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Literature summary extracted from
- The new human tissue kallikrein gene family: structure, function, and association to disease (2001), Endocr. Rev., 22, 184-204.
Activating Compound
| EC Number | Activating Compound | Comment | Organism | Structure |
|---|---|---|---|---|
| 3.4.21.B10 | androgens | slight up-regulation | Homo sapiens | |
| 3.4.21.B10 | estrogen | up-regulaion | Homo sapiens |  |
| 3.4.21.B10 | progestins | up-regulaion | Homo sapiens | |
| 3.4.21.B12 | androgens | up-regulation of gene expression | Homo sapiens | |
| 3.4.21.B12 | progestins | up-regulation of gene expression in breast carcinoma | Homo sapiens | |
| 3.4.21.B39 | androgens | slight up-regulation | Homo sapiens | |
| 3.4.21.B39 | estrogen | up-regulaion | Homo sapiens | |
| 3.4.21.B39 | progestins | up-regulaion | Homo sapiens | |
| 3.4.21.77 | androgens | upregulation | Homo sapiens | |
| 3.4.21.77 | progestins | upregulation in breast cancer | Homo sapiens | |
| 3.4.21.117 | additional information | estrogen and glucocorticoids cause up-regulation of gene expression | Homo sapiens |
Application
| EC Number | Application | Comment | Organism |
|---|---|---|---|
| 3.4.21.B12 | medicine | enzyme might be useful as diagnostic marker in ovarian cancer | Homo sapiens |
| 3.4.21.77 | medicine | enzyme is a marker for cancer | Homo sapiens |
| 3.4.21.77 | medicine | used in the diagnosis of prostate cancer | Homo sapiens |
Cloned(Commentary)
| EC Number | Cloned (Comment) | Organism |
|---|---|---|
| 3.4.21.B10 | gene KLK6, genetic organization and structure of the kallikrein gene family, clustered on chromosome 19q13.3-q13.4 | Homo sapiens |
| 3.4.21.B12 | - |
Homo sapiens |
| 3.4.21.35 | genetic organization and structure of the kallikrein gene family, clustered on chromosome 19q13.3-q13.4 | Homo sapiens |
| 3.4.21.B39 | gene KLK5, genetic organization and structure of the kallikrein gene family, clustered on chromosome 19q13.3-q13.4 | Homo sapiens |
| 3.4.21.77 | gene hK3 or KLK3, genetic organization and structure of the kallikrein gene family, clustered on chromosome 19q13.3-q13.4 | Homo sapiens |
| 3.4.21.117 | gene KLK7, genetic organization and structure of the kallikrein gene family, clustered on chromosome 19q13.3-q13.4 | Homo sapiens |
| 3.4.21.118 | gene KLK6, genetic organization and structure of the kallikrein gene family, clustered on chromosome 19q13.3-q13.4 | Homo sapiens |
| 3.4.21.118 | gene KLK8, genetic organization and structure of the kallikrein gene family, clustered on chromosome 19q13.3-q13.4 | Homo sapiens |
Inhibitors
| EC Number | Inhibitors | Comment | Organism | Structure |
|---|---|---|---|---|
| 3.4.21.35 | Protein C inhibitor | cleaves the inhibitor at Arg354-Ser355 without inactivating it; covalent complex formation with K2 | Homo sapiens |
Localization
| EC Number | Localization | Comment | Organism | GeneOntology No. | Textmining |
|---|---|---|---|---|---|
| 3.4.21.77 | extracellular | secretion | Homo sapiens | - |
- |
Natural Substrates/ Products (Substrates)
| EC Number | Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|---|
| 3.4.21.B10 | amyloid precursor proteins + H2O | Homo sapiens | enzyme may play a role in development of Alzheimer's disease | ? | - |
? | |
| 3.4.21.B10 | additional information | Homo sapiens | enzyme is involved in breast and ovarian cancer | ? | - |
? | |
| 3.4.21.B10 | additional information | Homo sapiens | regulation by steroid hormones | ? | - |
? | |
| 3.4.21.B10 | polypeptide + H2O | Homo sapiens | - |
peptides | - |
? | |
| 3.4.21.B12 | additional information | Homo sapiens | enzyme is regulated by steroid hormones, contains androgen response elements in the proximal promotor region | ? | - |
