› 3lvp

X-ray diffraction
3Å resolution

Crystal structure of bisphosphorylated IGF1-R Kinase domain (2P) in complex with a bis-azaindole inhibitor

Released:
DOI: 10.2210/pdb3lvp/pdb
PDB entry 3lvp coloured by chain, front view.
PDB entry 3lvp coloured by chain, side view.
PDB entry 3lvp coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Design of potent IGF1-R inhibitors related to bis-azaindoles.
Nemecek C, Metz WA, Wentzler S, Ding FX, Venot C, Souaille C, Dagallier A, Maignan S, Guilloteau JP, Bernard F, Henry A, Grapinet S, Lesuisse D
Chem Biol Drug Des 76 100-6 (2010)
PMID: 20545947

Function and Biology Details

Reaction catalysed: 
ATP + a [protein]-L-tyrosine = ADP + a [protein]-L-tyrosine phosphate
Biochemical function:
Biological process:
Cellular component:
Sequence domains:

Structure analysis Details

Assembly composition:
monomeric (preferred)
Assembly name:
PDBe Complex ID:
PDB-CPX-139909 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Insulin-like growth factor 1 receptor beta chain Chains: A, B, C, D
Molecule details ›
Chains: A, B, C, D
Length: 336 amino acids
Theoretical weight: 38.47 KDa
Source organism: Homo sapiens
Expression system: Escherichia coli
UniProt:
  • Canonical: P08069 (Residues: 951-1286; Coverage: 25%)
Gene name: IGF1R
Sequence domains: Protein tyrosine and serine/threonine kinase
Structure domains:

Ligands and Environments

3 bound ligands:
Ligand PDR 4 x PDR
Ligand EPE 1 x EPE
Ligand SO4 2 x SO4
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: ESRF BEAMLINE ID14-4
Spacegroup: P43212
Unit cell:
a: 94.95Å b: 94.95Å c: 322.29Å
α: 90° β: 90° γ: 90°
R-values:
R R work R free
0.226 0.226 0.279
Expression system: Escherichia coli

Quick links

Citations

1 review citation

7-Azaindole Analogues as Bioactive Agents and Recent Results.
Sharma et al. (2019)
6 other articles

9 mentions without citation

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