› 3rhk

X-ray diffraction
1.94Å resolution

Crystal structure of the catalytic domain of c-Met kinase in complex with ARQ 197

Released:
DOI: 10.2210/pdb3rhk/pdb
PDB entry 3rhk coloured by chain, front view.
PDB entry 3rhk coloured by chain, side view.
PDB entry 3rhk coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Discovery of a novel mode of protein kinase inhibition characterized by the mechanism of inhibition of human mesenchymal-epithelial transition factor (c-Met) protein autophosphorylation by ARQ 197.
Eathiraj S, Palma R, Volckova E, Hirschi M, France DS, Ashwell MA, Chan TC
J Biol Chem 286 20666-76 (2011)
PMID: 21454604

Function and Biology Details

Reaction catalysed: 
ATP + a [protein]-L-tyrosine = ADP + a [protein]-L-tyrosine phosphate
Biochemical function:
Biological process:
Cellular component:
  • not assigned
Sequence domains:

Structure analysis Details

Assembly composition:
monomeric (preferred)
Assembly name:
PDBe Complex ID:
PDB-CPX-140186 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Hepatocyte growth factor receptor Chains: A, B
Molecule details ›
Chains: A, B
Length: 318 amino acids
Theoretical weight: 35.99 KDa
Source organism: Homo sapiens
Expression system: Escherichia coli BL21(DE3)
UniProt:
  • Canonical: P08581 (Residues: 1038-1346; Coverage: 23%)
Gene name: MET
Sequence domains: Protein tyrosine and serine/threonine kinase
Structure domains:

Ligands and Environments

1 bound ligand:
Ligand M97 2 x M97
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: NSLS BEAMLINE X29A
Spacegroup: P1
Unit cell:
a: 53.47Å b: 58.67Å c: 64.96Å
α: 88.41° β: 68.1° γ: 85.52°
R-values:
R R work R free
0.203 0.2 0.254
Expression system: Escherichia coli BL21(DE3)

Quick links

Citations

39 review citations

Targeting MET in cancer: rationale and progress.
Gherardi et al. (2012)
38 more

9 mentions without citation

Bisindolyl Maleimides and Indolylmaleimide Derivatives-A Review of Their Synthesis and Bioactivity.
Cooney et al. (2023)
8 more