› 2x7o

X-ray diffraction
3.7Å resolution

Crystal structure of TGFbRI complexed with an indolinone inhibitor

Released:
DOI: 10.2210/pdb2x7o/pdb
PDB entry 2x7o coloured by chain, front view.
PDB entry 2x7o coloured by chain, side view.
PDB entry 2x7o coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Design, synthesis, and evaluation of indolinones as inhibitors of the transforming growth factor β receptor I (TGFβRI).
Roth GJ, Heckel A, Brandl T, Grauert M, Hoerer S, Kley JT, Schnapp G, Baum P, Mennerich D, Schnapp A, Park JE
J Med Chem 53 7287-95 (2010)
PMID: 20919678

Function and Biology Details

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

Structure analysis Details

Assembly composition:
monomeric (preferred)
Assembly name:
PDBe Complex ID:
PDB-CPX-153250 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
TGF-beta receptor type-1 Chains: A, B, C, D, E
Molecule details ›
Chains: A, B, C, D, E
Length: 342 amino acids
Theoretical weight: 38.92 KDa
Source organism: Homo sapiens
Expression system: Spodoptera frugiperda
UniProt:
  • Canonical: P36897 (Residues: 162-503; Coverage: 73%)
Gene names: ALK5, SKR4, TGFBR1
Sequence domains:
Structure domains:

Ligands and Environments

1 bound ligand:
Ligand ZOP 5 x ZOP
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: SLS BEAMLINE X06SA
Spacegroup: C2221
Unit cell:
a: 179.929Å b: 246.561Å c: 131.617Å
α: 90° β: 90° γ: 90°
R-values:
R R work R free
0.267 0.267 0.273
Expression system: Spodoptera frugiperda

Quick links

Citations

2 review citations

Exploring anti-TGF-β therapies in cancer and fibrosis.
Hawinkels et al. (2011)
1 more

11 mentions without citation

Lumican binds ALK5 to promote epithelium wound healing.
Yamanaka et al. (2013)
10 more