› 5uab

X-ray diffraction
1.9Å resolution

MET Tyrosine Kinase Inhibition Enhances the Antitumor Efficacy of an HGF Antibody

Released:
DOI: 10.2210/pdb5uab/pdb
PDB entry 5uab coloured by chain, front view.
PDB entry 5uab coloured by chain, side view.
PDB entry 5uab coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
MET Tyrosine Kinase Inhibition Enhances the Antitumor Efficacy of an HGF Antibody.
Farrell PJ, Matuszkiewicz J, Balakrishna D, Pandya S, Hixon MS, Kamran R, Chu S, Lawson JD, Okada K, Hori A, Mizutani A, Iwata H, de Jong R, Hibner B, Vincent P
Mol Cancer Ther 16 1269-1278 (2017)
PMID: 28341789

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: 343 amino acids
Theoretical weight: 38.58 KDa
Source organism: Homo sapiens
Expression system: Spodoptera frugiperda
UniProt:
  • Canonical: P08581 (Residues: 1023-1360; Coverage: 25%)
Gene name: MET
Sequence domains: Protein tyrosine and serine/threonine kinase
Structure domains: Transferase(Phosphotransferase) domain 1

Ligands and Environments

3 bound ligands:
Ligand 84M 1 x 84M
Ligand GOL 1 x GOL
Ligand CL 1 x CL
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: SSRL BEAMLINE BL9-2
Spacegroup: P212121
Unit cell:
a: 42.333Å b: 47.167Å c: 159.821Å
α: 90° β: 90° γ: 90°
R-values:
R R work R free
0.197 0.195 0.229
Expression system: Spodoptera frugiperda

Quick links

Citations

3 review citations

MET/HGF Co-Targeting in Pancreatic Cancer: A Tool to Provide Insight into the Tumor/Stroma Crosstalk.
Modica et al. (2018)
2 more

1 mention without citation

Conserved regulatory motifs in the juxtamembrane domain and kinase N-lobe revealed through deep mutational scanning of the MET receptor tyrosine kinase domain.
Estevam et al. (2023)