› 2rku

X-ray diffraction
1.95Å resolution

Structure of PLK1 in complex with BI2536

Released:
DOI: 10.2210/pdb2rku/pdb
PDB entry 2rku coloured by chain, front view.
PDB entry 2rku coloured by chain, side view.
PDB entry 2rku coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Selectivity-determining residues in Plk1.
Kothe M, Kohls D, Low S, Coli R, Rennie GR, Feru F, Kuhn C, Ding YH
Chem Biol Drug Des 70 540-6 (2007)
PMID: 18005335

Function and Biology Details

Reaction catalysed: 
ATP + a protein = ADP + a phosphoprotein
Biochemical function:
Biological process:
Cellular component:
  • not assigned
Sequence domains:

Structure analysis Details

Assemblies composition:
monomeric (preferred)
homo dimer
Assembly name:
PDBe Complex ID:
PDB-CPX-156752 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Serine/threonine-protein kinase PLK1 Chain: A
Molecule details ›
Chain: A
Length: 294 amino acids
Theoretical weight: 33.82 KDa
Source organism: Homo sapiens
Expression system: Spodoptera frugiperda
UniProt:
  • Canonical: P53350 (Residues: 37-330; Coverage: 49%)
Gene names: PLK, PLK1
Sequence domains: Protein kinase domain
Structure domains:

Ligands and Environments

5 bound ligands:
Ligand ZN 1 x ZN
Ligand R78 1 x R78
Ligand TLA 2 x TLA
Ligand SRT 2 x SRT
Ligand TAR 1 x TAR
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: APS BEAMLINE 17-ID
Spacegroup: P3221
Unit cell:
a: 66.593Å b: 66.593Å c: 154.11Å
α: 90° β: 90° γ: 120°
R-values:
R R work R free
0.192 0.19 0.241
Expression system: Spodoptera frugiperda

Quick links

Citations

13 review citations

Targeting cancer with small molecule kinase inhibitors.
Zhang et al. (2009)
12 more

35 mentions without citation

Drug Discovery Targeting Bromodomain-Containing Protein 4.
Liu et al. (2017)
34 more