Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 3.4.21.73 extracted from

  • Katz, B.A.; Mackman, R.; Luong, C.; Radika, K.; Martelli, A.; Sprengeler, P.A.; Wang, J.; Chan, H.; Wong, L.
    Structural basis for selectivity of a small molecule, S1-binding, submicromolar inhibitor of urokinase-type plasminogen activator (2000), Chem. Biol., 7, 299-312.
    View publication on PubMed
Search for more literature for 3.4.21.73

Application

Application Comment Organism
medicine associated with tumor metastasis and invasion, selective inhibitors of uPA may have potential as therapeutically useful drugs for prostate, breast and other cancers Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
cloning of low molecular weight uPA, expression in Pichia pastoris Homo sapiens

Crystallization (Commentary)

Crystallization (Comment) Organism
crystallized by vapor diffusion in hanging drops in complex with 4-iodobenzo[b]thiophene-2-carboxamidine and benzamidine, space group C2, ProteinDataBank accession code 1C5Z for uPA-benzamidine, 1C5Y for uPA-thieno[2,3-b]pyridine-2-carboxamidine Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
4-iodobenzo[b]thiophene-2-carboxamidine APC-6860, competitive inhibition Homo sapiens
benzamidine
-
 Homo sapiens
benzo[b]thiophene-2-carboxamidine APC-7377 Homo sapiens
thieno[2,3-b]pyridine-2-carboxamidine APC-7538 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
 human
-

Purification (Commentary)

Purification (Comment) Organism
recombinant enzyme Homo sapiens

Synonyms

Synonyms Comment Organism
Urokinase-type plasminogen activator
-
 Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00021
-
 4-iodobenzo[b]thiophene-2-carboxamidine pH 7.4, 37°C Homo sapiens
0.0023
-
 benzo[b]thiophene-2-carboxamidine pH 7.4, 37°C Homo sapiens
0.063
-
 thieno[2,3-b]pyridine-2-carboxamidine pH 7.4, 37°C Homo sapiens
0.097
-
 benzamidine pH 7.4, 37°C Homo sapiens