablating tissue kallikrein in mice results in dilated decompensated cardiomyopathy | Mus musculus |
| physiological function | elicits a hypotensive action. It is effective in the treatment of patients with acute brain infarction when injected within 48 h after stroke onset. Overexpression of human tissue kallikrein in transgenic rats causes a decrease of isoproterenol-induced cardiac hypertrophy and fibrosis. Human tissue kallikrein gene transfer rescues ischemic tissues in normal mice, and in hypertensive or diabetic animals. Transgenic rats expressing human tissue kallikrein have reduced interstitial fibrosis. Intracerebro-ventribular injection of adenovirus carrying the human tissue kallikrein gene immediately after reperfusion provides neuroprotection against cerebral ischemia injury in a rat model with middle cerebral artery occlusion and in cultured cells by enhancing glial cell migration and inhibiting apoptosis through suppression of oxidative stress and activation of Akt-Bcl-2 signaling pathway | Homo sapiens |
| physiological function | oral administration of tissue kallikrein purified from porcine pancreas results in blood pressure reduction in hypertensive patients | Sus scrofa |
| physiological function | tissue kallikrein/kinin infusion not only prevents but also reverses kidney injury, inflammation and fibrosis in salt-induced hypertensive rats. Wide time window for kallikrein administration in protection against ischemic brain infarction: delayed kallikrein infusion for 24 h after cerebral ischemia in rats is effective in reducing neurological deficits, infarct size, apoptosis and inflammation. Tissue kallikrein induces contraction of isolated rat uterus in the absence of kinin formation, and elicites cardioprotection by direct kinin B2 receptor activation in kininogen-deficient Brown Norway rats. A subdepressor dose of kallikrein protein or kinin peptide restores impaired cardiac function in rats with postinfarction failure by inhibiting hypertrophy and fibrosis and promoting angiogenesis through increased NO formation and inhibition of oxidative stress and TGF-beta expression. Local application of tissue kallikrein promotes skin wound healing in rats | Rattus norvegicus |
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