? | |
| 3.4.21.B12 | polypeptide + H2O | Homo sapiens | - |
peptides | - |
? | |
| 3.4.21.35 | kininogen + H2O | Homo sapiens | best substrate | kallidin + kinin heavy chain + kinin light chain | - |
? | |
| 3.4.21.35 | kininogen + H2O | Homo sapiens | enzyme is involved in inflammation, sepsis, pancreatitis, bone metabolism, heart disease, renal disease, and cancer through release of kallidin, i.e. Lys-bradykinin | kallidin + kinin heavy chain + kinin light chain | - |
? | |
| 3.4.21.35 | polypeptide + H2O | Homo sapiens | - |
peptides | - |
? | |
| 3.4.21.35 | polypeptide + H2O | Homo sapiens | implicated in processing of growth factrors and peptide hormones | peptides | - |
? | |
| 3.4.21.B39 | additional information | Homo sapiens | involved in ovarian cancer | ? | - |
? | |
| 3.4.21.B39 | additional information | Homo sapiens | regulation by steroid homones | ? | - |
? | |
| 3.4.21.77 | Fibronectin + H2O | Homo sapiens | - |
? | - |
? | |
| 3.4.21.77 | insulin-like growth factor binding protein-3 + H2O | Homo sapiens | - |
insulin-like growth factor I + ? | i.e. IGF-I | ? | |
| 3.4.21.77 | additional information | Homo sapiens | enzyme is regulated by steroid hormones, it contains 2 androgen-response elements in the proximal PSA promotor | ? | - |
? | |
| 3.4.21.77 | additional information | Homo sapiens | stimulates cell detachment and facilitates tumor spread | ? | - |
? | |
| 3.4.21.77 | plasminogen + H2O | Homo sapiens | - |
plasmin + ? | - |
? | |
| 3.4.21.77 | polypeptide + H2O | Homo sapiens | enzyme possibly is involved in the processing of insulin-like growth factor binding protein 3 | peptides | - |
? | |
| 3.4.21.77 | proform of transforming growth factor-beta + H2O | Homo sapiens | - |
transforming growth factor-beta + ? | i.e. IGF-beta | ? | |
| 3.4.21.77 | semenogelin + H2O | Homo sapiens | - |
semenogelin fractions | - |
? | |
| 3.4.21.117 | polypeptide + H2O | Homo sapiens | involved in pathological keratinization, psoriasis, and ovarian cancer | peptides | - |
? | |
| 3.4.21.118 | additional information | Homo sapiens | enzyme might be involved in ovarian cancer, brain damage and kindling epilepsy | ? | - |
? | |
| 3.4.21.118 | polypeptide + H2O | Homo sapiens | - |
peptides | - |
? | |
Organism
| EC Number | Organism | UniProt | Comment | Textmining |
|---|---|---|---|---|
| 3.4.21.B10 | Homo sapiens | Q92876 | gene KLK6 | - |
| 3.4.21.B12 | Homo sapiens | Q9Y5K2 | - |
- |
| 3.4.21.35 | Homo sapiens | - |
- |
- |
| 3.4.21.35 | Homo sapiens | P06870 | gene KLK1 | - |
| 3.4.21.B39 | Homo sapiens | Q9Y337 | gene KLK5 or SCTE | - |
| 3.4.21.B39 | Homo sapiens | Q9Y337 | gene KLK5 | - |
| 3.4.21.77 | Homo sapiens | P07288 | - |
- |
| 3.4.21.117 | Homo sapiens | P49862 | - |
- |
| 3.4.21.118 | Homo sapiens | O60259 | gene KLK8 | - |
Posttranslational Modification
| EC Number | Posttranslational Modification | Comment | Organism |
|---|---|---|---|
| 3.4.21.77 | proteolytic modification | enzyme can be activated by recombinant kallikrein 2 | Homo sapiens |
Reaction
| EC Number | Reaction | Comment | Organism | Reaction ID |
|---|---|---|---|---|
| 3.4.21.B10 | proteolytic cleavage of polypeptides | substrate binding pocket contains an Asp residue | Homo sapiens | |
| 3.4.21.B12 | proteolysis of polypeptides | substrate binding pocket contains an Asp residue | Homo sapiens | |
| 3.4.21.B12 | proteolysis of polypeptides | enzyme is a serine protease | Homo sapiens | |
| 3.4.21.35 | Preferential cleavage of Arg-/- bonds in small molecule substrates. Highly selective action to release kallidin (lysyl-bradykinin) from kininogen involves hydrolysis of Met-/- or Leu-/-. The rat enzyme is unusual in liberating bradykinin directly from autologous kininogens by cleavage at two Arg-/- bonds | substrate binding pocket contains an Asp residue | Homo sapiens | |
