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Literature summary for 3.4.21.122 extracted from

  • Lucas, J.M.; Heinlein, C.; Kim, T.; Hernandez, S.A.; Malik, M.S.; True, L.D.; Morrissey, C.; Corey, E.; Montgomery, B.; Mostaghel, E.; Clegg, N.; Coleman, I.; Brown, C.M.; Schneider, E.L.; Craik, C.; Simon, J.A.; Bedalov, A.; Nelson, P.S.
    The androgen-regulated protease TMPRSS2 activates a proteolytic cascade involving components of the tumor microenvironment and promotes prostate cancer metastasis (2014), Cancer Discov., 4, 1310-1325 .
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.4.21.122

Application

Application Comment Organism
medicine primary prostate cancer and prostate cancer metastases. TMPRSS2 expression is significantly higher in both neoplastic prostate and in the epithelium of prostatic hyperplasia compared to normal epithelium. TMPRSS2 expression is further elevated in higher Gleason grade cancers (patterns 4 and 5) compared to pattern 3. In most high-grade cancers, TMPRSS2 is mislocalized, being expressed in the cytoplasm as well as in the cell membrane Homo sapiens
medicine TMPRSS2 protease is highly expressed in metastatic prostate cancers and promotes cancer invasion and metastasis Mus musculus

Inhibitors

Inhibitors Comment Organism Structure
bromhexine treatment significantly reduces the migration and invasion phenotypes promoted by TMPRSS2-activated HGF Mus musculus

Localization

Localization Comment Organism GeneOntology No. Textmining
cytoplasm in most high-grade cancers, TMPRSS2 is mislocalized, being expressed in the cytoplasm as well as in the cell membrane Homo sapiens 5737
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membrane in most high-grade cancers, TMPRSS2 is mislocalized, being expressed in the cytoplasm as well as in the cell membrane Homo sapiens 16020
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Organism

Organism UniProt Comment Textmining
Homo sapiens O15393
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Mus musculus Q9JIQ8
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Source Tissue

Source Tissue Comment Organism Textmining
breast low expression level Homo sapiens
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colon low expression level Homo sapiens
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epididymis low expression level Homo sapiens
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prostate gland TMPRSS2 protein is abundantly expressed in the prostate. Protein is specifically localized to the secretory epithelium, with enhanced expression in the plasma membrane orientated towards the ductal lumen Homo sapiens
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prostate gland cancer cell primary prostate cancer and prostate cancer metastases. TMPRSS2 expression is significantly higher in both neoplastic prostate and in the epithelium of prostatic hyperplasia compared to normal epithelium. TMPRSS2 expression is further elevated in higher Gleason grade cancers (patterns 4 and 5) compared to pattern 3 Homo sapiens
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prostate gland cancer cell TMPRSS2 protease is highly expressed in metastatic prostate cancers Mus musculus
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seminal plasma TMPRSS2 is a component of the normal seminal fluid proteome Homo sapiens
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stomach low expression level Homo sapiens
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Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Boc-Gln-Ala-Arg-MCA + H2O
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 Mus musculus Boc-Gln-Ala-Arg + 7-amino-4-methylcoumarin
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 ?
additional information at the P1 position, TMPRSS2 strongly prefers substrates with an arginine rather than a lysine. The P1' position may comprise a hydrophobic amino acid (isoleucine or valine) to bind to the large, hydrophobic S1 pocket of TMPRSS2 Mus musculus ?
-
 ?
pro-hepatocyte growth factor + H2O
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 Mus musculus ?
-
 ?
pro-kallikrein 2 + H2O
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 Mus musculus ?
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 ?

Expression

Organism Comment Expression
Mus musculus TMPRSS2 expression is regulated by androgens in vivo additional information
Homo sapiens TMPRSS2 protein expression is regulated by androgens up