› 4i6f

X-ray diffraction
2.9Å resolution

Selective & Brain-Permeable Polo-like Kinase-2 (Plk-2) Inhibitors that Reduce -Synuclein Phosphorylation in Rat Brain

Released:
DOI: 10.2210/pdb4i6f/pdb
PDB entry 4i6f coloured by chain, front view.
PDB entry 4i6f coloured by chain, side view.
PDB entry 4i6f coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Selective and brain-permeable polo-like kinase-2 (Plk-2) inhibitors that reduce α-synuclein phosphorylation in rat brain.
Aubele DL, Hom RK, Adler M, Galemmo RA, Bowers S, Truong AP, Pan H, Beroza P, Neitz RJ, Yao N, Lin M, Tonn G, Zhang H, Bova MP, Ren Z, Tam D, Ruslim L, Baker J, Diep L, Fitzgerald K, Hoffman J, Motter R, Fauss D, Tanaka P, Dappen M, Jagodzinski J, Chan W, Konradi AW, Latimer L, Zhu YL, Sham HL, Anderson JP, Bergeron M, Artis DR
ChemMedChem 8 1295-313 (2013)
PMID: 23794260

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

Assembly composition:
monomeric (preferred)
Assembly name:
PDBe Complex ID:
PDB-CPX-192722 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Serine/threonine-protein kinase PLK2 Chain: A
Molecule details ›
Chain: A
Length: 308 amino acids
Theoretical weight: 35.83 KDa
Source organism: Homo sapiens
Expression system: Escherichia coli
UniProt:
  • Canonical: Q9NYY3 (Residues: 57-360; Coverage: 44%)
Gene names: PLK2, SNK
Sequence domains: Protein kinase domain
Structure domains:

Ligands and Environments

1 bound ligand:
Ligand 1C7 1 x 1C7
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: ALS BEAMLINE 5.0.2
Spacegroup: C2
Unit cell:
a: 103.824Å b: 60.123Å c: 53.119Å
α: 90° β: 107.14° γ: 90°
R-values:
R R work R free
0.235 0.235 0.321
Expression system: Escherichia coli

Quick links

Citations

6 review citations

Recent Advances and New Strategies in Targeting Plk1 for Anticancer Therapy.
Lee et al. (2015)
5 more

1 mention without citation

Plk2 Loss Commonly Occurs in Colorectal Carcinomas but not Adenomas: Relationship to mTOR Signaling.
Matthew et al. (2018)