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

GRK3 (P35626) - Overview - Molecular Target Synopsis

Protein


GRK3, Beta-adrenergic receptor kinase 2
Enzyme Classification 2.7.11.15
UniProt P35626

Also Known as ARBK2_HUMAN, GRK3, ADRBK2, BARK2

Specifically phosphorylates the agonist-occupied form of the beta-adrenergic and closely related receptors.

Isoforms / Transcripts (Protein Coding)


Protein Length Ensembl Gene Ensembl Transcript Ensembl Protein Uniprot Isoform
688ENSG00000100077ENST00000324198ENSP00000317578P35626-1
45ENSG00000100077ENST00000455558ENSP00000393688

Sub-cellular localization


GO terms: GRK3 is active in the following subcellular-locations: cytosol, plasma membrane.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project GRK3 has gain in 2 cell-lines, loss in 1 cell-lines and no signal in 1002 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are:

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are:

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:

(see details)

RNA Interference


GRK3 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: CROE33, H2228. (see details)

3D Structures


At greater than 75% identity similarity to GRK3 there are:
28 structures (31 chains) solved
20 are solved in complex with at least one small molecule ligand
1 are solved with an approved drug

GRK3 is solved in complex with the approved drug(s):

8PR/PAROXETINE (3V5W_A).

(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


GRK3 has been screened with 53 compounds (60 bioactivities), 18 compounds have bioactivities that show binding affinity of <= 500nM (18 bioactivities). (see details)