› 7tva

X-ray diffraction
2.84Å resolution

Stat5a Core in complex with AK2292

Released:
DOI: 10.2210/pdb7tva/pdb
Model geometry
Fit model/data
PDB entry 7tva coloured by chain, front view.
PDB entry 7tva coloured by chain, side view.
PDB entry 7tva coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
A selective small-molecule STAT5 PROTAC degrader capable of achieving tumor regression in vivo.
Kaneshige A, Bai L, Wang M, McEachern D, Meagher JL, Xu R, Wang Y, Jiang W, Metwally H, Kirchhoff PD, Zhao L, Jiang H, Wang M, Wen B, Sun D, Stuckey JA, Wang S
Nat Chem Biol (2023)
PMID: 36732620

Function and Biology Details

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

Structure analysis Details

Assembly composition:
monomeric (preferred)
Assembly name:
PDBe Complex ID:
PDB-CPX-154577 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Signal transducer and activator of transcription 5A Chains: A, B
Molecule details ›
Chains: A, B
Length: 573 amino acids
Theoretical weight: 65.83 KDa
Source organism: Homo sapiens
Expression system: Escherichia coli
UniProt:
  • Canonical: P42229 (Residues: 136-705; Coverage: 72%)
Gene names: STAT5, STAT5A
Sequence domains:

Ligands and Environments

3 bound ligands:
Ligand KOO 2 x KOO
Ligand PEG 2 x PEG
Ligand MLI 1 x MLI
No modified residues

Experiments and Validation Details

wwPDB Validation report is not available for this entry.
X-ray source: APS BEAMLINE 21-ID-D
Spacegroup: R3
Unit cell:
a: 232.476Å b: 232.476Å c: 112.473Å
α: 90° β: 90° γ: 120°
R-values:
R R work R free
0.205 0.202 0.246
Expression system: Escherichia coli

Quick links

Citations

2 review citations

PROTACs: A novel strategy for cancer drug discovery and development.
Han et al. (2023)
1 more