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Literature summary for 3.4.21.109 extracted from

  • Damalanka, V.C.; Han, Z.; Karmakar, P.; ODonoghue, A.J.; La Greca, F.; Kim, T.; Pant, S.M.; Helander, J.; Klefstroem, J.; Craik, C.S.; Janetka, J.W.
    Discovery of selective matriptase and hepsin serine protease inhibitors useful chemical tools for cancer cell biology (2019), J. Med. Chem., 62, 480-490 .
    View publication on PubMed

Crystallization (Commentary)

Crystallization (Comment) Organism
molecular docking of inhibitor. The P1 and P2 binding sites are occupied by the conserved Arg and then the variable second side chain, respectively. The 9-fluorenylmethyloxycarbonyl group forms pi-pi interactions with the conserved Trp in the P4 pocket Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
9-fluorenylmethyloxycarbonyl-GR-ketobenzothiazole potent and selective inhibitor for matriptase over hepsin Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens Q9Y5Y6
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Boc-QAR-Amc + H2O
-
Homo sapiens ?
-
?

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00000013
-
9-fluorenylmethyloxycarbonyl-GR-ketobenzothiazole pH not specified in the publication, temperature not specified in the publication Homo sapiens

General Information

General Information Comment Organism
physiological function hepsin alone and not matriptase or HGFA plays a key role in diminishing epithelial cell membrane integrity through degradation of desmogelin-2 in breast cancer cells Homo sapiens