› 5amn

X-ray diffraction
2.57Å resolution

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-139854 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Soluble RET kinase fragment Chain: A
Molecule details ›
Chain: A
Length: 299 amino acids
Theoretical weight: 34.35 KDa
Source organism: Homo sapiens
Expression system: Spodoptera frugiperda
UniProt:
  • Canonical: P07949 (Residues: 705-1012; Coverage: 27%)
Gene names: CDHF12, CDHR16, PTC, RET
Sequence domains: Protein tyrosine and serine/threonine kinase
Structure domains:

Ligands and Environments

2 bound ligands:
Ligand DTQ 1 x DTQ
Ligand FMT 7 x FMT
1 modified residue:
Ligand PTR 2 x PTR

Experiments and Validation Details

Entry percentile scores
X-ray source: DIAMOND BEAMLINE I03
Spacegroup: P43212
Unit cell:
a: 50.57Å b: 50.57Å c: 242.84Å
α: 90° β: 90° γ: 90°
R-values:
R R work R free
0.186 0.183 0.237
Expression system: Spodoptera frugiperda

Quick links

Citations

4 review citations

The molecular basis for RET tyrosine-kinase inhibitors in thyroid cancer.
De Falco et al. (2017)
3 more

3 mentions without citation

The discovery of 2-substituted phenol quinazolines as potent RET kinase inhibitors with improved KDR selectivity.
Newton et al. (2016)
2 more