› 6fek

X-ray diffraction
2.3Å resolution

Oncogenic point mutation of RET receptor tyrosine kinase

Released:
DOI: 10.2210/pdb6fek/pdb
PDB entry 6fek coloured by chain, front view.
PDB entry 6fek coloured by chain, side view.
PDB entry 6fek coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
A secondary RET mutation in the activation loop conferring resistance to vandetanib.
Nakaoku T, Kohno T, Araki M, Niho S, Chauhan R, Knowles PP, Tsuchihara K, Matsumoto S, Shimada Y, Mimaki S, Ishii G, Ichikawa H, Nagatoishi S, Tsumoto K, Okuno Y, Yoh K, McDonald NQ, Goto K
Nat Commun 9 625 (2018)
PMID: 29434222

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-139853 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Soluble RET kinase fragment Chain: A
Molecule details ›
Chain: A
Length: 299 amino acids
Theoretical weight: 34.31 KDa
Source organism: Homo sapiens
Expression system: Spodoptera frugiperda
UniProt:
  • Canonical: P07949 (Residues: 705-1013; 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 FMT 3 x FMT
Ligand ADN 1 x ADN
1 modified residue:
Ligand PTR 2 x PTR

Experiments and Validation Details

Entry percentile scores
X-ray source: SLS BEAMLINE X10SA
Spacegroup: P43212
Unit cell:
a: 50.901Å b: 50.901Å c: 242.515Å
α: 90° β: 90° γ: 90°
R-values:
R R work R free
0.203 0.201 0.244
Expression system: Spodoptera frugiperda

Quick links

Citations

25 review citations

State-of-the-Art Strategies for Targeting RET-Dependent Cancers.
Subbiah et al. (2020)
24 more

2 mentions without citation

A secondary RET mutation in the activation loop conferring resistance to vandetanib.
Nakaoku et al. (2018)
1 more