› 5dg5

X-ray diffraction
2.6Å resolution

CRYSTAL STRUCTURE OF THE TYROSINE KINASE DOMAIN OF THE HEPATOCYTE GROWTH FACTOR RECEPTOR C-MET IN COMPLEX WITH ALTIRATINIB ANALOG DP-4157

Released:
DOI: 10.2210/pdb5dg5/pdb
PDB entry 5dg5 coloured by chain, front view.
PDB entry 5dg5 coloured by chain, side view.
PDB entry 5dg5 coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Altiratinib Inhibits Tumor Growth, Invasion, Angiogenesis, and Microenvironment-Mediated Drug Resistance via Balanced Inhibition of MET, TIE2, and VEGFR2.
Smith BD, Kaufman MD, Leary CB, Turner BA, Wise SC, Ahn YM, Booth RJ, Caldwell TM, Ensinger CL, Hood MM, Lu WP, Patt TW, Patt WC, Rutkoski TJ, Samarakoon T, Telikepalli H, Vogeti L, Vogeti S, Yates KM, Chun L, Stewart LJ, Clare M, Flynn DL
Mol Cancer Ther 14 2023-34 (2015)
PMID: 26285778

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:
homo dimer (preferred)
Assembly name:
PDBe Complex ID:
PDB-CPX-140197 (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 5B4 2 x 5B4
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: ALS BEAMLINE 5.0.2
Spacegroup: P21
Unit cell:
a: 37.13Å b: 115.88Å c: 90.16Å
α: 90° β: 92.92° γ: 90°
R-values:
R R work R free
0.206 0.204 0.245
Expression system: Escherichia coli BL21(DE3)

Quick links

Citations

10 review citations

NTRK fusion-positive cancers and TRK inhibitor therapy.
Cocco et al. (2018)
9 more

4 mentions without citation

Insights into Current Tropomyosin Receptor Kinase (TRK) Inhibitors: Development and Clinical Application.
Yan et al. (2019)
3 more