› 4wnk

X-ray diffraction
2.42Å resolution

Crystal Structure of Bovine G Protein Coupled-Receptor Kinase 5 in Complex with CCG215022

Released:
DOI: 10.2210/pdb4wnk/pdb
PDB entry 4wnk coloured by chain, front view.
PDB entry 4wnk coloured by chain, side view.
PDB entry 4wnk coloured by chain, top view.
Source organism: Bos taurus
Primary publication:
Crystal Structure of G Protein-coupled Receptor Kinase 5 in Complex with a Rationally Designed Inhibitor.
Homan KT, Waldschmidt HV, Glukhova A, Cannavo A, Song J, Cheung JY, Koch WJ, Larsen SD, Tesmer JJG
J Biol Chem 290 20649-20659 (2015)
PMID: 26032411

Function and Biology Details

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

Structure analysis Details

Assembly composition:
monomeric (preferred)
Assembly name:
PDBe Complex ID:
PDB-CPX-155003 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
G protein-coupled receptor kinase 5 Chain: A
Molecule details ›
Chain: A
Length: 598 amino acids
Theoretical weight: 69.04 KDa
Source organism: Bos taurus
Expression system: Trichoplusia ni
UniProt:
  • Canonical: P43249 (Residues: 1-590; Coverage: 100%)
Gene names: GPRK5, GRK5
Sequence domains:
Structure domains:

Ligands and Environments

2 bound ligands:
Ligand 453 1 x 453
Ligand SO4 1 x SO4
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: APS BEAMLINE 21-ID-F
Spacegroup: P212121
Unit cell:
a: 48.106Å b: 70.104Å c: 182.825Å
α: 90° β: 90° γ: 90°
R-values:
R R work R free
0.196 0.194 0.243
Expression system: Trichoplusia ni

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Citations

8 review citations

The expanding GRK interactome: Implications in cardiovascular disease and potential for therapeutic development.
Hullmann et al. (2016)
7 more

11 mentions without citation

Crystal Structure of G Protein-coupled Receptor Kinase 5 in Complex with a Rationally Designed Inhibitor.
Homan et al. (2015)
10 more