› 2v0z

X-ray diffraction
2.2Å resolution

Crystal Structure of Renin with Inhibitor 10 (Aliskiren)

Released:
DOI: 10.2210/pdb2v0z/pdb
PDB entry 2v0z coloured by chain, front view.
PDB entry 2v0z coloured by chain, side view.
PDB entry 2v0z coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Structure-based drug design: the discovery of novel nonpeptide orally active inhibitors of human renin.
Rahuel J, Rasetti V, Maibaum J, Rüeger H, Göschke R, Cohen NC, Stutz S, Cumin F, Fuhrer W, Wood JM, Grütter MG
Chem Biol 7 493-504 (2000)
PMID: 10903938

Function and Biology Details

Reaction catalysed: 
Cleavage of Leu-|- bond in angiotensinogen to generate angiotensin I.
Biochemical function:
Biological process:
Cellular component:
  • not assigned
Sequence domains:

Structure analysis Details

Assembly composition:
monomeric (preferred)
Assembly name:
PDBe Complex ID:
PDB-CPX-133565 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Renin Chains: C, O
Molecule details ›
Chains: C, O
Length: 340 amino acids
Theoretical weight: 37.27 KDa
Source organism: Homo sapiens
Expression system: Cricetulus griseus
UniProt:
  • Canonical: P00797 (Residues: 67-406; Coverage: 89%)
Gene name: REN
Sequence domains: Eukaryotic aspartyl protease
Structure domains: Acid Proteases

Ligands and Environments

2 bound ligands:
Ligand NAG 2 x NAG
Ligand C41 2 x C41
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: ENRAF-NONIUS FR591
Spacegroup: P213
Unit cell:
a: 141.6Å b: 141.6Å c: 141.6Å
α: 90° β: 90° γ: 90°
R-values:
R R work R free
0.205 0.205 0.266
Expression system: Cricetulus griseus

Quick links

Citations

56 review citations

Renin inhibition with aliskiren: where are we now, and where are we going?
Azizi et al. (2006)
55 more

15 mentions without citation

A Comprehensive Review on Cannabis sativa Ethnobotany, Phytochemistry, Molecular Docking and Biological Activities.
Hourfane et al. (2023)
14 more