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Literature summary for 3.4.24.B28 extracted from

  • Lorenzatti Hiles, G.; Bucheit, A.; Rubin, J.R.; Hayward, A.; Cates, A.L.; Day, K.C.; El-Sawy, L.; Kunju, L.P.; Daignault, S.; Lee, C.T.; Liebert, M.; Hussain, M.; Day, M.L.
    ADAM15 Is functionally associated with the metastatic progression of human bladder cancer (2016), PLoS ONE, 11, e0150138 .
    View publication on PubMedView publication on EuropePMC
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Application

Application Comment Organism
medicine ADAM15 ranks in the top 5% of amplified genes and its mRNA is significantly overexpressed in invasive and metastatic bladder cancer compared to noninvasive disease. In metastatic samples, increased ADAM15 immunoreactivity is associated with increasing cancer stage and exhibits significantly stronger staining. The knockdown of ADAM15 mRNA expression significantly inhibits bladder tumor cell migration and reduces the invasive capacity of bladder tumor cells through MatrigelTM and monolayers of vascular endothelium. The knockdown of ADAM15 in a human xenograft model of bladder cancer inhibits tumor growth by 45% compared to controls Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
adamastat sulfonamide inhibitor, binds to the active site of the ADAM15 metalloproteinase domain with a calculated binding energy of -9.0 kcal/mol.In the preferred binding mode, the biphenyl amino side chain of the inhibitor resides in the deep amphipathic S1' amino acid recognition pocket of the ADAM15 catalytic domain. Adamastat significantly inhibits the viability of UM-UC-9 and UM-UC-6 cells at 10 microM Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
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-
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Source Tissue

Source Tissue Comment Organism Textmining
bladder
-
 Homo sapiens
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carcinoma cell
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 Homo sapiens
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Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
dabcyl-HGDQMAQKSK(5FAM)-NH2 + H2O
-
 Homo sapiens ?
-
 ?