› 4l9i

X-ray diffraction
2.32Å resolution

Bovine G Protein Coupled Receptor Kinase 1 in Complex with Paroxetine

Released:
DOI: 10.2210/pdb4l9i/pdb
PDB entry 4l9i coloured by chain, front view.
PDB entry 4l9i coloured by chain, side view.
PDB entry 4l9i coloured by chain, top view.
Source organism: Bos taurus
Primary publication:
Structural and functional analysis of g protein-coupled receptor kinase inhibition by paroxetine and a rationally designed analog.
Homan KT, Wu E, Wilson MW, Singh P, Larsen SD, Tesmer JJ
Mol Pharmacol 85 237-48 (2014)
PMID: 24220010

Function and Biology Details

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

Structure analysis Details

Assembly composition:
homo dimer (preferred)
Assembly name:
PDBe Complex ID:
PDB-CPX-151206 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Rhodopsin kinase GRK1 Chains: A, B
Molecule details ›
Chains: A, B
Length: 504 amino acids
Theoretical weight: 57.36 KDa
Source organism: Bos taurus
Expression system: Trichoplusia ni
UniProt:
  • Canonical: P28327 (Residues: 30-533; Coverage: 90%)
Gene names: GRK1, RHOK
Sequence domains:
Structure domains:

Ligands and Environments

3 bound ligands:
Ligand 8PR 2 x 8PR
Ligand MES 1 x MES
Ligand CL 2 x CL
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: APS BEAMLINE 21-ID-G
Spacegroup: P212121
Unit cell:
a: 66.788Å b: 122.089Å c: 152.892Å
α: 90° β: 90° γ: 90°
R-values:
R R work R free
0.188 0.186 0.231
Expression system: Trichoplusia ni

Quick links

Citations

8 review citations

Structural insights into G protein-coupled receptor kinase function.
Homan et al. (2014)
7 more

5 mentions without citation

Paroxetine-Overview of the Molecular Mechanisms of Action.
Kowalska et al. (2021)
4 more