| 3.4.21.35 | Preferential cleavage of Arg-/- bonds in small molecule substrates. Highly selective action to release kallidin (lysyl-bradykinin) from kininogen involves hydrolysis of Met-/- or Leu-/-. The rat enzyme is unusual in liberating bradykinin directly from autologous kininogens by cleavage at two Arg-/- bonds | trypsin-like serine protease | Homo sapiens | |
| 3.4.21.B39 | proteolytic cleavage of polypeptides | substrate binding pocket contains an Asp residue | Homo sapiens | |
| 3.4.21.77 | Preferential cleavage: -Tyr-/- | enzyme is a serine protease | Homo sapiens | |
| 3.4.21.77 | Preferential cleavage: -Tyr-/- | enzyme contains a serine residue in the substrate binding pocket | Homo sapiens | |
| 3.4.21.77 | Preferential cleavage: -Tyr-/- | enzyme shows chymotrypsin-like activity | Homo sapiens | |
| 3.4.21.117 | cleavage of proteins with aromatic side chains in the P1 position | substrate binding pocket contains an Asn residue | Homo sapiens | |
| 3.4.21.118 | cleavage of amide substrates following the basic amino acids Arg or Lys at the P1 position, with a preference for Arg over Lys | substrate binding pocket contains an Asp residue | Homo sapiens |
Source Tissue
| EC Number | Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|---|
| 3.4.21.B10 | breast | high expression level | Homo sapiens | - |
| 3.4.21.B10 | breast carcinoma cell | up-regulated in primary tumors | Homo sapiens | - |
| 3.4.21.B10 | breast carcinoma cell | highly down-regulated at metastatic breast cancer sites | Homo sapiens | - |
| 3.4.21.B10 | BT-474 cell | breast carcinoma cell line, enzyme is up-regulated by estrogens, progestin and slightly by androgen | Homo sapiens | - |
| 3.4.21.B10 | central nervous system | high expression level | Homo sapiens | - |
| 3.4.21.B10 | kidney | high expression level | Homo sapiens | - |
| 3.4.21.B10 | ovarian carcinoma cell | up-regulated in primary tumors | Homo sapiens | - |
| 3.4.21.B10 | ovary | - |
Homo sapiens | - |
| 3.4.21.B10 | salivary gland | - |
Homo sapiens | - |
| 3.4.21.B10 | spleen | - |
Homo sapiens | - |
| 3.4.21.B10 | testis | - |
Homo sapiens | - |
| 3.4.21.B10 | uterus | high expression level | Homo sapiens | - |
| 3.4.21.B12 | BT-474 cell | breast carcinoma cell line, enzyme is upregulated by progetsins and androgens | Homo sapiens | - |
| 3.4.21.B12 | cell culture | breast carcinoma cell line | Homo sapiens | - |
| 3.4.21.B12 | LNCaP cell | prostate carcinoma cell line, enzyme is upregulated by androgens | Homo sapiens | - |
| 3.4.21.B12 | ovarian carcinoma cell | gene overexpression | Homo sapiens | - |
| 3.4.21.35 | breast | lower content | Homo sapiens | - |
| 3.4.21.35 | endometrium | activity is higher during the middle of the menstrual cycle, possible up-regulation by estrogens | Homo sapiens | - |
| 3.4.21.35 | intestine | - |
Homo sapiens | - |
| 3.4.21.35 | intestine | low content | Homo sapiens | - |
| 3.4.21.35 | kidney | - |
Homo sapiens | - |
| 3.4.21.35 | neutrophil | low content | Homo sapiens | - |
| 3.4.21.35 | pancreas | - |
Homo sapiens | - |
| 3.4.21.35 | pituitary gland | - |
Homo sapiens | - |
| 3.4.21.35 | placenta | lower content | Homo sapiens | - |
| 3.4.21.35 | prostate gland | - |
Homo sapiens | - |
| 3.4.21.35 | prostate gland | low content | Homo sapiens | - |
| 3.4.21.35 | salivary gland | - |
Homo sapiens | - |
| 3.4.21.35 | sweat gland | low content | Homo sapiens | - |
| 3.4.21.35 | testis | lower content | Homo sapiens | - |
| 3.4.21.35 | uterus | low content | Homo sapiens | - |
| 3.4.21.B39 | brain | high expression level | Homo sapiens | - |
| 3.4.21.B39 | breast | high expression level | Homo sapiens | - |
