› 1a5h

X-ray diffraction
2.9Å resolution

CATALYTIC DOMAIN OF HUMAN TWO-CHAIN TISSUE PLASMINOGEN ACTIVATOR COMPLEX OF A BIS-BENZAMIDINE

Released:
DOI: 10.2210/pdb1a5h/pdb
PDB entry 1a5h coloured by chain, front view.
PDB entry 1a5h coloured by chain, side view.
PDB entry 1a5h coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Structural mapping of the active site specificity determinants of human tissue-type plasminogen activator. Implications for the design of low molecular weight substrates and inhibitors.
Renatus M, Bode W, Huber R, Stürzebecher J, Prasa D, Fischer S, Kohnert U, Stubbs MT
J Biol Chem 272 21713-9 (1997)
PMID: 9268299

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 domain:

Structure analysis Details

Assembly composition:
hetero dimer (preferred)
Assembly name:
PDBe Complex ID:
PDB-CPX-133300 (preferred)
Entry contents:
2 distinct polypeptide molecules
Macromolecules (2 distinct):
Tissue-type plasminogen activator chain A Chains: C, D
Molecule details ›
Chains: C, D
Length: 7 amino acids
Theoretical weight: 841 Da
Source organism: Homo sapiens
Expression system: Escherichia coli
UniProt:
  • Canonical: P00750 (Residues: 298-304; Coverage: 1%)
Gene name: PLAT
Tissue-type plasminogen activator chain B Chains: A, B
Molecule details ›
Chains: A, B
Length: 252 amino acids
Theoretical weight: 28.16 KDa
Source organism: Homo sapiens
Expression system: Escherichia coli
UniProt:
  • Canonical: P00750 (Residues: 311-562; Coverage: 47%)
Gene name: PLAT
Sequence domains: Trypsin
Structure domains: Trypsin-like serine proteases

Ligands and Environments

1 bound ligand:
Ligand BBA 2 x BBA
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: RIGAKU RUH2R
Spacegroup: C2
Unit cell:
a: 151.83Å b: 60.5Å c: 62.61Å
α: 90° β: 110.5° γ: 90°
R-values:
R R work R free
0.178 0.178 not available
Expression system: Escherichia coli

Quick links

Citations

5 review citations

Structural and energetic determinants of the S1-site specificity in serine proteases.
Czapinska et al. (1999)
4 more

20 mentions without citation

Systems pharmacological study illustrates the immune regulation, anti-infection, anti-inflammation, and multi-organ protection mechanism of Qing-Fei-Pai-Du decoction in the treatment of COVID-19.
Zhao et al. (2021)
19 more