› 6ggc

X-ray diffraction
1.24Å resolution

p53 cancer mutant Y220C in complex with small-molecule stabilizer PK9320

Released:
DOI: 10.2210/pdb6ggc/pdb
PDB entry 6ggc coloured by chain, front view.
PDB entry 6ggc coloured by chain, side view.
PDB entry 6ggc coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
A structure-guided molecular chaperone approach for restoring the transcriptional activity of the p53 cancer mutant Y220C.
Bauer MR, Jones RN, Tareque RK, Springett B, Dingler FA, Verduci L, Patel KJ, Fersht AR, Joerger AC, Spencer J
OpenAccess logo Future Med Chem 11 2491-2504 (2019)
PMID: 31633398

Function and Biology Details

Biochemical function:
Biological process:
Cellular component:
Sequence domains:

Structure analysis Details

Assembly composition:
monomeric (preferred)
Assembly name:
PDBe Complex ID:
PDB-CPX-138105 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Cellular tumor antigen p53 Chains: A, B
Molecule details ›
Chains: A, B
Length: 219 amino acids
Theoretical weight: 24.53 KDa
Source organism: Homo sapiens
Expression system: Escherichia coli
UniProt:
  • Canonical: P04637 (Residues: 94-312; Coverage: 56%)
Gene names: P53, TP53
Sequence domains: P53 DNA-binding domain
Structure domains: Immunoglobulin-like

Ligands and Environments

4 bound ligands:
Ligand ZN 2 x ZN
Ligand EXN 2 x EXN
Ligand EDO 2 x EDO
Ligand GOL 1 x GOL
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: DIAMOND BEAMLINE I02
Spacegroup: P212121
Unit cell:
a: 64.894Å b: 71.172Å c: 105.016Å
α: 90° β: 90° γ: 90°
R-values:
R R work R free
0.151 0.15 0.166
Expression system: Escherichia coli

Quick links

Citations

17 review citations

Targeting mutant p53 for cancer therapy: direct and indirect strategies.
Hu et al. (2021)
16 more

6 mentions without citation

A structure-guided molecular chaperone approach for restoring the transcriptional activity of the p53 cancer mutant Y220C.
Bauer et al. (2019)
5 more