› 3krw

X-ray diffraction
2.9Å resolution

Human GRK2 in complex with Gbetgamma subunits and balanol (soak)

Released:
DOI: 10.2210/pdb3krw/pdb
PDB entry 3krw coloured by chain, front view.
PDB entry 3krw coloured by chain, side view.
PDB entry 3krw coloured by chain, top view.
Source organisms:
Primary publication:
Structure of human G protein-coupled receptor kinase 2 in complex with the kinase inhibitor balanol.
Tesmer JJ, Tesmer VM, Lodowski DT, Steinhagen H, Huber J
J Med Chem 53 1867-70 (2010)
PMID: 20128603

Function and Biology Details

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

Structure analysis Details

Assembly composition:
hetero trimer (preferred)
PDBe Complex ID:
PDB-CPX-150375 (preferred)
Entry contents:
3 distinct polypeptide molecules
Macromolecules (3 distinct):
Beta-adrenergic receptor kinase 1 Chain: A
Molecule details ›
Chain: A
Length: 688 amino acids
Theoretical weight: 79.56 KDa
Source organism: Homo sapiens
Expression system: Spodoptera frugiperda
UniProt:
  • Canonical: P25098 (Residues: 2-689; Coverage: 100%)
Gene names: ADRBK1, BARK, BARK1, GRK2
Sequence domains:
Structure domains:
Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1 Chain: B
Molecule details ›
Chain: B
Length: 340 amino acids
Theoretical weight: 37.42 KDa
Source organism: Bos taurus
Expression system: unidentified baculovirus
UniProt:
  • Canonical: P62871 (Residues: 1-340; Coverage: 100%)
Gene name: GNB1
Sequence domains: WD domain, G-beta repeat
Structure domains: YVTN repeat-like/Quinoprotein amine dehydrogenase
Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2 Chain: G
Molecule details ›
Chain: G
Length: 74 amino acids
Theoretical weight: 8.41 KDa
Source organism: Bos taurus
Expression system: unidentified baculovirus
UniProt:
  • Canonical: P63212 (Residues: 1-68; Coverage: 96%)
Gene name: GNG2
Sequence domains: GGL domain
Structure domains: Transducin (heterotrimeric G protein), gamma chain

Ligands and Environments

2 bound ligands:
Ligand BA1 1 x BA1
Ligand MG 1 x MG
1 modified residue:
Ligand CMT 1 x CMT

Experiments and Validation Details

Entry percentile scores
X-ray source: APS BEAMLINE 21-ID-G
Spacegroup: C2
Unit cell:
a: 182.351Å b: 73.522Å c: 121.216Å
α: 90° β: 114.26° γ: 90°
R-values:
R R work R free
0.216 0.213 0.265
Expression systems:
  • Spodoptera frugiperda
  • unidentified baculovirus

Quick links

Citations

12 review citations

G protein-coupled receptor kinases: more than just kinases and not only for GPCRs.
Gurevich et al. (2012)
11 more

7 mentions without citation

Understanding molecular recognition by G protein βγ subunits on the path to pharmacological targeting.
Lin et al. (2011)
6 more