› 2vnt

X-ray diffraction
2.2Å resolution

UROKINASE-TYPE PLASMINOGEN ACTIVATOR INHIBITOR COMPLEX WITH A 1-(7- SULPHOAMIDOISOQUINOLINYL)GUANIDINE

Released:
DOI: 10.2210/pdb2vnt/pdb
PDB entry 2vnt coloured by chain, front view.
PDB entry 2vnt coloured by chain, side view.
PDB entry 2vnt coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Selective urokinase-type plasminogen activator inhibitors. 4. 1-(7-sulfonamidoisoquinolinyl)guanidines.
Fish PV, Barber CG, Brown DG, Butt R, Collis MG, Dickinson RP, Henry BT, Horne VA, Huggins JP, King E, O'Gara M, McCleverty D, McIntosh F, Phillips C, Webster R
J Med Chem 50 2341-51 (2007)
PMID: 17447747

Function and Biology Details

Reaction catalysed: 
Specific cleavage of Arg-|-Val bond in plasminogen to form plasmin.
Biochemical function:
Biological process:
Cellular component:
  • not assigned
Sequence domains:

Structure analysis Details

Assembly composition:
monomeric (preferred)
Assembly name:
PDBe Complex ID:
PDB-CPX-133249 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Urokinase-type plasminogen activator chain B Chains: A, B, C, D, E, F
Molecule details ›
Chains: A, B, C, D, E, F
Length: 276 amino acids
Theoretical weight: 31.17 KDa
Source organism: Homo sapiens
Expression system: Escherichia coli
UniProt:
  • Canonical: P00749 (Residues: 156-431; Coverage: 67%)
Gene name: PLAU
Sequence domains: Trypsin
Structure domains: Trypsin-like serine proteases

Ligands and Environments

2 bound ligands:
Ligand QGG 6 x QGG
Ligand SO4 9 x SO4
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: SRS
Spacegroup: C2
Unit cell:
a: 104.557Å b: 181.108Å c: 104.363Å
α: 90° β: 94.8° γ: 90°
R-values:
R R work R free
0.244 0.241 0.295
Expression system: Escherichia coli

Quick links

Citations

4 review citations

Modulators of the urokinase-type plasminogen activation system for cancer.
Hildenbrand et al. (2010)
3 more

2 mentions without citation

Can EGCG Alleviate Symptoms of Down Syndrome by Altering Proteolytic Activity?
Wyganowska-Świątkowska et al. (2018)
1 more