| 3.4.21.B39 | ovarian carcinoma cell | gene overexpression in a subset of more aggressive ovarian tumors | Homo sapiens | - |
| 3.4.21.B39 | prostate | - |
Homo sapiens | - |
| 3.4.21.B39 | salivary gland | - |
Homo sapiens | - |
| 3.4.21.B39 | skin | high expression level | Homo sapiens | - |
| 3.4.21.B39 | testis | high expression level | Homo sapiens | - |
| 3.4.21.B39 | thymus | - |
Homo sapiens | - |
| 3.4.21.B39 | thyroid gland | - |
Homo sapiens | - |
| 3.4.21.B39 | trachea | - |
Homo sapiens | - |
| 3.4.21.77 | breast | female | Homo sapiens | - |
| 3.4.21.77 | breast carcinoma cell | - |
Homo sapiens | - |
| 3.4.21.77 | BT-474 cell | breast carcinoma cell line, enzyme is upregulated by progestins and androgens | Homo sapiens | - |
| 3.4.21.77 | lung | - |
Homo sapiens | - |
| 3.4.21.77 | prostate | highest expression level | Homo sapiens | - |
| 3.4.21.77 | prostate cancer cell | upregulation of gene expression by androgens | Homo sapiens | - |
| 3.4.21.77 | prostate cancer cell | metastatic prostate adenocarcinoma cell line LNCaP | Homo sapiens | - |
| 3.4.21.77 | salivary gland | - |
Homo sapiens | - |
| 3.4.21.77 | seminal plasma | - |
Homo sapiens | - |
| 3.4.21.77 | T47-D cell | breast carcinoma cell line, enzyme is upregulated by progestins and androgens | Homo sapiens | - |
| 3.4.21.77 | thyroid gland | - |
Homo sapiens | - |
| 3.4.21.77 | trachea | - |
Homo sapiens | - |
| 3.4.21.117 | breast | - |
Homo sapiens | - |
| 3.4.21.117 | BT-474 cell | breast carcinoma cell line, enzyme is upregulated by estrogens and slightly by glucocorticoids | Homo sapiens | - |
| 3.4.21.117 | central nervous system | - |
Homo sapiens | - |
| 3.4.21.117 | kidney | - |
Homo sapiens | - |
| 3.4.21.117 | ovarian carcinoma cell | overexpression of the enzyme | Homo sapiens | - |
| 3.4.21.117 | ovary | - |
Homo sapiens | - |
| 3.4.21.117 | placenta | low content | Homo sapiens | - |
| 3.4.21.117 | salivary gland | low content | Homo sapiens | - |
| 3.4.21.117 | skin | - |
Homo sapiens | - |
| 3.4.21.117 | testis | low content | Homo sapiens | - |
| 3.4.21.117 | thymus | low content | Homo sapiens | - |
| 3.4.21.117 | thyroid gland | low content | Homo sapiens | - |
| 3.4.21.117 | trachea | low content | Homo sapiens | - |
| 3.4.21.117 | uterus | low content | Homo sapiens | - |
| 3.4.21.118 | central nervous system | high expression level | Homo sapiens | - |
| 3.4.21.118 | ovarian carcinoma cell | overexpression | Homo sapiens | - |
| 3.4.21.118 | ovary | high expression level | Homo sapiens | - |
| 3.4.21.118 | skin | high expression level | Homo sapiens | - |
Substrates and Products (Substrate)
| EC Number | Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|---|
| 3.4.21.B10 | amyloid precursor proteins + H2O | - |
Homo sapiens | ? | - |
? | |
| 3.4.21.B10 | amyloid precursor proteins + H2O | enzyme may play a role in development of Alzheimer's disease | Homo sapiens | ? | - |
? | |
| 3.4.21.B10 | additional information | enzyme is involved in breast and ovarian cancer | Homo sapiens | ? | - |
? | |
| 3.4.21.B10 | additional information | regulation by steroid hormones | Homo sapiens | ? | - |
? | |
| 3.4.21.B10 | polypeptide + H2O | - |
Homo sapiens | peptides | - |
? | |
| 3.4.21.B12 | additional information | enzyme is regulated by steroid hormones, contains androgen response elements in the proximal promotor region | Homo sapiens | ? | - |
? | |
| 3.4.21.B12 | polypeptide + H2O | - |
Homo sapiens | peptides | - |
? | |
| 3.4.21.35 | angiotensinogen + H2O | - |
Homo sapiens | angiotensin | - |
? | |
| 3.4.21.35 | kininogen + H2O | best substrate | Homo sapiens | kallidin + kinin heavy chain + kinin light chain | - |
? | |
