› 5ety

X-ray diffraction
2.9Å resolution

Crystal Structure of human Tankyrase-1 bound to K-756

Released:
DOI: 10.2210/pdb5ety/pdb
PDB entry 5ety coloured by chain, front view.
PDB entry 5ety coloured by chain, side view.
PDB entry 5ety coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
The Discovery and Characterization of K-756, a Novel Wnt/β-Catenin Pathway Inhibitor Targeting Tankyrase.
Okada-Iwasaki R, Takahashi Y, Watanabe Y, Ishida H, Saito J, Nakai R, Asai A
Mol Cancer Ther 15 1525-34 (2016)
PMID: 27196752

Function and Biology Details

Reaction catalysed: 
NAD(+) + (ADP-D-ribosyl)(n)-acceptor = nicotinamide + (ADP-D-ribosyl)(n+1)-acceptor
Biochemical function:
Biological process:
  • not assigned
Cellular component:
  • not assigned
Sequence domain:

Structure analysis Details

Assembly composition:
monomeric (preferred)
Assembly name:
PDBe Complex ID:
PDB-CPX-131875 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Poly [ADP-ribose] polymerase tankyrase-1 Chains: A, B, C, D
Molecule details ›
Chains: A, B, C, D
Length: 257 amino acids
Theoretical weight: 29.29 KDa
Source organism: Homo sapiens
Expression system: Escherichia coli
UniProt:
  • Canonical: O95271 (Residues: 1091-1324; Coverage: 18%)
Gene names: PARP5A, PARPL, TIN1, TINF1, TNKS, TNKS1
Sequence domains: Poly(ADP-ribose) polymerase catalytic domain
Structure domains: Phosphoenolpyruvate Carboxykinase; domain 3

Ligands and Environments

2 bound ligands:
Ligand ZN 4 x ZN
Ligand K56 4 x K56
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: PHOTON FACTORY BEAMLINE BL-5A
Spacegroup: P21212
Unit cell:
a: 158.846Å b: 74.68Å c: 84.603Å
α: 90° β: 90° γ: 90°
R-values:
R R work R free
0.258 0.255 0.305
Expression system: Escherichia coli

Quick links

Citations

13 review citations

Wnt signaling in breast cancer: biological mechanisms, challenges and opportunities.
Xu et al. (2020)
12 more

1 mention without citation

Novel Thioether-Bridged 2,6-Disubstituted and 2,5,6-Trisubstituted Imidazothiadiazole Analogues: Synthesis, Antiproliferative Activity, ADME, and Molecular Docking Studies.
Ozcan et al. (2023)