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Ligands
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BEN Benzamidine
FLC Citrate anion
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Glycosylation
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Code : 1C5Z   PDBj   RCSB PDB   PDBe
Header : BLOOD CLOTTING
Title : STRUCTURAL BASIS FOR SELECTIVITY OF A SMALL MOLECULE, S1-BINDING, SUB-MICROMOLAR INHIBITOR OF UROKINASE TYPE PLASMINOGEN ACTIVATOR
Release Data : 2000-12-22
Compound :
mol_id molecule chains
1 PROTEIN (UROKINASE-TYPE PLASMINOGEN ACTIVATOR) A
ec: 3.4.21.73
fragment: SHORT CHAIN
mol_id molecule chains
2 PROTEIN (UROKINASE-TYPE PLASMINOGEN ACTIVATOR) B
ec: 3.4.21.73
fragment: CATALYTIC DOMAIN
Source :
mol_id organism_scientific organism_common expression_system
1 Homo sapiens  (taxid:9606) Human Pichia pastoris  (taxid:4922)
expression_system_strain: HISTIDINE DEFICIENT GS115
expression_system_vector_type: PLASMID
expression_system_plasmid: PPIC9
mol_id organism_scientific organism_common expression_system
2 Homo sapiens  (taxid:9606) Human Pichia pastoris  (taxid:4922)
expression_system_strain: HISTIDINE DEFICIENT GS115
expression_system_vector_type: PLASMID
expression_system_plasmid: PPIC9
Authors : Katz, B.A., Mackman, R., Luong, C., Radika, K., Martelli, A., Sprengeler, P.A., Wang, J., Chan, H., Wong, L.
Keywords : selective, S1 site inhibitor, structure-based drug design, urokinase, trypsin, thrombin, BLOOD CLOTTING
Exp. method : X-RAY DIFFRACTION ( 1.85 Å )
Citation :

Structural basis for selectivity of a small molecule, S1-binding, submicromolar inhibitor of urokinase-type plasminogen activator.

Katz, B.A.,Mackman, R.,Luong, C.  et al.
(2000)  Chem.Biol.  7 : 299 - 312

PubMed: 10779411
DOI: 10.1016/S1074-5521(00)00104-6

Chain : B
UniProt : P00749 (UROK_HUMAN)
Reaction: EC: Evidence:
Physiological Direction:
Specific cleavage of Arg-|-Val bond in plasminogen to form plasmin. 3.4.21.73 -
-