› 4leo

X-ray diffraction
2.64Å resolution

Crystal structure of anti-HER3 Fab RG7116 in complex with the extracellular domains of human Her3 (ERBB3)

Released:
DOI: 10.2210/pdb4leo/pdb
PDB entry 4leo coloured by chain, front view.
PDB entry 4leo coloured by chain, side view.
PDB entry 4leo coloured by chain, top view.
Source organisms:
Primary publication:
RG7116, a therapeutic antibody that binds the inactive HER3 receptor and is optimized for immune effector activation.
Mirschberger C, Schiller CB, Schräml M, Dimoudis N, Friess T, Gerdes CA, Reiff U, Lifke V, Hoelzlwimmer G, Kolm I, Hopfner KP, Niederfellner G, Bossenmaier B
Cancer Res 73 5183-94 (2013)
PMID: 23780344

Function and Biology Details

Reaction catalysed: 
ATP + a [protein]-L-tyrosine = ADP + a [protein]-L-tyrosine phosphate
Biochemical function:
  • not assigned
Biological process:
  • not assigned
Cellular component:
  • not assigned
Sequence domains:

Structure analysis Details

Assembly composition:
hetero trimer (preferred)
Assembly name:
PDBe Complex ID:
PDB-CPX-210841 (preferred)
Entry contents:
3 distinct polypeptide molecules
Macromolecules (4 distinct):
RG7116 Fab heavy chain Chain: A
Molecule details ›
Chain: A
Length: 227 amino acids
Theoretical weight: 24.37 KDa
Source organism: Mus musculus
Expression system: Cricetulus griseus
Structure domains: Immunoglobulins
RG7116 Fab light chain Chain: B
Molecule details ›
Chain: B
Length: 220 amino acids
Theoretical weight: 24.23 KDa
Source organism: Mus musculus
Expression system: Cricetulus griseus
Structure domains: Immunoglobulins
Receptor tyrosine-protein kinase erbB-3 Chain: C
Molecule details ›
Chain: C
Length: 621 amino acids
Theoretical weight: 68.38 KDa
Source organism: Homo sapiens
Expression system: Cricetulus griseus
UniProt:
  • Canonical: P21860 (Residues: 20-631; Coverage: 46%)
Gene names: ERBB3, HER3
Sequence domains:
Structure domains:

Ligands and Environments

Carbohydrate polymer : NEW Components: NAG
Carbohydrate polymer
1 bound ligand:
Ligand NAG 5 x NAG
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: ESRF BEAMLINE ID23-2
Spacegroup: P1
Unit cell:
a: 54.458Å b: 59.359Å c: 103.661Å
α: 97.64° β: 106.85° γ: 96.83°
R-values:
R R work R free
0.23 0.228 0.258
Expression system: Cricetulus griseus

Quick links

Citations

26 review citations

ERBB receptors: from oncogene discovery to basic science to mechanism-based cancer therapeutics.
Arteaga et al. (2014)
25 more

7 mentions without citation

Discovery of amivantamab (JNJ-61186372), a bispecific antibody targeting EGFR and MET.
Neijssen et al. (2021)
6 more