› 5u6c

X-ray diffraction
2.1Å resolution

Crystal structure of the Mer kinase domain in complex with a macrocyclic inhibitor

Released:
DOI: 10.2210/pdb5u6c/pdb
PDB entry 5u6c coloured by chain, front view.
PDB entry 5u6c coloured by chain, side view.
PDB entry 5u6c coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
The Axl kinase domain in complex with a macrocyclic inhibitor offers first structural insights into an active TAM receptor kinase.
Gajiwala KS, Grodsky N, Bolaños B, Feng J, Ferre R, Timofeevski S, Xu M, Murray BW, Johnson TW, Stewart A
J Biol Chem 292 15705-15716 (2017)
PMID: 28724631

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-171420 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Tyrosine-protein kinase Mer Chains: A, B
Molecule details ›
Chains: A, B
Length: 315 amino acids
Theoretical weight: 36.24 KDa
Source organism: Homo sapiens
Expression system: Spodoptera frugiperda
UniProt:
  • Canonical: Q12866 (Residues: 570-864; Coverage: 30%)
Gene names: MER, MERTK
Sequence domains: Protein tyrosine and serine/threonine kinase
Structure domains: Transferase(Phosphotransferase) domain 1

Ligands and Environments

1 bound ligand:
Ligand 7YS 2 x 7YS
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: APS BEAMLINE 17-ID
Spacegroup: P21
Unit cell:
a: 51.692Å b: 92.33Å c: 69.269Å
α: 90° β: 100.8° γ: 90°
R-values:
R R work R free
0.214 0.211 0.257
Expression system: Spodoptera frugiperda

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Citations

7 citation in other articles

HGF-induced formation of the MET-AXL-ELMO2-DOCK180 complex promotes RAC1 activation, receptor clustering, and cancer cell migration and invasion.
Li et al. (2018)
6 more

4 mentions without citation

An Intriguing Purview on the Design of Macrocyclic Inhibitors for Unexplored Protein Kinases through Their Binding Site Comparison.
Bhujbal et al. (2023)
3 more