Molecular Target Synopsis
Overview
Domains and Structures
Drugs and Clinical Candidates
Druggability
Chemistry
Ligand Efficiency Plot
Pathways
Family Cladogram
Interaction Network
Gene Expression
Gene Copy Number Variation
RNAi
Mutations
Germline Genetics

GRK4 (P32298) - Overview - Molecular Target Synopsis

Protein


GRK4, G protein-coupled receptor kinase 4
Enzyme Classification 2.7.11.16
UniProt P32298

Also Known as GRK4_HUMAN, GRK4, GPRK2L, GPRK4

Specifically phosphorylates the activated forms of G protein-coupled receptors. GRK4-alpha can phosphorylate rhodopsin and its activity is inhibited by calmodulin; the other three isoforms do not phosphorylate rhodopsin and do not interact with calmodulin. GRK4-alpha and GRK4-gamma phosphorylate DRD3. Phosphorylates ADRB2. Interacts with DRD3.

4YHJ
STRUCTURE AND FUNCTION OF THE HYPERTENSION VARIANT A486V OF G PROTEIN- COUPLED RECEPTOR KINASE 4 (GRK4)
RCSB/PDB
Inspect Structure
See all 3D Structures for GRK4

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: GRK4 is active in the following subcellular-locations: cell cortex, cytoplasm.
GO terms: GRK4 is active in the following subcellular-locations: cell cortex, cytosol, dendrite, neuronal cell body, photoreceptor disc membrane.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project GRK4 has gain in 0 cell-lines, loss in 5 cell-lines and no signal in 1000 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: SR, MCF7, HL_60

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: SCLC-21H, SCLC-22H, NCI-H1395

In Array Express (RNA-seq of long poly adenylated RNA and long non poly adenylated RNA from ENCODE cell lines), the highest expressing cell lines are: SK-N-SH, NHLF, HMEC

(see details)

RNA Interference


GRK4 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: HCC1954, H460. (see details)

3D Structures


For GRK4 there are:
1 structures (2 chains) solved
1 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


GRK4 has been screened with 112 compounds (126 bioactivities), 13 compounds have bioactivities that show binding affinity of <= 500nM (16 bioactivities). (see details)