› 4hw7

X-ray diffraction
2.9Å resolution

Crystal structure of FMS kinase domain with a small molecular inhibitor, PLX647-OME

Released:
DOI: 10.2210/pdb4hw7/pdb
PDB entry 4hw7 coloured by chain, front view.
PDB entry 4hw7 coloured by chain, side view.
PDB entry 4hw7 coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Design and pharmacology of a highly specific dual FMS and KIT kinase inhibitor.
Zhang C, Ibrahim PN, Zhang J, Burton EA, Habets G, Zhang Y, Powell B, West BL, Matusow B, Tsang G, Shellooe R, Carias H, Nguyen H, Marimuthu A, Zhang KY, Oh A, Bremer R, Hurt CR, Artis DR, Wu G, Nespi M, Spevak W, Lin P, Nolop K, Hirth P, Tesch GH, Bollag G
Proc Natl Acad Sci U S A 110 5689-94 (2013)
PMID: 23493555

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

Assemblies composition:
monomeric (preferred)
homo dimer
Assembly name:
PDBe Complex ID:
PDB-CPX-139513 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Macrophage colony-stimulating factor 1 receptor Chain: A
Molecule details ›
Chain: A
Length: 343 amino acids
Theoretical weight: 38.64 KDa
Source organism: Homo sapiens
Expression system: Spodoptera frugiperda
UniProt:
  • Canonical: P07333 (Residues: 542-919; Coverage: 35%)
Gene names: CSF1R, FMS
Sequence domains: Protein tyrosine and serine/threonine kinase
Structure domains:

Ligands and Environments

1 bound ligand:
Ligand 64M 1 x 64M
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: ALS BEAMLINE 8.3.1
Spacegroup: P43212
Unit cell:
a: 62.964Å b: 62.964Å c: 182.78Å
α: 90° β: 90° γ: 90°
R-values:
R R work R free
0.222 0.22 0.267
Expression system: Spodoptera frugiperda

Quick links

Citations

11 review citations

Tumor-associated macrophages: implications in cancer immunotherapy.
Petty et al. (2017)
10 more

8 mentions without citation

The azaindole framework in the design of kinase inhibitors.
Mérour et al. (2014)
7 more