| 3.4.21.35 | kininogen + H2O | enzyme is involved in inflammation, sepsis, pancreatitis, bone metabolism, heart disease, renal disease, and cancer through release of kallidin, i.e. Lys-bradykinin | Homo sapiens | kallidin + kinin heavy chain + kinin light chain | - |
? | |
| 3.4.21.35 | low density lipoprotein + H2O | - |
Homo sapiens | ? | - |
? | |
| 3.4.21.35 | low-molecular-weight kininogen + H2O | - |
Homo sapiens | kallidin + kinin | kallidin is Lys-bradykinin | ? | |
| 3.4.21.35 | low-molecular-weight kininogen + H2O | cleavage sequence and sites | Homo sapiens | kallidin + kinin | kallidin is Lys-bradykinin | ? | |
| 3.4.21.35 | polypeptide + H2O | - |
Homo sapiens | peptides | - |
? | |
| 3.4.21.35 | polypeptide + H2O | implicated in processing of growth factrors and peptide hormones | Homo sapiens | peptides | - |
? | |
| 3.4.21.35 | precursor of atrial natriuretic factor + H2O | - |
Homo sapiens | natriuretic factor | - |
? | |
| 3.4.21.35 | pro-collagenase + H2O | - |
Homo sapiens | collagease | - |
? | |
| 3.4.21.35 | pro-insulin + H2O | - |
Homo sapiens | insulin + insulin signal peptide | - |
? | |
| 3.4.21.35 | pro-renin + H2O | - |
Homo sapiens | renin | - |
? | |
| 3.4.21.35 | Vasoactive intestinal peptide + H2O | - |
Homo sapiens | ? | - |
? | |
| 3.4.21.B39 | additional information | involved in ovarian cancer | Homo sapiens | ? | - |
? | |
| 3.4.21.B39 | additional information | regulation by steroid homones | Homo sapiens | ? | - |
? | |
| 3.4.21.77 | Fibronectin + H2O | - |
Homo sapiens | ? | - |
? | |
| 3.4.21.77 | insulin-like growth factor binding protein-3 + H2O | - |
Homo sapiens | insulin-like growth factor I + ? | i.e. IGF-I | ? | |
| 3.4.21.77 | additional information | enzyme is regulated by steroid hormones, it contains 2 androgen-response elements in the proximal PSA promotor | Homo sapiens | ? | - |
? | |
| 3.4.21.77 | additional information | stimulates cell detachment and facilitates tumor spread | Homo sapiens | ? | - |
? | |
| 3.4.21.77 | plasminogen + H2O | - |
Homo sapiens | plasmin + ? | - |
? | |
| 3.4.21.77 | polypeptide + H2O | - |
Homo sapiens | peptides | - |
? | |
| 3.4.21.77 | polypeptide + H2O | enzyme possibly is involved in the processing of insulin-like growth factor binding protein 3 | Homo sapiens | peptides | - |
? | |
| 3.4.21.77 | proform of transforming growth factor-beta + H2O | - |
Homo sapiens | transforming growth factor-beta + ? | i.e. IGF-beta | ? | |
| 3.4.21.77 | semenogelin + H2O | semenogelins I and II | Homo sapiens | semenogelin fragments | - |
? | |
| 3.4.21.77 | semenogelin + H2O | - |
Homo sapiens | semenogelin fractions | - |
? | |
| 3.4.21.117 | polypeptide + H2O | - |
Homo sapiens | peptides | - |
? | |
| 3.4.21.117 | polypeptide + H2O | involved in pathological keratinization, psoriasis, and ovarian cancer | Homo sapiens | peptides | - |
? | |
| 3.4.21.118 | additional information | enzyme might be involved in ovarian cancer, brain damage and kindling epilepsy | Homo sapiens | ? | - |
? | |
| 3.4.21.118 | polypeptide + H2O | - |
Homo sapiens | peptides | - |
? | |
Synonyms
| EC Number | Synonyms | Comment | Organism |
|---|---|---|---|
| 3.4.21.B10 | protease M | - |
Homo sapiens |
| 3.4.21.B12 | EMSP1 | - |
Homo sapiens |
| 3.4.21.B12 | K4 | - |
Homo sapiens |
| 3.4.21.B12 | PRSS17 | - |
Homo sapiens |
| 3.4.21.35 | pancreatic/renal kallikrein | - |
Homo sapiens |
| 3.4.21.35 | renal kallikrein | - |
Homo sapiens |
| 3.4.21.B39 | K5 | - |
Homo sapiens |
| 3.4.21.B39 | SCTE | - |
Homo sapiens |
| 3.4.21.77 | K3 | - |
Homo sapiens |
| 3.4.21.77 | prostate-specific antigen | - |
Homo sapiens |
| 3.4.21.117 | K7 | - |
Homo sapiens |
| 3.4.21.117 | SCCE | - |
Homo sapiens |
| 3.4.21.118 | ovasin | - |
Homo sapiens |
| 3.4.21.118 | TADG14 | - |
Homo sapiens |
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