› 2zm3

X-ray diffraction
2.5Å resolution

Complex Structure of Insulin-like Growth Factor Receptor and Isoquinolinedione Inhibitor

Released:
DOI: 10.2210/pdb2zm3/pdb
PDB entry 2zm3 coloured by chain, front view.
PDB entry 2zm3 coloured by chain, side view.
PDB entry 2zm3 coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Lead identification to generate isoquinolinedione inhibitors of insulin-like growth factor receptor (IGF-1R) for potential use in cancer treatment.
Mayer SC, Banker AL, Boschelli F, Di L, Johnson M, Kenny CH, Krishnamurthy G, Kutterer K, Moy F, Petusky S, Ravi M, Tkach D, Tsou HR, Xu W
Bioorg Med Chem Lett 18 3641-5 (2008)
PMID: 18501599

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 domain:

Structure analysis Details

Assemblies composition:
monomeric (preferred)
homo octamer
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: 308 amino acids
Theoretical weight: 35.34 KDa
Source organism: Homo sapiens
Expression system: Not provided
UniProt:
  • Canonical: P08069 (Residues: 981-1286; Coverage: 23%)
Gene name: IGF1R
Sequence domains: Protein tyrosine and serine/threonine kinase
Structure domains:

Ligands and Environments

1 bound ligand:
Ligand 575 4 x 575
1 modified residue:
Ligand PTR 12 x PTR

Experiments and Validation Details

Entry percentile scores
X-ray source: ALS BEAMLINE 5.0.2
Spacegroup: C2
Unit cell:
a: 137.725Å b: 135.962Å c: 86.38Å
α: 90° β: 114.27° γ: 90°
R-values:
R R work R free
0.204 0.201 0.257
Expression system: Not provided

Quick links

Citations

1 review citation

Inhibition of the insulin-like growth factor-1 receptor (IGF1R) tyrosine kinase as a novel cancer therapy approach.
Li et al. (2009)
11 other articles

9 mentions without citation

Deep-Sea Sponges and Corals off the Western Coast of Florida-Intracellular Mechanisms of Action of Bioactive Compounds and Technological Advances Supporting the Drug Discovery Pipeline.
Iskandar et al. (2023)
8 more