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Literature summary for 3.4.21.73 extracted from

  • Schweinitz, A.; Steinmetzer, T.; Banke, I.J.; Arlt, M.J.; Sturzebecher, A.; Schuster, O.; Geissler, A.; Giersiefen, H.; Zeslawska, E.; Jacob, U.; Kruger, A.; Sturzebecher, J.
    Design of novel and selective inhibitors of urokinase-type plasminogen activator with improved pharmacokinetic properties for use as antimetastatic agents (2004), J. Biol. Chem., 279, 33613-33622.
    View publication on PubMed

Application

Application Comment Organism
medicine treatment of cancer with small-molecule active-site inhibitors with a C-terminal 4-amindinobenzylamide residue to prevent metastasis. Inhibitor dose of 2 x 1.5 mg/kg/day of inhibitor N-(benzylsulfonyl)-D-seryl-N-(4-carbamimidoylbenzyl)-L-serinamide reduces number of metastases to 4.6% in mice Homo sapiens

Crystallization (Commentary)

Crystallization (Comment) Organism
in complex with inhibitor N-[(4-chlorobenzyl)sulfonyl]-D-seryl-N-(4-carbamimidoylbenzyl)-L-alaninamide, N-(benzylsulfonyl)-D-seryl-N-(4-carbamimidoylbenzyl)-L-serinamide and N-(benzylsulfonyl)-D-seryl-N-(4-carbamimidoylbenzyl)glycinamide Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
N-(benzylsulfonyl)-D-seryl-N-(4-carbamimidoylbenzyl)-L-alaninamide comparison of specificity with five additional trypsin-like serine-proteases Homo sapiens
N-(benzylsulfonyl)-D-seryl-N-(4-carbamimidoylbenzyl)-L-prolinamide comparison of specificity with five additional trypsin-like serine-proteases Homo sapiens
N-(benzylsulfonyl)-D-seryl-N-(4-carbamimidoylbenzyl)-L-serinamide comparison of specificity with five additional trypsin-like serine-proteases Homo sapiens
N-(benzylsulfonyl)-D-seryl-N-(4-carbamimidoylbenzyl)glycinamide comparison of specificity with five additional trypsin-like serine-proteases Homo sapiens
N-[(4-aminobenzyl)sulfonyl]-D-seryl-N-(4-carbamimidoylbenzyl)glycinamide comparison of specificity with five additional trypsin-like serine-proteases Homo sapiens
N-[(4-chlorobenzyl)sulfonyl]-D-seryl-N-(4-carbamimidoylbenzyl)-L-alaninamide comparison of specificity with five additional trypsin-like serine-proteases Homo sapiens
N-[(4-chlorobenzyl)sulfonyl]-D-seryl-N-(4-carbamimidoylbenzyl)-L-serinamide comparison of specificity with five additional trypsin-like serine-proteases Homo sapiens
N-[(4-methylbenzyl)sulfonyl]-D-seryl-N-(4-carbamimidoylbenzyl)-L-alaninamide comparison of specificity with five additional trypsin-like serine-proteases Homo sapiens
N-[(4-nitrobenzyl)sulfonyl]-D-seryl-N-(4-carbamimidoylbenzyl)glycinamide comparison of specificity with five additional trypsin-like serine-proteases Homo sapiens
N-[[4-(methoxycarbonyl)benzyl]sulfonyl]-D-seryl-N-(4-carbamimidoylbenzyl)-L-alaninamide comparison of specificity with five additional trypsin-like serine-proteases Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P00749
-
-

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0076
-
N-[(4-chlorobenzyl)sulfonyl]-D-seryl-N-(4-carbamimidoylbenzyl)-L-alaninamide
-
Homo sapiens
0.0077
-
N-(benzylsulfonyl)-D-seryl-N-(4-carbamimidoylbenzyl)-L-alaninamide
-
Homo sapiens
0.01
-
N-[(4-methylbenzyl)sulfonyl]-D-seryl-N-(4-carbamimidoylbenzyl)-L-alaninamide
-
Homo sapiens
0.013
-
N-(benzylsulfonyl)-D-seryl-N-(4-carbamimidoylbenzyl)-L-prolinamide
-
Homo sapiens
0.018
-
N-[(4-aminobenzyl)sulfonyl]-D-seryl-N-(4-carbamimidoylbenzyl)glycinamide
-
Homo sapiens
0.018
-
N-[[4-(methoxycarbonyl)benzyl]sulfonyl]-D-seryl-N-(4-carbamimidoylbenzyl)-L-alaninamide
-
Homo sapiens
0.02
-
N-(benzylsulfonyl)-D-seryl-N-(4-carbamimidoylbenzyl)-L-serinamide
-
Homo sapiens
0.023
-
N-[(4-chlorobenzyl)sulfonyl]-D-seryl-N-(4-carbamimidoylbenzyl)-L-serinamide
-
Homo sapiens
0.024
-
N-[(4-nitrobenzyl)sulfonyl]-D-seryl-N-(4-carbamimidoylbenzyl)glycinamide
-
Homo sapiens
0.036
-
N-(benzylsulfonyl)-D-seryl-N-(4-carbamimidoylbenzyl)glycinamide
-
Homo sapiens