› 1tvo

X-ray diffraction
2.5Å resolution

The structure of ERK2 in complex with a small molecule inhibitor

Released:
DOI: 10.2210/pdb1tvo/pdb
PDB entry 1tvo coloured by chain, front view.
PDB entry 1tvo coloured by chain, side view.
PDB entry 1tvo coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Identification of a selective ERK inhibitor and structural determination of the inhibitor-ERK2 complex.
Ohori M, Kinoshita T, Okubo M, Sato K, Yamazaki A, Arakawa H, Nishimura S, Inamura N, Nakajima H, Neya M, Miyake H, Fujii T
Biochem Biophys Res Commun 336 357-63 (2005)
PMID: 16139248

Function and Biology Details

Reaction catalysed: 
ATP + a protein = ADP + a phosphoprotein
Biochemical function:
Biological process:
Cellular component:
Sequence domains:

Structure analysis Details

Assembly composition:
monomeric (preferred)
Assembly name:
PDBe Complex ID:
PDB-CPX-151230 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Mitogen-activated protein kinase 1 Chain: A
Molecule details ›
Chain: A
Length: 368 amino acids
Theoretical weight: 42.23 KDa
Source organism: Homo sapiens
Expression system: Escherichia coli
UniProt:
  • Canonical: P28482 (Residues: 1-360; Coverage: 100%)
Gene names: ERK2, MAPK1, PRKM1, PRKM2
Sequence domains: Protein kinase domain
Structure domains:

Ligands and Environments

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

Experiments and Validation Details

Entry percentile scores
X-ray source: SPRING-8 BEAMLINE BL32B2
Spacegroup: P21
Unit cell:
a: 48.86Å b: 69.99Å c: 63.3Å
α: 90° β: 116.5° γ: 90°
R-values:
R R work R free
0.266 0.263 0.272
Expression system: Escherichia coli

Quick links

Citations

18 review citations

ERK1/2 MAP kinases: structure, function, and regulation.
Roskoski R. (2012)
17 more

32 mentions without citation

Extracellular-Signal Regulated Kinase: A Central Molecule Driving Epithelial-Mesenchymal Transition in Cancer.
Olea-Flores et al. (2019)
31 more