› 6e3u

X-ray diffraction
2.85Å resolution

Crystal Structure of the Heterodimeric HIF-2 Complex with Agonist M1001

Released:
DOI: 10.2210/pdb6e3u/pdb
PDB 6e3u coloured by chain and viewed from the front.
PDB 6e3u coloured by chain and viewed from the side.
PDB 6e3u coloured by chain and viewed from the top.
Source organism: Mus musculus
Primary publication:
Bidirectional modulation of HIF-2 activity through chemical ligands.
Wu D, Su X, Lu J, Li S, Hood BL, Vasile S, Potluri N, Diao X, Kim Y, Khorasanizadeh S, Rastinejad F
OpenAccess logo Nat Chem Biol 15 367-376 (2019)
PMID: 30804532

Function and Biology Details

Biochemical function:
  • not assigned
Biological process:
  • not assigned
Cellular component:
  • not assigned
Sequence domains:

Structure analysis Details

Assembly composition:
hetero dimer (preferred)
Entry contents:
2 distinct polypeptide molecules
Macromolecules (2 distinct):
Aryl hydrocarbon receptor nuclear translocator Chain: A
Molecule details ›
Chain: A
Length: 384 amino acids
Theoretical weight: 43.44 KDa
Source organism: Mus musculus
Expression system: Escherichia coli BL21(DE3)
UniProt:
  • Canonical: P53762 (Residues: 81-464; Coverage: 49%)
Gene name: Arnt
Sequence domains:
Endothelial PAS domain-containing protein 1 Chain: B
Molecule details ›
Chain: B
Length: 368 amino acids
Theoretical weight: 42.16 KDa
Source organism: Mus musculus
Expression system: Escherichia coli BL21(DE3)
UniProt:
  • Canonical: P97481 (Residues: 3-362; Coverage: 41%)
Gene names: Epas1, Hif2a
Sequence domains:

Ligands and Environments

1 bound ligand:
Ligand HNJ 1 x HNJ
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: APS BEAMLINE 19-ID
Spacegroup: P21
Unit cell:
a: 48.951Å b: 98.846Å c: 77.077Å
α: 90° β: 107.2° γ: 90°
R-values:
R R work R free
0.202 0.199 0.258
Expression system: Escherichia coli BL21(DE3)

Quick links

Citations

4 review citations

Current strategies and progress for targeting the "undruggable" transcription factors.
Zhuang et al. (2022)
3 more

1 mention without citation

Bidirectional modulation of HIF-2 activity through chemical ligands.
Wu et al. (2019)