› 3vw8

X-ray diffraction
2.1Å resolution

Crystal structure of human c-Met kinase domain with its inhibitor

Released:
DOI: 10.2210/pdb3vw8/pdb
PDB entry 3vw8 coloured by chain, front view.
PDB entry 3vw8 coloured by chain, side view.
PDB entry 3vw8 coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Structure-based design, synthesis, and evaluation of imidazo[1,2-b]pyridazine and imidazo[1,2-a]pyridine derivatives as novel dual c-Met and VEGFR2 kinase inhibitors.
Matsumoto S, Miyamoto N, Hirayama T, Oki H, Okada K, Tawada M, Iwata H, Nakamura K, Yamasaki S, Miki H, Hori A, Imamura S
Bioorg Med Chem 21 7686-98 (2013)
PMID: 24216091

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 Chain: A
Molecule details ›
Chain: A
Length: 328 amino acids
Theoretical weight: 37.08 KDa
Source organism: Homo sapiens
Expression system: Spodoptera frugiperda
UniProt:
  • Canonical: P08581 (Residues: 1024-1352; Coverage: 24%)
Gene name: MET
Sequence domains: Protein tyrosine and serine/threonine kinase
Structure domains:

Ligands and Environments

2 bound ligands:
Ligand DF6 1 x DF6
Ligand CL 1 x CL
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: ALS BEAMLINE 5.0.3
Spacegroup: P212121
Unit cell:
a: 42.69Å b: 78.786Å c: 89.969Å
α: 90° β: 90° γ: 90°
R-values:
R R work R free
0.215 0.212 0.259
Expression system: Spodoptera frugiperda

Quick links

Citations

2 review citations

Applications of Palladium-Catalyzed C-N Cross-Coupling Reactions.
Ruiz-Castillo et al. (2016)
1 more

4 mentions without citation

Data driven polypharmacological drug design for lung cancer: analyses for targeting ALK, MET, and EGFR.
Narayanan et al. (2017)
3 more